Title of Invention	TETRAHYDROQUINOLINE DERIVATIVES AND A PROCESS FOR PREPARING THE SAME
Abstract	TETRAHYDROQUINOLINE DERIVATIVES AND A PROCESS FOR PREPARING THE SAME The present invention relates to novel compound of the formula (I) fwherein the substituent groups are as herein described, and process of preparing the compound. This invention also relates to a pharmaceutical composition comprising the said compound.

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DESCRIPTION TETRAHYDROQUINOLINE DERIVATIVES AND A PROCESS FOR PREPARING THE SAME TECHNICAL FIELD The present invention relates to a novel tetrahydroquinoline derivative having an inhibitory activity against cholesteryl ester transfer protein (CETP). BACKGROUND ART Hypercholesterolemia, especially high serum level of low-density lipoprotein (LDL) cholesterol, has been revealed to be a risk factor of arteriosclerotic diseases by a number of epidemiologies! surveys. Actually, drugs capable of decreasing LDL cholesterol level such as 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase inhibitors have been used with the aim of preventing coronary artery diseases, and demonstrated to have some benefits in many large scale clinical tests. However, their preventive effect on coronary diseases is limited to some extent, and is not satisfactory enough yet. Recently, low serum level of high density lipoprotein (HDL) cholesterol has been revealed to be a potent risk factor of arteriosclerotic diseases by a number of epidemiological surveys and large scale clinical tests. HDL is known to have various antiarteriosclerotic effects and attnetion is focused on the potentiality of drugs increasing HDL cholesterol level as a means for prevention or treatment of arteriosclerotic diseases. However, there are no drugs that can be used in a satisfactory manner for this purpose. Fibrates and HMG-CoA reductase inhibitors have only low activity of increasing HDL cholesterol; nicotinic acid derivatives can significantly increase HDL, but have serious toleration issues. Accordingly, there has been a demand for a well-tolerated agent which can significantly elevate HDL cholesterol levels, thereby preventing or reversing the progression of atherosclerosis. It is known that many proteins are involved in the regulation mechanism for catabolism of various lipoproteins. Among them, the role of cholesteiyl ester transfer protein (CETP) became to draw attention. CETP is a protein responsible for transfer of cholesteryl ester (CE) and triglyceride between lipoproteins, and mediate the transfer of CE from HDL to LDL or to very low density lipoprotein (VLDL). Accordingly, CETP activity affects greatly the lipid composition in lipoprotein particles. For example, it is known that administration of a neutralizing monoclonal antibody to CETP to rabbit or hamster elevates HDL cholesterol levels and lower LDL cholesterol levels. Furthermore, human being having decreased or eliminated CETP activity due to gene mutation shows raised t>lood HDL cholesterol level and. lowered blood LDL cholesterol level. On the other hand, it is known that transgenic mice and rats made to express CETP show lowered HDL cholesterol level and raised LDL cholesterol level. Thus, it is considered that CETP greatly contribute to the regulation of serum lipids, and thereby affecting the change of serum lipid profile such as decrease of HDL cholesterol level and increase of LDL cholesterol. Accordingly, it is assumed that a high value of CETP activity would induce arteriosclerosis. In fact, CETP activity varies depending on animal species. It is known that, arterio sclerotic lesions are readity formed by cholesterol loading in animals with high CETP activity such as rabbits, whereas such lesions hardly occur in animals with low CETP activity suchL as rats. Furthermore, it is confirmed that continuous suppression of CETP activit}?" by administration of antisense oligodeoxynuclotide resulted in effects such as increase of blood HDL cholesterol level and reduction in arteriosclerotic lesions in cholesterol-fed rabbits. The above findings indicate that CETP activity is in negative correlation with HDL cholesterol, and that inhibition of CETP activity-would decrease the degree of risk for arteriosclerotic diseases. It is therefore expected that compounds capable of inhibiting CETP activity can block the traixsfer of cholesterol from HDL to LDL, and thereby increasing HDL cholesterol that tends to prevent arteriosclerosis while lowering LDL cholesterol th_at tends to promote arteriosclerosis. In this way, such compounds can serve as a useful preventive or therapeutic agent for arteriosclerotic diseases, hyperlipemia or dyslipidemia and provide effective medical treatment for the first time. Examples of compounds having CETP inhibitory activity include tetrahydroquinoline derivatives. See, WO00/17164, WO00/ 17165, WO00/17166. However, these compounds have defects. That is, they are poorly soluble in water and cannot be absorbed enough in vivo, a sufficient blood level for taking medicinal effect can hardly be achieved even when administered as an ordinary formulation for oral administration. See, WO03/63868. Accordingly, novel compounds in which the above-mentioned defects have been solved are highly demanded. DISCLOSURE OF INVENTION The present invention provides novel tetrahydroquinoline derivatives having an excellent CETP inhibitory activity wherein defects of existing CETP inhibitory compounds are rectified. Thus, the present invention provides a compound of the fonmxla (I): wherein R1 is a hydrogen atom, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, an optionally substituted alkyl group, an optionally substituted alkanoyl group, a. saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfixr and nitrogen atoms (the heterocyclic group is optionally substituted), or a saturated or unsaturated monocyclic or bicyclic heteroc}'clic caxbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted),; R2 is a hydrogen atom or an optionally substituted alkyl group; R3 is a hydrogen atom or an optionally substituted alkyl group; R4 is an optionally substituted alkylene group; R5 is a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatonxs selected independent^ from oxygen, sulfur and nitrogen atoms, wherein the heterocyclic group is substituted by 1 to 5 substituents selected from th.e following groups, or said heterocyclic group is substituted b}^ 1 to 5 substituents selected from the following groups and further by a halogen atom, an oxo and/or hydroxy group: cj'ano group, nitro group, carboxyl group, sulfo group, C3-10 alkyl group, substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted allcenyl group, C3-10 alkoxy group, substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxycarbonyl group, optionally substituted carbamoyl group, optionally substituted carbamimidosd group, optionally substituted alkylttaio group, optionally substituted alkylsulfinyl group, optionally substituted alkylsulfonyl group, optionally substituted amino group, optionally substituted sulfamoyl group, optionally substituted alkanoyl group, a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted), a saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen, atoms (the heterocyclic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from, oxygen, sulfur and nitrogen atoms (the heterocyclic carbonyl group is optionally substituted); R6, R7, R8 and R9 are independently a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a cyano group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an optionally substituted alkylsulfonyloxy group or an optionally substituted amino group; or R6 and R7, or R7 and R8, or R8 and R9 may combine at the ends to form an alkylene group which, alkylene group may contain 1 to 3 heteroatoms selected independently from nitrogen, sulfur and oxygen atoms, and ma.y have a substituent(s); and R10 is an aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxrygen, sulfur and nitrogen atoms (the aromatic ring is optionally substituted), or a pharmaceutically acceptable salt thereof The compound (I) of the present invention encompasses a mixture of stereoisomers, respective stereoisomers in a purified or substantially purified form. For example, the compounds of the formula (I) may have one or more asymmetric carbon atoms and therefore may occur as individual enantiomers or diastereomers, or a mixture thereof. The present compounds include respective isomers and a mixture thereof. In addition, when the compound (I) has a double bond, geometric isomers may occur (cis- and trans-forms), and when the compound (I) has a group containing an unsaturated bond such as carbonyl, tautomeric forms may occur, and the present compounds include respective isomers and a mixture thereof. Further, the pharmaceuticalfy- acceptable salts of compound (I) of the present invention include an intramolecular salt, a hydrate, solvate, or the like. As used herein, the term "aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms11 refers to preferably a "5- to Z-membered monocyclic aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms'* including specifically phenyl, furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, azepinyl, oxepinyl and thiepinyl groups, and the like. The term "saturated or \xnsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" refers to preferably a "saturated or unsaturated 5- to 8-membered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" including specifically the following groups. Examples of 5-membered heterocyclic group include 2H-pyrrolyl, 3H-pyrrolyl, 2-pyrrolyl, 3-pyrrolyl, pyrrolidin3'l, 1,3-dioxolanyl, oxazolyl, oxazolinyl, oxazolidinyl, thiazolyl, imidazolyl, imidazolinyl, inoidazolidinyl, pyrazolyl, 2-pyrazolinyl, pyrazolidinyl, isoxazolyl, isothiazolyl, tetrazolyl, 1,2-dithiolyl, 1,3-dithiolyl, 3H-1,2-oxathiolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazotyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,3,4-thiadiazolyl, 1,2,3,4- oxatriazolyl, 1,2,3,5-oxatriazolyl, 3H-1,2,3-clioxazolyl, 1,2,4-dioxazolyl, 1,3,2-dioxazolyl, 1,3,4-dioxazolyl, 5H-l,2,5-oxeithiazolyl and 1,3-oxathiolyl groups, and the like. Examples of 6-membered heterocyclic group include 2H-pyranyl, 4H-pyranyl, pyridyl, piperidinyl, 1,2-dioxinyl, 1,3-dioxinyl, 1,4-dioxanyl, morpholinyl, 1,4-dithianyl, thiomorpholinyl, p3rridazinyl, pyrimidinyl, pyrazinyl, piperazinyl, 1,3,5-triazinyl, 1,2,4-triazinyl, 1,2,3-triazinyl, 1,3,5-trithianyl, 4H-1,2-oxazinyl, 2H-1,3-oxazinyU 6H-1,3-oxazinyl, 6H-1,2-oxazinyl, 1,4-oxazinyl, 2H-l,2-oxazinyl, 4H-1,4—oxazinyl, 1,2,5-oxathiazinyl, 1,4-oxazinyl, o-isoxazinyl, p-isoxazinjd, 1,2 75-ozathiazin3d, 1,2,6-oxathiazinyl, 1,4,2-oxadiazinyl and 1,3,5,2-oxa.diazinyl groups; and the like. Examples of 7-membered heterocyclic group include azepinyl, oxepinyl and thiepinyl groups, and the like. Examples of 8-membered heterocyclic group include azocinyl, oxocinyl and thiocinyl groups, and the like. As used herein, the heterocyclic moiety of the "saturated or unsaturated monoc3'clic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms", "saturated or unsaturated monocyclic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms", and "a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonylamino group containing 1 to 4 heteroatoms selected independently from ozxygen, sulfur and nitrogen atoms" refers to the aforementioned "saturated or unsaturated monoc3^clic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms". In such cases where the binding position for these aromatic ring, heterocyclic group, and the like is not specifically defined, the definition is meant to encompass all the possible binding positions. For example, the term "pyridyl group" means 2-, 3- or 4-pjTidyL group, and the term "thienyl group" means 2- or 3-thienyl group. Thie same is applied to other aromatic rings and heterocyclic groups. When the saturated or un&aturated monocyclic or bicyclic heteroc3^clic group, heterocyclic oxy groxip, heterocyclic carbonyl group and heterocyclic carbonylamino group each containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms have a substituent(s), the substitution includes oxidation of heteroatom(s) in the heterocycle in the respective groups. Specifically, compounds having a heteroatom(s) in the heterocycle of said groups as N-oxide, S-oxide (SO) or S,S-dioxide (SO2) also fall within the scope of the present invention. The term "halogen" refers to fluorine, chlorine, bromine or iodine. The term "alkyl group" or "allcyl" means a straight or branched saturated hydrocarbon chain having 1 to 10 carbon atoms and a cyclic saturated hydrocarbon chain having 3 to 10 carbon atoms. As a straight or branched hydrocarbon chain, those having 2 to 10 carbon atoms are preferred and those having 2 to 6 carbons are more preferred. Other preferred examples are straight chain alkyl groups having 1 to 6 carbon atoms, especially those having 1 to 4 carbon atoms. Examples of alkyl group include methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, hexyl and isohexyl groups, and the like. The term "alkoxy group" or "alleoxy" means a straight or branched alkyloxy group having 1 to 10 carbon atoms and a cyclic alkyloxy group having 3 to 10 carbon atoms. As a straight or branched hydrocarbon chain, those having 2 to 10 carbon atoxns are preferred and those having 2 to 6 carbons are more preferred. Other preferred examples are straight chain alkoxy groups having 1 to 6 carbon atoms, especially those having 1 to 4 carbon atoms. Examples of alkoxy group include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutox^^, tert-butoxy, pentoxy, isopentoxy, neopentoxy, tert-pentoxy, hexoxy and isohexoxy groups, and the like. The term "alkylene group" or "alkylene" means a saturated hydrocarbon chain wherein a hydrogen atom is removed from each of the terminal carbons of a straight hydrocarbon chain. Preferred examples include an alkylene group having 1 to 6 carbon atoms, specifically, methylene, ethylene, trimethylene and tetramethylene groups, and the like. When an alkylene group herein used contains 1 to 3 heteroatoms selected independently from nitrogen, sulfur and oxygen atoins, the term "alkylene" includes a group of the formula:-O-(CH2)m-O-, -S-(CH2)m-S-, -NH-(CH2)m-NH-, or -O-(CH2)m-NH- (wherein m is an integer of 1 to 4), or the like. The term "alkanoyl group" or "alkanojd" means a straight or branched alkylcarbonyl group having 1 to 10 carbon atoms, preferably an alkylcarbonyl group having 1 to 6 carbon atoms 9 more preferably an alkylcarbonyl group having 1 to 4 carbon atoms. Examples of alkanoyl group include acetyl, propionyl, butyiyl, valeryl and pivaloyl groups, and the like. The term "alkenyl group" or "alkenyl" means a straight or branched hydrocarbon chain having 2 to 10 carbon atoms and containing at least one double bond, preferably an alkenyl group having 2 to 6 carbon atoins, more preferably an alkenyl group having 2 to 4 carbon atoms Examples of alkenyl group include vinyl, 1-propenyl, allyl, isopropenyl, butenyl, butadienyl and pentenyl groups, and the like. As herein used throughout the claims and specification, when the term "mono- or di-alkyl" refers to di-alkyl, the aJkyl moieties may be independent from each other. In addition, a compound of the formula below means that it takes the configuration (2R*,4S*), wherein (2R*,4S*) refers to a mixture of (2R?4S) and (2S,4R). N H The compounds of the present invention iiave CETP inhibitory activity and are effective for increasing HDL cholesterol and lowering LDL cholesterol. Accordingly, the said compounds are useful in prevention and/or treatment of diseases such as arteriosclerosis, hyperlipemia, and the like. BEST MODE FOR CARRYING OUT THE INVENTION Preferred compounds of the present invention are those wherein R5 is a saturated or unsaturated monocj^clic or bicjrclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, wherein the heterocyclic group is substituted by 1 to 5 substituents selected from the following groups, or said heterocyclic group is substituted by 1 to 5 substituents selected from the following groups along with halogen atom, oxo and/or hydroxy group: cyano group, nitro group, carboxyl group, sxilfo group, C3-10 alkyl group, substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, C3-10 alkioxy group, substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxycarbonyl group, carbarn oyl group, optionally substituted mono- or di-alkylcarbamoyl group, optionally substituted carbamimidoyl group, optionally substituted alkylthio group, optionally substituted alkylsulfinyl group, optionally substituted alkylsulfonyl group, amino group, optionally substituted mono- or di-alkylamino group, optionally substituted alkanoylamino group, optionally substituted alkoxycarbonylamiao group, optionally substituted alkylsulfon3rlamino group, optionally substituted mono- or di-alkylcarbamoylamino group, a saturated or tansaturated monoc3'clic or bicyclic heterocyclic carbonylamino group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonylamino group is optionally substituted), sulfamoyl group, optionally substituted mono- or di-alkyl sulfamoyl group, optionally substituted alkanoyl group, a saturated or unsaturated monoc3'clic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen., sulfur and nitrogen atoms (the heterocyclic group is optionally substituted), a saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocj'clic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bicyclic heterocyclic carbon3>l group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the bieterocyclic carbonyl group is optionalfy substituted); and R10 is an aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, which aromatic ring is optionally substituted by 1 to 4 substitueixts selected from the following groups: halogen atom, carboxyl group, optionally substituted alkoxycarbonyl group, carbamoyl group, optionally substituted mono- or di-alkylcarbamoyl group, optionally substituted alkyl group, optionally substituted alkoxy group, hydroxy group, nitro group, cyano group, amino group, optionally substituted mono- or di-alkylainino group, optionally substituted alkanoyl group, optionally substituted alkylthio group, and a saturated or unsaturated monocj'clic or bicyclic heteroc3^clic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted). The substituent(s) for substituted alkyl group, optionally substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, substituted alkoxy group, optionally substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxycarbonyl group, optionally substituted mono- or di-alkylcarbamoyl group, optionally substituted alkylthio group, optionally substituted alkylsulfinyl group, optionally substituted alkylsulfonyl group, optionally substituted mono- or di-alkylamino group, optionally substituted alkanoylamino group, optionally substituted alkoxycarboriylamino group, optionally substituted alkylsulfonylamino group, option.ally substituted mono- or di-alkylcarbamoylamino group, optionally substituted mono- or di-alkylsulfamoyl group, optionalfy substituted alkanoyl group, optionally substituted alkylene group, a saturated or unsaturateci nxonocyclic or bicyclic heterocyclic carbon^ylamino group containing 1 to 4 heteroatoms selected independentfy from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonylamino group is optionally substituted), a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfuir and nitrogen atoms (the heterocyclic group is optionally substituted),, a saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfuir and nitrogen atoms (the heterocyclic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bic3'clic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heteroc3'clic carbonyl group is optionally substituted) ma}' be 1*5 groups selected from the following groups: halogen atom; cyano group; hydroxy group; nitro group; carboxyl group; oxo group; thioxo group; sulfo group; cycloalkyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkoxycarbonyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxrycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; carbamoyl group; mono- or di-alkylcarbamoj'l group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group * phenyl group or morpholinyl group; alkyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyt group or morpholinyl group; alkanoyl group optionally substituted b}' hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkoxy group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkano3'loxy group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, m_ono- or di-alkylamino group, phen3'l group or morpholinyl group; alkylthio group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkylsulfonyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkylsulfinyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; mono- or di-alkylsulfamoyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; amino group; mono- or di-alkylamino group optionally substituted b}' hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; mono- or di-alkylsulfamoylamino group optionally substituted b}^ hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholin}'! group; mono- .or di-alkylureido group optionally substituted by Itydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; and a group of the formulas: wherein X* and X3 are independently CH2, NH, 0, S, SO or SO2; X2 and X5 are independently CH2, 0> S, SO or S02; X4 is NH, O? S, SO or SO2; X6 and X7 are independently 0 or S; X8 is S or SO; and n, o, p, q and r are independently an integer of 1 to 4, wherein each group of the above formula is optionally substituted b5^ 1 to 3 substituents selected from the following groups: halogen atom, carboxyl group, hydroxy group, cyano group, oxo group, thioxo group, alkyl group, hydroxyalkyl group, alkoxycarbonylalkyl group, carboxyalkyl group, morpholinylalkyl group, phenylalkyl group, alkanoyl group, hydroxyalkanoyl group, alkoxyalkanoyl group, alkoxy group, phenylalkoxy group, alkoxycarbonyl group, benzyloxycarbonyl group, mono- or di-alkylamino group, mono- or di-alkylcarbamoyl group, mono- or di-alkylsulfamoyl group, alkylsiilfonyl group and tetrazolyl group. Furthermore, the "aromatic ring optionally containing 1 to 3 heteroatoxns selected independently from oxygen, sulfur and nitrogen atoms" is preferably a phenyl, naphthyl, pyridyl,-quinolyl, isoquinolyl? furyl, pyrimidinyl, triazolyl or thienyl group; The "saturated or unsaturated monoc3?"cLic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is preferably a moirpholinyl, thiomorpholinyl, piperazinyl, pyrrolidinyl, piperidinyl, hexataydroazepinyl, pyrrolinyl, imidazolidinyl, oxazolidinyl, tetrahydropyranyl, tetrahydrofuranyl, dioxolanyl, oxiranyl, pyrimidinyl, pyridyl, triazolyl, tetrazolyl, oxadiazolyl, dihydropyrimidinjd, pyrazirtyl, thiazolyl, oxazolinyl, oxazolyl, pyridazinyl, imidazolinyl, imidazolyl, pyrazinyl, thienyl, pyrrolyl, furyl or dihydrooxazinyl group. The "saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is preferably a morpholinyloxy, thiomorpholinyloxy piperazinyloxy, pyrrolidkiyloxy, piperidinjdoxy, hexahydroazepinyloxy, pyrrolinyloxy, imidazolidinyloxj7", oxazolidinyloxy, tetrahydrop3?ranylosy, tetrahydrofuranyloxy, iioxolanyloxy, oxiranyloxy, pyrimidinyloxy, pyridyloxy, triazolyloxy, tetrazolylo>T7, oxadiazolyloxj^ dihydrop37iimidinylox5?>, pyraziny loxy, thiajzolyloxy, oxazolinyloxj', oxazolylox}^ pyridazinyloxy, imidazolinyloxy, irxiidazolyloxy, pyrazinyloxy, thienjdoxy, pyrrolylo^, futyloxy or dihydrooxazir^loxy group. The "saturated or unsaturated monocyclic or bicyclic heterocyclic carbon}4 group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is preferably a morpholinylcarbonyl, thiomorpholinylcarbonyl piperazinylcarbonyl, pyrrolidinylcarbonyl, piperidinylcarbonyl, hexahydroazepinylcarbonyl, p3Trolinylcarbonyl, imidazolidinylcarbonyl, oxazolidinylcarbonyl, tetrahydropyranylcaLrbon34, tetrahydrofuranylcarbonyl, dioxolanylcarbonyl, oxiranylcarbonyl P3oimidinylcarbonyl, pyridylcarbonyl, triazotylcarbonyl, tetrazolylcarbonyl, oxadiazolylcarbonyl, dih3^dropyrimidinylcarbonyl, pyrazin3dcarbonyl? thiazolylcarbonyl, oxazolinylcarbonyl, oxazolylcarbonyl, pyTidazinyl- carbonyl, imidazolinylcarbonyl, iinidazolylcarbonjrl, pyrazinylcarbon}4, thienylcarbon3^1, pyrrolylcarbonyl, furylcarbonyl or diliydrooxaz^dcarbonyl group. The "saturated or unsaturated rnonocyclic or bicyclic heterocyclic carbonylamino group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is preferably a morpholin34caxbonylamino, thiomorpholinylcarbonylamino piperazinyl- carbonylamino, pyrrolidinylcarbonjdamino, piperidinjdcarbonylamino, hexahydroazepinylcarbon3damino? pyrrolinjdcarbonylamino, imidazolidinyl- carbonylamino, oxazolidinylcarbonj^lamino, tetra!hydrop3'Tanylcarbon3'l- amino, tetrahydrofuranylcarbonylamino, dioxolan3dcarbonylamino, oxiran3rlcarbonylamino, pyrimidinylcarbon3damino, p3aidylcarbonylamino, tria2olylcarbon3rlamino, tetrazolylcgirbonylainino, oxadiazolylcarbonylamino, dihydropyrimidinylcarbonylainino, py razinylcarbo xiylamino, thiazolyl- carbonylamino y oxazolin3rlcarbonylamino, oxazolylcarbonylamino, pyridazinylcarbonylamino, imidazolinylcarbonylamino, imidetzolyl-carbonylamino ? pyrazinylcarbo^lamino, thienylcar-bon34amino, pyrrotyl-carbon3'lainino ? fuiylcarbon34amino or dihydro oxazinylcarbonylamino group. In a preferred embodiment of the present invention, R1 is a hydrogen atom; an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independent^ from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkox3'carbonyl group, carbozxyalkoxy group and alkoxycarbonylalkoxy group), aikylthio group, alkylsulfonyl group, alkenyl group, amino group, mono- or di-alkylamino group, tetrazolyl group, carbamoyl group, mono- or di-alkylcarbamoyl gro-up (said mono- or di-alkylcarbamoyl group is optionally substituted by-.l^to 3 substituents selected independently from carboxyl group and alkoxyca_rbonyl group) , alkanoylamino group (said alkanoylamino group is optiorxally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, hydroxy group and halogen atom), halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted bj' 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonsrl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), ph_enyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl groxip, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), morpholinyl group optionally substituted by oxo group, piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independent^ from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbo^lalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), pyrrolidinyl group (said pynrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), and pyrimidinyl group (said pyrimidinyl grouip is optionally substituted by 1 to 3 substituents selected independently from carboxyalkyl group, alkoxycarbonylalkyl group, carboxya-lkoxy group and alkoxycarbonylalkoxy group); a carbamoyl group optionally substituted b3' alkoxy group; a dihydrooxazolyl group optionally substituted by 1 to 2 substituents selected independently ifrom carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonjylalkyl group and hydroxyalkyl group; a dihydroimidazolyl group optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; a dihydrooxazinyl group optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl gr-oup, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; mono- or di-alkylcarbamoyl group optionally substituted by 1 to 5 sixbstituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylamino group, morpholin}^ group, pyridyl group, cycloalkyl group (said cj^cloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); an alkyl group optionally substituted by 1 to 5 substituents selected independent^ from halogen atoim, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, aocnino group, mono-or di-alkylamino group, morpholinyl group, pyridyl gromp, cycloalkyl group (said cj^cloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 suh>stituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); an alkanoyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy gxoup, amino group, mono- or di-alkylamino group, morpholinyl gromp, pyridyl group, cycloalkyl group (said cj^cloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, aikoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, aikoxycarbonyl group, halogen atom, amino group and hydroxy group); a morpholinylcarbonyl group ; a piperazinylcarbonyl group optionally substituted by alkyl group, carboxyalkyl group or alkoxycarbonj'lalkyl group; a pyrrolidinylcarbonyl group optionally substituted by 1 to 3 substituents selected independently from carboxyl group, aJkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group; or a piperidinylcarbonyl group optionally substituted by 1 to 3 substituents selected independent^ from carboxyl group, aikoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group; R5 is a saturated or unsaturated 5- to 8-membeired heterocj^clic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms; wherein said heterocyclic group is substituted by 1 to 4 substituents selected from the following groups, or said ineterocyclic group is substituted by 1 to 4 substituents selected from the following groups along with a halogen atom, an oxo and/or hydroxy group: cyano group; nitro group; carboxyl group; sulfo group; cycloalkyl group optionally substituted b}^ carboxyl or alkoxycarbonj'l group; C3-10 alkyl group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, caxboxyl group, alkoxycaxbonyl group, tetrazolyl group, mono- or di-alkylcarbamoyl group, alkoxy group (said alkoxy group is optionally substituted by phenyl, carboxyl or hydros group), alkanoyl group, alkanoyloxy group, aikylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group optionally substituted by carboxjd or altcoxy group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxirairyl group, dioxolanyl group optionally substituted by alkyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, pyrrolidinyl group optionally substituted by alkoxycarbonylaLkyl or carboxyalkyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidusyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperazin3rl group optionally substituted by alkyl group, hexahydroazepinyl group, morpholinyl group, and piperidinyloxy group optionally substituted "by alkyl group; alkenyl group optionally substituted by a group selected from cyano group, hydroxy group, carboxjd group, benzyloxycarbonyl group, and tetrazolyl group; alkenyloxy group optionally substituted by carboxyl group; C3-10 alkoxy group; alkoxy group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, tetrazolyl group, carbamoyl group, mono- or di-alkylcarbamoyl group (said mono- or di-alkylcarbamoyl group is optionally substituted by carboxyl, alkoxycarbonyl or hydroxy group), alkoxy group (said alkoxy group is optionally substituted by carboxjKL formyl or hydroxy group), alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, aminosulfon}?! group, amino group, mono- or di-alkylamino group substituted by carbox3rl or alkoxy group, mono- or di-alkylsuHam^lamino group, mono- or di-adkylureido group optionally^* substituted by morpholinyl group, cycloalkyl group optionally substituted by carboxyrnethyl group, oxiranyl group, phenyl group optionally substituted b}' alkoxy or carboxyl group, morpholinyl group, pyrrolidinyl group optionally substituted b3' alkoxycarfoonyl or carboxyl group, pyrrolidinyl group optionally substituted by allcoxycarbonylalkyl or carboxyalkyl group, pyrrolidinyl group substituted by oxo group, piperidinyl group optionally substituted by alkoxycarfc>on3rl or carboxyl group, piperidinyl group optionally substituted by alkzoxycarbonj'lalkyl or carboxyalkyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepkryl group, pjiimidinyl gro"up, pyridyl group, dioxolanyl group optionally substituted by alkyl group, oxadiazolyl group optionally substituted by oxo group, oxathiiadiazolyl group optionally substituted by oxo group, pyrrolidinylcarbonji. group optionally substituted by carboxyl group, piperidk^loxy group optionally substituted by alkyl group, and morpholinylcarbonj^l group; alkoxycarbonyl group optionally substituted by phenol group; carbamoyl group; mono- or di-alkylcarbamoyl group optionally substituted by a group selected from carboxyl group, morpholinyl group and alkoxy group; hjrdroxycarbamimidoj'l group; alkylthio group optionally substituted by a groiip selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamoyl group; alkylsulfinyl group; alkylsulfonyl group optionally substituted by a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group and mono- or di-alkylcarbamoyl group; amino group; mono- or di-alkylamino group optionally substituted by a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino-group and moirpholinyl group; mono- or di-alkanoylamino group optionally substituted by a group selected from hydroxy group, alkoxy group, cajrboxyl group and amino group; mono- or di-alkylcarbamoylamino group optionally substituted by alkoxy group; morphoHnylcarbo^lamino group; sulfarnoyl group; mono- or di-alkylsulfamoyl group; alkanoyl group optionally substituted by a groiap selected from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group and morpholinyl group; or* a group selected from the following groups: wherein X* and X3 are independently CH2, NK, O, S, SO or SO2; X2 and X5 are independently CH2> 0, S, SO or S02; Xl« is NH, O, S, SO or S02; and n, o, p, q and r are independently an integer of 1 to 4, wherein each group of the above formula is optionally substituted by a substituent(s) selected from the following gromps: carboxyl group, hydroxy group, cyano group , oxo group, alkyl group, hydroxyalkyl group, alkoxycarbonylalkyl group, carboxyalkyl group, morphoHffylalkyl - group, phen3'lalkyl group, alkanoyl groups-:: hydroxyalkanoyl group, alkoxyalkanoyl group, alkoxy group, phenylalkoxy group, alkoxycarborryl group, benzyloxycarbonyl group, mono- or di-alkylamino group, mono- or di-alkylcarbamoyl group, mono- or di-alkylsulfamoyl group, alkylsulfonyl group and tetrazofyl group; R6, R7, R8 and R9 are independently a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a cyano group, an alkyl group, an alkoxy group, or a mono- or di-alkylamino group, wherein said alkyl, alkoxy and mono- or di-alkylamino groups are optionally substituted by 1 to 6 substituents selected independently from halogen atom, hydroxy group, alkoxy group, alkylthio group, amino gxoup, nitro group, cyano group, oxo group, carboxyl group, alkoxycarbonyl group and mono- or di-alkylamino group; or R6 and R7, or R7 and R8, or R8 and RP nnay combine at the ends to form an alkylene group which alkylene group ma}' contain 1 to 3 heteroatoms selected independent from nitrogen, siilfur and oxygen atoms; R10 is aji aromatic monocyclic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms; wherein the rnonoc3'clic aromatic ring is optionally substituted by 1 to 4 substituents selected independently from halogen atom, carboxyl group, alkoxycarbonyl group, carbamoyl group, mono- or di- alkylcarbamoyl group, alkyl group, alkoxy group, hydroxy group, nitro group, cyano group, amino grou_p, mono- or di-alkylamino group, alkanoyl group, alkylthio group, tetrazolyl group and dihydrooxazolyl group, wherein the alkyl, alkoxy, mono- or di-alkylamino, mono- or di- alkylcarbamoyl, alkanoj'l and alkylthio groups are optionally substituted by a substituent(s) selected independently from halogen atom, and hydroxy, alkoxy, amino, morpholrrtyl, piperidinyl, pyrrolidinyl, piperazinyl, alkylpiperazinyl and alkanoylpiperazinyl groups. Furthermore, in the preferred compounds, the "aromatic monocyclic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a phenyl group, a pyridyl group, a pyrimidinyl group, a furyl group or a thienty group; and the "saturated or unsaturated 5- to 8-membered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a pyrimidktyl group, a pyridyl group, a triazolyl group, a tetrazolyl group, a oxadiazolyl grou_p, a dihydropjoimidinyl group, a pyrazinyl group, a thiazolyl group, an oxazolyl group, an imidazolyl group, a dihydrooxazinyl group, a dihydropyrazinyl group or a pyrazolyl group. In more preferred compounds, R1 is a hydrogen atom; an alkoxycarbonyl group optionally substituted bj^ 1 to 5 substituents selected independent^ from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylaxtiino group, halogen atom, carboxyl group, alkoxy carbonyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), alkylthio group, alkylsulfonyl group, alkenyl group, amino group, mono- or di-edkylamino group, tetrazolyl group, carbamoyl group, mono- or di-alkylcaxbamoyl group (said mono- or di-alkylcarbamoyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group and alkoxycarbonyl group) , alkanoylamino group (said alkanoylarnino group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, ttydroxy group and halogen atom), halogen atom, cj'cloalkyl group (said cycloalkyl group is optionally substituted b3' 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxj^carbonylalkoxy group), phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), morpholinyl group optionally substituted by oxo group, piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonjd group, carboxyalkyl group, alkoxycarbonylalkyl group and carboxyalkoxy group, alkoxycarbonylalkoxy group), pyrrolidinyl group (said pyrrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylarriino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), and pyrimidinyl group (said pyrirnidinyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyalkyl group, alkoxycarbonjrlalkyl group and carboxyalkoxy group, alkoxycarbonylalkoxy group); dihydrooxazofyl group optionally substituted by 1 to 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; or a mono- or di-allcylcarbamoyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylamino group, morpholinyl group, pyridyl group, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxryl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); R2 is am alkyl group; R3 is a hydrogen atom; R4 is an alkylene group; R5 is a heterocyclic group selected from pyrimidinyl group, pyridyl group, triazolyl group, tetrazolyl group, oxadiazolyl group, dihydropyrimidinyl group, pyrazinyl group, thiazolyl group, oxazolyl group, imidazolyl group, dibydrooxazinyl group, pyrazotyl group and dihydropyrazinyl group, wherein said heterocyclic group is substituted by 1 to 4 substituents selected from the following groups, or~ 1 to 4 substituents selected from the following groups and oxo group: cyano group; nitro group; carboxyl group; sulfo group; C3-10 alkyl group; alkyl group substituted by a groxip selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, tetrazolyl group, mono- or di-alkylcarbairxoyl group, alkoxy group (said alkoxy group is optionally substituted b>y phenyl, carboxyl or hydroxy group), alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group optionally substituted by carboxyl or alkoxy group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted b}^ rnorpholinyl groxip, oxiranyl group, dioxolanyl group optionally substituted by alkyl group, pyrrolidktyl group optionally substituted by alkoxycarbonyl. or carboxyl group, pyrrolidinyi group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperidinyl group optionally substituted b}^ alkoxycarbonyl or carboxyl group, piperidinyl group optiona^y substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepinyl group, morpholinyl group, and piperidinyloxy group optionally substituted by alkyl group; alkenyl group optionally substituted by a group selected from cyano group, hydroxy group, carboxyl group, benzyloxycarbonyl group, and tetrazolyl group; alkenyloxy group optionally substituted by carboxyl group; C3-10 alkoxy group; alkoxy group substituted, by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, tetrazolyl group, carbarnoyl group, mono- or di-alkylcarbamoyl group optionally substituted t>y hydroxy group, alkoxy group optionally substituted bj' carboxyl or hydroxy group, alkanoyloxy group, alkylthio group, alkylsulfon3>l gromp, alkylsulfinyl group, aminosulfonyl group, amino group, mono- or di-alkylamino group substituted by carboxyl or alkoxy group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, cycloalkyl group optiorxally substituted by carboxymethyl group, oxiranyl group, phenyl group optionally substituted by alkoxy or carboxyl group, rnorpholinyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, pyrrolidinyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, pyrrolidinyl group optionally substituted by oxo group, piperidinyl group optionally substituted b}^ alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarboriylalkyl or carboxyalkyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepinyl group, pyrimidinyl group, pyridyl' group, dioxolanyl group optionally substituted by alkyl group, oxadiazolyl group optionally substituted b3^ oxo group, oxathiadiazolyl group .^optioaaUy substituted by oxo group, pyrrolidinylcarboriyl. grojutp optionally substituted by carboxyl group, piperidinyloxy group optionally substituted by alkyl group, and morpholinylcarbonyl group; alkoxycarbonyl group optionally substituted by phenyl group; carbamojd group; mono- or di-alkylcarbamoyl group optionally substituted by a group selected from carboxyl group, morpholinyl group and alkoxy group; hydroxycarbamimidoyl group; alkylthio group optionally substituted by a group selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamoyl group; alkylsulfinyl group; alkylsulfonyl group optionally substituted b}' a group selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamo3>l group; amino group; mono- or di-alkylamino group optionally substituted b3' a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group and morpholin}d group; alkanoylamino group optionally substituted by a group selected from hydroxy group, alkoxy group, carboxyl group and arnino group; mono- or di-alkylureido group optionally substituted by alkoxy group; morpholinylcarbonylarnino group; sulfamoyl group; mono- or di-alkylsulfarnoyl group; morpholinyl group optionally substituted by a group selected from oxo group and carboxyl group; optionally oxidized thiomorpholinyl group; piperazinyl group optionally substituted bjr a group selected from cyano group, alkyl group, lydroxyalkyl group, alkoxycarbohylalkyl group, carboxyalkyl group, alkanoyl group, hydroxyalkano3d group, alkoxyalkanoyl group, benzyloxycarbonyl group, mono- or di-alkylcarbamoyl group, mono- or di-alkylsuifamoyl group, alkylsulfozxyl group and tetrazolyi group; piperidinyl group optionally substituted by a group selected from carboxyl group, hycLroxy group, oxo group, alkyl group, hydroxyalkyl group, carboxyalkyl group, alkanoyl group, alkoxy group, phenylalkoxy group, alkoxycarbonyl group and alkoxycarbonylalkyl group; pyrrolidinyl group optionally substituted by a group selected from oxo group, carboxyl group, alkanoyl group and mono- or di-alkylarnino group; pyrrolinyl group optionally substituted by oxo group; hexahydrodiazepinyl group optionally substituted by alkanoyl group; diazolidinyl group optionally substituted by oxo group; dioxolanyl group op"tionally substituted by alkyl group; pyridyl group optionally substituted by carboxyl group, hydroxy group or h}rdroxyalkyl group (said pyridyl group is optionally further oxidized); tetrazolyl group substituted by hydroxy group or alkyl group that is optionally substituted b3>" morpholinyl group; dihj'drooxadiazolyl group optionally substituted by oxo group; dihydroimidazolyl group; dihydrooxazolyl group; oxazolidinj'l group optionally substituted by oxo group; tetrahydropyridyl group optionally substituted by benzyl group; pyrimidinyl group; tetralydropyranyl group; piperidinyloxy group optionally substituted by a group selected from alkyl group, carboxyl group, carboxyalkyl group and alkanoyl group; pyrrolidinyloxy group optionally substituted by a group selected from alkyl group, carboxyl group, carboxyalkyl group and alkanoyl group; tetrahydropyranyloxy group; tetrahydrofui;anyloxy group; optionally oxidized thianyloxy group; morpholinylcarbonyl group; piperazinylcarbonyl group optionally substituted by a group selected from alkanoyl group and atkyl group; and pyrrolidixrylcarbonyl group; R6 and R9 each are a hydrogen atom; R7 and R8 are independently a hydrogen atom, an alkyl group optionally substituted Toy halogen atom, an alkoxy group, a mono- or di-aikylamino group or halogen atom; or R7 and R8 combine at the ends to form an alkylenedioxy group; and R10 is a pherxyl or pyridyl group, which phenyl or pyridyl group is optionally substituted "by 1 to 4 substituents selected from alkyl group optionally substituted toy halogen atom, alkoxy group, hydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. In further preferred compounds, R1 is an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independently from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group and alkoxycarbonyl group), alkenyl group, halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylaLkyl group), phenyl group (said phenyl group is optionally substituted "by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonjd group, carboxyalkyl group and alkoxycarbonylalkyl group), piperidinyl group (said piperidinyi. group is optionally substituted by 1 to 3 substituents selected independently from hydroxy gro up, halogen atom, carboxyl group, alkoxycarbo my 1 group, carboxyalkyl group and alkoxycarbonylalkyl- group), aftd pyrrolidinyl group (said p3?rrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from Itydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, cart>oxyalkyl group and alkoxycarbonylalkyl group); or a dihydrooxazolyl group optionally substituted by 1 or 2 substituents selected independently from carboxyl group, alkoxycarbonyl gxoup, carboxyalkyl group, alkoxycarbonylalkjd group and hydroxyalkyl group; R5 is a pyrimidin3>"l group, a pyridyl group, a triazolyl group, a tetrazolyl group, an oxadiazolyl grou.p, a dihydrop3>rimidin3>l group, a pyrazinyl group, a thiazolyl group, an oxazolyl group, a dihydrooxazinyl group, a pyrazolyl group or a dihydrop3>razinyl group, said group being substituted by 1 to 4 substituents selected from, the following groups: cyano group; nitro group; carboxyl group; sulfo group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, a_lkoxy group optionally substituted by carboxyl or hydroxy group, alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsixlfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkj^isulfamoylamino group, mono- or di-alkylureido group optionally substituted by morphiolinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidmyl group optionally substituted by alkoxycarbonyl or oarboxyl group, piperazin3rl group optionally substituted by alkyl group, hexahydroazepinyl group and morpholinyl group; alkenyl group optionally substituted b3' carboxyl group, cyano groxip or benzyloxycarbonyl group; alkoxy group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group optionally substituted by carboxyl or hydroxy group, alkano3^1oxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylaxnino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolan}^ group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperazinyl group optionally substituted b3^ alkyl group, hexahydroazepinjd group and morpholinjd group; alkoxycarbonj^l group optionally substituted by phenyl group; mono- or di-alkylcarbamojd group optionally substituted by carboxyl group; hydroxycarbam_iinido3>"l group; alkylthio group; alkylsulfLnyl group; alkylsulfonyl group optionally substituted by carboxyl group; mono- or di-alkrylamino group optionally substituted by hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group or morpholinyl group; mono- or di-alkylsulfamoyl group; morpholinyl group; optionally oxidized thiomorpholinyl group; piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; piperidinyl groiip optionally substituted by a group selected from carboxyl group, alkyl group and alkoxycarbonyl group; dioxolan34 grou_p optional^ substituted by alkyl group; tetrazolyl group optionally substituted by alkyl group, hydroxy alkyl group or morpholinylalkyl group; ■* dihydrooxadiazolyl group optionally substituted b3' oxo group; pyriinidinyl group; or tetrahydropyranyl group; and R10 is a phenyl or pyridyl group, which phenyl or pyrid}'! group is optionally substituted by 1 to 4 substituents selected from alkyl group optionally substituted by halogen atom, alkoxy group, hydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. Another embodiment of the present invention include compounds of the formula (I) wherein R5 is a. group of the formula: wherein Ring A is a saturated or unsaturated 5- to 8-membered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, and Ru is a group selected from the following groups: cyano group; nitro group; carboxyl group; sulfo group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by phenyl, hydroxy or carboxyl group), alka_noyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted "by morpholuryl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted t>y alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted bj? alkoxycarbonyl or carboxyl group, piperazkryl group optionally substituted by alkyl group, hexahydroazepnryl group and morpholinyl group; alkenyl group optionally substituted by carboxyl group, cyano group or benzyloxycarbonyl group; alkoxy group substituted by a group selected from halogen atom, C3^ano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by phenyl, hydroxy or carboxyl group), alkano3>loxy group, alkylthio group, alkylsulfonyl group, allcylsulfinyl group, amino group, mono- or di- alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkylclioxolanyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, pipera^inyl group optionally substituted by alkyl group, hexahydroazepinyl group and morpholinyl group; alkoxycarbonyl group optionally substituted by phenyl group; mono- or di-alkylcarbairaoyl group optionally substituted by carboxyl group; hydroxycarbamimidoyl group; alkylthio group; alkylsulfinyl group; alkylsulfon}'! group optionally substituted by carboxyl group; mono- or di-alkylatnino group optionally substituted by hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di- alkylamino group or morpholinyl group; mono- or di-alkylsulfamoyl group; morpholinyl group; optionally oxidized thioirxorpholinyl group; piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; pyrrolidinyl group optionally substituted by carboxyl group, carboxyalkyl group, alkyl group, alkoxycarbonyl groiap or alkoxycarbonyla_Ucyl group; piperidinyl group optionally substituted by carboxyl group , carboxyalkyl group, alkyl group, alkoxycarbonyl gro xxp or alkoxycarbonyletlkyl group; dioxolanyl group optionally substituted by alkyl group; tetrazolyl group optionally substituted by alkyl group, hydroxyalkyl group or morpholinylalkyl group; dihydrooxadiazolyl group optionally substituted by oxo group; pyrimidinyl grouip; or tetrahydropyranyl group; which compound is shown by the formula (I-A): wherein each symbol has the same meaning as defined above. More preferred embodiment includes compounds of the formula (I) wherein R1 is a hydrogen atom; an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independently from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independent^ from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkoxy group and alkoxyoarbonylalkoxy group), alkylthio group s alkylsulfonyl group, alkenyl group, amino group,,. apapjao- or di-alkylamino group, tetrazolyl group, carbamoyl group, mono- or di-alkylcarbamo}?i group (said mono- or di-alkylcarbarnoyl group is optionally substituted by L to 3 substituents selected independently from carboxyl group and alkoxycarbonyl group) , alkanoylamino group (said alkanoylamino group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycaxbonyl group, hydroxy group and halogen atom), halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycaxbonyl group, carboxyalkyi group, alkoxycarbonylalkyl groutp, carboxyalkoxy group and alkoxycarbonylalkoxy group), phenyl group (sa_id phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyi group, alkoxycarbonylalkyl group, carboxyalkoxy group and aJkoxycaxbonylalkoxy group), morpholinyl group optionally substituted t>y oxo group, piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyi group, alkoxycarbonjdalkyl group and carboxyalkoxy group, alkoxycarbonylalkoxy group), pyrrolidinyl group (said pyrrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen, atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyi group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), and pyrimidinyl group (said pyrimidinyl group is optionally substituted by 1 to 3 substituents selected independent^ from carboxyalkyi group, alkoxycarbonylalkyl group and carboxyalkoxy group, alkoxycarbonsrlalkoxy group); dihydrooxazofyl group optionally substituted ■ — by 1 to 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; or a mono- or di- alkylcarbamoyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylamino group, morpholinyl group, pyridyl group, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen, atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, slkoxycarbon3>l group, halogen atom, amino group and hydroxy group); R2 is an alkyl gromp; R3 is a hydrogen atom; R4 is an alkylene group; Ring A and R" are the same groups as defined above; R6 and R9 each are a hydrogen atom; R7 and R8 are independently a hydrogen atom, an alkyl group optionally sbustituted by halogen atom, alkoxy group, or mono- or di-alkylamino group; or combine at the ends to form an alkylenedioxy group; and R10 is a phenyl or pyridyl group, which phenyl or pyridyl group is optionally substituted by 1 to 4 substituents selected from alkyl group optionally substiuted by halogen atom, alkoxy group, hydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. Another preferred embodiment includes compounds of the formula (I) wherein Ring A is a saturated or unsaturated 5- to 8-me'rnbered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfiar and nitrogen atoms, and R*1 is a group selected from the followings groups:. cyano group; nitro group; carboxyl group; sulfo group; alkyl group substituted by a group selected from halogen atom, hydroxy group, carboxyl group, alkoxycaLrbonyl group, alkoxy group optionally substituted by phenyl or hydroxy group, alkaz^loxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionalfy substituted b}' morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted b}' alkoxycarbonyl or carboxyl group, piperazinyl group optional^ substituted by alkyl group, hexahydroazepinyl group and morpholinyl group; alkenyl group optionally substituted bjr carboxyl group or benzyloxycarbonyl group; alkoxy group substituted by carboxyl group, Itydroxy group, alkoxy group, alkylthio group, alkylsulfonyl group or alkoxyphenyl group; alkoxycarbonyl group optionally substituted by phenyl group; mono- or di-alkylcarbamojd group optionally substituted by carboxyl group; hydroxycarbamimidoyl group; alkylthio group; alkylsulfinyl group; alkylsulfonyl group optionally substituted by alkoxycarbonyl group; mono- or di-alkylamino group optionally substituted by hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group or morpholinyl group; mono- or di-alkylsulfamoyl group; morpholktyl group; optionally oxidized thiomorpholin3rl group; piperazinyl group optionally substituted bj' a group selected from alkyl group, alkanoyl group and hydroxy alkanoyl group; piperidinyl group optionally substituted by carboxyl group, alkyl group or alkoxycarbonyl group; dioxolanyl group optionaHy substituted by alkyl group; tetrazolyl group substituted "by alkyl group, hydroxyalkyl groxip or morpholinylalkyl group; dihydrooxa-diazolyl group optionally substituted by. oxo group; pyrimidinyl group; or tetrahydropyranyl group. More preferred embodiment herein includes compounds of the formula (I) wiferein W is an alkoxycarbonyl group optionally substituted by^'"**' a group selected from hydroxy group and alkoxy group; or a dihydrooxazolyl group optioxially substituted by hydroxyalkyl group; R2 is an alkyl group; R3 is a hydrogen atom; R* is an alkylene group; Ring A and R11 are the same groups as defined above; R6 and R9 each are a hydrogen atom; and R7 and R8 are independently a hydrogen atom, an alkyl group optionally sbustituted by 1 to 9 halogen atoms, an alkoxy group, or a mono- or di- alkylarnino group; or combine at the ends to form an alkylenedioxy group; R10 is a phenyl or pjTidyl group, which phenyl or pyridyl group is optionally substituted by 1 to 4 sut>stituents selected from alkyl group optionally substiuted by 1 to 9 halogen atoms, alkoxy group, hydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. Examples of Ring A include a pjTimidinsd group, a pj'ridyl groxip, a triazolyl group, a tetrazolyl group, an oxadiazolyl group, a dihydropyrimidinyl group, a pyrazinyl group, a thiazolyl group, an oxazolyl group, a dihydrooxazinyl group, an imidazolyl group, a pyrazolyl group, a dihydropyrazinyl group, and the like. More preferred compounds include those wherein Ring A is a pyrimidinjd group, a pyridy^l group, a tetrazolyl group, an oxadiazolyl group, a pyrazinyl group, a thiazolyl group or an oxazolyl group; and Ru is a carboxyl group; a cyano group; a nitro group; an alkyl group substituted by a group selected from hydroxy group, cyano group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, hydroxyalkoxy group, cart>oxyalkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino.group, mono- or di-alkylamino group, mono- or di-allg4sulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanjd group, pyrrolidinyl group optionally substituted by carboxyl group, piperidinyl group optionally substituted by carboxyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted t>y a group selected from hydroxy group, cyano group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, hydroxyalkoxy group, carboxj^alkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylarnino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxola^l group, P3>xrolidinyl group optionally substituted by carboxyl group, piperidinyl group optionally substituted by carboxyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; an alkoxycarbonyl group; a hydrox3^carbamimido3d group; alkylthio group; an alkylsulfonyl group optionally substituted by carboxyl group; a mono- or di-alkylamino group optionally substituted b3' hydra?^ group, carboxyl group, alkoxy group or mono- or di-alkylamirxo group; a morpholinyl group; an optional^ oxidized thiomorpholinyl group; a piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; a pyrrolidinyl group optionally substituted by carboxyl group, alkyl group carboxyalkyl group or alkoxycarbonyl group; a piperidinyl group optionally substituted by carboxyl group, alkyl group, carboxyalkyl group or alkoxycarbonyl group; a tetrazolyl group optionally substituted by alkyl group, hydroxyallsyl group, or morpholkiylalkyl group; an oxodihydrooxadiazolyl group; a pyrimidinyl group; or a tetrahydropyrao^yl group. Still more preferred compounds include those wherein R* is an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independently from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group and alkoxycarbonyl group), alkenyl group, halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbo^lalkyl group), phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), and pyrrolidinyl group (said pyrrolidinyl gr~oup is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group); or a dUrydrooxazolyl group optionally substituted by 1 or 2 substituents selected independent^ from carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; R*° is a phenyl group substituted by 1 to 3 substituents selected from alkyl group optionally substituted by halogen atom, alkoxy group, halogen atom and cyano group; Ring A is a pyrimidinyl group, a pyridyl group, a tetrazolyl group, an oxadiazofyl group or a thiazoiyl group; and Rn is a carboxyl group; a cyano group; a nitro group; an alkyl group substituted by a group selected from tiydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, carboxyalkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, piperazinyU group optionally substituted by alkyl group and morpholinyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted b}' a group selected from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl gromp, alkoxy group, phenylalkoxy group, carboxyalkoxy group, alkyltlxio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; a hydroxycarbamimidoyl group; an alkylthio group; an alkylsulfonyl group optionally substituted by alkoxycarbonyl group; a mono- or di-alkylamino group optionally substituted bj' hydroxy group, carboxyl group or alkoxy group; a morpholinyl group; optionally oxidized thiomorpholinyl group; a piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; a pyrrolidinyl group optionally substituted "by carboxyl group, alkyl group carboxyalkyl group or alkoxycarbonyl group; a piperidinyl group optionally substituted by carboxyl group, alkyl group, carboxyalkyl group or alkoxycarbonyl group; a tetrazolyl group optionally substituted by alkyl group, hydroxyalkyl group, or morpiiolinylalkyl group; an oxodihydrooxadiazolyl group; a pyrimidinyl group; or a tetraliydropyranyl group. Still furthermore preferred compounds include those wherein R1 is an alkoxycarbonjd group optionally substituted by 1 or 5 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, hydroxy group and cycloalkyl group; R10 is a phenyl group substituted by 1 to 3 substituents selected from cyano group, alkyl group optionally substituted by halogen atom and alkoxy group; Ring A is a pyrimidinyl group, a pyridyl group, a tetrazolyl group or an oxadiazolyl group; - ■—-■■- R11 is a carboxyl group; an alkyl group su"bstituted by hydroxy group, carboxyl group, alkoxy group or alkylsulfonyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted by cyano group, carboxyl group, hydroxy group, alkoxy group, alkylthio group or alkylsulfonyl group; a mono- or di-alkylamino group optionally substituted by carboxyl group or alkoxy group; a morpholinyl group; a piperidinyl group substituted by carboxyl group; or a tetrazolyl group substituted by hydroxyalkyl group; R7 is an alkyl group optionally sbustituted by halogen atom, alkoxy group, or mono- or di-alkylamino group; and R8 is a hydrogen atom. Especialfy preferred compounds include those wherein R1 is an ethoxycarbonjd group, a hydroxyethoxycarbonyl group, a 2-fluoroethoxycarbonyl group, a 2,2-difLuoroeth.oxycarbonyl group or a 2,2,2-trifluoroethoxycarbonyl group; R2 is an ethyl group; R10 is a phenyl group substituted b}' 1 to 2 substituents selected from cyano group, trifluoromethyl group and methoxy group; Rr is a trifluoromethyl group or a methoxy group. In this regared, other examples of especially preferred compounds include those wherein R1 is a carboxy(C2-ioalkoxy)carbonyl group or an alkoxycarbonyl(C2-ioalkoxy)caxbo:nyl group, and R2, R10 and R7 are the same above. Especially more preferred compounds include those wherein R1 is an ethoxycarbonyl group or a hydroxyethoxyca_xbonyl group; R2 is an ethyl group; R10 is a phenyl group substituted by 1 to 2 substituents selected from cyano group, trifluoromethyl group and methoxy group; R7 is a trifluoromethyl group or a methoxy group. Most preferred compounds include those listed below. (2R,4S)-4-{[3,5-Bis(txmuoromethyl)benzyIH^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydxo-2H-quinoline-1 -carboxylic acid ethyl-tester; (2R,4S)-4-[[3,5-Bis(taifluorom amino}pyrimidin-2-yl)]an^ quinoline-1-carboxylic acid ethyl ester; (2R?4S)-4-{[3,5-Bis(txifluoromefo^ 2-yl]}amino-2-ethyl-6-trifluoromethyl"3,4-dihydrc> -2H»quinoline-1- carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromefoyl)ben^ 2-ethyl-6-trifl"uoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trinuoromethyl)be^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4»dihydro-2 H-quinoline- 1-carboxylic acid ethyl ester; (2R,4S)-4-([3,5-Bis(trmuoromethyl)benz}d]"{5-[2-(2-hydroxyethyl)-2H- tetrazol-5-yl]pyrimidin-2-yl})ainino-2-ethyl-6-triflTuoromethyl-3,4-dihydro- 2H-quinoline-1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trffluorome^^ 3d]}ainino-2-ethyl-6-methoxy-3f4-dih3^dro-2H-quirioline-1 -carboxylic acid ethyl ester; (2R,4S)-4-{(3,5-Dimethoxybenzyl)-[5-( 2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinolixLe-1 -carboxylic acid ethyl ester; (2R,4S)-4-{(3,5-Dicyanobenzyl)-[5-(mor^ ethyl-6-trifluoromethyl-3,4»dihydro-2H-quinoline» 1 -carboxylic acid ethyl ester; (2R,4S)-4-{(3-Cyanoben2yl)-[5-(moi^ ethyl-6-trifluoromethyl-3>4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester; (2R*,4S*)-4-([3,5-Bis(trifluoromethyl)benzyl]-{5-[2-(2-hydroxyethyl)-2H- tetra2ol-5-34]p5n-iinidin-2-yl})amino-2-ethyl-6-methoxy-3,4-dihydro-2H quinoline-1-carboxj^lic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trinuorom 5-34]}ainino-2-ethyl-6-trifluoromethyl-3,4niih3'dro-2H-quinoline-1 -carboxylic acid ethyl ester; (2R,4SH-{[3,5-Bis(txffluoromet^ 2H-te1xa2ol-5-yl]}amino-2-ethyl-6-trifluioromethyl-3,4-dihydro-2H-quinoline-1-carbo^lic acid ethyl ester; (2R,4S)-4-{(3-Cyano-5-1xifluorom 2-yl]}amino-2-ethyl-6-iTifluoromethyl-3J4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2^4S*)-4-{[3,5-Bis(trffluorome&y^^ 2-34]}amino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro»2H-quinoline-1 -carboxylic acid 2-hydroxyethyl ester; (2R,4S)-4-{[3,5-Bis(txifluoromethyl)benzyl]-[5-(4-carboxyp3^peridin-l-yl)pyrimidin-2-yl]}arnino-2"eth3d-6-ine1:hoxy-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester; (2R,4S)-4-{(3-C3'ano-5-trifluoromet^ 2-yl]}amino-2-ethyl-6-trifluorometh3;'l- 3,4-dihydro-2H-quinoline-1 -carboxs^lic acid ethyl ester; (2R,4S)-4-[[3,5«Bis(trifluoromethyl)benzyl]«(5-{[methyl«(2-carbo^ethyl)]amino)pyrimidin-2-yl)]axnino-2-eth3d-6-trifluoromethyl-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethy^ 2-yl]}amino-2-ethyl-6»trifluoromethyl» 3,4-dihydro-2H-quinoline-1 -caxboxylic acid ethyl ester; (2R,4S)-4-([3,5-Bis(trifluorom propoxy]p3oimidin«2-yl})amino-2-eth3^1-6-iTifluorome1±Lyl-3?4^ quinoline-1-carboxylic acid ethyl estex; (2R,4S)-4-{[3,5-Bis(1xifluorometiiyl)beri2yl]-[5-(4-carboxybuto^)p3n^ 2-yl]}ammo-2-ethyl-6-txifluoro carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(txffluoromethyl^ pyrimidin-2-yl]}ammo-2-^ 1-carboxylic acid ethyl ester; (2R,4S)«4-{[3,5-Bis(trifluoromethyl)h>en2yl]-[5«(2"Carboxyetho^)pyrimidin-2- jd]}amino-2 -ethyl-6-trifluoromethyl- 3,4-dihj^dro-2H-quinoline-1 -carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trffluorometh^^ yl)pyrimidin-2-3d]}amino-2-eiiiyl-6-trifluoromethyl-3,4-dihydro-2H- quinoline-1 -carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)b^ yl]}amino-2 -ethyl-6-trifluoromethyl- 3,4-dihydro-2 H-quinoline-1 -carboxylic acid ethyl ester; (2R)4S)-4-{[3,5-Bis(1iifluoromethyl)lDen^l]-[5-(4-carboxybuto^)pyridin-2- yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dih3'dro-2H-quinoline- 1-carboxylic acid ethyl ester; (2R,4S)-4-{(3-Cyano~5-trifluoromet^ pyriinidin-2-yl]}ainino-2-ethyl-6-triJQuorornethyl-3,4-dihydro-2H-quinolin^ l-carboxj4ic acid ethyl ester; (2R>4S)-4-{[3?5-Bis(trifluoromethyl)benz5d]-[5-(3-carboxypropoxy)pyrimidin- 2"yl]}aminO"2-eth34-6-methoxy-3,4-dihydro-2H-quinoline-l-carbo3Qdic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(1rifluoromethy 2-yl]}amino-2-eth3'l-6-dimethylamixio-3,4-dihydro-2H-quinoline-1 - carbox3^1ic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(txifluorome^ yl)pyrimidin-2-yl]}ainino-2-ethyl-6-trifluoromethyl-3?4-d^ quinoline-1-carboxylic acid 2,2,2-txifluoroethyl ester; (2R>4S)-4-([3J5-Bis(trifluoromethyl)benzyl]-[5-(4-carboxyp3'peridin-l- yl)pyrirnidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H- quinoline-1-carboxtlic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromet^ 2»yl]}amino»2-ethyl-6-trifiuoxomethyl-3 ,4-dihydro-2H-quinoline-1 - carboxylic acid 2,2,2-trifluoroethyl ester; (2R,4S)-4-{(3-Cyano-5-txifluoromethyfo^ pyrimidin-2-3d]}amino-2-ethyl-6-1xifluoromethyl-3,4-dihydro-2H-quin 1-carboxylic acid 2,2,2-trifhxoroethyl ester; (2R,4S)-4-p,5-Bis(txffluorometiiy^ yl)pyrimidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro quinoline-l-carboxj^lic acid 2-hydro3C7ethyl ester; (2R,4S)-4-{[3,5-Bis(trffluoro yl]}amino-2-ethyl-6-1xifluorainethyl-3,4-dih3^dro-2H-quinoline-l-carb acid 2-carboxyeth3rl ester; (2R,4S)-4-{[3,5-Bis(trifluororxiethyl)ben2yl]-[5-(moipholin-4-yl)pyi^ yl]}amino-2-et±iyl-6-trifluoraxne1±i3d-3,4-dihydro-2H-quinoline-l-cajboxyU^ acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(trifluorornet^ yl]}ainino-2-e1±i3^1-6-trifluorc>ineth3d-3,4-dihydro-2H-quinoline-l-caT acid 4-carbo^butyl ester; (2R,4S)-4-{[3,5-Bis(triftuorometlty^^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid 2-caxboxy-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoroxnethyl)ben^d]-[5-(morpholin-4-yl)pyri^ yl]}amino-2-e1±iyl-6-iTifluoroinethyl-3,4-dih3^dro-2H-quinoline-l-ca acid 5-carboxypentyl ester; (2R,4S)-4-p?5-Bis(trmuoro33ie1±iyl)benzyl]-[5-(2-hydro^e1iioxy)pyi^ 2-yl]}amino-2«eth3'l-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 - carboxylic acid 2-carboxyetli34 ester; (2R,4S)-4-{[3J5-Bis(1xifluoroxne1iiyl)beri2yl]-[5-(2-hydro^etiioxy)pyr^ 2-yl]}ainino-2-ethyl-6-iTifluorornethyl-3,4-dihydro-2H-quinolm carboxylic acid 5-carboxypentyl ester; (2R,4S)-4-{[3,5-Bis(txifluoromethyl)ben^ 2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l- carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3?5-Bis(txifluorome^ 2-34]}amino«2"ethyl-6-trifluoromet±iyl-3J4-di]rydro-2H-quinoline-l- carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[33-Bis(trffluoromet^ 2-3rl]}amino-2-eth34-6-txifluoro^ carboxylic acid 4-carboxybutyl ester; (2R,4S}-4-{[3,5-Bis(1xifluorome1iiyl)benzyl]-[5-(3-cyanopropo^)pyrim j4J}ainino«2-etJiyl-6-1xifluoromethyl-3?4-dihyclro-2H-quinoline-l-carb acid 2-carboxyethyl ester; or (2R,4S)-4-{[3?5-Bis(trifluorome1±yl)ben^d]-(5-diinethylaminopyrimidin- yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihy(aro-2H-quinoline-1-carboxs'-lic acid 2-carboxyethyl ester;or a pharmaceutically acceptable salt thereof. Further examples of most preferrred compounds include: (2R,4S)-4-{[3,5"Bis(trifluoromethyl)ben^d]"[5-(2-hydro^ethoxy)pyrimidin-2-3d]}amino-2-ethyl-6-trifluoromethyl-3,4-dihLydro-2H-quinoline-1 -carboxs^lic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5"Bis(trifluoromethyl)ben2yl]-[5-(2-hydroxyet^oxy)pyrimidin-2-34]}amino-2-ethyl"6-trifluoromethyl-3 ?4-dib.3'*dro-2H-quinoline-1 -carbox3^1ic acid 4-carboxybutyl ester; (2R,4S)-4-{[3?5-Bis(trifluorometh3d)be:i^ 2-yl]}amino-2-ethyl-6-trifluoromethyl-3>4«dihiydro-2H-quinoline-l-carboxylic acid 2-carboxy-2-methylpropyl ester; (2R,4S)-4-{I3,5-Bis(trifluorometoyl)ben23d]-[5-(2-methoxyetho^)pyrimidin^ 2-yl]}ainino-2-etiiyl-6-trifluoromethyl-3,4-dil3.ydro-2H»quinolin 1 -- carboxylic acid 2-caxboxy»2-methylprop34 es"ter; (2R,4S)-4-{[3,5-Bis(trifluoro^ 2-}d]}ainino-2-ethyl-6~trifluoromet^^ carboxylic acid 5-carboxypentyl ester; (2R/*S)-4-{[3,5-Bis(trifluoromethyl^^ yl]}amino-2-eth34-6-trifluoromethyl-3,4-dihydxo-2H*quinoline-l-carboxylic acid 3-carboxypropyl ester; (2R?4S)-4-{[33-Bis(1rifluoromefo^ yl]}aunino-2-ethyl"6-trifluorome1iiyl-3,4-dihydxo-2H-quinoUne-l-carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3?5-Bis(trifluoromethyl)ben2yl]-[5- (3-cyanopropoxy)pyrimidin-2- yl]}araino-2-ethyl-6"trifluoromet±iyl"3,4*dihydro-2H«quinoline-l-carbo^ acid 2-carboxy«2»methylpropyl ester; (2R,4S)-4-{J3 ?5-Bis(trifluoromethyl)benz54]- [5- (3-cyanopropo^)pyrimidin-2- yl]}amino-2-ethyl-6-trifluoromethyl-3 ?4-dihy±ro-2H-quinoline-1 -carboxylic acid 5-carboxypentyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh34)benryl]-(5- dimethylaminopyrimidin»2- yl)}ainino-2»ethyl-6-trifluoromethyl-3,4-dihyiro«2H-quinoiine-l-carboxylk acid 3-carbo^propyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^ yl)}ainino-2-ethyl-6-trifluoromethyl-3,4-dihycLro-2H-quinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)b^ yl)}amino-2-ethyl»6-trifluoromethyl-3 )4-dihy(iro«2H-quinoline-1 -carboxylic acid 2-caxboxy-2-methylpropyl ester; (2R,4S)-4-{[3?5-Bis(trifluoromethyfy^ 3^l)}amino-2-ethyl-6-1xifluoromethyl-3,4-dihyciro-2H-quinoline-l-ca^ acid 5-carboxypentyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorometft^^^ 2-yl]}ainino-2-etiiyl-6-txifluorome1±iyl-3?4-dibLydro-2H^ carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoro 2-yl]}ammo-2-ethyl-6-trifl carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethyfo^ 2-yl]}amino-2-ethyl-6-trifluoromethyl"3,4-dihydro-2H-quinoline-1 - carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{(3-Cyano-5-triftuoromethylben^ 2-3d]}amino-2-ethyl-6-trifluoromethyl-3 54-dihydro-2H-quinoline« 1 - carboxylic acid 2-carboxy-2-methylprop3>l ester; (2R,4S)-4-{(3-Cyano-5«trifluoromethylbenzyl)-[5-(2- met±Lo:^ethoxy)pyrimidin-2-y$ dihydro-2H»quinoline-l-carbox3^1ic acid 2-carboxyethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(2- methox3^ethoxy)pyrimidin-2-3d]}amino-2-ethyl-6-trifluororneth3'l-3,4- dihydro-2H-quinoline-l-carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(2- methoxyethoxy)p3^rimidin-2 -3^1]}amino-2 -ethyl-6- trifluoromethyl-3,4- dihydro-2H-quinoline-l-carbox3'lic acid 4-carboxybutyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(2- methoxyeiJioxy)pyrimidin"2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4- dihydro-2H-quinoline-l-carbox3dic acid 2-carboxry-2-methylpropyl ester; (2R,4S)-4-{I3,5-Bis(triflu^^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-carboxyeth3^1 ester; (2R,4S)-4-{[3,5-Bis(tri£luoromethyl)beri^ll-[5-(m(>ipholin yl]}amino-2-eth3^1-6-trifluorometh34-3,4-dihydro-2H»quinoline-1 -carboxylic acid 3-carboxypropyl ester; (2R?4S)-4-{[3,5-Bis(lxmuorome1±^ yl]}amino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluor©m yl]}ainino-2-et3iyl-6-triflu^ acid 2-carboxy-2-methylprop3d ester; (2R,4S)-4-P,5-Bis(triftuorome1^^ yl]}ainino-2 -ethyl-6-trifluoromethyl-3,4-dihydro-2H-quino line-1 -carboxylic acid 2-carboxy-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometftyl)ben^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quino line-1 -carboxylic acid 2-carboxyethyl ester; (2R?4S)-4-{[3,5-Bis(trmuorome1±iyl)benzylj«[5-(2-me&oxye1^oxy)p^^ yl]}amino-2«et±i34-6-txifluorome&yl-3,4-dihydro-2H-quina line- 1-carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(1xffluoromet^ yl]}amino-2-ethyl«6-1xifluorome1±Lyl-3,4"dih3^dro-2H-quinaline" 1 -carboxylic acid 4-carbox}rbutyl ester; (2R)4S)-4-{[3,5«Bis(trmuoromefeyl)benzyl}-[5-(2-methoxyethoxy)p3n^ yl]}arruno-2-etiiyl-6"trifluoromethyl-3,4"dihydrO"2H-qiiinc>line-l" acid 2-carboxy-2-meth3dpropyl ester; (2R,4S)-4-{[3,5-Bis(tTifluoromethyl)benzyl]-[5»(3«cyanopropoxy)pyTidin-2- 34]}amino-2-ethyl-6-trifluoromethyl«3,4-dihydro-2H-quino line-1 -carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[33-Bis(txifluorome1iiyl)ben^l]-(5-dimethylajnainop3Tridin-2- yl)}amino-2-ethyl-6-trifluoromethyl«3,4-dihydro-2H-quinoline-1 -carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3?5-Bis(trifluorome13i3^ yl)}amino-2»eth3^1-6-trifluorometh3d-3,4-dih3^dro-2H-quinoline- 1-carboxylic acid 3-carbox3^propyl ester; (2R,4S)-4-{[3?5-Bis(trifluoromet±^^ yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-qiiinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluoro yl)}amino-2 -ethyl-6«trifluoromethyl«3,4-dihydro -2H-quinoline-1 -carboxylic acid 2-carboxy-2-methylpropyl ester; (2R,4S)-4-{(3-Ctyano-5-trifluorom^ yl]}amino-2 -ethyl-6-trifluoromethyl-3,4-dihydro -2H-quinoline-1 -carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylben^ yl]}amino-2-ethyl-6-1xifluorom acid 3-carboxypropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylberi2yl)-[5-(morpholm yl]}amino-2-ethyl-6-trifluorometh3d-3,4-dihydr> -2H-quinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R>4S)-4-{(3-Cyano-5-txifluorome1±LylberLzyl)-[5-(morpholin-4-yl)p 3^1]}amino-2»eth3d-6-trifluoromethyl-3,4-dihydrc>-2H-quinoUne-l»carbo^lic acid 2-carboxy-2-meth34propyl ester; (2R)4S)-4-{(3-Cyano-5-trifluoromet±Lylben^l)-[5-(2-met±ioxyetho^)pyri^ 2-3d]}amino-2-eth34-6-trifluoromethyl-3 t4-dihyc3.ro-2H-quinoline-1 -carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trmuoromethyl)ben^l)45»(ixiorpholin«4-yl)p3T^midin-2-yl]}amino-2-ethyl-6-methoxy-3,4-dihydro-2H-q"uinoline- 1-carbosylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5«(rmorpholin«4-yl)py^^ yl]}aitiino-2-eth34-6-methoxy-3,4-dihydro-2H-q"uinoline- 1-carboxylic acid 3-carbox3'"propyl ester; (2R,4S)-4-{[3,5-Bis(tnfluorome^ 3d]}aniino-2-eth34»6-me1Jioj^-3?4-dih3^dro-2H-c[_TJ:inoline- 1-carboxylic acid 4« carboxj^butyl ester; (2R,4S)-4-{[3,5-Bis(1xmuorome1±Lyl)berLzyl]-[5-(r3iorpholm^ yl]}ammo-2-et±iyl-6-metJiox3^3?4-dihydro-2H-q^xiinoline-l-caxboxylic acid 2~ ) carboxy-2-methylpropyl ester; (2R,4S)-4-{(3-Cyajio-5-trifLuorometh^ 2-yl]}ainino-2-ethyl-6-inethor7-3J4-dihydro-2H-qiiinoline- 1-carboxylic acid 4-carboxybutyl ester; (2R,4S}-4-{(3-C^aiio~5-trifluorometh^ 2-yl]}amino-2-ethyl-6-metho:^-3,4-^ acid 2-carboxy-2-meth34propyl ester; (2R,4S)-4-fl3,5-Bis(trifluorom yl]}amino-2-ethyl-6-methoxy»3,4-dihydro-2H-quinolio.e-l-carboxy'Hc acid 2- carboxyethyl ester; (2R,4S}-4-{[3,5-Bis(ttfluoromet±iyl)ben^ yl]}aiiiino-2-e1^yl-6-methoxy-3,4-dihydro-2H-quinolirae-l-carboxy'lic acid 3- carboxypropyl ester; (2R,4S)-4-{[33-Bis(trifluoromethyl)ben2yl]-[5-(morpholin-4-yl)^ 34]}amino-2-e1±Lyl-6-metho^-3,4-dihydro-2H-quinolir^e-l-caTbo^ acid 4- carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluorome1iiyl)ben^l]-[5-(moipholin-4-yl)pyridm yl]}amino-2-efeyl-6-methoxy-3,4-dihydro-2H-quinolirie-l-carboxylic acid 2- carboxy-2-methylpropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorome^ yl]}amino--2-ethyl-6-methox3j'-3?4-dihydro-2H-quinoliirie-l-carboxylic acid 4- carbo^butyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorome^ yl]}ainino-2-ethyl-6-methosy-3,4-dihydro-2H-quinolirie- l-carboxj^lic acid 2- carboxy-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(1rifluoromettiyl)benzyl]-[5-(morphoUn-4-yl)pyi^ 3^]}amino-2-ethyl-6,7 -ethylenedioxy-3,4-dihydro-2H- c[uinoline-1 -carboxylic acid 2-carboxyethyl ester; or (2R,4S)-4-{(3-Cyano-5-trmuorom methoxyethoxy)pyrimidin-2 -yl]}amino-2 -ethyl-6,7-ettiylenedioxy-3,4- dihydro-2H-quinoline-l-carboxylic acid 2-carboxyethi34 ester ; or a pharmaceutically acceptable salt thereof. The present compound (I) or a pharmaceutically acceptable salt thereof can be administered either orally or parenteraJly, and can be formulated into pharmaceutical preparations with a conventional pharmaceutically acceptable carriers used therefor. The pharmaceutically acceptable salts of the compound (I) may include, for example, alkali metal salts such as lithium, sodium or potassium salt; alkali earth metal salts such as calcium or magnesium salt; salts with zinc or aluminum; salts with organic bases such as ammonium, choline, diethanolamine, lysine, ettrylenediamine, tert-butylamine, tert-octylamine, tris(hydroxymethyl)amiriome thane, N-methylglucosamie, triethanolamine or dehydroabiethjdamine; salts with inorganic acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid or phosphoric acid; salts with organic acids such as formic acid, acetic acid, propionic acid, oxalic acid, malonic acid, succinic acid, fumaric acid, maleic acid, lactic acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, etharxesulfonic acid, benzenesulfonic acid or toluenesulfonic acid; or salts derived from acidic amino acids such as aspartic acid or glutamic acid. Additionally, the pharmaceutical^ acceptable salts of the compound (I) may include, for example, quaternary salts formed between a compound of the formula (I) and an alkyl halide or phenylalkyl halide. Preferred pharmaceutical preparations for oral administration of the present compound (I) or a pharmaceutically acceptable salt thereof include solid formulations such as tablets, granules, capsules or powders; and liquid formulations such as solutions, suspensions or emulsions. Preferred pharmaceutical preparations for parenteraJ administration include injections or infusions formulated with injectable distilled-water, physiological saline or aqueous glucose solution; suppository; or inhalation preparation. These pharmaceutical preparations comprise a compound (I) of the present invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier which is usually used for oral or parenteral administration. The pharmaceutically acceptable carriers for oral administration include, for example, a binder (syrup, gum acacia, gelatin, sorbit, tragacanth, polyvinylpyrrolidone, and tlie like), an excipient (lactose, sugar, cornstarch, potassium phosphate, soirbit, glycine, and the like), a lubricant (magnesium stearate, talc, polyethylene glycol, silica, and the like), a disintegrant (potato starch, and the like), and a wetting agent (anhydrous sodium lauiyl sulfate , and the like). The pharmaceutically acceptable carriers for parenteral administration include, for example, injectable distilled-water, physiological saline and aqueous glucose solution. The dose of a compound (I) of the present invention or a pharmaceutically acceptable salt thereof varies depending on the administration route, age, body weight, disease, and condition/severity, of the patient. It however can usually be in the range of about 0.001 - 1,000 mg/kg/day, preferably in the range of about 0.01 - 1O0 mg/kg/day, more preferably in the range of about 0.1-10 mg/kg/day. The compounds of the present invention have an inhibitory activity against CETP and show effects of increasing HDL cholesterol and lowering LDL cholesterol. Accordingly, they are useful in the prophylaxis or treatment of a subject (particularly, mammal including human) suffering from arteriosclerosis, peripheral vascular disease, dyslipidemia, hyperbetalipoproteinemia, hypoalphalipoproteinemia, hypercholesteremia, h3^pertriglyceridemia, familial-h33percholesteremia, cardiovascular diseases, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, restenosis after angioplasty, hypertension, cerebral infarction, cerebral stroke, diabetes, vascular complication of diabetes, thrombotic diseases, obesity, endotoxemia, or the like. In addition, the compounds of the present invention ma}' be used in combination with other drugs useful for treatment of these: diseases. For example, a compounds of the present invention may be used in combination with an inhibitor of cholesterol synthesis suclh as HMG-CoA reductase inhibitor, an inhibitor of cholesterol absorption such as anion exchange resin, fibrates, a triglyceride lowering agent suah as niacin or other cholesterol reducer such as ACAT inhibitor. The compounds of the present invention are characterized by that an amino group substituted by a heterocycle having a snbstituent(s) as defined above is introduced into the 4-position of tetra-hydroquinoline skeleton, whereby they can exhibit an excellent inhibitory activity against CETP and have an improved bioavailability. Above all, compounds having a carboxyl group at the terminal position of resepctive substituents R1 - Rn, especialty those having a carboxyl group at the terminal position of Ri and/or R5, or R1 and/or R11 are preferred. The compound (I) of the present invention can be prepared b)^ the following methods. PROCESS 1 The compound (I) of the present invention can be prepared by condensing a compound of the formula (II): (II) wherein the symbols have the same meaning as defined above with a compound of the formula (III): Ri°-R4-Zi (HI) wherein Z1 is a leaving group and the other symbols Hiave the same meaning as defined above. The condensation can be carried out in the presence of a base in a suitable solvent. The leaving group includes a halogen atom including chlorine atom, bromine atom, iodine atom, and a substituted sulfonyloxy group including methanesulfonyloxy group, p-toluenesulfonyloxy groiip, trifluoro-methanesulfonyloxy group. A conventional base can be used as the base, and for example, alkaline metal hydride including sodium hydride, potassium hydride; alkaline metal hydroxide including sodium hydroxide, potassium hydroxide; alkaline earth metal hydroxide including barivam hydroxide; alkaline metal alkoxide including sodium methoxide, sodium ethoxide, potassium ethoxide, potassium tert-butoxide; alkaline metal carbonate including sodium carbonate, potassium carbonate, cesimm carbonate; alkaline metal bicarbonate including sodium bicarbona_*te, potassium bicarbonate; amines including trie thylamine, diisopro pyle thylamine, methylpiperidine, dimethylaniline, 1,8-diazabicyclo[5.4.0]uxidecene, 1,4- diazabicyclo[2.2.2]octane, l,5-diazabicyclo[4.3.0]nonene; pyridines including pyridine., dimethylaminopj'ridine can be preferably used. An3' solvent which dose not disturb the reaction can. be preferably used, and such a solvent includes, for example, hydrocarbons including pentane, hexane; aromatic trydrocarbons including bensene, toluene, nitrobenzene; halogenated hydrocarbons including dichlorome thane, chloroform; ethers including diethylether, tetrahydrofciran; amides including dimethylformamide, N-methylp3>rrolidone, 1,3-dimethyl-imidazolidin-2 -one; sulfoxides including dimethylsulfoxide; alcohols including methanol, ethanol; esters including ethyl acetate, butyl acetate; ke tones including acetone, methyl ethyl ketone; nitriles including acetonitrile; water, or a mixed solvent thereof. The reaction is carried out from under cooling to under heating, preferably from -78°C to 200°C, more preferably from -30°C to 100°C. PROCESS 2 Among the compound of the formula (I-A), a compound of the formula (I-b); (I-b) wherein the symbols have the same meaning as defined above can be prepared by (a) cyanating a compound of the formula (IV): wherein the symbols have the same meaning as defined above to provide a compound of the formula (V): wherein the symbols have the same meaning as defined above, (b) reacting the compound (V) with hydroxyiamine or a salt thereof to provide a compound of the formula (VI): wherein the symbols have the same meaning as defined above, (c) alkanoylating the compound (VI) to provide a compound of the formula (VII): wherein the symbols have the same meaning as defined above, and further (d) cyclizing the compound (VII) with a base. The cyanation in the process (a) can be carried out by reacting a halogenated cyanogen in the presence of a base in a suitable solvent. Cyanogen bromide is preferable as the halogenated cyanogen. A conventional base can be preferably used as the base, and alkaline metal carbonate including potassium carbonate, or alkaline metal bicarbonate including sodium bicarbonate can be preferably used. An37 solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. The reaction with hydroxylamine in the process (b) can be carried out in the presence of a base in a suitable solvent. Tertiary alkylamines including triethylamine, diisopropylethylamine, and the like can be preferably used as the base. Any solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. The alkanoylation in the process (c) can be carried out with an alkanoyl halide in the presence of a base in a suitable solvent. A conventional base can be used as the base, and amines including triethylamine or diisopropylethylamine, or pyridines including pyridine, 4-dimethylaminopyridine can be preferably used. Any solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. In the cyclization in the process (d), a conventional base can b>e used as the base, and amines including triethylamine or diisopropylethylamine; P3nridines including pyridine, 4-dimeth34aminopyridine; or alkaline metal alkoxide including sodium methoxide can be preferably used. Any solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. Additionally, the cyclization following the alkanoylating can also be carried out in situ. The reaction is carried out from under cooling to under treating, preferably from -50°C to 100°C, more preferably from 0°C to 50°C. PROCESS 3 Among the compound of the formula (I-A), a compound of the formula (I-c): wherein the symbols have the same meaning as defined above can be prepared by reacting a compound of the formula (V): wherein the S3^mbols have the same meaning as defined above with 3-buten-1-ol to provide a compound of the formula (VIII): wherein the symbols have the same meaning as defined above, followed by cyclizing the resulting compound in the presence of iodine, N-iodosuccinimide, or the like. The reaction with 3-buten-l-ol can be carried out in the presence of a base in a suitable solvent. Any base which dose not disturb the reaction can be used and the base referred to in the PROCESS 1 can be preferably used. Any solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. In the cyclization any solvent which dose not disturb the reaction can be used and the solvent referred to in the PROCESS 1 can be preferably used. The reaction is carried out from under cooling to under heating, preferably from -50°C to 100°C, more preferably from 0°C to 50°C. PROCESS 4 The compound of the formula (I-A) can also be prepared by the following methods with a compound of the formula (IX): wherein X10 is a hydrogen atom, a halogen atom or a hydroxy group and the other symbols have the same meaning as defined above. In each process of following (A) to (K), unless otherwise specified, the base referred to in the PROCESS 1 can be preferably used as the base. Additionally, in each process of following (A) to (K) a conventional acid can be used as an acid, and unless otherwise specified, a mineral acid including hydrochloric acid, nitric acid, sulfuric acid; an organic acid represented by sulfonic acids (e.g., methanesulfonic acid, p-toluenesulfonic acid, trifluoromethanesulfonic acid, and the like) can be preferably used. Additionally, in each process of following (A) to (K), any solvent which dose not disturb the reaction can be used as the solvent, and specifically, the solvent referred to in the PROCESS 1 can be preferably used. The leaving group includes a halogen atom including chlorine atom, bromine atom, iodine atom, and a substituted sulfonyloxy group including methanesulfonyloxy group, and trifluoromethanesulfonyloxy group, toluenesulfonyloxy group. (A) The compound wherein Ring A is a tetrazofyl group and R11 is an alkyl group having 3 to 10 carbon atoms or a substituted alkyl group can be prepared by alkylating a compound of the formula (IX) wherein Ring A is a tetrazolyl group and X10 is a hydrogen atom. The alkylation can be carried out by reacting a starting compoumd with a compound of the formula: RHA-Z2 wherein RHA is an alkyl group having 3 to 10 carbon atoms or a substituted alkyl group and Z2 refers to a leaving group in a suitable solvent in the presence or absence of a base, or reacting with a compound of the formula: RIIA-OH wherein the symbol has the same meaning as defined above in a suitable solvent in the presence of phosphines and azodicarboxylic esters. The reaction proceeds more preferably when a catalytic amount of an alkaline metal iodide (e.g., potassium iodide, and the like) is added. Both phosphines and azodicarboxylic esters which usually employed in Mitsunobu reaction can be preferably used. Phosphines include, for example, triphenylphosphine, tributylphosphine, and the like, and azodicarboxylic esters include diethyl azodicarboxylate, diisopropyl azodiformate, and the like. (B) The compound wherein Ring A is 2-oxodihydropyrimidinyl group and R11 is an alkyl group having 3 to 10 carbon atoms or a substituted alkyl group can be prepared by alkylating a compound of the formula (IX) wherein Ring A is 2-hydroxypyrimidinyl group and X10 is a hydrogen atom with a compound of the formula: R11A-Z2 wherein the symbols have the same meaning as defined above. The reaction can be carried out in the same manner as (A). (C) The compound wherein R11 is an optionally substituted amino group or a group of the formula: wherein the symbols have the same meaning as defined above can be prepared by reacting a compound of the formula (IX) wherein X10 is a halogen atom with a corresponding amine or a compound of the formula: wherein the S3>mbols have the same meaning as defined above. The reaction can be carried out in the presence or absence of a base, and in the presence or absence of a palladium catalyst in a suitable solvent. As the palladium catalyst, a conventional palladium catalyst including palladium acetate, tetrakis(triphenylphosphine)palladium, tris(dibenzylideneacetone)dipalladium, dichlorobis(triphenylphosphine)- palladium, dichlorobis(tri-o-tolylphosphine)paUadium, bis- (triphen3rlphosphine)palladium acetate, or the like can be used. As the base, alkaline metal hydroxide including sodium hydroxide, potassium hydroxide; alkaline earth metal hydroxide including barium hydroxide; alkaline metal alkoxide including sodium methoxide, sodium ethoxide, potassium ethoxide, potassium tert-butoxide; alkaline metal carbonate including sodium carbonate, potassium carbonate, cesium carbonate; alkaline metal bicarbonate including sodium bicarbonate, potassium bicarbonate; alkaline metal phosphate including potassium phosphate; amines including triethylamine, diisopropyle thylamine, methylpiperidine, dicyclohexylmethylamine; and pyridines including pyridine, 4-dimethylaminop3nridine can be preferabfy used. Additionally, phosphines may be added in the present reaction. As the phosphines, triphenylphosphine, tributylphosphine, tri-tert-butylphosphonium tetrafluoroborate, l,3-bis(diphenylphosphino)propane, 2,2'-bis(diphen3'lphosphino)-1,1'-binaphthyl, 1, l'-bis(diphenylphosphino)-ferrocene, 2-(di-tert-butylphosphino)biphenyl, 2-dicyclohexylphosphino-2'-(N,N-dimethylamino)biphenyl, 2-(dicyclohexylphosphino)biphenyl, and the like can be preferably used as the phosphines. (D) The compound wherein R11 is an optionally substituted amino group can be prepared b3' coupling a compound of the formula (IX) wherein X10 is a halogen atom with a compound of the formula: (R20)3Sn-NR2iR22 wherein R20 is an alkyl group and NR21R22 is an optionally substituted ammo group. The coupling reaction can be carried out in the presence of a palladium catalyst in the presence or absence of a base in a suitable solvent. The palladium catalysts, bases, and phosphines referred to in (C) can be used in the same manner as (C) above. (E) The compound wherein Ru is a cyano group can be prepared b}' cyanating a compound of the formula (IX) wherein X10 is a halogen atom. The cyanation can be carried out by reacting a starting compound with a metal cyanide including sodium cyanide, potassium cyanide, or zinc cyanide in the presence of a palladium catalyst in a suitable solvent. The same palladium catatyst as that described in (C) can be preferably used. (F) The compound wherein R11 is an optionally substituted alkoxycarbonyl group can be prepared by reacting a compound of the formula (IX) wherein X10 is a halogen atom with a corresponding alkylalcohol under carbon monoxide using a palladium catalyst in the presence of a base in a suitable solvent. The same palladium catalyst and base as those described in (C) can be preferably used. Additionally, the reaction can be more preferably carried out by adding a ligand, and phosphines referred to in (C) can be preferably used as the ligand. (G) The compound wherein R11 is an optionally substituted alkenyl group can be prepared by coupling a compound of the formula (IX) wherein X10 is a halogen atom with a corresponding alkene. The coupling reaction can be carried out in the presence of a palladium catalyst in the presence or absence of a base in a suitable solvent The same palladium catalyst as that described in (C) can be preferably used. The same base as referred to in (C) can be preferably used and silver carbonate can also be used. Additionally, the reaction can be more preferably carried out by adding a ligand, and phosphines referred to in (C) can be preferably used as the ligand. (H) The compound wherein R11 is an alkoxy group having 3 to 10 carbon atoms or a substituted alkoxy group can be prepared by alkoxylating a compound of the formula (IX) wherein X10 is a halogen atom. The alkoxylation can be carried out by optionally adding a copper catalyst to react a starting compound with a corresponding alcohol in a suitable solvent or neat in the presence of a base. The same base as referred to in (C), in particular, cesium carbonate can be preferably used. The copper catalyst including copper iodide, copper bromide, copper chloride, copper acetate, copper trifluoromethanesulfonate, and the like can be preferably used. Additional^, the reaction proceeds more preferably when 1,10-phenanthroline, 2-aminopyridine, or the like is added. (I) The compound wherein R11 is an optionally substituted heterocyclic group can be prepared by coupling a compound of the formula (IX) wherein X10 is a halogen atom with a corresponding heterocyclic boronic acids or a corresponding heterocyclic boronic ester. The coupling can be carried out in the presence of a palladium catalyst, and in the presence or absence of a base in a suitable solvent. The reaction can be carried out in the same manner as (C). (J) The compound wherein R11 is an alkoxycarbonjdalkylsulfonj7'! group can be prepared bjr reacting a compound of the formula (IX) wherein X10 is a halogen atom with an alkoxycarbonylalkylsulfinic acid alkaline metal salt. The alkoxycarbonylalkylsulfinic acid alkaline metal salt can be prepared according to the method described, for example, in Baskin et al., Tetrahedron Lett, 43, 8479 (2002). Additionally, the reaction can be carried out in the presence of a copper catalyst in a suitable solvent according to the method described in the said literature. The same copper catalyst as described in (H) can be used, and in particular, copper iodide can be preferably used. (K) The compound wherein R11 is a group of the formula: wherein the symbols have the same meaning as defined above can be prepared by condensing a compound wherein R11 is a hydroxy group with a compound of the formula: wherein X11 is O, SO, SO2 or NRP (RP is a protecteing group) and q is an integer from 1 to 4, and if needed, removing a protecting group for amino group. As a protecting group, a conventional protecting group including benzyloxycarbonyl group, tert-butoxycarbonyl group, and the like can be used. The reaction can be carried out in a suitable solvent in the presence of phosphines and azodicarboxylic esters. The reaction can be carried out in the same manner as the PROCESS 4-(A). The removal of a protecting group can be carried out in a conventional manner including catalytic reduction, acid-treatment, and the like, depending on the type of a protecting group. The reactions (A) to (K) for conversions of Rn can also be applied for conversion in the same manner of an other substituent (R1, R2, R3, R4, R5, Re, R7, R8, R9 or Rio) as appropriate. Additionally, a substituent(s) of a compound (I) of the present invention can be converted into different one(s) within the scope of the compound (I) according to the following methods as appropriate. In the following each process, a conventional base can be used as a base, and unless otherwise specified, the base referred to in the PROCESS 1 can be preferably used. Additional^, in the following each process, a conventional acid can be used as an acid, and unless otherwise specified, a mineral acid including hydrochloric acid, nitric acid, sulfuric acid, or an organic acid represented by sulfonic acids (e.g., methanesulfonic acid, p-toluenesulfonic acid, trifluoromethanesulfonic acid) or carboxylic acids (e.g., acetic acid, trifluoroacetic acid) can be preferably used. Further additional!}', in the following each process, any solvent which dose not disturb the reaction can be used, and as such, the solvent referred to in the PROCESS 1 can be preferably used. The leaving group includes a halogen atom including chlorine atom, bromine atom, iodine atom, and a substituted sulfonyloxy group including methanesulfonyloxy group, trifluoromethanesulfonyloxy group, and toluenesulfonyloxy group. In addition, in the following each process, "a saturated or unsaturated monocyclic or bicyclic heterocyclic group having one to four heteroatoms independently selected from oxygen atom, sulfur atom and nitrogen atom" in R5 is simpty referred to as "a heterocyclic group". > (1) The compound wherein R5 is a heterocyclic group substituted by an optionally substituted amino group or a group of the formula: wherein the symbols have the same meaning as defined above can be prepared by reacting a compound (I) wherein R5 is a heterocyclic group substituted by an optionally substituted alkylsulfonyloxy group with a corresponding amine or a compound of the formula: wherein the symbols have the same meaning as defined above in the presence of a palladium catalyst, and in the presence or absence of a base in a suitable solvent or neat. The reaction can be carried out in the same manner as the PROCESS 4-(C). (2) The compound wherein R5 is a heterocyclic group substituted by an optionally substituted amino group or a group of the formula : wherein the symbols have the same meaning as defined above can also be prepared bj' reacting a compound wherein R5 is a heterocyclic group substituted by a halogen atom or an optionally substituted alkylsulfonyloxy group with a corresponding amine or a compound of the formula: wherein the symbols have the same meaning as defined above. The reaction can be carried out by optionally adding a copper catalyst in the presence or absence of a base in a suitable solvent. Copper iodide, copper bromide, copper chloride, copper acetate, copper trifluoromethanesulfonate, and the like can be preferably used as the copper catalyst. The same base as referred to in the PROCESS 4-(C) can be preferably used. Additionally, the reaction proceeds more preferabty when N;N'-dimethjdethylenediamine, 1,10-phenanthroline, etltylene glycol, phenylphenol, and the like is added. (3) The compound wherein R5 is a heterocyclic group substituted bj' an optionally substituted alkylthio group can be prepared by reacting a compound wherein R5 is a heterocyclic group substituted by a halogen atom or an optionally substituted alkylsulfonyloxy group with a corresponding alkylthiol. The reaction can be carried out in the same manner as previously described in the PROCESS 4-(H) and facilitated by adding 1,10-phenanthroline or ethylene glycol. (4) The compound wherein R5 is a heterocyclic group substituted by an optionally substituted heterocyclic group can be prepared by coupling a compound wherein R5 is a heterocyclic group substituted by a halogen atom or an optionally substituted alkylsulfonyloxy group with a corresponding heterocyclic alkyl tin compound. The reaction can be carried out in the same manner as the PROCESS 4-(D). (5) The compound wherein R5 is a heterocyclic group substituted by an alkoxy group or an alkoxyphenylalkoxy group can be prepared by reacting a compound wherein R5 is a heterocyclic group substituted bj' an alkylsulfon3rl group with a corresponding alkaline metal alkoxide in a suitable solvent. The corresponding alkaline metal alkoxide can be obtained by treating a corresponding alkylalcohol with alkaline metal hydride or alkaline metal in the said solvent. (6) The compound having an aminoalkyl group as a substituent on R5 can be prepared by catalytically reducing a compound having a cyano group or a cyanoalkyl group as a substituent on R5. The catalytic reduction can be carried out by using a catalyst under hydrogen in a suitable solvent according to a conventional manner. The catalyst includes a palladium catalyst including palladium-carbon, a nickel catalyst including Raney nickel, a platinum catalyst including platinum-carbon, and the like. (7) The compound having an optionally substituted mono- or di- adkylsulfamoylanunoalkyl group as a substituent on R5 can be prepared by reacting a compound having an aminoalkyl group as a substituent on R5 with a corresponding halogenated mono- or di-alkylsulfamoyl. The reaction can be carried out in a suitable solvent in the presence of a base. (8) The compound having an optionally substituted mono- alkylcarbamoylaminoalkyl group as a substituent on R5 can be prepared by reacting a compound having an aminoalkyl group as a substituent on R5 with a corresponding alkyl isocyanate in a suitable solvent. (9) The compound having a group of the formula: wherein R12 is an alkyl group and the other symbol has the same meaning as defined above as a substituent on R5 can be prepared by reacting a compound having a group of the formula: i wherein the symbols have the same meaning as defined above as a substituent on R5 with a corresponding alkyl isocyanate (R^NCO). The reaction can be carried out in the same manner as (8). (10) The compound having an optionally substituted mono- or di- alkylcarbamoylaminoalkyl group as a substituent on R5 can be prepared by condensing a compound having an aminoalkyl group as a substituent on R5 with an optionally substituted mono- or di-alkylamine using a carbonylating agent in a suitable solvent in the presence or absence of a base. A conventional carbonylating agent such as carbonyldiimidazole, phosgene, triphosgene, and the like can be used. (11) The compound having a morpholi^dcaxbonylamino group as a substituent on R5 can be prepared by condensing a compound having an amino group as a substituent on R5 with morphoiine using a carbonylating agent in a suitable solvent. The reaction can be carried out in the same manner as (10). (12) The compound having a group of the formula: wherein X12 is O or NH as a substituent on R5 can be prepared by treating a compound having a group of the formula H-X«-CH2-CONH- wh.erein the symbols have the same meaning as defined above as a substituent on R5 with a carbonylating agent in a suitable solvent. The reaction can be carried out in the same manner as (10). (13) The compound having an optionally substituted carbamoyl group as a substituent on R5 can be prepared by condensing a compound having a carboxyl group as a substituent on R5 with a desirable amine. The condensation can be carried out using a condensing agent in a suitable solvent. A conventional condensing agent such as dicyclohexylcarbodiimide, l-ethyl-3-(3-dimethylaiiiinopropyl)carbodiimide? carbonyldiimidazole, and the like can be preferably used. Additionally, the condensation can be more preferably carried out by adding an activating agent including 1 -hydroxybenzotriazole, 1 -hydro:sysuccinimide, and the like. (14) The compound having a group of the formula: wherein the symbols have the same meaning as defined above as a substituent on R5 can be prepared by condensing a compound having a carboxyl group as a substituent on R5 with a compound of the formula: wherein the symbols have the same meaning as defined above. The reaction can be carried out in the same manner as (13). (15) The compound having a tetrazolyl group as a substituent on R5 can be prepared by reacting a compound having a C3^ano group as a substituent on R5 with an alkaline metal azide in the presence of an acid in a suitable solvent. The alkaline metal azide includes sodium azide, lithium azide, and the like. An ammonium salt of a halogenated hydrogen including ammonium chloride can be preferably used as the acid. (16) The compound having an optionally substituted alkyl tetrazolyl group as a substituent on R5 can be prepared by alkylating a compound having a tetrazolyl group as a substituent on R5. The alkylation can be carried out in the same manner as the PROCESS 4-(A). (17) The compound having an optionally substituted amino group or a group of the formula: wherein the symbols have the same meaning as defined above as a substituent on R5 can be prepared by reacting a compound having a halogen atom or an optionally substituted alkylsulfonyloxy group as a substituent on R5 with a corresponding amine or a compound of the formula: wherein the symbols have the same meaning as defined above. The reaction can be preferably carried out in the presence or absence of a base in a suitable solvent. (18) The compound having an optionally substituted alkylamino group or a group of the formula: wherein R13 is an alkyl group optionally substituted by a hydroxy group, an alkoxycarbonjd group, a morpholinyl group or a phenyl group, and n has the same meaning as defined above as a substituent on R5 can be obtained by reacting a compound having an amino group or a group of the formula: wherein the symbols have the same meaning as defined above as a substituent on R5 with a corresponding alkyl halide or a corresponding sulfonic alkyl ester. The sulfonic alkyl ester including methanesulfonic ester, toluenesulfonic ester, trifluoromethanesulfonic ester, and the like can be preferably used. The reaction can be preferably carried out in the presence or absence of a base in a suitable solvent. (19) The compound having a group of the formula: wherein X13 is 0 or NH, and the other symbols have the same meaning as defined above as a substituent on R5 can be prepared by ring-closing a compound having a group of the formula: Z3-(CH2)n-Xi3-CH2-CONH- wherein Z3 is a leaving group and the other S3>rnbols have the same meaning as defined above as a substituent on R5. The reaction can be preferably carried out in the presence or absence of a base in a suitable solvent. (20) The compound having a carboxyl group as a substituent on R5 can be prepared by hydrolyzing a compound having an alkoxycarbonyl group as a substituent on R5. The hydrolysis can be carried out by treating a starting compound with a base or an acid in a suitable solvent according to a conventional manner. An alkaline metal hydroxide can be preferably used as the base. (21) The compound containing a carboxyl group as a substituent on R5 can be prepared by hydrolyzing a compound containing a cyano group as a substituent on R5. The hydrolysis can be carried out by treating a starting compound with an acid in a suitable solvent. (22) The compound containing a carbamoyl group as a substituent on R.5 can be prepared by hydrolyzing a compound containing a cyano group as a substituent on R5. The hydrolysis can be carried out by treating a starting compound with an acid in a suitable solvent. (23) The compound having a carboxyalkyl group as a substituent on R5 can also be prepared by catalytically reducing a compound having a carboxyalkenyl group, a benzyloxycarbonylalkenyl group or a benzyloxycarbonj'lalkyl group as a substituent on R5. The catalytic reduction can be carried out in the same manner as (6). (24) The compound having a hydroxy group as a substituent on R5 can be prepared by hydrolyzing a compound wherein R5 has an alkanoyloxy group. The hydrolysis can be carried out in the same manner as (20). (25) The compound containing sulfin (SO) or sulfoxide (SO2) in a substituent on R5 can be prepared by oxidizing a compound having S in a substituent on R5 (e.g., a compound having a thiomorpholinyl group or an alkylthioalkyl group as a substituent on R5). The oxidation can be carried out by treating a starting compound with an oxidizing agent in a suitable solvent. Peroxides such as hydrogen peroxide, m-chloroperbenzoic acid, acetyl hydroperoxide, and the like can be preferably used as the oxidizing agent. (26) The compound containing N-oxide in a substituent on R5 can be prepared by oxidizing a compound having N in a substituent on R5 (e.g., a compound having a pyridyl group as a substituent on R5). The oxidation can be carried out in the same manner as (25), (27) The compound having a 1,2-dihydroxyalkyl group as a substituent on R5 can be prepared by treating a compound having an alkyl group substituted by mono- or di-alkyldioxolanyl group as a substituent on R5 with an acid in a suitable solvent. A strongfy acidic resin can also be preferably used as the acid, in addition to those previously described. (28) The compound having an alkyl group substituted by a hydoxy group and an optionally substituted alkoxy group as substituents on R5 can be prepared by reacting a compound having an oxylanylalkyl group as a substituent on R5 with an alkaline metal salt of the corresponding alcohol in a suitable solvent. The alkaline metal salt of alcohol includes a lithium salt, a sodium salt, a potassium salt, and the like. (29) The compound having an alkyl group substituted by a hydoxy group and an amino group, or an alkyl group substituted by a hydroxy group and an optionalty substituted mono- or di-alkylamino group as substituents on R5 can be prepared by reacting a compound having an oxyla^lalkyl group as a substituent on R5 with ammonia or a corresponding mono- or di-alkylamines in a suitable solvent. (30) The compound having a hydroxycarbamimidoyl group as a substituent on R5.can be prepared b}' reacting a compound having a cyano group as a substituent on R5 with hydroxylamine or a salt thereof in a suitable solvent. This process can be carried out in the same manner as the PROCESS 2-(b) previously described. (31) The compound having an oxodiltydrooxadiazolyl group as a substituent on R5 can be prepared by reacting a compound having a hydroxycarbamimidoyl group as a substituent on R5 with a carbonylating agent in a. suitable solvent in the presence or absence of a base. The same carbonylating agent as that described in (10) can be used. (32) The compound having a sulfo group as a substituent on R5 can be prepared by hydrolyzing a compound having an alkoxycarbonylalkylsulfonyl group as a substituent on R5. The hydrolysis can be carried out in the same manner as (20). (33) The compound having a sulfamoyl group as a substituent on Rs can be prepared by condensing a compound having a sulfo group as a substituerxt on R5 with a desirable amine. The condensation can be carried out b}^ treating a compound having a sulfo group as a substituent on R5 with a halogenating agent in a suitable solvent, followed by reacting the resulting compound with a desirable amine in the presence or absence of a base. A conventional halogenating agent including thionyl halide, phosphorus oxyhalide, or the like can be used. (34) The compound having a hydroxyalkyl group as a substituent on R5 can be prepared by reducing a compound having a carboxyalkyl group as a substituent on R5, or by converting the carboxyl group into an acid anhydride or an ester and reducing the resulting compound. A process for conversion into an acid anhydride can be carried out by reacting a starting compound with a halogenated alkyl formate in a suitable solvent in the presence of a base. A process for conversion into an ester can be carried out by reacting a starting compound with an alcohol in the presence of a condensing agent in a suitable solvent. This process can be carried out in the same manner as (33) except that a desirable alcohol is used in place of amine. The reduction can be carried out by treating the resulting compound with a reducing agent in a suitable solvent. Boron hydrides (sodium borohydride, and the like), aluminum hydrides (lithium-aluminum hydride, diisobutylaluminum hydride, and the like) can be preferably used as the reducing agent. (35) The compound wherein R10 is an aromatic group substituted by a cj'ano group, optionally having one to three heteroatoins independently selected from oxygen atom, sulfur atom and nitrogen atom (hereinafter ,referred to as "an aromatic group"), can be prepared by cj^anating a. compound wherein R10 is an aromatic group substituted by a halogen atom. The cyanation can be carried out in the same manner as the PROCESS 4-(E). (36) The compound wherein R1 is a hydrogen atom can be prepared by acid-treatment or reduction of a compound wherein R1 is a tert- butoxycarbonyl group or a benzyloxycarbonyl group. The acid-treatment can be carried out in the same manner as (27) and the reduction can be carried out in the same manner as (23). (37) The compound wherein R1 is an optionally substituted alkoxycarbonyl group, or an optionally substituted carbamoyl group can be prepared by reacting a compound wherein R1 is a hydrogen atom with a carbonylating agent, or a desirable alcohol or a desirable amine in a suitable solvent. The reaction can be carried out in the same manner as (10). (38) The compound having an amino group as a substituent on R5 can be prepared by reacting a compound having a carboxyl group as a substituent on R5 under Curtius rearrangement reaction condition. Curtius rearrangement reaction can be carried out using a conventional azidating agent (e.g., diphenylphosphorylazide) in a suitable solvent in the presence of a base. The reaction may also be carried out by adding an alcohol to provide a compound having an optionally substituted alkoxycarbonylamino group as a substituent on R5, followed by removing the alkoxycarbonyl group. The removal of the alkoxycarbonyl group can be carried out in a conventional manner such as an acid-treatment or a reduction depending on the type of alkoxycarbon}^ group to be removed. The acid-treatment can be carried out in the same manner as (27) and the reduction can be carried out in the same manner as (23). (39) The compound having a hydroxy group as a substituent on R5 can be prepared by catalytically reducing a compound having a benzyloxy group as a substituent on R5. The reduction can be carried out in the same manner as (23). (40) The compound having an oxo group as a substituent on R5 can be prepared by oxidizing a compound having a hydroxy group as a siabstituent on R5. The oxidation can be carried out by using an oxidizing agent in a suitable solvent. A conventional oxidizing agent can be used as the oxidizing agent, such as chromate-pyridine complex, pyridinium chlorochromate, pyridinium dichromate, Dess-Martin reagent (1,1, l-tris(acetoxy)-1,1-dthydro-l,2-benziodoxol-3-(lH)-one), dime tirylsulfoxide, and the like. (41) The compound containing an optionally substituted alkoxy group as a substituent on R5 can be prepared b}^ alkylating a compound containing a hydroxy group as a substituent on R5. The alkylation can be carried out b3^ using a corresponding compound in the same manner as the PROCESS 4-(A). (42) The compound having an optionally substituted alkanoylamino group as a substituent on R5 can be prepared by condensing a compound having an amino group as a substituent on R5 with a corresponding carboxylic acid or a reactive derivative thereof. The condensation with the corresponding carboxylic acid can be preferably carried out in a suitable solvent in the presence of a condensing agent. The reaction can be carried out in the same manner as (13). Additionally, the condensation with the reactive derivative of the corresponding carboxylic acid can be carried out in a suitable solvent or neat in the presence or absence of a base. The reactive derivative includes an acid halide, an acid anhydride, an activated ester, an activated amide, and the like. (43) The compound having a group of the formula: wtaerein R14 is an alkanoyl group optionally substituted by a hydroxy group or an alkoxy group, and n has the same meaning as defined above as a substituent on R5 can be prepared by condensing a compound of a group of the formula: wherein the symbols have the same meaning as defined above as a substituent on R5 with a corresponding carboxylic acid or a reactive derivative thereof. The reaction can be carried out in the same manner as (42). (44) The compound having a maleimide group as a substituent on R5 can be prepared by reacting a compound having an ammo group as a substituent on R5 with a maleic anhydride. The reaction can be carried out in a suitable solvent. (45) The compound having an alkyl group substituted by a pyridyl group and a hydroxy group as substituents on R5 can be prepared by reacting a compound having an alkyl group substituted by a pyridyl group of which nitrogen atom is oxidized as a substituent on R5 with a trifluoroacetic anhydride. The reaction can be carried out in a suitable solvent. (46) The compound having a halogen atom as a substituent on R5 can be prepared by treating a compound having a hydroxy group as a substituent on R5 with a halogenating agent. As the halogenating agent, a conventional halogenating agent including thionyl chloride, phosphorus oxychloride, as well as carbon tetrahalicie (e.g., carbon tetrachloride, carbon tetrabromide, and the like) and phosphines (e.g., triphenylphosphine, tritolylphosphine, triethylphosphine, and the like) can be preferably used. (47) The compound having a cyanoalkyl group as a substituent on R5 can be prepared by reducing a compound having a cyanoalkenyl group as a substituent onR5. The reduction can be carried out by treating a starting compound with a reducing agent or b}' catalytically reducing in a suitable solvent. Any reducing agent can be used subject that it reduces only a double bond without affecting a C3jfano group. For example, sodium bis(2-met±ioxyethoxy)alu.minum hydride in the presence of a copper bromide can be preferabty used. The catafytic reduction can be carried out in the same manner as (23). (48) The compound having a hydroxyalkyl group as a substituent on R5 can be prepared by reducing a compound having a formyl group as a substituent on R5. The reduction can be carried out by treating a starting compound with a reducing agent in a suitable solvent. The reaction can be carried out in the same manner as the process for reducing in (34). (49) The compound wherein R7 is a hydroxy group can be prepared by demethylating a. compound wherein R7 is a methoxy group. The demethylation can be carried out by treating a starting compound with a demethylating agent in a suitable solvent. A conventional agent including trimethylsilyl iodide, hydrogen bromide/acetic acid, boron tribromide, concentrated sulfuric acid, and the like can be used as the demethylating agent. (50) The compound wherein R7 is an optionally substituted alkoxy group can be prepared by alkylating a compound wherein R7 is a hydroxy group. The alkylation can be carried out in the same manner as the PROCESS 4-(A). (51) The compound wherein R7 is an optionally substituted alkylsulfonyloxy group can be prepared by alkylsulfonylating a compound wherein R7 is a hydroxy group. The alkylsulfonylation can be carried out by reacting a corresponding alkylsulfonyl halide or a corresponding alkylsulfonic anhydride in a suitable solvent in the presence or absence of a base. (52) The compound wherein R7 is a cyano group can be prepared by cyanating a compound wherein R7 is an optionally substituted alkylsulfonyloxy group. The cyanation can be carried out in the same manner as the PROCESS 4-(E). (53) The compound wherein R7 is an aminoalkyl group can be prepared by reducing a compound wherein R7 is a cj^ano group. The reduction can be carried out in the same manner as (6). (54) The compound wherein R7 is an alkyl group can be prepared by alkylating a compound wherein R7 is an optionally substituted alkylsulfonyloxy group. The alkylation can be carried out by reacting alkyl aluminums in the presence of a palladium catalyst, a silver catalyst and a copper catalyst in a suitable solvent. Tetrakis(triphenylphosphine)palladium as the palladium catalyst, silver carbonate as the silver catalyst, copper (I) chloride as the copper catalyst can be preferably used. (55) The compound having an imidazolinyl group or an oxazolinyl group as a substituent on R5 can be prepared by (i) reacting a compound containing a cj'ano group as a substituent on R5 with a desirable alcohol in the presence of an acid in a suitable solvent or neat to provide a compound containing an alkoxycarbonimidoyl group as a substituent on R5, and (ii) reacting the compound containing an alkoxycarbonimido3d group as a substituent on R5 with 2-aminoethanol or ethylene diamine in a suitable solvent or neat. (56) The compound having a carboxyl group as a substituent on R* can be prepared by (i) oxidizing a compound containing a hydroxyalkyl group as a substituent on R1 in the same manner as (40) to provide a compound containing an oxo group as a substituent on R1, and (ii) oxidizing the compound containing an oxo group as a substituent on R1. The oxidization for the second step can be carried out by using an oxidizing agent in a suitable solvent. Sodium chlorite, Silver (I) oxide, Sodium periodate and the like can "be preferably used as the oxidizing agent. (57) The compound having a carboxyl group as a substituent on R1 can be directly prepared by oxidizing a compound containing a hydroxyalkyl group as a substituent on R1. The oxidization can be carried out by using Jones reagent, potassium permanganate, and the like as the oxidizing agent. (58) The compound wherein Rl is hydrogen atom can be prepared by treating a compound wherein R1 is ethoxycarbonyl group with a silyl halides or a base. Trimethylsilyl iodide can be preferably used as the silyl halides. Sodium hydroxide can be preferably used as the base. In each process for preparing a compound of the formula (I) described above, when protection of a functional group contained in any compound is needed, the protection can be carried out in a conventional manner ad libitum. General statement related to protecting groups and their use is provided by Greene, Protective Groups in Organic Synthesis, John Wiley and Sons, New York, 1991. When an amino group is protected by a benzyloxycarbon}*! group, the protecting group can be removed by a catalytic reduction under hydrogen in a suitable solvent. When a hydroxy group is protected by a benzyl group, the protecting group can also be removed by a catalytic reduction in a similar manner as above. When an arnino group is protected by a t-butoxycarbonyl group, the protecting group can be removed by treating a starting compound with an acid (e.g., hydrochloric acid, trifluoroacetic acid, toluenesulfonic acid, and the like) in a suitable solvent. When a hydroxy group is protected by a tetrahydropyranyl group, the protecting group can also be removed by treating a starting compound with an acid in a similar manner as above. The reactions (1) to (58) for canversion of R1, R5, R7 or R10 can also be applied for conversion in the same manner of an other substituent of the present compouind (I) as appropriate. The starting compound (II) is a novel compound, and can be prepared b}^ condensing a compound of the formula (X): wherein the sj^mbols have the same meaning as defined above with a compound of the formula (XI): R5-Z-* (XI) wherein Z4 is a leaving group and R5 has the same meaning as defined above. As the leaving group, a halogen atom including chlorine atom, bromine atom, iodine atom, and a substituted sulfonyloxy group including methanesulfonyloxy group, p-toluenesulfonyloxy group, trifluoro-methanesulfonyloxy group are preferably used. The reaction can be carried out in a suitable solvent (e.g., 1,4-dioxane, dimethylformamide, 1,3-dimethylimidazolidinone, and the like) in the presence or absence of a base (e.g., diisopropylethylamine, and the like) from room temperature to under heating. The reaction can also be carried out by adding a palladium catalyst (e.g., tris(dibenzylidenacetone)dipalla.dium) and a phosphine [for example, triphenylphosphine, tributylphosphine, or 2-(di-tert-butyl- phosphinojbiphenyl] at room temperature in the presence of a base (e.g., sodium tert-butoxide), if desired. A compound of the formula (X) cajn be prepared according to the method described in WO00/17165 or US 6313142. Alternatively, the compound (X) caji be prepared according to the following scheme: wherein R15 is a protecting group for amixxo group and the other symbols have the same meaning as defined as above. A conventional protecting group including a benzyloxycarbonyl group can be used as the protecting group for amino group. Additionally, an optically-active compound (X) can be prepared by protecting amino group with an opticalfy-active protecting group for amino group (e.g., an optically-active a-substituted benzyloxycarbonyl group having a chiral center at the benzyl position, such as a-meth3dbenzyloxycarbonyl group), resolving diastereomers in the process for preparation of compound (XII) or compound (XIII), and removing the protecting group. A compound of the formula (XV) can be prepared by reacting benzotriazole, a compound of the formula (XVI) and a compound of the formula (XVII) in a suitable solvent (e.g., toluene) at room temperature. A compound of the formula (XIII) can be prepared by reacting a compound of the formula (XIV) with a compound of the formula (XV) in the presence of an acidic catalyst (e.g., an organic acid including p-toluenesulfonic acid, acetic acid, methanesulfonic acid, or Lewis acid including boron trifluoride-diethylether complex, titanium tetrachloride, aluminum chloride) in a suitable solvent (e.g., toluene, tetrahydrofuran, xxxethylene chloride, and the like) under heating or at room temperature (e.g., 0°C to 150°C, preferably 25°C to 120°C). A compound of the formula (XII) can be prepared by alkanoylation, alkoxycarbonylation, alkylation, and the like of a compound of the formula (Kill) as appropriate. A compound of the formula (X) can be prepared by removing a protecting group for amino group of a compound of the formula (XII). The removal of the protecting group can be carried out in a conventional manner including acid-treatment, base-treatment, reduction, and the like depending on the type of the protecting group. When a benzyloxycarbonyl group or an a-substituted benzyloxycarbonyl group is used, they can be removed by a catalytic reduction in a suitable solvent (e.g., ethanol, methanol, tetrahj^drofuran, acetic acid, and the like) under hydrogen. The removal of a protecting group for amino group of a compound of the formula (XIII) can be carried out in the same manner as the removal of the protecting group for amino group of a compound of the formula (XII). When an opticalfy-active protecting group such as a-substituted benzyloxycarbonyl group is used as a protecting group for amino group, resolution of a diastereomer can be carried out in a conventional manner such as recrystallization or column chromatography. A compound of the formula (XIII) can also be prepared by reacting a compound of the formula (XIV) with a compound of the formula (XVIII). This reaction can be carried out in the same manner as the reaction of a compound of the formula (XIV) with a compound of the formula (XV). Additionally, respective substituents Ri, R5, Re, R7, Rs and R* can be converted into a desirable substituent in accordance with any one of processes from the PROCESS 4-(A) to (K) and from (1) to (58). A compound of the formula (IV) can be prepared by condensing a compound of the formula (X) with a compound of the formula (III) R10.R4-Z1 (HI) wherein the symbols have the same meaning as defined above. The condensation can be carried out in the same manner as described in WO00/17165 or the PROCESS 1 above. A compound of the formula (IX) can be prepared by condensing a compound of the formula (IV) with a compound of the formula: wherein Z5 is a leaving group and the other symbols have the same meaning as defined above. As the leaving group, a halogen atom including chlorine atom, bromine atom, iodine atom; a substituted sulfonyloxy group including methanesulfonyloxy group, p-toluenesulfonyloxy group, trifluoro-methanesulfonyloxy group can be preferably used. The condensation can be carried out in the same manner as the one of the said compound (X) with the compound (XI). Additionally, the compound of the formula (IX) wherein Ring A is a tetrazolyl group and X10 is a hydrogen atom can be prepared by reacting a compound of the formula (V) with an alkyl metal azide. The reaction can be carried out in the same manner as (15) described above. Further, the compound of the formula (IX) wherein X10 is a hydroxyl group can be prepared by (i) reacting a compound wherein X10 is a halogen atom witti diboron or borane to provide a compound wherein X10 is a boronic esters, and (ii) reacting the compound wherein X10 is a boronic esters with, peroxides. Hydrogen peroxide solution, m-chloroperbenzoic acid or OXONE™ (Manufactured by DuPont) can be preferably used as the peroxides. Marry of starting materials and reagents for preparation of the aforementioned compound of the formula I are either commercially available or disclosed in literatures, or can be readily prepared by a method that is disclosed in literatures or used generally in the organic synthesis. As used herein, n3,4-dihydro-2H-quinoline" represents the same structure as t%2?3,4-tetrahydroquinoline". Experiment The inhibitory activity of the compounds of the present invention against CETP was tested in this experiment. Preparation of Acceptor Microemulsion A solution of l-Palmitoyl-2-oleoyl-sn~glycero-3-phosphocholine (3.5 mg), cholesteryl oleate (3mg) and triolein (0.7 mg) in chloroform was mixed and lipid 'was air-dried under nitrogen gas to remove solvent. 1,4-Dioxane (0.25 ml) -was then added and the mixture was stirred for dissolution. The resultant lipid solution (0.2 ml) was slowly injected under the surface of Tris-saline-EDTA(TSE) buffer solution [lOmM Tris/HCl (pH 7.4), 0.15M NaCI, 2mM EDTA] (10 ml) with Hamilton syringe, while sonicating in ice-bath. After 1-hour-sonication in ice-bath, the solution was stored at 4 °C. Pre-paration of Donor Microemulsion A solution of egg PC (phosphatidylcholine) (0.33 mg) and BODIPY-CE (0.62 mg) in chloroform was mixed. After removing solvent by air-diying lipid under nitrogen gas, TSE buffer solution (3 ml) was added and the solution was sonicated in ice-bath. This solution was filtered to sterilize through 0.22 ]xm filter and stored at 4 °C. Inhibitory Activity against CETP in vitro A test solution was prepared using dimethyl sulfoxide as a solvent. Plasma from a healthy volunteer was diluted to 0.64 % with TSE buffer, and to the resultant plasma solution (187 -pi) was added a test solution (3 \il) or the solvent alone followed by incubation at 37 °C for 24 hours. After addition of TSE buffer solution (10 y\L) containing 5 % donor micro-emulsion and 5 % acceptor microemulsion, the mixture was incubated at 37 °C for 3 hours. Before and after the incubation, the fluorescence intensity was measured at Ex.550nm/Em.600nm. CETP activity was defined as the difference between the measurements obtained before incubation and after incubation. The decreasing rate of the difference in the sample was defined as the inhibition rate of CETP activity. IC50 for each sample was calculated from the inhibition rate of CETP activity. EXAMPLES The present invention is illustrated in more detail by Examples and Reference Examples, but the present invention should not be construed to be limited thereto. In Examples, the compounds having a structure of the formula: indicate that the configuration thereof is (2R*,4S*). Besides, Me means a methyl group. Example 1 (1) (2R,4S)-4-Amino-2-etliyl-6-trifluoromethyl-3,4-dihydro-2H^ quinoline-1-carboxylic acid ethyl ester (3 g) and 5-broino-2-chiloro~ pyrimidine (3.7 g) are dissolved in N,N-dimeth3dformamide (30 ml), and the mixture is stirred at 150°C for 5 hours. The reaction solution is cooled to room temperature, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified b}' column chromatography (silica gel; hexane:ethyl acetate = 8:1—+4:1) to give (2R,4S)«4-(5-bromop3^imidi3n-2«yl)aniino--2-ethyl-6-trifluoromethyl-3)4-- dihydro-2H-quinoline-l-car"boxylic acid ethyl ester (2.2 g). MS (rn/z): 473/475 [M+H]+ (2) (2R,4S)-4-(5-Bromopy-rimidin»2-yl)amino-2-ethyl«6-trifluoromethLyl- 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (2.2 g) is dissolved in N.N-dimethylformamide (20 ml), and thereto is added sodium hydride (62.7 %, 223 mg) under ice-cooling, and the mixture is stirred at room temperature for 30 minutes. To the mixture is added 3,5-bis(trifhaoro- methyl)benzyl bromide (1.3 ml) under ice-cooling, and the mixture is stirred at room temperature for one hour. A saturated brine and ethyl acetate are added to the mixture, and the organic layer is dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane: ethyl acetate = 10:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)ben?yl]-(5-bromo- pyrimidin-2-yl)}amino-2-ethyl-6-txifluoromethyl-3,4-dihydro-2H l-carboxylic acid ethyl ester {2.75 g). MS (m/z): 699/701 [M+H]+ (3) (2R,4S)-4-P,5-Bis(toifluorometJi3d)benz34]-(5-bromopyrimidin amino-2 -ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (94 mg), tris(di"benzylideneacetone)dipalladium (2.5 rug), sodium tert-butoxide (19 mg), 2-(di»tert-butylphosphino)biphenyl (3 mg), morpholine (18 ]i\) are dissolved in toluene (1 ml), and the mixture is stirred at room temperature under nitrogen atmosphere for 60 hours. To the reaction solution is added acetic acid, and thereto are added water and ethyl acetate. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 19:1—>3:2) to give (2R,4S)"4-{[3,5-bis(trifluoromet±tyl)ben2yl]-[5-(morpholin-4-3d)" pyrimidin-2-yl]}amino-2-et±iyl-6-txifluorom 1-carboxylic acid ethyl ester (40 mg). MS (m/z): 706 [M+H]+ Examples 2-6 The corresponding starting compounds are treated in a similar manner to Example l-(3) to give the compounds as listed in Table 1. Example 7 (2R,4S)-4-{[3,5-Bis(trifluorom 3d)pyrimidin-2-yl]}ajnino-2-eti^ quinoline-1-carboxylic acid ethyl ester (75 mg) is dissolved in chloroform (3 ml), and thereto is added m-chloroperbenzoic acid (2 5 mg), and the mixture is stirred at room temperature overnight. To the reaction solution are added water and chloroform, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; chloroform:acetone = 10:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-[5-(l-oxo1±domorpholin»4-yl)pyriinidin-2-yl]}amino-2-e1Jiyl-6-1rifluoror3iethyl-3,4-dihydro-2H-quinoline-l»carbo^lic acid ethyl ester (34 mg). MS (m/z): 738 [M+H]+ Example 8 (2R,4S)-4-{[3f5-Bis(trifluoromethyl)benzyl]-(5-bromopyriniidin-2-}d)}amino-2 -ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (250 mg) and dichlorobis(tri-o-tolylphosphine)palladiuin (5.9 mg) are dissolved in toluene (2 ml), and the mixture is heated at 100°C under nitrogen atmosphere. To the reaction solution is added (dimethyl-amino)trimethyltin (118 mg), and the mixture is stirred for 2 hours. The mixture is allowed to cool to room temperature, and the reaction solution is concentrated under reduced pressure. The resulting residue is purified by column chromatography (NH-silica gel; hexane:ethyl acetate = 5:1) to give (2R,4S)-4-{[3,5-bis(1xifluoromethyl)ber^ yl)}aniino-2-ethyl-6-iTifluoromethyl-3,4-dihydro-2H-quinoline-l-carbo3cylic acid ethyl ester (18 mg). MS (m/z): 664 [M+H]+ Example 9 (1) (2R,4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H" quinoline-1-carboxylic acid ethyl ester (600 mg) and 2-chloro-5- propylpyrimidine (1.5 g) are dissolved in 1,3-dimefoylimidazolidinone (10 ml), and the mixture is stirred at 135°C for 72 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexanetethyl acetate = 6:1—4:1) to give (2R,4S)-2-ethyl-4-(5- propylpyrimidin-2-yl)amino-6-trifl^ 1 - carboxylic acid ethyl ester (250 mg). MS (m/z): 437 [M+H]+ (2) (2R,4S)-2-Ethyl-4-(5-propylpyrfciudin-2-yl)amino-6-1xifluoromethyl- 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (240 mg) and 3,5- bis(trifluoromethyl)benzyl bromide (337 mg) are dissolved in N,N-dimethyl- formamide (3 ml), and thereto is added sodium hydride (62.7 %, 32 mg) at room temperature, and the mixture is stirred at the same temperature for 2 hours. To the reaction solution is added acetic acid, and water and ethyl acetate are added thereto. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 49:1—7:3) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(5- propylpyrimidin-2-yl)}ainJn^ quinoline-1-carboxylic acid ethyl ester (130 mg). MS (m/z): 663 [M+H]+ Example 10 To (2R,4S)-4-P,5-bis(trffluoro yl)}amino-2-ethyl-6-txifluorometh34-3,4-dihydro-2H«quinoUne acid ethyl ester (1 g) are added N,N-dimethylformamide (10 ml), tetrakis-(triphenylphosphine)pallaciiutn (a catalytic amount), and zinc cyanide (176 mg), and the mixture is stirred at 110°C under nitrogen atmosphere for 4 hours. The reaction solution is cooled to room temperature, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The orgaixic Ia3'er is washed with a saturated brine, dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 10:1—*4:1) to give (2R,4S)-4-{[3,5-bis(trifluoro-mefoyl)benzyl]-(5-cyanopyriimdm^ 3,4-dibydro-2H-quinoline- 1-carboxylic acid ethyl ester (760 mg). MS (m/z): 646 [M+H]+ Example 11 (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-(5-cyanop5Timidin-2-yl)}amino-2-ethyl-6-trifluo romethyl~3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (200 mg) is dissolved in ethanol (3 ml), and thereto is added a catafytic amount of Raney nickel, and the mixture is stirred at room temperature overnight under hydrogen atmosphere. The catalyst is removed by filtration, and the filtrate is concentrated under reduced pressure. The residue is purified by column chromatography (silica gel; hexane: ethyl acetate * 1:1) to give (2R,4S)-4-{(5-aminomethylpyrimidin-2-yl)-[3,5-bis(trifluoromethyl)benzyl]}arnino--2-ethyl-6"trifluoromethyl--3,4-dihydro-2H-quinoline-l-csrboxylic acid ethyl ester (142 mg). MS (m/z): 650 [M+H]+ Example 12 (2R,4S)-4-{[3,5-Bis(1xffiuoromethyl)te pyrimidm-2-yl)}ainmo-2-ethyl-^ 1-carboxylic acid ethyl ester (92 mg) and an excess amount of triethyl-amine axe dissolved in methylene chloride (2 ml), and thereto is added an excess amount of N,N-dimethylsialfamoyl chloride under ice-cooling. The mixture is stirred at room temperature for 2 hours, and to the reaction solution are added a saturated brine and ethyl acetate. The organic layer is dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified b}^ column chromatography (silica gel; hexane:ethyl acetate = 4:1-^67:33) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)ben^l]-[5-(N?N-dime1fty amino-2-ethyl-6-trifluoromethyl-3 ,4-dilrydro-2H-quinoline-1 -carboxylic acid ethyl ester (54 mg). MS (m/z): 757 [M+H]+ Example 13 Acetic acid (88 ]il) is dissolved in toluene (3 ml), and thereto are added triethylamine (236 jal) and diphenylphosphoryl azide (466 yd). The mixture is stirred at 70 °C for 1.5 hour. To the reaction solution is added (2R,4S)-4-{(5-ajninome1liylpyr^ ben^l]}ainino-2-ethyl-6-trifluoroirieth34-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (100 mg), and the mixture is stirred at the same temperature for 4 hours. The mixture is allowed to cool to room temperature, and to the reaction solution are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic laj'er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (NH-silica gel; hexane:ethyl acetate = 1:2) to give (2R,4S)-4-([3,5-bis(txiQuoromethyl)beri2yl]-{5-[(3-me1ii34ureido)me1iiyl]-pyrimidin-2-yl})ainino-2-ethyl-6-trifluoromethyl-3,4'dihydro-2H-quinoline-1-carboxylic acid ethyl ester (63 m.g). MS (m/z): 707 JM+H]+ Example 14 4-(2-Aminoethyl)morpholine (100 mg) is dissolved in tetrahydrofuran (3 ml),..and. thereto is added N,N"'-carbon3^1diimidazole (125 mg), and the mixture is stirred at 70°C for one hour. To the reaction solution is added (2R,4S)-4-{[3,5-bis(trifluoromethyl) benzyl]- (5-aminometiiylpyrimiciin"2-34)}amino-2»ethyl-6-trifluoromethyl-3,4-ditiydro-2H-quinoline-1 -carboxylic acid ethyl ester (100 mg), and the mixture is stirred at the same temperature for 4 hours. The mixtuxe is allowed to cool to room temperature, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. Th.e organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato-graphy (NH-silica gel; ethyl acetate) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)ben^4]-[5-[3-(2-morpholm-4^ 3'l]}amino-2-ethyl-6-txifluorom acid ethyl ester (118 mg). MS (m/z): 806 [M+H]+ Example 15 (2R,4S)-4-{[3?5-Bis(1xifluorom l)}ammo-2-ethyl-6-txifluorometi^ acid ethyl ester (300 mg), palladium acetate (12 mg), l,r-bis(diphenyl-phosphino)ferrocene (55 mg), benzyl alcohol (970 mg) and triethylamine (625 )il) are dissolved in N,N-dimethylfonraamide (1 ml), and the mixture is stirred at room temperature under cartoon monoxide atmosphere for 3 minutes. Subsequently, the mixture is heated at 90°C and stirred overnight. The reaction solution is cooled to at room temperature, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, ajnd concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:etbyl acetate « 24:1-^-3:1) to give (2R,4S)-4-{(5~benzyl-oxycarbonylpyrimidin-2-yl}-[3?5-bis(txffl^ 6-trifluorometh54-3,4-dihydro-2H-quinolin.e-l-carboxylic acid ethyl ester (250 mg). MS (m/z): 755 [M+H]+ Example 16 (2R,4S)-4-{(5-Ben^loxycarbonylpyrin^ metfryl)benzyl]}amino-2-eth^ l-carbo^lic acid ethyl ester (220 mg) is dissolved in a mixture of methanol (2 ml) and tetrahydrofuran (6 ml), and thereto is added 10 % palladium-carbon (100 mg), and the mixture is stirred at room temperature under hydrogen atmosphere for 30 minutes. The catalyst (10 % palladium-carbon) is removed by filtration, and the filtrate is concentrated under reduced pressure. The resulting residue is purified by column chromato-graphy (silica gel; ethyl acetate) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)-ben2yl]-(5-carboxypyrimidin-2-yl)}am^^ dihydro-2H-quinoline-l-carboxylic acid ethyl ester (178 mg). MS (m/z): 665 [M+H]+ Example 17 (2R,4S)-4-{[3,5-Bis(1xffluoromethyl^ yl)}ammo-2-e1±Lyl-6-1xifluorom acid ethyl ester (100 mg) and an excess amount of 1-hydroxybenzotriazole hydrate are dissolved in N,N-dimeth3^1fonixamide (5 ml), and thereto is added an excess amount of l-ethyl-3-(3-diiaethylaminopropyl)carbodiimide hydrochloride, and the mixture is stirred at room temperature for 10 minutes. To the reaction solution are added glycine tert-butyl ester Itydrochloride (50 mg) and an excess amount of triethylamine, and the mixture is stirred at room temperature for 10 minutes. To the reaction solution are added an aqueous citric acid solution and ethyl acetate, and the organic layer is washed with a saturated aqueous sodium hydrogen carbonate solution, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato-graphy (silica gel; hexane:ethyl acetate = 9: 1—*1:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)ben^l]-(5-tert-buto^ pyriixudm-2-yl)}ammo-2-e1±yl-6-t 1-carboxylic acid ethyl ester. Then, to the mixture is added a 4N hydrochloric acid in 1,4-dioxane (2 ml) a"t room temperature, and the mixture is stirred overnight. The reaction solution is concentrated under reduced pressure, and the concentrated residue is purified bj^ column chromatography (silica gel; hexane:etlxyl acetate = 1:1—►chloro-formrmethanol = 19:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(5-carboxjnmethylcarbamoylpyrimidin^ 3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (13 mg). MS (m/z): 722 [M+H]+ Example 18 (1) (2R,4S)-4-{[3,5-Bis(trffluoromefo^ yl)}amino-2-etiiyl-6-trifluoromet^ acid ethyl ester (300 mg), acrylic acid benzyl ester (125 mg), tris(di-benzylideneacetone)dipalladium (12 mg), diisopropylethylamine (90 \il), tri-tert-butylphosphonium tetrafluoroborate (7.5 mg) are dissolved in 1,4-dioxane (3.5 ml), and the mixture is stirred under nitrogen atmosphere at room temperature for 3 days. To the reaction solution are added an aqueous citric acid solution and ethyl acetate, and the organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by colunxn chromatography (silica gel; hexane:ethyl acetate = 97:3-^13:7) to give (2R,4S)-4-{[5-(2-benz54ox5r-carbonylvinyl)pyriinidin-2-3d]-[3,5-bis(trifluoromethyl)ben2yl]}amino-2» ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (186 mg). MS (m/z): 781 [M+H]+ (2) (2R,4S)-4-{[5-(2-Benzyloxycarb^ (trifluorometh3d)ben2yl]}am quinoline-l-carboxjdic acid ethyl ester (180 nig) is dissolved in a mixture of methanol (5 ml) and tetrahydrofuran (10 mJ), and thereto is added 10 % palladium-carbon (300 mg). The mixture is stirred at room temperature i under hydrogen atmosphere for 3 hours. The catalyst is removed by filtration, and the filtrate is concentrated under reduced pressure to give (2R,4S)-4-{[3,5-bis(tri^ yl]}ainino-2-etii3d-6-txifluoromethyl-3,4--dihydro»2H-quinoline--1 -carboxylic acid ethyl ester (40 mg). MS (m/z): 693 [M+H]+ Example 19 (2RJ4S)-4-{[3,5-bis(trifluoromethLyl)ben2yl]-(5-cyanopyrimidin»2-34)}amino-2-ethyl-6-1xifluoromethyl-3?4--dihydro-2H-quinoline-l-carboxylic acid ethyl ester (880 mg), sodium azicle (886 mg) and ammonium chloride (729 mg) are dissolved in N^N-dimethj^lformamide (5 ml), and the mixture is stirred at 100°C for 4 hours. The mixture is allowed to cool to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give (2R,4S)-4-{[3?5-bis(trifluoro-me1&yl)ben2ylH5-(te1xa2ol-5-yl)pyri meth3d-3,4-dihydro-2H-quinoline-l-caLxbox5^1ic acid ethyl ester (920 mg). MS (m/z): 689 [M+H]+ Example 20 (2R,4S)-4-{[3,5-Bis(1xifluorometl^34)benzyl]"[5-(tetrazol-5-yl)pyrimidin-2-yl]}amino-2-ethyl-6-1xifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (150 mg), potassium carbonate (60 mg), and an excess amount of methyl iodide are dissolved in N,N-dimethylformamide (2 ml), and the mixture is stirred at 50°C for 4 hours. The mixture is allowed to cool to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatographLy (silica gel; hexane: ethyl acetate = 9:1->4:1) to give (2R,4S)-4-p,5-bis(trifluoromethyl)benzyl]-[5-(2-methyl-2H-te1xazol"5"3d)p3Timidin-2-yl]}ajnino-2-ethyl-6-trifluoromethyl-3?4-dih3rdro-2H-quinolme-l-carboxylic acid, ethyl ester (107 mg). MS (m/z): 703 [M+H]+ Examples 21-22 The corresponding starting compounds are treated in a similar manner to Example 20 to give the compounds as listed in Table 2. Table 2 Example 23 (2R,4S)-4-{[3,5-Bis(txinuorometh3^1)benzyl]-[5-(tetra2ol-5-3d)pyrimidin-2-yl]}amino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quinoline"l-carboxylic acid ethyl ester (127 mg), 4-(2-hydrox^yethyl)morpholine (35 |il), and triphenylphosphine (76 mg) are dissolved in tetrahydrofuran (3 ml), and thereto is added dropwise 40 % solution of a-zodicarboxylic acid diethyl ester in toluene (113 pi) under ice-cooling, and the mixture is stirred at room temperature for 4 hours. To the reaction solution are added water and ethyl acetate, and the organic laj^er is washed with a saturated brine, dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chrornatography (NH-silica gel; hexanerethyl acetate = 9: l->67:33) to give (2 R,4S)-4-([3,5- bis(trifliioromethyl)ber^ yl]pyrimidin-2-yl})amino-2-etliyl-6- quinoline-1-carboxylic acid ethyl ester (136 nig). MS (m/z): 8O2 [M+H]+ Example 24 (1) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)be^ yl)}ainino-2-e&34-6-txifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (1.00 g) is dissolved in 1,4-dioxane (4.0 ml), and thereto are added sodium iodide (857 mg), copper iodide (27 mg) and trans-N,N'- dimethylcyclohexane-l,2-diamine (43 mg), and the mixture is stirred at 110 °C under nitrogen atmosphere overnight. The mixture is allowed to cool to room temperature, and thereto is added a diluxted aqueous ammonia, and the mixture is extracted with ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b}' column chromatography (silica gel; hexane:ethyl acetate = 97:3—^70:30) to give (2R,4S)»4-{[3,5-bis(trmuorometh3d)benzyl]-(5-iodopyximidin-2-tvl)}- amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline" 1-carboxylic acid ethyl ester (969 mg). MS (m/z): 747 [M+H]+ (2) To (2R,4S)-4»{[3,5"bis(trifluoromethyl)ben2yl]-(5-iodaepyrimidin-2- yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline» 1-carboxylic acid ethyl ester (200 mg) are added 2-methoxyethanol (l.O ml), cesium carbonate (350 mg), copper iodide (23 mg) and 1,10-phenanthroline (44 mg), and the mixture is stirred at 110°C for 4 days. The mixtiire is allowed to cool to room temperature, and thereto is added water, and the mixture is extracted with ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b3' column chromato graphy (silica gel; hexane:ethyl acetate = 10:1, and NH-silica gel; hexane:ethyl acetate = 10:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)- ben^l]-[5-(2-methoxyethoxy)p3T^ methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (90 mg, MS (m/z): 695 [M+H]+) and (2R,4S)-4-fl3,5-bis(txiflu^^ methoxyethoxy)priniidin-2-yl]iodop3T^ txifluorometh3d"3,4-dihydro-2H"quinoline-l--carbo^'lic acid 2-rnethoxyethyl ester (28 mg, MS (m/z): 725 [M+H]+). Example 25 (1) (2R,4S)-4-Amino-2-etiiyl-6-trifluoromethyl-3,4-dihydrO"2H- quinoline-1-carboxylic acid ethyl ester (1 g), 6-chloronicotinonitrile (1.76 g), dusopropylethylamine (804 |il) are dissolved in N,N-dimethylformamide (15 ml), and the mixture is stirred at 100°C overnight. The reaction solution is cooled to room temperature, and thereto are added an aqueoiis citric acid solution and ethyl acetate. The organic layer is washed withL a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chr-omatography (silica gel; chloroform:hexane:ethyl acetate = 5:5:1) to give (2R,4S)-4-(5- cyaJiop3^ridin-2-yl)airiino«2«e1±i3d«6"trifluorometh3^«3,4-dihydro -2H- quinoline-1-carboxylic acid ethyl ester (800 mg). MS (m/z): 4L 9 [M+H]+ (2) (2R,4S)-4-(5-Cyanop3Tidin-2-yl)amino-2-eth3d-6-triiluorome&34-3,4- dihydro-2H~quinoline-l-carboxylic acid ethyl ester (790 mg) and 3,5-bis- (trifluoromethyl)benzyl bromide (1.159 g) are dissolved in N,N-dimethyl- formamide (9 ml), and thereto is added sodium hydride (62.7 ^b, 108 mg) at room temperature, and the mixture is further stirred for 15 minutes. To the reaction solution is added acetic acid, and thereto are added a saturated brine and ether. The organic layer is washed witti a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chiromatography (silica gel; hexane:ethyl acetate = 19:1-^17:8) to give (2R,4S)-4-{[3,5-bis- (trifluorome1hyl)ben2yl]-(5-cyauiop3^din-2-yl)}amino-2-ethyl-6-trifluoro- meth34-3,4rdihydro-2H-quinoline-l"Carboxylic acid ethyl ester (700 jng). MS (m/z): 645 [M+H]+ Example 26 (2R?4S)-4-p,5-Bis(trifluoromethyl)benzyl]-(5-cyanopyridin-2^1)^ aimno-2-et±iyl-6"trifiuoromethyl-3,4-dihydro-2H~quinoline-1 -carboxylic acid ethyl ester (127 ing), sodium azide (300 mg) and ammonium chloride (300 mg) are dissolved in N,N«dimethylformamide (5 rnl), and the mixture is stirred at 95°C overnight. The mixture is allowed to cool to roozni temperature, and thereto are added water and ethyl acetate. The organ_ic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)benzylH5-(tetrazol-5-yl)pyridm^ methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (128 mg). MS (m/z): 688 [M+H]+ Example 27 (1) (2R,4S}-4-Aniino-2"eth3^-6-trifluoromethyl-3,4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (1.5 g) and 2-chloro-5-nitropyridine (3.795 g) axe dissolved in l,3-dimeth3^1imidazolidinone (25 ml), and tfcie mixture is stirred at 140°C for 74 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. Tfcie organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; chloroform—*hexane: ethyl acetate = 3:1) to give (2R?4S)-2-ethyl-4-(5-nitropyridin-2^1)amino-^- trifluoromethyl-3>4-dih3^dro-2H-quinoline«l-carboxylic acid ethyl ester (991 mg). MS (m/z): 439 [M+H]+ (2) (2R,4S)-2-Ethyl-4-(5-nitropyridin-2-3d)amino-6-trifluorometh3d-3,4- dih3'dro-2H-quinoline~l-carboxylic acid ethyl ester (980 mg) and 3,5- bis(trifluoromettryl)benzyl bromide (1.372 g) are dissolved in N,N-dimethyl- formamide (10 ml), and thereto is added sodium hydride (62.7 %, 171 vcxg) at room temperature t and the mixture is stirred for 15 minutes. To tine reaction solution is added acetic acid, and thereto are added water and ethyl acetate. The organic layer is washed again with water, and the organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato-graphy (silica gel; hexane:ethyl acetate = 49:1-^13:7) to give (2R,4S)-4-{[3,5-bis(trifluoromettiyl)be^ trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (650 mg). MS (m/z): 665 [M+H]+ Example 28 (1) (2R,4S)-4-[3,5-Bis(1rffluorome1±Lyl)ben^ methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (600 mg) is dissolved in ethanol (5.0 ml), and thereto are added cyanogen bromide (129 mg) and sodium hydrogen carbonate (283 mg), and the mixture is stirred at room temperature for 23 hours and 15 minutes. Distilled warer is added to the mixture, and the mixture is extracted with ether. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chrornatography (silica gel; hexane:ethyl acetate = 4:l->3:2) to give (2R,4S)-4-{[3,5* bis(trifluoromethyl)benzyl]-cya^ dihydro-2H-quinoline-l-carboxylic acid ethyl ester (581 mg). MS (m/z): 585 [M+H20]+ (2) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-cyano}amino-2-ethyl-6- 1rifluoroxnethyl-3,4-dihydro-2H-quinoline-l'Carboxylic acid ethyl ester (50 mg) is dissolved in N7N-dimethylformamide (1 ml), and thereto are added sodium azide (57.2 mg) and ammonium chloride (47.1 mg), and the mixture is stirred at 100°C for 16.5 hours. The mixture is allowed to cool to room temperature, and thereto is added distilled water, and the mixture is extracted with ethyl acetate. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chrornatography (silica gel; chloroform:methanol = 9:1) to give (2R,4S)-4-{[3T5-bis(trifluoromethyl)benzyl]-(te1xazol-5-yl)amino}-2-ethyl-6-trifluorometh3d-3?4--ciihydro-2H--quinoline-- 1-carboxylic acid ethyl ester (45 rng). MS (m/z): 611 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(1rifluoro^ ethyl-6-trifluorometh3^1-3,4-dih3^dro-2H-quinoline-l-carboxylic acid etiryl ester (150 mg) is dissolved in tetralrydrofuran (2.5 ml), and thereto is added sodium hydride (62.7 %, 9.6 mg), and the mixture is stirred for 10 minutes. To the mixture is added propane 1-bromide (23 p.1), and the mixture is stirred for 27 hours. Distilled water is added to the mixture, and the mixture is extracted with ethyl acetate. The extract is washed with a saturated brine, and the organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexanerettryl acetate = 10:1^4:1) to give (2R,4S)-4"{[3,5-bis(trifluoromethyl)benzyl]-(2-prop3d-2H-tetrazol-5-yl)}amino-2-eth3=rl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (26 mg). MS (m/z): 653 [M+H]+ Examples 29-30 The corresponding starting compounds are treated in a similar manner to Example 28-(3) to give the compounds as listed in Table 3. Example 31 (2R,4S)-4-{[3,5-Bis(trmuoromethyl)benzyl]-(tetrazol-5-yl)}amino-2-etihyl-6-tiifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (100 mg) is dissolved in N?N-dimethylformamide (1 ml), and thereto are added 3-bromopropionic acid methyl ester (103.6 |il)> triethylamine (2 ml) and a catalytic amount of potassium iodide, and the mixture stirred at 70°C for 48 hours. Distilled water is added to the mixture, and the mixture is extracted with ether. The extract is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatograptry (silica gel; hexane:ethyl acetate = 9:1->4:1) to give (2R,4S)-4-{[3,5-bis(trifluorometh3d)benzyl]-[2-(2-methoxy-carbonylethjd)-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (581 mg). MS (m/z): 697 [M+H]+ Examples 32-34 The corresponding starting compounds are treated in a similar manner to Example 31 to give the compounds as listed in Table 4. Example 35 (2R,4S)-44[3,5-Bis(trifluorometh34)benzyl]-(tetrazol-5-yl)}amino-2-ethyl-6-trifluorometh3d-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (200 mg) is dissolved in tetrahj'drofuran (5 ml), and thereto are added 2-dimeth3^aminoethanol (50 \xL), a 40 % solution of diethyl azo-dicarboxylate in toluene (220 ]al) and triphenylphosphine (131.1 mg), and the mixture is stirred at room temperature for 1.5 hours. Distilled water is added thereto, and the mixture is extracted with ethyl acetate. The extract is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b3' column chromatography (silica gel; hexane:ethyl acetate = 9:1—4:1) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)benz3>"l]- [2 - (2 -dimetJiylaminoe1±Lyl)-2H-teiTazol-5-yl]}ajnino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quinoline-1 -carbosylic acid ethyl ester (155 mg). MS (m/z): 682 [M+H]+ Examples 36-45 The corresponding starting compounds are treated in a similar manner to Example 35 to give the compounds as listed in Table 5. Example 46 (2R?4S)»4-{[3,5-Bis(1xinuoromethyl)benz3^l]-[2-(2-inethoxycarbonyl-2-methylpropyl)"2H"tetrajsol-5-3d]}amino-2-ethyl-6-trifluoroinethyl-3>4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (300 mg) is dissolved in a mixture of ethanol (3 ml) and distilled water (0.5 ml), and thereto is added lithium hydroxide monohydrate (34.7 mg) under ice-cooling. The mixture is stirred at room temperature for 4 days, and thereto is added a saturated aqueous citric acid solution, and the mixture is extracted with methylene chloride. The organic Ia3^er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate - 2:1^1:2) to give (2R?4S)-4-{[3,5-bis(trifluoromethyl)-benzyl]-[2-(2-carbo^-2-meth3dpropyl}-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H«quinoline-l-carboxylic acid ethyl ester (262 mg). MS (m/z): 709 [M-H]-Examples 47-49 The corresponding starting compounds are treated in a similar manner to Example 46 to give the compounds as listed in Table 6. Example 50 (2R,4S)-4-{[3?5-Bis(1rmuorome1ii34)ben2yl]-[2-(3-methylthiopropyl)-2H-tetra^ol-5-34]}aroino-2-e1±iyl-6-trifluoromethyl-3,4-dihydro-2H--quinoline-1-carboxylic acid ethyl ester (175 mg) is dissolved in chloroform (2 ml), and thereto is added m-chloroperbenzoic acid (422.8 mg), and the mixture is stirred at room temperature for 30 minutes. To the mixture is added a saturated aqueous sodium hydrogen carbonate solution, and the mixture is extracted with ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato-grapby (silica gel; hexane:ethyl acetate = 7:3—^1:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benz5d]-[2-(3-methanesulfonylpropyl)-2H-tetra2ol-5-yl]}ainino-2-eth3d-6-iTifluoromethyl-3,4-dih3^dro-2H-'quinoline-l-carboxylic acid ethyl ester (180 mg). MS (m/z): 731 [M+H]+ Example 51 (2R,4S)-4-{[3,5-Bis(1rifluorometo^ tetra2ol-5-yl]}arnino-2-ethyl-6-1rifluorornethyl-3,4-dihydro-2H-quinoline-l-carbox3dic acid ethyl ester (200 mg) is dissolved in chloroform (2 ml), and thereto is added m-chloroperbenzoic acid (100.1 mg), and the mixture is stirred at room temperature for 2.5 hours. To the mixture is added a saturated aqueous sodium hydrogen carbonate solution, and the mixture is extracted with, methylene chloride. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; chloroform:methanol = 49:1—^19:1) to give (2R,4S}-4-{[3?5-bis(trifluoromefeyl)ben2yl]-[2-(2-methanesulfm34ethyl)-2H-tetr£Lzol-5-34]}amino-2-ethyl-6-trifluoroinethyl-3,4-'dihydro-2H-quinoline-l-' carboxylic acid ethyl ester (91.9 mg, MS {m/z): 701 [M+H]+) and (2R,4S)-4-{[3,5-bis(trifluorometh34)benz3d]-[2«(2-methanesulfonylethyl)-2H-tetrazol-5-ylDamino^-ethj^l-G-trifluoromethyl-S ,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (118.6 mg, MS (m/z): 717 [M+H]+). Example 52 (2R,4S)-4-{[3?5-Bis(trifluoromethyl)benz3d]-[2-(2?2-dimethyl-tl?3]di oxolan-4-ylmethyl)-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dittydro-2H-quinoline~ 1 -carboxylic acid ethyl ester (260mg) is dissolved in ethanol (2 ml), ajnd thereto is added Dowex [H+-tj>pe] (manufactured by The Dow Chemical Company) (4 g)> and the mixture is stirred at room temperature for 39.5 hours. The mixture is filtered by using methanol, and the filtrate is concentrated under reduced pressure. The resulting residue is purified bj^ column chromatograplry (silica gel; hexane:ethyl acetate = 9:1^4:1) to give (2R?4S)-4-{[3?5-bis(trifluoromethyl)benzyl]-[2« (2^-dih3'droxypropyl)-2H-tetrazol-5-yl]}^^ 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (200 rng). MS (m/z): 685 [M+H]+ Example 53 (2R,4S)-4-{[3?5-Bis(1rifluoromethyl)ben2yl]-(2-oxolanylmethyl-2H-tetrazol-5-yl)}am_ino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ettryl ester (100 mg) is dissolved in a solution which is previously prepared by adding sodium hydride (62.7 %, 0.6 mg) into ethanol (2 ml), and stirred at room temperature for 5 minutes, and the mixture is stirred for 18 hours and 40 minutes. Distilled water is added thereto, and the mixture is extracted with ether. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 9:1-^3:1) to give (2R,4S)-4-{[3?5-bis(trifluoromethyl)-benzyl]-[2«(3-ethox5r-2"hi3^drox3^propyl)-2H-tetrajzol-5-yl]}amino-2-eth3d-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (92.7 mg). MS(m/z);713 [M+H]+ Example 54 (2R,4S)-4-{[3>5-Bis(trifluoromethyl)ben2yl]-(2-oxolan3^1inethyl-2H-tetiB2ol-5-yl)}amino-2-ethyl-6-trifluoromethyl*3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (120 mg) is dissolved in ethanol (1 ml), and thereto is added a 28 °/o aqueous ammonia (1 ml). The mixture is stirred at room temperature for 18.5 hours. The reaction solution is concentrated under reduced pressure, and the resulting residue is purified b}' column chromatograph}' (silica gel; chloroformtmethanol = 49:1—> 19:1) to give (2R?4S)-4-{[2-(3-amino-2-hydroxyprop3d)-2H-tetrazol-5-yl)-[3,5-bis(trifluoro-methyl)ben^yl]}amino-2--ethyl-6-trifluoroinethyl-3)4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (51.2 mg). MS (m/z): 684 [M+H]+ Examples 55-58 The corresponding starting compounds are treated in a similar manner to Example 54 to give the compounds as listed in Table 7. Example 59 (1) (2R,4S)-4-{[3?5-Bis(trmuorometh3rl)benz34]cyano}amino-2-ethyl-6- trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (15 g) is dissolved in ethanol (150 ml), and thereto are added hydroxylamine hydrochloride (2.1 g) and trie thy lamine (4.2 ml), and the mixture is stirred at room temperature for 18 hours. Distilled water is added to the mixture, and the mixture is extracted with ether. The organic Ia3^er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato- graphy (silica gel; hexane-.ethyl acetate = 19:1—>7:3) to give (2R,4S)-4- {[amino(hj^droxyimino)meth34]-[3,5-bis(trifluoromethyl)benj^4]}ainino-2- ethyl-6-trifluorometh3'l-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (5.02 g). MS(m/z):601 [M+H]+ (2) (2R,4S)-4-{[Amino(hydroxyimino)m ben2yl]}ammo-2-et±Lyl-6-trifi^ carboxylic acid ethyl ester (60 mg) is dissolved in methylene chloride (1 ml) and thereto are added diisopropylethylamine (35 p.1) and hexanoic acid chloride (18 )al), and the mixture is stirred for 16 hours. Distilled water is added to the mixture, and the mixture is extracted with ether. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b}^ column chrornatography (silica gel; hexane:ethyl acetate « 19:1—>9:1) to give (2RJ4S}-4-[(amino{[(l"OXohex34)ox3^]imino}meth34)-[3,5-bis(trifluoro-- nxeth3^1)ben^d]]amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (60.6 mg). MS (m/z): 699 [M+H]+ (3) (2R>4S)-44(Amxno{[(l-oxohexyl}o^]iinino}methyl)-[3,5-bis(trifluoro-naethyl)benz5^]]ainino-2-ethyl-6-trifluoroineth3d-3,4-dihydro-2H-quinoline-l-carbox}rlic acid ethyl ester (37 mg) is dissolved in ethanol (1 ml), and thereto is added sodium methoxide (0.3 mg), and the mixture is stirred for one hour. Distilled water is added to th.e mixture, and the mixture is extracted with ether. The organic Ia3^er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 9:1) to give (2R.?4S)-4-{[3,5-bis(trifluoromethyl)-benzyl]-(5-pentyl-[l,2,4]oxadia2ole-3-yl)}ari]Lino-2-eth3'l-6'-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (60.6 mg). MS (m/z): 681 [M+H]+ Example 60 (2R,4S)-4-{[Amino(hydroxyimino)metln3d]«[3,5-bis(trifluoromethyl)-benzyll}amino-2-eth3d-6"trifluoromethyl-3,4 -dihydro-2H~quinoline-1-carbox3dic acid ethyl ester (154 mg) is dissolved in methylene chloride (1.5 ml), and thereto sure added diisoprop34etti34amine (89 jil) and methoxy-acetic acid chloride (30 p.1), and the mixture is stirred for 18 hours. Distilled water is added to the mixture, and the mixture is extracted with ether. The organic Ia3'er is washed with, a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b3' column chrornatography (silica gel; hexane:ethyl acetate « 2:1) to give (2R.,4S)-4-{[3,5-bis(trifluoromethyl)- benzyl]-(5-metho;symethyH ^ methyl-3>4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (118.3 mg). MS (m/z): 655 [M+H]+ Examples 61-63 The corresponding starting compounds are treated in a similar manner to Example 60 to give the compounds as listed in Table 8. Example 64 (2R?4S)-4-{(5-Aceto^methyl"[l?2,4]oxadiazol-3-yl)-[3J5-bis(trifluoro-methyl)benz5^1]}£Lrnino-2-ethyl-6-trifluoroTne&yl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (30 mg) is dissolved in ethanol (1 ml), and thereto is added potassium carbonate (60.8 rng), and the mixture is stirred for 30 minutes. Distilled water is added, and the mixture is extracted with ether. The organic layer is washed with a. saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane;ethyl acetate » 4:l-*7:3) to give (2RJ4S)-4-{[3,5-bis(trifluoromethyl)-ben2yl]~(5-hydroxymethyl-[l?2,4]oxadia2ol-3^ methyl-3,4-dihydro-2H-quinoline-l'Carbox5;plic acid ethyl ester (22 mg). MS (m/z):6-41 [M+H]+ Example 65 (2R,4S}~4-{[3,5-Bis(txifluorometiiyl^ oxadiazol-3-yl)}amino-2-ethyl-6-trifluorom 1-carboxylic acid ethyl ester (100 mg) is dissolved in a mixture of methanol (0.5 ml) and tetrahydrofuran (0.5 ml), and thereto is added morpholine (0.1 ml). The mixture is stirred at 45°C for 2 hours. The mixture is allowed to cool to room temperature, and thereto is added IN hydrochloric acid, and the mixture is extracted with ether. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato-graphy (silica gel; hexane;ethyl acetate = 4:l->7:3) to give (2R,4S)-4-{[3,5-bis(triflu.oromei±iyl)ben254]-[5-(morpholin-4-3d)meth3^1-[l?2,4]oxadiazol-3-yl]}amino-2-eth34-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (69 mg). MS (m/z): 710 [M+H]+ Examples 66-67 The corresponding starting compounds are treated in a similar manner to Example 65 to give the compounds as listed in Table 9. Example 68 (2R,4S)-4--([3,5-Bis(trifluoromethyl)benzyl]«{[5-((2S)-2-tert-butoxy-carbonylpyn^oUciin- l-yl)methyl]-[l ,2,4]oxadiazol-3-yl})ainino-2 -ethyl-6-txifiuorornethyl-3,4-dih3^dro-2H-quinoline-l-carbox3^1ic acid ethyl ester (55 mg) is dissolved, in a 4 N hydrochloride 1,4-dioxane solution (0.5 ml)? and the mixture is stirred at room temperature overnight. The reaction solution is concentrated under reduced pressure, and the resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 4: ^chloroform) to give (2R,4S)-4-([3,5-bis(trifluoromethyl)benzyl]-{[5-((2S)-2-carboxypyrrolidin-l-yl)methyl]-[l!2;4]oxadiazol-3"yl})amino-2-ethyl-6-trifluoromethyl-3!,4-dihydro"2H-quinoline-l-carboxylic acid ethyl ester (27.5 mg). MS (m/z): 738 [M+H]+ Example 69 (1) (2R,4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carfeoxylic acid ethyl ester (1 g), 4,6-dichloropyrixnidine (1.9 g)> and diisopropylamine (824 mg) are dissolved in N,N-dimethylformamide (15 ml), and the mixture is stirred at 80°C for 3 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatograpby (silica gel; hexane:ethyl acetate * 19:l-*7:3) to give (2R,4S)-4-(6-chloropyrimidin-4-yl)airiino-2-ethyl-6-trifluoromethyl- 3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (1.088 g). MS (m/z): 429/431 [M+H]+ (2) (2R,4S}-4-(6"Chlorop3^rimidin-4-yl)amino-2-ethyl-6-triflu 3?4-dihydro-2H-quinoline-l-caxboxylic acid ethyl ester (100 mg), 3,5-bis- (trifluoromethyl)benzyl bromide (143 ing), and sodium hydride (62.7 %> 18 rng) are dissolved in N,N-dimethylformaniide (2 ml), and the mixture is stirred at 55°C for 15 minutes. The reaction solution is cooled to room temperature, and thereto are added an aqueous citric acid solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatograph.y (silica gel; hexane:ethyl acetate - 49:1->3:1) to give (2R,4S)-4-{[3,5-bis(trifluoro- me1±L3d)benzyl]-(6-chloropyrimidm^ 3,4-dihydro-2H-quinoline-l-caxboxylic acid ethyl ester (75 rag). MS (m/z): 655/657 [M+H]+ (3) A mixture of (2R,4S)-4-{[3,5-bis(trifluoromethyl)ben.zyl]-(6-chloro- pyriirudin-4-yl)}arnino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (220 mg) and morpholine (4 ml) is stirred at 70°C for 20 minutes. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 19:1—>3:2) to give (2R)4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-[6-(morpholin-4-yl)- pyrirnidin-4-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (110 mg). MS (m/z): 706 [M+H]* Examples 70-75 The corresponding starting compounds are treated in a similar manner to Example 69-(3) to give the compounds as listed in Table 10. Example 76 (1) (2R,4S)-4-Aminio-2-ethyl-6-trifluoroineth34-3>4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (1 g), 4-chloro-2-methylthio-pyrixnidine (2.04 g), and diisoprop34ethylamine (890 pi) are dissolved in N,N-dimethylformamide (15 ml), and the mixture is stirred at 100 °C overnight. The reaction solution is cooled to room temperature, and thereto are added an_ aqueous citric acid solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over ma_gnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 9:l->3:2) to give (2R,4S)-2-eto34-4-(2-methylthiopyrimidin-4-yl)amino-6-trifluorometh3d-3?4-dihydro-2H-quinoline-l-carboxylic acid ethjd ester (1.07 g). MS (m/z): 4-41 [M+H]+ (2) (2R,4S)-2-Eth3^1-4-(2-methylthiopyrimidin-4^yl)amino-6-trifluoro-methyl-3f4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.05 g) and 3?5-bis(trifluorometh3d)benzyl bromide (1.465 g) are dissolved in N?N-dimethylformamide (10 ml), and thereto is added sodium hydride (62.7 %9 137 mg) at room temperature, and the mixture is stirred for one hour. To the reaction solution is added acetic acid, and thereto are added water and ether. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 9:l->7:3) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)benzyl]-(2 methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.35 g). MS (m/z): 667 [M+H]+ Example 77 (2R>4S)-4-{[3,5-Bis(triQuoromethyl)benzyl]-(2-methylthiopyrimidin-4-yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (133.2 mg} is dissolved in chloroform (3 ml), and thereto is added m-chloroperbenzoic acid (64,5 mg) at room temperature, and the mixture is stirred for 5 minutes. To the reaction solution is added NH-silica gel, and the NH-silica gel is removed by filtration, and the filtrate is concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 4:1—►0:l) bis(trifluoromethyl)benzyl]-(2- 6-trifluoromethyl-3?4-dihydro-2H"quinoline- 1-carboxylic acid ethyl ester (66 mg, MS (xn/z): 699 [M+H]+). Example 78 Hydroxylamine hydrochloride (2(59 mg) is suspended in dimethyl-sulfoxide (3 ml), and thereto is added triethylamine (0.54 ml). The insoluble materials are collected by filtration, and washed with tetrahydro-furan. Tetrahydrofuran is removed from the filtrate by evaporation under reduced pressure to give a solution of bLydroxylamine in dime thy lsulfoxide. To this solution is added (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(5-cyanopyrimidin-2-yl)}arnino-2-ethyl-6-trifluorornethyl-3,4-dih3^dro-2H-quinoline-1-carboxylic acid ethyl ester (500 mg), and the mixture is stirred at 75°C for 30 minutes. The mixture is allowed to cool to room temperature, and to the reaction solution are added ethyl acetate and a saturated brine. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give {2R,4S)-4-{[3>5-bis(trifluoromethyl)benzy^l]-[5-(N-h3'rdroxycarbamimidoyl)-p3n:imidin-2-yl]}amino-2-eth34-6-trifluorc>methyl-3>4--dihydro-2H-quinoline-1-carboxylic acid ethyl ester (520 mg). MS (m/z): 679 [M+H]+ Example 79 (2R,4S)-4-{I3,5-Bis(iTifluoromethyl)benzyl]-(2-methylsulfonyl-pyrimidin-4-yl)}amino-2-ethyl«6-trifluoromethyl-3?4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (100 mg) and an excess amount of 2-amino-ethanol are dissolved in 1,3-dimeth3^1imidazolidinone (2 ml), and the mixture is stirred at 90°C for one hour. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatograplry (silica gel; hexane:ethyl acetate =3:2^1:4) to give (2R,4S)-4-{[3?5-bis(triiluoromethyl)benzyl]-[2-(2-hydro^- ethylammo)pyrimidin-4-y^ 2H-quinoline-l-carboxylic acid ethyl ester (72 mg). MS (m/z): 680 [M+H]+ Examples 80-82 The corresponding starting compounds are treated .in a similar manner to Example 79 to give the compounds as listed in Table 11. Example 83 4-Methoxybenzyl alcohol (136 mg) is dissolved in N,N-dimeth3'l-formamide (3 ml), and thereto is added sodrum hydride (62.7 %, 42 rng) at room temperature, and the mixture is stixred for 30 minutes. To the reaction mixture is further added (2R,-4S}-4-{[3,5-bis(trifluoromethyl)-benzyl]-(2-methylsulfonylp3oimidin^ 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (686 mg), and the mixture is stirred for 5 hours. Acetic acid is added to the reaction solution, , and thereto are added water and ethyL acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. Thte resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 9:1-+1:1) to give (2R,4S)-4-{[3,5-bis(trifluo^ P3rrimidin-4-yll}amino-2-ethyl-6-trifluoroiaethyl-1-carboxylic acid ethyl ester (600 mg). MS (m/z): 757 [M+H]+ Example 84 (1) (2R,4S)-4-{[3?5-Bis(trifluoromethyl)benzyl]-[2-(4-methoxybenz3doxy)- P3^rimidin-4-3d]}amino-2-ethyl-6-trifluoroniethyl-3?4-dih3^dro-2H-quinoline- 1-carboxylic acid ethyl ester (570 mg) is dissolved in 1,4-dioxane (4 ml), and thereto is added cone, hydrochloric acid (4 ml) at room temperature. The reaction solution is stirred for 15 minutes, and neutralized with a saturated aqueous sodium hydrogen carbonate solution. Ethyl acetate is added to the reaction solution, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato graphy (silica gel; hexanerethyl acetate = 1:1—►Orl) to give (2R?4S)-4-{[3,5- bis(txifluoromeiJiyl)benzyl]-(2-hydrox3^pyrinaidin-4-yl)}amino-2-eth34-6- trifluoromethyl-3>4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (410 mg). MS (m/z): 637 [M+H]+ (2) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-(2-h3^droxypyrimidin-4- 3d)}amino-2-ethyl-6-trifluorometh34-3,4-dihi3^dro-2H-quinoline- 1-carboxylic acid ethyl ester (376 mg), 2-iodoethanol (305 mg), and cesium carbonate (1.152 g) are dissolved in N,N-dimethylforrxiamide (5 ml), and the mixture is stirred at 60°C for 3 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic Ia3^er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. Thte resulting residue is purified b3^ column chromatograph3r (NH-silica gel; hiexane:ethyl acetate = 1:1—>0:l), further by column chromatography (silica gel; hexarae: ethyl acetate = 3:7-^0:1) to give (2R,4S)-4-fl3,5-bis(1xifluoro e1±Lyl)-2-oxo-l,2-dihydropyrimidin-4-yl]}amm 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (240 mg, MS (rn/z): 681 [M+H]+) and (2R,4S)-4-([3,5-bis(trifluoromethLyl)benzyl]-{l-[2-(2-hydrox5^ethoxy)ethyl]-2-oxo-l,2-dihydrop3^rimidin-4-yl})arnino-2-ethyl-6-trifluoromethyl-3>4--dih3^dro-2H-quinoline-l-'CarboxyIic acid ethyl ester'( 7 mg, MS (m/z): 725 [M+H]+). Example 86 (1) (2R,4S)-4-Amino-2-ethyl-6-trifluoromethyl-3>4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (5 g) is dissolved in toluene (50 ml), and thereto are added tris(dibenzylideneacetone)dipalladium (293 mg), sodium tert-butoxide (3.8 g), 2-(di-tert-butylphosphino)b>iphenyl (376 mg), and 2,6-dichloropyrazine (4.7 g). The mixture is stirred at room temperature under nitrogen atmosphere for 23 hours. To the mixture is added a saturated aqueous sodium hydrogen carbonate solution, and the mixture is extracted with ether. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato- graphy (silica gel; hexanerethyl acetate = 6:1—»3:1) to give (2R,4S)-4-(6- chloropyrazin-2-yl)amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (5.3 g). MS (m/z): 429 [M+H]+ (2) (2R,4S)-4-(6-Chloropyrazin-2-yl)amino-2-ethyl-6-trifluorometh3d-3,4- dihydro-2H-quinoline-l-carboxylic acid etitryl ester (3 g) is dissolved in N,N- dimethylformamide (35 ml), and thereto are added sodium hydride (62.7 %, 348 mg) and 3,5-bis(trifluorometh3d)ben25?'l bromide (9 mL), and the mixture is stirred at room temperature for 48 hours. Distilled water is added to the mixture, and the mixture is extracted with ether. The organic laj'er is washed with saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexaneiethyl acetate = ethyl-6-ixifluoromethyl-3,4-dihydro-2H-qu^^ acid ethyl ester (1.6 g). MS (m/z): 655 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(triflu^^ 3d)}amuao-2-efeyl-6-trifluoromethyl-3,4-dihydro-2H-quinolirae-l -carboxylic acid ethyl ester (200 mg) is dissolved in 1,3-dimethylimidazolidinone (2 ml), and thereto are added diisopropylethylamine (80 ]il) and rnorpholine (140 pi). The mixture is stirred at 80°C for 51 hours, and allowed to cool to room temperature. A saturated aqueous citric acid solution is added to the mixture, and the mixture is extracted with ether. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexanerethyl acetate = 4:1—► 13:7) to give (2R,4S)-4-{[3,5-bis(trifluoromethfcyl)benzyl]-[6-(morpholin-4-yl)pyrazin-2-yl]}amino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quino line-1 -carboxylic acid ethyl ester (132.8 mg). MS (m/z): 706 [M+H]+ Example 87 The corresponding starting compound is treated in a similar manner to Example 86 to give the compound of Example 87, MS (rrx/z): 708 [M+H]* Example 88 (1) (2R)4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydr-o-2H-quinoline-1-carboxyiic acid ethyl ester (200 mg) and 2-chloro-5-nitro-thiazole (416 mg) are dissolved in N,N-dimethylformamide (1 ml), and the mixture is stirred at 100°C for 3 hours. The reaction solution is cooled to room temperature, and thereto are added an aqueous citric acid solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 4:1->1:1) to give (2R,4S)-2-ethyl-4-(5-nitorthiaz:ol-2- yl)ajiiino-6-iTifluoroinethyl-3)4-dihydro-2H-quinoline-l-carbo3C7lic acid ethyl ester (148 mg). MS (m/z): 445 [M+H)+ (2) (2R,4S)-2-Eiiayl-4-(5-nitro1±Liazol-2-yl)amino--6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (133 mg) and 3,5-bis(trifluoromethy 1)benzyl bromide (179 mg) are dissolved in tetrahydro-furan (3 ml), and thereto is added sodium hydride (62.7 %, 34 rag), and the mixture is stirred at room temperature overnight. To the reaction solution is added acetic acid, and thereto are added water and ethyl acetate. The organic layer is' washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue-is purified by column chromatography (silica gel; hexanerethyl acetate =■■ 4:1->2:1) to give (2R)4S)-4-{t3,5-bis(trifluoromethyl)benzyl]-(5-nitrothiazo]-2-yl)}ajnino-2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (58 mg). MS (m/z): 671 [M+H]+ Example 89 (1) (2R,4S)-4-{[3,5-Bis(1xffluorome1iiyl)benzyl]-cyano}amino-2-ethyl-6-trifluorornethyl-3,4-dihydro-2H--quinoline-l-carboxylic acid ethyl ester (327.9 mg) is dissolved in tetrahydrofuran (3 ml), and thereto is added sodium hydride (62.7 %, 13.9 mg). The mixture is stirred with ice-cooling under nitrogen atmosphere for one hour. To the reaction solution is slowly added dropwise a solution of 3-buten-l-ol (41.8 mg) in tetrahydrofuran (A ml) under ice-cooling, and the mixture is stirred at room temperature jo; 29 hours. Distilled water is added under ice-cooling, and the mixture is extracted with ethyl acetate. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 4:1) to give (2R,4S)-4-{l-[3,5-bis(1rifluoromethyl)benzyl]-2-(3-buten-l-3d)}isoureido-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinolinerl-carboxylic acid ethyl ester (186.3 mg). MS (m/z): 640 [M+H]+ (2) (2R,4S)-4-{l-[3,5-Bis(trifluoromethyl)benzyl]-2-(3-buten-l-yl}isoureido-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (172 mg) is dissolved in chloroform (3 ml), and thereto is added N-iodosuccimide (72.5 mg). The mixture is stirred at room temperature for 1.5 hours, and thereto is added a saturated aqueous sodium thiosulfate solution. The mixture is extracted with ether, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(4-iodomethyl-5,6-dihydro-4H-[l,3]oxadin-2-}4)}-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carbox3dic acid ethyl ester (211 mg). MS (m/z): 766 [M+H]+ Example 90 (1) (2R,4S)-4-(5-Bromopyrimidin"2-yl)amino-2-ethyl-6-trifluoromethyl-3 ;4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (100 mg) is dissolved in NjN-dimethj^lformamide (1 ml), and thereto is added sodium hydride (62.7 %, 10.3 mg), and the mixture is stirred with ice-cooling under nitrogen atmosphere for 10 minutes. 3,5-Dimethoxybenzyl bromide (74 mg) is added to the mixture under ice-cooling, and the mixture is stirred at room temperature for 16.5 hours. Distilled water is added to the mixture under ice-cooling, and the mixture is extracted with ether. The organic laj'er is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b3r column chromatography (silica gel; hexane:ethyl acetate -9:1-^4:1) to give (2R,4S)-4-[(5-bromop3^rimidin-2-3d)-(3,5-dimethoxy-benzyl)]ajTLino-2-ethyl-6-trifluorornethyl--3>4-dihydro-2H-quinoline-l- carboxylic acid ethyl ester (95.1 mg). MS (m/z): 623/625 [M+H]+ (2) (2R,4S)-44(5-Bromopyrimidin-2-ylH3,5-dim^ ethyl-6-trifluorometh3'l-3,4-dihydro-2H-quinoline-1 -carboxylic acid eth3^1 ester (290 mg) is dissolved in toluene (4 ml), and tris(dibenzylidene -acetone)dipalladium (8.5 mg), sodium tert-butoxide (68.2 mg), 2-(di-tert-butylphosphino)biphenyl (11 mg) and morphoiine (62 ]xl) are added thereto. The reaction mixture is stirred under nitrogen atmosphere at room temperature for 4 days. The reaction solution is stirred at 80°C for 5.5 hours, and allowed to cool to room temperature. Distilled water is added to the mixture, and the mixture is extracted with ether. The organic layex is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (NH-silica gel; hexane:ethyl acetate = 4:1—>3:2) to give (2R,4S)-4-{(3,5-dimethox3^benzyl)-[5-(morpholin-4»yl)pyrimidin-2-yl]}-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l -carboxylic acid ethyl ester (141.5 mg). MS (m/z): 630 [M+H]+ Examples 91-94 The corresponding starting compounds are treated in a similar manner to Example 90 to give the compounds as listed in Table 12. Table 12 Example 95 (1) 6-Bromopyridin-2-carbaldehyde (5 g) is dissolved in a mixture of methanol (10 ml) and tetrahydrofuran (15 ml), and thereto is added sodium borohydride (3.05 g) at 0°C, and the mixture is stirred for 10 minutes. To the reaction solution are added an aqueous citric acid solution and ethyl acetate, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromato- grajphy (silica gel; hexane: ethyl acetate = 9:1-^2:3) to give (6-bromop3T^din- 2-yl)methanol (3.92 g). MS (m/z): 188/190 [M+H]+ (2) (6-Bromopyridin~2-yl)methanol (3.9 g) and triphenylphosphine (7.6 g) are dissolved in metttylene chloride (50 ml), and thereto is added carbon tetrabromide (8.25 g) under ice-cooling. The reaction solution is concentrated under reduced pressure, and the resulting residue is purified by column chromatography (silica gel; hexane:ethyl acetate = 49:1-^47:3) to give 2-bromo-6-bromomethylpyridine (2.96 g). MS (m/z): 250/252 [M+H]+ (3) (2R,4S)-4-(5-Bromop3'rimidin-2-yl)amino-2-^^ 3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (400 mg) is dissolved in N,N-dimethylforrnamide (4 ml), and thereto is added at 10°C sodium* hydride (62.7 %, 42 mg). The mixture is stirred at the same temperature for 10 minutes, and to the reaction solution is added 2-bromo-6-bromomethylpyridine (318 mg). The mixture is stirred at the same temperature for 15 minutes, and thereto is added acetic acid. A saturated aqueous sodium hydrogen carbonate solution and ethyl acetate are added to the mixture. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexanerethyl acetate = 48:2-^3:2) to give (2R,4S)-4-[(6-bromo-P3^ridin-2-34)rnethyl-(5-bromopyrimidin-2-3d)]ainino-2-ethyl-6-trifluoro-methyl-3,4-dihydro-2H-quinoUne-1-carboxylic acid ethyl ester (470 mg). MS (m/z); 642/644 [M+H]* (4) (2R,4S)-4-[(6-bromopyridin-2-yl)methyl-(5-bromopyrimidin--2- yl))amino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (150 mg), tetrakis(triphen3>lphosphine)paUadium (28 mg) and zinc cyanide (71.2 mg) are dissolved in N,N-dimethylformamide (3 ml), and the mixture is stirred at 95°C under nitrogen atmosphere overnight. The reaction solution is cooled to room temperature, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic layer is dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatograptty (silica gel; hexane:ethyl acetate = 47:3—>2:3) to give (2R?4S)-4-[(6-cyajiopyridm-2-yl)methyl-(5-c^ 2-ethyl-6-trifluoromethyl-3>4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (105 mg). MS (m/z): 536 [M+H]+ Examples 96-97 (2^4S*)-4-Amino-2-ethyl-6-^^ carboxylic acid ethyl ester is treated in a similar manner to Example 1 to give the compounds as listed in Table 13. The corresponding starting compound is treated in a similar manner to Example 10 to give the compound of Example 98. MS (m/z): 60S [M+H]+ ml) and tetrahydrofuran (1 ml), and a catalytic amount of 10 % palladium-carbon is added thereto, and the mixture is stirred at room temperature under hydrogen atmosphere overnight. The catalyst is removed by filtration, and the filtrate is concentrated under reduced pressure. The resulting residue is purified by column chromatograptiy (silica gel; hexane:ethyl acetate = 4:1) to give (2R*,4S*)-4-{[3?5-bis(trifluoromethyl)ben25^1]-[5-(2-carboxyeth3d)p3rrimidin-2-yl]}amino-2-ethyl-6-methoxy-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (35 mg). MS (m/z): 655 [M+H]+ Example 102 (2R?4S)-4-Amino-2-ethyl-6-methoxy-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester is treated in a similar manner to Example 1 to give the compound of Example 102. MS (m/z): 668 [M+H]+ Example 103 The corresponding starting compound is treated in a similar manner to Example 19 to give the compound of Example 103. MS (m/z): 651 [M+H]+ Examples 104-105 The corresponding starting compounds are treated in a similar manner to Example 20 to give the compounds as listed in Table 14. Examples 106-109 The corresponding starting compounds are treated in a similar manner to Example 35 to give the compounds as listed in Table 15. Examples 114-115 The corresponding starting compounds are treated in a similar manner to Example 60 to give the compounds as listed in Table 16. Example 116 The corresponding starting compound is treated in a similar manner to Example 64 to give the compound of the following formula. MS (m/z): 620 [M+H2O]+ Example 145 The corresponding starting compound is treated in a similar manner to Example 50 to give the compound of Example 145. MS (m/z): 667" [M+H]+ Examples 146-149 The corresponding starting compounds are treated in a similar" manner to Example 96 to give the compounds as listed in Table 21. Example 150 (2R,4S)-4-{[5-(4-Ben2yloxycar^ [3,5-bis(1rifluoromethyl)benzyl]}amino-2-e1±iyl-6-me1±ioxy-3,4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (1.78 g) is dissolved in ethanol (50 ml), and thereto is added 10 % palladium-carbon (300 mg). The mixture is stirred at room temperature under hydrogen atmosphere for 3 hours. The catalyst (10 % palladium-carbon) is removed by filtration, and the filtrate is concentrated under reduced pressure, and the resulting residue is purified by column chromatography (NH-silica gel; hexanerethyl acetate = 4:1-* 1:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-[5-(piperazin-l- yl)pyrimidin-2-yl]}amino-2-ethyl-6-methoxy-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (470 mg). MS (m/z): 667 [M+H]+ Example 151 (1) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(pipera2in-l-yl)-p3oiinidin-2-yl]}ainino-2-et±iyl-6-metho^-3?4-dihydro-2H-quinoline-l^ carboxylic acid ethyl ester (100 mg) and pyridine (18 "p.1) are dissolved in methylene chloride (1 ml), and thereto is added acetoxyacetic acid chloride (19.4 yd) at room temperature. The mixture is stirred overnight, and washed with a IN hydrochloric acid. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by column chromatography (silica gel; hexaneiethyl acetate = 7:3—>2:3) to give (2R,4S)-4-({5-[4-(2-acetoxyacetyl)piperazm-1-yl]pyrim benzyl])ammo-2-ethyl-6-m acid ethyl ester (110 mg). MS (m/z): 767 [M+H]+ (2) (2R,4S)-4-({5-[4-(2-Acetoxyacetyl)piperazm^ bis(trifluorome1±Lyl)benzyl])arDino-2-ethyl-6-ine1±ioxy quinoline-1-carboxylic acid ethyl ester (87 mg) is dissolved in ethanol (1 ml), and thereto is added potassium carbonate (23 rng) at room temperature, and the mixture is stirred overnight. The insoluble materials are removed by filtration, and the filtrate is concentrated under reduced pressure to give (2R,4S)-4-([3,5-bis(Mfluoromethyl)beri^l]-{5-[4-(2-hydro3^acetyl)pipera2in- 1 -yl]pyriinidin-2-yl})ajnino-2-ethyl-6-inetho3cy-3,4-dihydro-2H-quinoline-1 - carboxylic acid ethyl ester (83 mg). MS (m/z): 725 [M+H]+ Example 152 The corresponding starting compound is treated in a similar manner to Example 124 to give the compound of Example 152. MS (m/z): 710 [M+H]+ Example 153 The corresponding starting compound is treated in a similar manner to Example 68 to give the compound of Example 153. MS (m/z): 684 [M+H]+ Examples 154-156 The corresponding starting compounds are treated in a similar manner to Example 90 to give the compounds as listed in Table 22. The corresponding starting compound is treated in a similar manner to Example 134 to give the compound of Example 157. MS (m/z): 582 [M+H]+ Example 158 (2R,4S)-4-{[3,5-Bis(txifluoromet^ yl)}amino-2-et±iyl-6-1xifluorometh^ acid ethyl ester (200 nag), an excess amount of triethylarnine, and aminoacetic acid tert-butyl ester (501 mg) are dissolved in 1,3-dimethyl- imidazolidinone (4 ml), and the mixture is stirred at 90°C for 3 days. The reaction solution is cooled to room temperature, and thereto are added a saturated aqueous citric acid solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 19:1—> 13:7) to give (2R?4S)-4-{[3,5-bis(trifluoromethjd)ben2yl]-[6-(tert-butoxycarbon3d- methylamino)pyrimidin-4-yl]}amino-2--ethyl-6-trifluoromethyl-3>4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (22 mg). MS (m/z): 750 [M+H]+ Examples 159-161 The corresponding starting compounds are treated in a similar manner to Example 158 to give the compounds as listed in Table 23. Example 162-163 The corresponding starting compounds are treated in a similar manner to Example 68 to give the compounds as listed in Table 24. Example 164 The corresponding starting compound is treated in a similar manner to Example 124 to give the compound of Example 164. MS (m/z): 722 [M+H]+ Example 165 (1) (2R,4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (1.5 g) and 3-bromobenzaldehyde (974 mg) are dissolved in l?2-dichloroethane (15 ml), and thereto is added triacetoxy sodium borohj'dride (2.14 g) at room temperature. The mixture is stirred for 3 hours, and thereto are added an aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic layer is washed, with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatographj'- (hexane:ethyl acetate * 19:1—^7:3) to give (2R,4S)-4-(3- bromobenzyl)amino-2-e1±Lyl-6-trifl^ carboxylic acid ethyl ester (2.45 g). MS (m/z): 485/487 [M+H]+ (2) (2R,4S)-4-(3-Bromoben2yl)amino-2-ethyl-6-trmuoromethyl-3»4- dihydro-2H-quixioline-l-carboxylic acid ethyl ester (2.32 g), bromocyane (609 mg), and sodium hydrogen carbonate (1.22 g) are suspended in ethanol (30 ml), and the mixture is stirred at room temperature overnight. To the reaction solution are added an aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give (2RJ4S)-4-[cyano-(3-bromobenz54)]amino-2-ethyl-6- trifluoroxneth}4-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (2.43 g). MS (m/z): 527/529 [M+H2O]+ (3) (2R,4S)-4-[Cyajio-(3-bromobenzyl)]amino-2-ethyl-6-tTffluoromethyl- 3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (2.43 g), sodium azide (3.12 g), and ammonium chloride (2.56 g) are dissolved in N,N-dimethylformamide (20 ml), and the mixture is stirred at 95°C overnight. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure to give (2R,4S)-4-[(3-bromobenzyl)-(tetra2ol-5-yl)]amino-2-eth3^1-6-trifluoromethyl-3>4-dihydro-2H-quinoline-l-carbo3sylic acid ethyl ester (2.58 g). MS (m/z): 553/555 [M+H]+ (4) (2R,4S)-4-[(3-Bromobenzyl)-(tetrazol-5-yl)]amino-2-ethyl-6- trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (500 mg), 2-bromoethanol (271 mg), and potassium carbonate (375 mg) are dissolved in N,N-dimethylformamide (3 ml), and the mixture is stirred at 50°C overnight- The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate * 9:1—»2:3) to give (2R,4S)-4-{(3-bromobenzyl)-[2-(2-hyd^ trifluoroinethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (394 mg). MS (m/z): 597/599 [M+H]+ Example 166 The corresponding starting compound is treated in a similar manner to Example 165-(4) to give the compound of Example 166. MS (m/z): 611/613 [M+H]+ Example 167 (1) (2R,4S)-4-[(3-Bromobenzyl)-(tetrazol-5-yl)]amino-2-ethyl-6- trifluoromethyl-3,4-dihydro-2H-quinoline-l-carbox3^1ic acid ethyl ester (500 mg), glycidol (89 ]al), and triphen3dphosphine (711 mg) are dissolved in tetrahydrofuran (3 rnl), and thereto is added 40% azodicarboxylic acid diethyl ester in toluene (1180 mg) at room temperature, and the mixture is stirred for 15 minutes. To the reaction solution are added water and ethyl acetate, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 19:l->3:2) to give (2R,4S)-4-[(3-bromobenzyl)-(2- oxiranylinethyl-2H-tetrazol-5-yl)]ajnino-2-ethyl-6-trifluorometh3d--3,4- dihydro-2H-quinoline-l-carboxylic acid ethyl ester (347 mg). MS'(m/z): 609/611 [M+H]+ (2) (2R>4S)-4^(3-Bromobexizyl)-(2-oxiranylmethyl-2H-tetrazol-5-yl)] amino-2-ethyl-6-trifliaororaethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (330 mg) and morpholine (1 ml) are dissolved in ethanol (3 ml), and the mixture is stirred at room temperature overnight. To the reaction solution are added water and ethyl acetate, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate « 2:3-*0:l) to give (2R,4S)-4-{(3-bromobenzyl)"[2-(2-hydroxy-3-morpholin-4-ylpropyl)-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluoromethyl-3 ,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (315 mg). MS (m/z): 696/698 [M+H]+ Example 168 (1) (2R,4S)-4-[(3-Bromoben2yl)-(tetra2ol-5-yl)]amino-2-ethyl-6- trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (500 mg) is treated in a similar manner to Example 167-(1) to give {2R?4S)-4-{(3- bromobenzyl)-[2-(2-methylsu.lfanyleth34)-2H-tetrazol-5-yl]}aniino-2-ethyl-6- trifluorometh3rl-3,4-dih3^dro-2H-quinoline-l-carboxylic acid ethj^l ester (524 mg). MS (m/z): 627/629 [M+H]+ (2) (2R,4S)-4"{(3-Bromobenzyl)"[2-(2-methylsulfanylethyl)-2H-tetrazol-5- yl]}amino-2"ethyl-6-trifluororneth3d-3,4-dihydro-2H-quinoline-l-carbox34ic acid ethyl ester (520 mg) is treated in a similar manner to Example 50 to give (2R?4S)-4-{(3-bromobenz3d)-[2-(2-methylsulfonylethyl)-2H-tetrazol-5- yl]}amino-2-ethyl-6"trifluoroinethyl-3,4--dihydrO'2H-quinoline-l -carboxylic acid ethyl ester (474 mg). MS (m/z): 659/661 [M+H]+ Examples 169-172 The corresponding starting compounds are treated in a similar manner to Example 10 to give the compounds as listed in Table 25. Exam-pie 173 (1) (2R*f4S*)-(4-Ben^loxycarbonyl€unino-2-ethyl-6-trffl dihydro-2H-quinoline (112.8 g) is dissolved in ethanol (1000 ml), and thereto is added 10 % palladium-carbon (5.64 g), and the mixture is stirred at room temperature under hydrogen atmosphere overnight. The catalyst (10 % palladium-carbon) is removed by filtration, and filtrate is concentrated under reduced pressure. To the residue is added hexane, and the precipitated crystals are collected by filtration to give (2R*,4S*)-4- amino-2-ethyl-6-trifluoromethyl-3,4-ciihydro-2H-quinoline (70.3 g). MS (m/z): 245 [M+H]+ (2) (2R*,4S*)"4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H- quinoline (70.0 g) is dissolved in tetrahydrofuran (500 ml), and thereto is added di-tert-butyl dicarbonate (68.2 g). The mixture is stirred at room temperature overnight, and concentrated under reduced pressure. Hexane is added to the residue, and the precipitated crystals axe collected by filtration to give (2R*,4S*)-4-tert-butoxycarbonylamino-2-ethyl-6-trffluoromethyl-3f4-dihydro-2H-quinoline (9O.7 g). MS (m/z): 345 [M+H]+ (3) (2R*,4S*)-4-tert-Butoxycarbon34amino(2-e1±iyl-6-trifluoromethyl«3,4- dihydro-2H-quinoline (90.58 g) and triethyismine (44 ml) are dissolved in methylene chloride (900 ml), and thereto is added triphosgene (31.2 g) under ice-cooling. The reaction solution is stirred at room temperature for one hour, and concentrated under reduced pressure. The resulting residue is dissolved in tetrahydrofuran (9O0 ml), and thereto are added benzyl alcohol (54.4 ml), and sodium hydride (60 %, 20.2 g) under ice- cooling. The mixture is stirred at the same temperature for 3 hours. Water and ethvl acetate are added to the reaction mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The residue is crystallized from diisopropyl ether to give (2R*,4S*)-4-tert- butoxycarbonylam.ino-2-ethyl-6-trifluoroinethyl-3>4--dihydro-2H-quinoline- 1-carboxylic acid benzyl ester (104.7 g). MS (m/z): 496 [M+H20]+ (4) (2R*?4S*)-4-tert-Buto5r7carbonylamino-2-ethyl-6-trifluoromethyl-3,4- dihydro-2H~quinoline-l-carboxylic acid benzyl ester (104.5 g) is dissolved in chloroform (500 ml), and thereto are added a 4N hydrochloric acid in ethyl acetate (500 ml) at room temperature. The mixture is stirred for 30 minutes, and concentrated under reduced pressure. To the residue is added diisopropyl ether, and the precipitated crystals are collected by filtration to .give (2R*,4S*)-4-amino-2-eth34-6-trifluoromethyl-3,4-dihydro- 2H-quinoline-l-carboxylic acid benzyl ester hydrochloride (88.0 g). MS (m/z): 379 [M+H]+ (5) (2R*?4S*)-4-Amino-2-eth34-6-trifluorornethyl-3?4-dihydro-2H- quinoline-1-carboxylic acid benzyl ester l^drochloride (25.0 g) is dissolved in a mixture of ethyl acetate and a saturated aqueous sodium hydrogen carbonate solution, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue (23 g) and 5-bromo-2-chloropyrimidine (29.3 g) are dissolved in 1,4-dioxane (100 ml), and thereto is added N,N-diisopropylethylamine (32 ml), and the mixture is refluxed overnight. The reaction solution is cooled to room temperature, and thereto are added water and diethyl ether, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate * 6:1—^2:1) to give (2R*,4S*)-4-(5-brorriopyrii] Ldin-2-yl)ainino-2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-l-ci -boxylic acid benzyl ester (24.0 g). MS (m/z): 535/537 [M+H]+ (6) (2^4S*)-4-(5-Bromopyriimdm~2-yl)am 3,4-dihydro-2H-quinoline-l-caxboxylic acid benzyl ester (13 g) is treated in a similar manner to Example l-(2) to give (2R*,4S*)-4-{[3,5-bis(1xifluoromethyl)benzyl]-(5-bromopyrimidin-2-yl)}ainino-2-ethyl-3,4-dihydro~2H-quinoline-l-carboxylic acid benzyl ester (20.6 g). MS (m/z): 761/763 [M+H]+ (7) (2R*,4S*)-44[3,5-Bis(trifluoromethyl)ben^l]-(5-bromopyrimidin-2'- yl)}ainino-2-ethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid benzyl ester (18.3 g) is treated in a similar manner to Example l-(3) to give (2R*,4S*)-4- {[3,5-bis(1xifiuoromethyl)benzylH ethyl-3,4-dihydro-6-trifluoromethyl-2H-quinoline-l-carboxylic acid benzyl ester (11.2 g). MS (m/z): 768 [M+H]+ (8) (2R*,4S*)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(morpholin-4-yl)- pyrimidm-2-yl]}ammo-2-ethyl-6-1r^ 1-carboxylic acid benzyl ester (11.2 g) is treated in a similar manner to Example 150 to give (2R*,4S*)-4-{[3,5-bis(trifluoromethyl)benzyl3-[5-(morpholm-4-yl)pyi±xridm-2-yl]}^^ dihydro-2H-quinoline (8.9 g). MS (m/z): 634 [M+H]+ Example 174 (2^4S*)-4-{[3,5-Bis(1rmuorom yl)pyrimidm-2-yl]}amino-2-et^^ quinoline (500 mg) and triethylamine (132 p.1) are dissolved in methylene chloride (5 ml), and thereto is added triphosgene (94 mg) at room temperature, and the mixture is stirred for one hour. The reaction solution is concentrated under reduced pressure, and the resulting residue is separated into ethyl acetate and a saturated aqueous sodium hydrogen carbonate solution. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is dissolved in tetrahydrofuran (5 ml), and ethylene glycol (0.5 ml), triethylamine (295 ml) and 4-dimethylaminopyridine (26 mg) are added thereto. The mixture is stirred at room temperature overnight. The reaction solution is separated into ethyl acetate and a saturated aqueous sodium hydrogen carbonate solution. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The residue is purified by silica gel column chromatography (hexanerethyl acetate = 3:1—+2:3) to give (2R*,4S*)-4-{[3,5-bis(trifluorome1±iyl)benzyl]-[5-(^ 2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-hydroxyethyl ester (430 mg). MS (m/z): 722 [M+H]+ Example 175 (1) (2R,4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (1.28 g), 2-chloroxazole-4-carboxylic acid ethyl ester (1.44 g) and diisopropylethylamine (1.42 ml) are dissolved in 1,4-dioxane (10 ml), and the mixture is stirred at 130°C overnight. The reaction solution is cooled to room temperature, and water and ethyl acetate are added thereto. The organic layer is washed with a saturated brine, dried over sodium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatographiy (hexane:ethyl acetate = 4:1—>1:1) to give (2R,4S)-4-(4»ethox3^carbon34oxa2ol-2-34)amino-2-eth3^-6-1rinuoroniethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.13 g). MS (rn/z): 456 [M+H]+ (2) (2R,4S)-4-(4-Etiio5^carboo3doxazol-2'yl)aniino-2-ethyl-6-trifluoro-methyl-3,4-dihydro-2H-quinoline-l-carbo35ylic acid ethyl ester (1.12 g) is treated in a similar manner to Example l-(2) to give (2R,4S)-4-{[3,5-bis-(triiluoromethyl)benzyl] - (4- ethoxy carbonyloxazol-2 ~yl)}amino- 2 -ethyl-6-trifluorotnethyl-3,4-dihydro-2H-ciuinoline-l-carboxylic acid ethyl ester (928 nag). MS (m/z): 682 [M+H]+ Example 176 The corresponding starting compound is treated in a similar manner to Example 124 to give the compound of Example 176. MS (m/z): 654 [M+H]+ Example 177 (1) (2R,4S)-4-{[3,5-Bis(trifluorometh3^1)benzyl]-(5-bromopyrimidin-2-yl)}amino-2-ethyl-6-trifluorometh.yl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (32.25 g), [l?lJ-bis(diphenylphosphino)ferrocene]-dichloropalladium (1.012 g), potassium acetate (13.6 g)? and bis-(pinacolate)diboron (17.56 g) are dissolved in dimethylsulfoxide (200 ml), and the mixture is stirred at 80°C under nitrogen atmosphere for one hour. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is dissolved in tetrahydrofuran (100 ml), and thereto is added dropwise a 30 % aqueous hydrogen peroxide solution (70 ml) under ice-cooling. One hour thereafter, a saturated aqueous sodium thiosulfate solution is added to the mixture, and the excess hydrogen peroxide is consumed. The mixture is separated into water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 5:1->3:1) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)ben2yl]-(5-hydroxypyrimidm 3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (19.22 g). MS (m/z): 637 [M+H]+ (2) (2R,4S)-4-{[3,5-Bis(trffluorome1^ yl)}ajnino-2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (6.5 g) and 4-bromobutyric acid ethyl ester (2.19 g) are dissolved in N?N-dimethylformamide (50 ml), and thereto is added potassium carbonate (1.69 g), and the mixture is stirred at 45°C overnight. Ethyl acetate and water are added to the mixture, and the organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 95:5—>3:1) to give (2R,4S)-4-{[3,5-bis(1xifluoromethyl)^ pyrimidin-2-yl]}amino-2-e1±Lyl-6-txffi^ 1-carboxylic acid ethyl ester (6.52 g). MS (m/z): 751 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(3-ethoxycarbonyl- propoxy)pyrimidm-2-yl]}ammo-2-e1^ quinoline-1-carboxylic acid ethyl ester (6.5 g) is dissolved in ethanol (65 ml), and thereto is added a 2N aqueous sodium hydroxide solution (13 ml). The mixture is stirred at room temperature overnight. The reaction solution is concentrated under reduced pressure, and to the residue are added ethyl acetate and a IN aqueous hydrochloric acid, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatograptry (chloroformtmethanol = 1:0—95:5) to give (2R,4S)-4-{[3,5«bis(trifluoromethyl)benzyl]-[5-(3-carboxypropoxy)pyrirnidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-l-carbox5rlic acid etttyl ester (6.16 g). MS (m/z): 723 [M+H]+ Example 178 (2R,4S}-4-{[3>5-Bis(trifluorometh3'l)bexiZ5^1]-[5-(3-carboxypropoxy)-pyrimidin-2-yl]}amino-2-ethyl-6-trifluorometh34-3)4-dih3^dro-2H-quinoline-1-carboxylic acid ethyl ester (3O0 mg) is dissolved in ethanol (3 ml), and thereto is added a 2N aqueous sodium hydroxide solution (207 p.1). The reaction solution is concenrated to dryness under reduced pressure to give (2R,4S)-4-{[3,5-bis(trifluorome1±tyl)ben2yl]-[5-(3-caTboxypropoxy)p3Timidin-2-yl]}amino-2-eth3?'l-6-trifluoroin.ethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester sodium salt (308 mg). MS (m/z): 721 [M-Na]-Example 179 (2R,4S)-4»{[3,5-Bis(trifluorometh3d)benzyl]-[5-(3-carboxypropoxy}-pyrimidin-2-yl]}amino-2-ethyl-6-trifluorometh3d-3,4-dihydro-2H-quinoline-1-carboxylic acid eth3d ester sodium salt (258 mg) is suspended in water (10 ml), and thereto is added a. solution of calcium chloride (154 mg) in water (0.6 ml), and the mixture is stirred at room temperature overnight. Chloroform and water are added to the mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The residue is dissolved in eth3'l acetate, and thereto is added n-hexane. The precipitated crystals are collected by filtration to give (2R,4S)-4-{[3,5-bis(trifluoromet&34)beriZ3d]-[5-(3-c ethyl-6-trifluorornethyl-3J4'-dihyciro-2H-quinoline-l-carbo5r7lic acid ethyl ester hemicalcium salt (169 mg). MS (m/z): 721 [M-l/2Ca]-Example 180 (2R,4S)-4-{[3,5-Bis(trffluoromethyl)te pyrimidin-2-yl]}amino-2-e1±t3d-6-tri^^ 1-carboxylic acid ethyl ester (250 mg) is dissolved in ethanol (2 ml), and thereto is added a 2N aqueous potassium hydroxide solution (173 pi). The reaction solution is concentrated to drynerss under reduced pressure to give (2R,4S)-4-{[3,5-bis(trifluoromethyr-l)benzyl]-[5-(3-carbo^propoxy)- pyrirnidin-2-yl]}amino-2-ethyl-6-trifluorornet:hyl-3>4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester potassium salt (266 mg). MS (m/z): 721 [M-K]-Examples 181-186 The corresponding starting compounds are treated in a similar manner to Example 177(2) to give the compounds as listed in Table 26. Example 187 (1) (2R,4S)-4-{[3,5-Bis(trffiuorom yl)}amino-2-eth34-6-txifiuoromethyl-3,4-d:^^ acid ethyl ester (2.0 g) is dissolved in N,I>J-dimettiylformamide (30 ml), and thereto are added ethyl bromoacetate (5 20 yil), potassium carbonate (650 mg). The mixture is stirred at room temperature for 3.5 hours. Water and ethyl acetate are added to the mixture, a_nd the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 19:1-^41:9) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(5-ethoxy-carbon34metho?ypyrimidin-2-3^1)}amino-2--ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (2.07 g). MS (m/z): 723 [M+H]+ (2) (2R,4S)-4-{[3?5-Bis(trifluoromethyl)l)enzyl]-(5-etho^carbonyl- methoxypyrimidin-2-yl)}aLmino-2-eth3^1-6-trifluoromethyl-3!4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (2.07 g) is dissolved in ethanol (30 ml), and thereto is added dropwise a. IN aqueous sodium hydroxide solution. The mixture is stirred for 2.5 hiours, and thereto are added a 6N hydrochloric acid and ethyl acetate. The mixture is separated, and the organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (chloroformrmethanol = 1:0-+9:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-(5-carboxy-met±Loxypyrimidm-2-yl)}ammo-2- quinoline-1-carboxylic acid ethyl ester (1.83 g). MS (m/z): 695 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(trmuorom pyrimidin-2-yl)}amino-2-e1±iyl-6-trifluoro 1-carboxylic acid ethyl ester (200 mg) is dissolved in tetrahydrofuran (4 ml), and thereto are added ethyl aminoacetate hydrochloride (48 mg), 1 - hydroxybenzotriazole dihydrate (47 mg), l-ethyl-3-(3-dimethylamino- propyl)carbodiimide hydrochloride (66 mg), and triethylamine (49 y\l), and the mixture is stirred at room temperature for one hour. Water and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 4:1^3:2) to give (2R,4S)-4-([3,5-bis(trifluoromethyl)benzyl]-{5- [(etiio^carbonybnethylcarbainoyl)metho^]p5n±Tiidin-2-yl})amino-2-ethyl-6-trifluoromethyl-3,4~dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (165 mg). MS (m/z): 780 [M+H]+ Examples 188-190 The corresponding starting compounds are treated in a similar manner to Example 187 (3) to give the compounds as listed in Table 27. Example 191 (1) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzy^ yl)}amino~2-eth34-6-trifluoromethyl-3,4-d^ acid ethyl ester (300 mg) is dissolved in tetrahydrofuran (4 ml), and thereto are added (2S,4R)-l-benzyloxycarbonyl-2-methoxycar-bonyl-4-hydroxy-pyrrolidine (395 mg) and triphenylphosphine (740 mg). To the mixture is added dropwise a 40 % solution of diethyl azodicarboxylate in toluene (1.23 ml) under ice-cooling, and the mixture is stirred at room temperature overnight. Water and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is washed with a. saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 9:1-»4:L) to give (2R,4S)-4-([3,5-bis(trifluoro- methyl)benzyIH5-[(S)~2-((S)-metho^^ pyrroUdin-4-yloxy]pyrimidm^ dihydro-2H-quinoline-l-carboxylic acid ethyl ester (543 nig) as a crude product. MS (m/z): 898 [M+H]+ (2) The crude (2R,4S)-4-([3,5-Bis(trifluoromethyl)benzyI]-{5-[(S)-2-((S)- methox3^carbonyl)-1 -benzyloxycarbonylpyrrolidin-4-34oxy]pyrirnidin-2 -yl})- ainino-2-eth34-6-trifluoroinethyl-3?4-dih3^dro-2H-quinoline-l-oarboxylic acid ethyl ester (1.39 g) is dissolved in methanol (15 ml), and thereto is added 10 % palladium-carbon (300 mg). The mixture is stirred under hydrogen atmosphere for 3 hours, filtered, and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 3:2—>2:3—>0:l) to give (2RT4S)-4- ([3,5-bis(trifluoromethyl)benz5d]-{5-[(S)-2-((S)-methox7carbon3^1)p3^rrolidin-4- yl]pyrixnidin-2-yloxy})amino-2-ethyl-6-trifluorometh34-3,4-dihy'dro-2H- quinoline-l-carbox3rlic acid ethyl ester (667 mg). MS (m/z): 764 [M+H]+ Example 192 (2R,4S)-4-([3,5-Bis(trifluoromethyl)benzyl]-{5-[(S)-2-((S)-3nethoxy-carbonyl)pyrrolidin-4-3doxy]pyrimidin-2-yl})amino-2-eth3d-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carbox3?'lic acid etliyl ester (200 mg) is dissolved in tetrabydrofuran (5 ml), and thereto are added acetyl chloride (44 yd) and triethylamine (88 yd) under ice-cooling. The mixture is stirred at room temperature for 4 hours, and separated into a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate. The organic Ia3'er is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatograptry (hexane:etihyl acetate = 3:2-^2:3) to give (2R,4S)-4-([3,5-bis(trifluorometh3d)benzyl] -{5-[(S)-2-((S)-methoxycarbonyl)-l-acefylp3nn-oUdin-4-yioxy]pyriniidin-2-yl})arnino-2-ethyl-6-trifluorometh3d-3,4-dihydro-2H-quinoline-l-carbox34ic acid ethyl ester (212 mg). MS (m/z): 806 [M+H]+ Example 193 (1) (2R,4S)-4-P£-Bis(1xifluorome^ yl)}amino-2-ethyl-6-txifluoromethyl-3^ acid ethyl ester (1.5 g) is dissolved in N,N-dimethylformamide (20 ml), axid thereto axe added 2-bromoethanol (1.25 ml) and potassium carbonate (4^0 mg), and the mixture is stirred at 60°C overnight. The reaction solution is cooled to room temperature, and water and ethyl acetate are added thereto, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexanerethyl acetate = 4:1—>1:1) to give (2R,4S)-4-{[3»5-bis(trifluoromethyl)benzylH^ ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-l-carboxylic acid ethyl ester (493 mg). MS (m/z): 681 [M+H]+ (2) (2R,4S)-4-{[3,5-Bis(iTffiuoro pyriinidin-2-3rl]}amino-2-e1liyl-6-trifluoromettxy 1-carboxylic acid ethyl ester (493 mg) is dissolved in methylene chlorLde (10 ml), and thereto are added triphenylphosphine (380 mg) and carbon tetrabromide (480 mg). The mixture is stirred at room temperature for 30 minutes, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and chloroform, and the mixture is separated. TIhe organic layer is washed with a saturated brine, dried over magnesiuxm sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatograph}?- (hexane:ethyl acetate * 9:1—4:1) to give (2R>4S)-4-{[3>5-bis(trifluoromethyl)benzyl]-[5-2H~quinoline-l-carbo>rylic acid ethyl ester (298 mg). MS {m/z): 743/7*45 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-{5-(2-bromoethoxy)- pyrimidin-2-3rl]}amm 1-carboxylic acici ethyl ester (298 ing) is dissolved in N,N-dimethyl-formamide (5 ml), and piperidine-4-carboxylic acid ethyl ester (185 \il) and potassium carbonate (166 mg) are added thereto, and the mixture is stirred at room temperature for 1.5 hour. The mixture is stir-red at 60°C for 2.5 hours. A saturated aqueous sodium hydrogen carborxate solution and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane: ethyl acetate = 1:1->1:4) to give (2R,4S)-4^([3?5-bis(trifluoromethyl)ben-2yl]-{5-[2-(4-ethoxycarbonylpiperidin-1 -yl)ethoxy]pyrimidin-2 -yl})amino-2 -ettayl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (245 mg). MS (m/z): 820 [M+H}+ Example 194 The corresponding starting compound is treated in a similar manner to Example 177 (3) and Example 178 to give the compound of Example 194. MS(m/z):790 [M-Na]-Example 195 The corresponding starting compound is treated in a similar manner to Example 177 (2)-(3) to give the compound of Example 195. MS (m/z): 721 [M+H]+ Example 196 The corresponding starting compound is treated in a similar manner to Example 187 (3) and Example 177 (3) to give the compourrd of Example 196. MS (m/z): 794 [M+H]+ Examples 197-208 The corresponding starting compounds are treated in a similar manner to Example 177 (3) to give the compounds as listed in Table 28. Example 209 (2R,4S)-4-{[3,5-Bis(trifluorometh^^ yl)}amino-2-ethyl-6-trifluorom acid ethyl ester (300 mg) is dissolved in tetrahydrofuran (3 ml), and thereto are added potassium tert-butoxide (53 mg) and (5-propiolactone (30 ]iL) at room temperature. The reaction solution is stirred at room temperature overnight, and thereto are added ethyl acetate and IN hydrochloric acid, and the mixture is separated. The organic layer is washed witti a saturated brine, and dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is dissolved in a mixture of tetrahydrofuran and methanol (5:1, 2 ml), and thereto is added a 2M solution of trimethjdsityldiazomethane in hexane (353 ]xl). Thirty miniates thereafter, the reaction solution is concentrated under reduced pressure, and the resulting residue is purified by NH-silica gel column chromato-graphy (hexane:ethyl acetate = 95:5-»3:l) to give (2R,4S)-4-{[3,5-t>is-(trifluoromethyl)benzyl]-[5-(2-me1±iox3rcarbon34ethoxy)pyrimidin-2-yl]}-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid etttyl ester (27 mg). MS (m/z): 723 [M+H]+ Example 210 (2R,4S)-4-{[3,5-Bis(trifluor^^ 3d)}amino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-l'Carboxylic acid ethyl ester (900 mg) is dissolved in tetrahydrofuran (9 ml), emd thereteo are added potassium tert-butoxide (158 mg) and p-propiolactone (89 pi) at room temperature. The reaction solution is stirred at room temperature overnight, and thereto are added ethyl acetate and 1N hydrochloric acid, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (chloroform:methanol = l:0-*9:l) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-[5-(2-carboxyethox7)pyrimidin-2-yl]}amino-2-ethyl-6-trifluorometh3d-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (178 mg). MS (m/z): 709 [M+H]+ Example 211 (1) (2R,4S)-4-p,5-Bis(txifluorom yl)}amino-2-ethyl-6-tri£luoronieth.yl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (500 mg) is dissolved in N,N-dimethylformamide (5 ml), and thereto are added 2-(2-chloroethoxy)ethanol (830 }il), and potassium carbonate (1.09 g), and the mixture stirred at room temperature for 3 hours. The reaction mixture is stirred at 60°C overnight. The reaction solution is cooled to room temperature, and the mixture is separated into water and ethyl acetate. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 4:1—>3:2) to give (2R,4S)-4-([3;,5-bis(trifluoromethyl)benz54]-{5-[2-(2-hydroxyethoxy)ethoxy]pyrimidin-2-yl})amino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-l-carboxylic acid ethyl ester (710 mg) as a crude product. MS (m/z): 725 [M+H]+ (2) The crude (2R,4S)-4-([3,5-bis(trifluoromethyl)benzyl]-{5-[2-(2- hydroxyethox5^)ethoxy]pyrimidin-2-yl})ainino-2-ethyl-6-trifluorometh3d-3?4- dihydro-2H-quinoline-l-carboxylic acid ethyl ester (706 mg) is dissolved in methylene chloride (10 ml), and thereto is added l,l,l-tris(acetoxy)-l,l- dih3'dro-l,2-benziodoxol-3-(lH)-one (826 mg), and the mixture is stirred at room temperature overnight. A saturated aqueous sodium hydrogen carbonate solution and ethyl acetate are added, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 4:l->3:2) to give (2R,4S)-4-{[3,5-bis(trifluoro-methyl)ben^l]-[5-(2-form3^1methoryethoxy)pyrimidin-2»yl]}ainino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (190 mg). MS (m/z): 723 [M+H]+ Example 212 (2R,4S)-4-([3,5-Bis(txinuoromefo^^ etfroxy]pyrimidm-2-yl})ammo- quinoline-1-carboxylic acid ethyl ester (160 mg) is dissolved in a mixture of tert-butanol (3 ml) and water (0.8 ml), and thereto are added potassium dihydrogen phosphate dihydrate (41.4 mg), sodium chlorite (85 mg), and 2-methyl-2-butene (103 pi), and the mixture is stirred at room temperature for 2 hours. To the reaction solution are added IN hydrochloric acid and ethyl acetate under ice-cooling, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (chloroform:methanol = 1:0—^9:1) to give (2R,4S)-4-{[3?5-bis(trifluorometh34)benzyl]-[5-(2-carbox3^methoxyethoxy)-pyrimidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (132 mg). MS (m/z): 739 [M+H]+ Example 213 (1) (2R,4S)'4-{[3?5-Bis(trifluoromethyl)benz34]-(5-hydroxyp3Timidin-2-yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (500 mg) is dissolved in N,N-dimeth3^1formamide (5 ml), and thereto is added 2-chloroethylcarbamic acid benzyl ester (402 mg) and potassium carbonate (260 mg), and the mixture is stirred at 80°C overnight. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by NH-silica gel column chromatography (hexane:ethyl acetate = 9:1—»4:1) to give (2R,4S)-4-{[5-(2-ben^loxycarbonylaminoeth^ bis(1xifluoromethyl)ben2yl]}ar^^ 2H-quinoline-l-carboxylic acid ethyl ester (249 mg). MS (m/z): 814 [M+H]+ (2) (2R,4S)-4-{[5-(2-Ben^loxycarbonylajninoethoxy)pyriinidin-2-yl]-[3,5-bis(trifluoromethyl)ben^l]}axnino-2-eiJiyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (240 mg) is dissolved in methanol (5 ml), and thereto is added 10 % palladium-carbon (100 mg), and the mixture is stirred under hydrogen atmosphere for 2 hours. The reaction solution is filtered and concentrated under reduced pressure. The resulting residue is purified by NH-silica gel column chromatography (hexane:ethyl acetate = 7:3—>2:3) to give (2R,4S)-4-{[5-(2-aminoethoxy)-pyrimidin-2-yl]-[3,5-bis(trifluoromethyty^ methyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (167 mg). MS (m/z): 680 [M+H]+ Example 214 (2R,4S)-4-{[3,5-Bis(trifluoromefo^ yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (975 mg) is dissolved in N,N-dimethylformamide (4.5 ml), and thereto is added sodium hydride (62.7 %, 70 mg) under ice-cooling, and the mixture is stirred for 10 minutes. To the reaction solution is added 4-bromobutyronitrile (0.2 ml), and the mixture is stirred at room temperature for one hour. To the reaction solution are added water and ethyl acetate under ice-cooling, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 4:1—>3:2) to give (2R,4S)-4-{[3,5-bis(1rifluoromethy^ yl]}ammo-2-ethyl-6-trifluorome^ acid ethyl ester (1.1 g). MS (m/z): 704 [M+H]+ Example 215 (2R,4S)-4-{[3,5-Bis(1xifluoromethy^ pyrimidin-2-yl]}amino-2 -ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (300 mg), sodium azide (462 rng), and ammonium chloride (380 mg) are dissolved in N,N-dimethylformamide (1 ml), and the mixture is stirred at 120°C for 27 hours. The reaction solution is cooled to room temperature, and thereto are added IN hydrochloric acid and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate aiid concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (chloroform :methanol = 1:0—9:1) to give (2R,4S)-4-([3,5-bis(1rmuorom yl) propoxy]pyrimidin- 2 -yl}) amino -2 - ethyl-6 - trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (169 mg). MS (m/z): 747 [M+H]+ Example 216 (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(3-cyanopropoxy)-pyrimidin-2-yl]}amino-2-ethyl-6-trffi^ 1-carboxylic acid ethyl ester (700 mg), hydroxylamine hydrochloride (140 mg) and sodium carbonate (212 mg) are dissolved in ethanol (3 ml), and the mixture is refluxed for 41 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 7:3—1:1) to give (2R,4S)-4-([3,5-bis(trifluoro- me thyl) benzyl]-{5 - [3 - (N-hy droxy carb ammo-2-ethyl-6-txifluoromefo acid ethyl ester (502 mg). MS (m/z): 737 [M+H]+ Example 217 (2R,4S)-4-([3,5-Bis(1rffluoromethyl)benzyl]-{5-[3-(N-hydro^^ carbamimidoyl)propoxy]pyrimidm^ 3?4-dih3^dro-2H"quinoline-l-caxboxylic acid ethyl ester (200 ing), and 1,1'-carbonyldiimidazole (66 mg) are dissolved in acetonitrile (1.5 ml), and the mixture is stirred at 60°C for 16.5 hours. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexanerethyl acetate « 7:3-+l:l) to give (2R,4S)-4-([3,5-bis(trifluoro-meth3d)benzyl]-{5-[3~(5-oxo-4,5-dihydro yl)propoxylpyrimidin-2-yl})amino^ quinoline-1-carboxylic acid ethyl ester (115 mg). MS (m/z): 763 [M+H]+ Example 218 (2R,4S)-4-([3,5-Bis(trifluoromethyl)ben234]-{5-[3-(N-h3^droxy-carbamijnidoyl)propox3^]pyriinidin-2-yl})ainino-2-ethyl-6-trifluorornethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (240 mg) and pyridine (106 p.1) are dissolved in tetrahydrofuran (7.5 ml), and thereto is added dropwise a solution of thionyl chloride (48 pi) in methylene chloride (3 ml), and the mixture is stirred for 2 hours and 40 minutes. The reaction solution is concentrated under reduced pressure, and thereto are added water and etiiyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexanerethyl acetate = 4:1—► 1:1) to give (2R,4S)-4-([3,5-bis(1xffluoro oxotftiazol-4-3d)propoxy]pyriimdm 3,4-dihydro-2H-quinoline-l-carbosylic acid ethyl ester (181 mg). MS (m/z): 783 [M+H]+ Example 219 3-Chloropropane-l-sulfonyl chloride (0.38 ml) is dissolved in methylene chloride (15 ml), and ammonia gas is blown into the mixture for 15 minutes. The reaction solution is stirred overnight, and the resulting ammonium chloride is removed by filtration. The filtrate is concentrated, and the resulting 3-chloropropane-l-sulfonamide and (2R?4S)-4-{[3,5-bis(iTifluorometh3d)ben2yl]-(5"h3^dro^pyrimidin-2-yl)}arriino-2-ethyl--6-trifluoromethyl-3)4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (500 mg), potassium iodide (1.3 g), and, potassium ttydroxide (352 mg) are dissolved in dimethylsulfoxide (4 ml), and the mixture is stirred at 60°C for 24 hours. The mixture is cooled to room temperature; and thereto are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified bj^ silica gel column chromatography (hexane:ethyl acetate = 9:1—>1:1) to give (2R,4S)-4-{[3?5-bis(trifluoromethyl)benz34]-[5-(3-sulfamoylpropo^)-pyrimidin-2-yl]}amino-2-ethyl-6-triiluorometh34-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (22 mg). MS (m/z): 758 [M+H]+ Example 220 (1) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]--(5-hydroxyp3Timidin-2-yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxy'lic acid ethyl ester (300 mg) is dissolved in tetrairydrofuran (5 ml), and thereto are added ettty 4-(hj^dro^methyl)cyclohexylacetate (141 mg) and triphen3'l-phosphine (370 mg). To the mixture is added dropwise a 40 % solution of diethyl azodicarboxylate in toluene (600 |il) under ice-cooling, and the mixture is stirred at room temperature for 2.5 hours. Water and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified b3^ NH-silica gel column chromatography (hexane;ethyl acetate « 19:1-^4:1) to give (2R,4S)-4-{[3,5-bis(trmu carbonylrnefoylcyclohexylmetho^ trifluorornethyl-3>4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (275 xng). MS (m/z): 819 [M+H]+ (2) (2R,4S)-4-{[3,5-Bis(1xifiuoromethyl)ben^ methylc3^clohexylmettioxy)p3oimidm^ 3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (220 mg) is dissolved in ethanol (5 ml)? and thereto is added dropwise a IN aqueous sodium hydroxide solution (1 ml), and the mixture is stirred at room temperature overnight. To the mixture are added IN l^drochloric acid and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified b3^ silica gel column chromatography (chloroform:methanol = 1:0-^9:1) to give (2R,4S)- 4-{[3,5-bis(trifluorometh34)benzyl]-[5-(4-carboxymethylcyclohex3rl- methoxy)pyrimidin-2-34]}amino-2-ethyl-6-trifluorometh3'l-3,4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (181 mg). MS (m/z): 791 [M+H]+ Example 221 The corresponding starting compound is treated in a similar manner to Example 178 to give the compound of Example 221. MS (m/z): 746 [M-Na]-Examples 222-224 The corresponding starting compounds are treated in a similar manner to Example 1(3) to give the compounds as listed in Table 29. Examples 225-226 The corresponding starting compounds are treated in a similar manner to Example 177 (3) to give the compounds as listed in Table 30. Example 227 (2R,4S)-4-[[3,5-Bis(trinuorome^^ carbonylethjd)]amino}pyrimidm^ dihydro-2H-quinoline-l-carboxylic acid ethyl ester (70 mg) is dissolved in a 4N hydrogen chloride in ethyl acetate (0.5 ml), and the mixture is stirred at room temperature for 3 hours. To the reaction solution are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure to give (2R,4S)-4-[[3,5-bis(trifluoromethyl)benzyl]-(5-{[ethyl-(2-carboxyethyl)]amino}pyrimidin-2-yl)]amino-2-ethyl-6-trifluoromethyl-3?4-ditiydro-2H-quinoline-l-carboxylic acid ethyl ester (65 mg). MS (m/z): 736 [M+H]+ Example 228 (1) (2R,4S)-4-{[3,5"Bis(trifluoromethyl)benzyl]-(5-iodopyrimidin-2-yl)}-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.0 g), copper iodide (13 mg), potassium carbonate (370 mg), ethylene glycol (0.15 ml), and 4-mercaptobutanol (0.14 ml) are dissolved in isopropyl alcohol (1.5 ml), and the mixture is stirred at 80°C under nitrogen atmosphere for 15 hours. The mixture is cooled to room temperature, and thereto is added ethyl acetate. The insoluble materials are removed by filtration, and the filtrate is concentrated under reduced pressure. The resulting residue is purified by silica gel column chromato-graphy (hexane:ethyl acetate = 9:l->7:3) to give (2R,4S)-4-{[3,5-bis-(txifluorome thy 1) benzyl]-[ 5 - (4-hydrox 2-et±iyl-6-txiiluoromethyl-3,4-dihydro-2H-quinoline-l--carbo3cy'lic acid ethyl ester (705 mg). MS (m/z): 725 [M+H]+ (2) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(4-hydroxybutyl- sulfajiyl)pyrirnidin-2-yl]}ainino-2-e1±iyl-6-trifluorome quinoline-1-carboxylic acid ethyl ester (500 mg) is dissolved in chloroform (2 ml), and thereto is added m-chloroperbenzoic acid (75 %, 636 mg) under ice-cooling. The mixture is stirred at room temperature for one hour, and thereto are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by NH-silica gel column chromatography (hexane:ethyl acetate = 7:3—>1:1) to give (2R,4S)-4-{[3,5-bis(trifluoromet^ pyrimidm-2-yl]}ammo-2-e1±Lyl-6-^ 1-carboxylic acid ethyl ester (309 mg). MS (m/z): 757 [M+H]+ (3) (2R,4S)-4-{[3,5-Bis(trmuorome sulfonyl)pyrimidin-2-yl]}amino-2-efo^ quinoline- 1-carboxylic acid ethyl ester (300 mg) and l,l,l-tris(acetoxy)-l,l-dihydro-l,2-benziodoxol-3-(lH)-one (269 mg) are dissolved in methylene chloride (2 ml), and the mixture is stirred for 2.5 hours. Water and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 9:1->1:1) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benzyl]-[5-(3-carboxy-propylsulfonyl) pyrirmdm-2-yl]}am^ 2H«quinoline-l-carboxylic acid ethyl ester (103 mg). MS (xn/z): 771 [M+Hj+ Example 229 (1) (2RJ4S}-4-.\mino-2-ettiyl-6-trmiaorornethyl-3?4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester (3 g), 2-chloro-4-methylthiazole-5- carboxylic acid ethyl ester (5.85 g) and diisopropylethylamine (3.3 ml) are dissolved in 1,4-dioxane (25 ml), and the mixture is stirred at 130°C for one week. The reaction solution is cooled to room temperature, and water and ethyl acetate are added thereto, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified b}7 silica gel column chrornatography (hexanerethyl acetate = 6:1—>4:1) to give (2R,4S)-4-(5-ethoxyca.rbonyl-4-methylthiazol-2-3d)amino-2- ethjd-6-trifluorome1±iyl-3)4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.93 g). MS (m/z): 486 {M+H]+ (2) (2R>4S)-4-(5-Ethoxycarbonyl-4-xnethyl1±Liazol-2-34)amino-2-ethyl-6- trifluoromethyl-3,4-dih3^dro-2H-quinoline-l-carboxyiic acid ethyl ester (1.9 g) is dissolved in N,N~dimethylfonna.mide (20 ml), and thereto is added sodium hydride (62.7 %, 282 mg) under ice-cooling. The reaction mixture is stirred at room temperature for 3O minutes, and thereto is added 3?5- bis(trifluorometh3d)benzyl bromide (1.56 ml) under ice-cooling. The mixture is stirred at room temperature for 3 hours, and a saturated aqueous citric acid solution and ethyl acetate are added thereto, and the mixture is separated. The organic Ia3'er is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatograpl^ (hexane:ethyl acetate « 9: l-*4:1) to give (2R,4S)-4-{[3,5-bis(trifluoro- methyl)benzyl]-(5-ethoxycarbonyl-4-inethylthiazol-2-yl)}amino-2-ethyl-6- trifluoromethyl-3J4-dih3^dro-2H-quinoline-l-carboxylic acid ethyl ester (1.62 g). MS (m/z): 712 [M+H]+ Example 230 (2R,4S)-4-{[3,5-Bis(trffluorom methylthiazol-2-yl)}amino-2-et±^ qulnoline-l-carboxylic acid ethyl ester (250 mg) and lithium hydroxide moxiohydrate (147 mg) are dissolved in a mixture of ethanol (5 ml) and a 2N aqueous sodium hydroxide solution (703 ill), and the mixture is stirred at T0°C for 2 hours. The reaction solution is cooled to room temperature, and acidified with a 2N aqueous hydrochloric acid. Subsequently, to the mixture is added ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified bj?" silica gel column chromatography (chloroformrmethanol = 1:0—> 19:1) to give (2R,4S)-4-{[3,5-bis(1xifluorome1Jiyl)ben^d]-(5-carboxy-4-raethyl1±iia2ol-2-y"l)}airiino-2-ethyl-6-trifluorometh34-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (189 mg). MS (m/z): 684 [M+H]+ Example 231 (1) (2R)4S)-4-Amino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H- quinoline-1-carboxylic acid ethyl ester (10.0 g), 2y5-dibromop3^ridine (15 g), tris(dibenzylideneacetone)dipalladium (2.9 g), 2-dic3'clohexylphosphino-2'- (N,IN-dimethylamino)biphenyl (2.5 g) and sodium, tert-butoxide (6.1 g) are dissolved in toluene (100 ml), and the mixture is stirred at 80°C for 15 hours under nitrogen atmosphere. The mixture is cooled to room temperature, and water and ethyl acetate are added thereto, and the mixture is separated. The organic layer is washed with water and a saturated brine, and thereto is added NH-silica gel, and the mixture is filtered. The filtrate is concentrated under reduced pressure, and the resxxlting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 9:1—^4:1) to give (2R,4S)-4-(5-bromopyridin-2- 3d)a_rn.ino-2-ethyl-6-trifluoroinet±iyl-3)4-dihydro-2H-qiiinoline-l-carboxylic acid ethyl ester (3.56 g). MS (m/z): 472/474 [M+H]+ (2) (2R,4S)-4-(5-Bromopyridin-2-yl)amino-2-ethL3^1-6-trifluoromethyl-3>4- dihydro-2H-quinoline-l-carboxylic acid ethyl ester (2.4 g) is dissolved in N>T-dimeth3?-lfoririajaiide (15 ml), and thereto is added sodium hydride (40 %, 335 mg) under ice-cooling. The mixture is stirred at room temperature for 30 minutes, and thereto is added 3?5-bis(trifluoromethyl-benzyl bromide (1.1 ml). The mixture is stirred at room temperature for 5 hours. To the mixture are added water and diethyl ether under ice-cooling, and the mixture is separated. The organic layer is washed with IN hydrochloric acid, water and a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane: ethyl acetate = 9:l-»7:3) to give (2R,4S)-4-{[3,5-bis(trifluoromethyl)benz3d]-(5-bromo. pyridin-2-34)}amino-2-ethyl-6-txifluorometh34-3)4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.72 g). MS (m/z): 698/700 [M+HJ+ (3) (2R74S)-4-{[3>5-Bis(trifluoromethyl)benzyl]-(5-bromopyridin-2-yl)}-amino-2-eth34-6-trifiuorometJiyl-3,4-dihydro-2H-quinoline-l-'Carboxylic acid ethyl ester (1.72 g), [l>r-bis(diphenylphosphino)ferrocene]dichloro-palladium (54 mg), potassium acetate (725 mg) and bis(pinacolate)diboron (938 mg) are dissolved in deaerated dimethylsulfoxide (7 ml), and the mixture is stirred at 80°C for one hour. The reaction solution is cooled to room temperature, and water and ethyl acetate are added thereto, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is dissolved in tetrattydrofuran (7.5 ml), and thereto is added a 30 % aqueous hydrogen peroxide solution (2.8 ml) under ice-cooling, and the mixture is stirred for 3 hours. A saturated aqueous sodium thiosulfate solution and ethyl acetate are added to the mixture under ice-cooling, and the mixture is separated. The organic layer is washed with water and a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatographj' (hexane;ethj4 acetate = 4:l-+3:2) to give (2R?4S)-4-{[3,5»bis(trifluoromethyl)'benzyl]-(5- hydxox3^yridin-2-yl)}ajoiino-2-eth^ quinoline-l~carboxylic acid ethyl ester (851 mg). MS (m/z): 636 [M+H]+ (4) (2R,4S)-4-fl3,5-Bis(trifluorometh^ yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (200 rng) is dissolved in N?N-dimethylformamide (1.5 ml), and thereto is added sodium hydride (15 mg) under ice-cooling. The mixture is stirred for 15 minutes, and thereto is added 4-bromobutyric acid ethyl ester (69 yd) ? and the mixture is stirred at room temperature for 1.5 hour. To the reaction solution are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified b3^ silica gel column ohromato-graphy (hexane:ethyl acetate = 9:1-+4:1) to give (2R,4S)-4~{(3,5-bis-(trifluoromethyl) benzyl] -[5-(3-ethoxycarbonylpropoxy)pyridin-2-yl]}amino-2~ ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (132 mg). MS (m/z): 750 [M+H)+ (5) (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(3-ethoxycarbonyl- propoxy)pyridin-2-3d]}aLxaino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-- quinoline-1 -carboxylic acid ethyl ester (120 mg) is dissolved in ethanol (0.8 ml), and thereto is added a 2N aqueous sodium hydroxide solution (0.24 ml), and the mixture is stirred for 3 hours. To the reaction solution are added a 2N hydrochloric acid solution (0.24 ml) and ethyl acetate, and the mixture is separated. The organic layer is washed with water and a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. Thte resulting residue is purified by silica gel column chromatography (hexaxie:ethyl acetate = 7:3—>1:1) to give (2R,4S)-4-{[3,5~ bis(trifluoromethyl)ben-zyl]-[5-^ eth34-6-trifluorometh3d-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (105 rng). MS (m/z): 722 [M+H]+ Example 232 The corresponding starting compound is treated in a similar manner to Example 231 (4)-(5) to give the compound of Example 232. MS (m/z): 736 [M+H]+ Example 233 (1) (2R,4S)-4-(5-Bromopyrimidin-2-yl)amino-^^ 3,4-dihydro-2H-quiinoline-l-carboxylic acid ethyl ester (18 g) is dissolved in tetrahydrofuran (180 ml), and thereto are added di-tert-butyl dicajrbonate (24.8 g) and a catalytic amount of dimeth34aminop3>ridine, and the mixture is stired at room temperature overnight. To the mixture are added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate, and the mixture is separated. The organic laj'er is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by NH-silica gel column chromatography (hexane:ethyl acetate = 8:1) to give (2R>4S)-4-[(5-bromopyrirnidin-2-yl)-tert-butoxjrcarbonyl]ainino-2-eth34-6-trifluoroxnethyl-3,4-dihydro-2H-qu.inoline«l-carboxylic acid ethyl ester (22.5 g). MS (m/z): 573/575 [M+H]+ (2) (2R,4S)-4-[(5-Bromopyrimidin-2-yl)-tert-butoxycarbonylJairiin.o-2- ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (22.5 g) is dissolved in 1,4-dioxane (110 ml), and thereto are, added copper (I) iodide (375 nig), sodium iodide (11.8 g) and N,N'-dimethylethane- 1 ,2-diamine (0.42 ml), and the mixture is refluxed under nitrogen atmosphere overnight. The reaction solution is cooled to room temperature, and thereto are added water and ethyl acetate, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexanerethyl acetate = 4:1) to give (2R,4S)-4-[tert-butoxycarbonyl-(5-iodopyrimidin-2-yl)]amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester (21.6 g). MS (m/z): 621 jM+H]+ (3) (2R?4S)-4"[tert-Butoxvcarbonyl-(5-iodopyrinxidin-2-yl)]amino-2-e1±iyl- 6-trifluorometh3^1-3!4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (1.0 g), [l,r-bis(diphenylphiosphino)ferrocene]dichloropalladium (35 rag), potassium acetate (475 ing) and bis(pinacolate)diboron (615 mg) are dissolved in deaerated dimethylsulfoxide (8 ml), and the mixture is stirred at 80°C for 18 hours. The reaction solution is cooled to room temperatizre, and water and ethyl acetate are added thereto, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is dissolved in tetraltydrofuran (8 ml), and thereto is added an excess amount of a 30 % aqueous hydrogen peroxide solution under ice-cooling, and the mixture is stirred for 6 hours. A saturated aqueous sodium thiosulfate solution and ethyl acetate are added to the mixture under ice-cooling, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate a_nd concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (chloroform:methanol - 1:0—*19:1) to give (2R,4S)-4-[tert-butox5^carbonyl-(5-h3^droxyp3rrimidin-2-yl)] amino-2-ethyl-6-trifluoromethyl-3,4-dLih3^dro-2H-quinoline-l-carboxylic acid ethyl ester (1.7 g). MS(m/z):511 [M+H]+ (4) (2R,4S)-4-[tert-Butox3rcarbon3^1-(5-h3^droxypyrimidin-2-yl)]amino-2- eth}4-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carbox3^1ic acid ethyl ester (800 mg) is dissolved in N,N-dimethylformamide (5 ml), and thereto is added sodium hydride (62.7 %, 72 ing) under ice-cooling. The mixture is stirred at room temperature for 15 minutes, and thereto is added 1-chloro-2-methylsulfanylethane (259 mg), a_nd the mixture is stirred at room temperature for 24 hours. Water and ethyl acetate are added to the reaction mixture under ice-cooling, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chrornatography (hexane:ethyl acetate = 4:l->3:7) to give (2R,4S)-4-{tert-butoxycarbon34-[5-(2-methylsulfanyl-ethox5^)pyrimidin-2-3d]}airiino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-1-carboxylic acid ethyl esteir (200 mg). MS (m/z): 585 [M+H]+ (5) (2R,4S)-4-{tert-Butox3'carbon3'H P3n±rridin-2-yl]}aixrino-2-ethyl-6^ l-carbox3dic acid ethyl ester (200 rng) is dissolved in a 4N hydrogen chloride in 1,4-dioxane (1.5 ml), axid the mixture is stirred at room temperature for 17.5 hours. To the reaction solution are added a 2N aqueous sodium hydroxide solution (3 ml) and diethyl ether, and the mixture is separated. The organic layer is concentrated under reduced pressure, and the resulting residue is purified b3' silica gel column chromatography (hexanerethyl acetate « 4:1—>1:1) to give (2R,4S)-2-ethyl-4-[5-(2-meth3^1sulfan3^1ethoxy)pyrimidin-2-3d]amino-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-l-carbos5dic acid ethyl ester (170 mg). MS (m/z): 485 [M+H]+ (6) (2R,4S)-2-Ethyl-4-[5-(2-methylsxilfanylethox30pyrimidin-2-34]amino- 6-trifluoromethyl-3,4-dih3'dro-2H-quinoline-1 -carboxylic acid ethyl ester (160 mg) is dissolved in N,N-dimethylformamide (1.5 ml), and thereto is added sodium hydride (62.7 %, 15 nxg) under ice-cooling. The mixture is stirred at room temperature for 30 minutes, and thereto is added 3,5-dibromobenz3'l bromide (141 mg), ajnd the mixture is stirred at room temperature for 19 hours. To the itiixture is added a 0.5N hydrochloric acid and diethyl ether under ice-cooling, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 9:l->7:3) to give (2R,4S)-4-{(3,5-dibromobenzyl)-[5-(2-meth3rlsulfanyl-ethox5^)pyrimidin-2-3d]}ainino-2-ethyl-6-trifluoromethyl-3>4-dih3^dro-2H-quinoline-1-carboxylic acid ethy^l ester (110 mg). MS (m/z): 733 [M+H]+ ' (7) (2R,4S)-4-{(3,5-Dibromobenzyl)-[5-(2-meth34sulfanylethoxy)- pyrimidin-2-yl]}ajnino-2-ethyl-6-trifluorometh3^1-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (100 mg) is dissolved in N,N-dimethyl- formamide (2 ml), and thereto are added zinc cyanide (35.3 mg) and a catalytic amount of tetrakis(triphenylphosphine)palladium, and the mixture is stirred at 110°C for 17.5 hours. The reaction solution is cooled to room temperature, and watex and diethyl ether are added thereto, and the mixture is separated. The organic layer is washed with a saturated brine, dried over magnesium sulfate and concentrated under reduced pressure. The resulting residue is purified by silica gel column chromato graphy (hexane:ethyl acetate = 9:l->7:3) to give (2R,4S)-4-{(3-bromo-5- cyanobenzyl)-[5-(2-inethylsulfan.34et±ioxy)pyriniidin-2-yl]}amino-2-ethyl-6- trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester (28 mg, MS (m/z): 678/680 [M+HJ-), and (2R,4S)-4-{(3,5-dicyanobenz3rl)-[5-(2- methylsulfan}4ethoxy)pyrimidin--2-3d]}aminO'-2"eth3d-6-trifluoromethyl-3,4- dihydro-2H-quinoline-l-carboxy^lic acid ethyl ester (50 mg, MS (m/z): 625 [M+H]+). (8) (2R,4S)-4-{(3-Bromo-5-cyanobenzjd)-[5-(2-methylsulfan34ethox30- P3^rimidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid ethyl ester (25 mg) is dissolved in chloroform (0.5 ml), and thereto is added m-chloroperbenzoic acid (75 %, 17 mg), and the mixture is stirred at room temperature for 35 minutes. A saturated aqueous sodium hydrogen carbonate solution and ethyl acetate are added to the mixture, and the mixture is separated. The organic layer is concentrated under reduced pressure, and the resulting residue is purified by silica gel column chromatography (hexane:ethyl acetate = 7:3—>1:1) to give (2R?4S)-4-{(3-bromo-5-cyanoben25d)-[5-(2-methylsulfonylethoxy)- pyrimidin-2-yl]}aiiiino-2-et±iyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline--1-carboxylic acid ethyl ester {29 ing). MS (m/z): 710/712 [M+H]+ Example 234 The corresponding starting compound is treated in a similar manner to Example 233 (8) to give the compound of Example 234. MS (m/z): 657 [M+H]+ Example 235 (1) (2R,4S)-4-(5-Bromopyrimidixi-2-yl)amino-2-eth3d-6-trifluorometh3d-3,4-dih3^dro-2H-quinoline-l-carboxylic acid ethyl ester (1.0 g) is dissolved in N,N-dimethylformamide (10 ml), and thereto is added sodium itydride (62.7 %, 89 mg) under ice-cooling. The mixture is stirred at room temperature for 15 minutes, and thereto are added 3-cyano-5-trifluoromethylbenzyl bromide (669 mg), and the mixture is stirred at room temperature for 20 hours. Water and diethyl ether are added to the mixture, and the mixture is separated. The organic layer is washed with water and a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. The resulting residue is purified b}' silica gel column chromatography (hexane:ethyl acetate = 9:1—^4:1) to give (2R,4S)-4-[(5-bromop3^rimidin-2-yl) »(3-cyano-5-trifluoromethylbenzyl)]- amino-2-ethyl-6-trifluorometayl^ acid ethyl ester (1.08 g). MS (xn/z): 656/658 [M+H]+ (2) (2R,4S)-4-[(5-Bromop3oriimd^ benzyl)]amino-2-ethyl-6-trifluoromethyl-3 >4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (250 ing), tris(dibenzylideneacetone)dipalladiuxn (35 mg), 2-(di-tert-butylphosphino)diphenyl (45 mg), sodium tert-butoxide (55 mg), and piperidine-4-cart>oxylic acid ethyl ester (88 ]il) are dissolved in toluene (2 ml), and the mixture is stirred at room temperature for 2.5 hours. The reaction solution is stirred at 80°C for 15 hours. To the reaction solution are added "water and ethyl acetate, and the mixture is separated. The organic layer is washd with a saturated aqueous sodium hydrogen carbonate solution and water, a saturated brine, dried over magnesium sulfate, and concentrated under reduced pressure. Ttxe resulting residue is purified b}^ silica gel column chromatograph.y (hexanerethyl acetate = 4:l->3:2) to give (2R?4S)-4-{(3-c3^ano-5-1xifluoromethylbenzyl)--[5-(4-etlTLOxycarbonylpiperidin-1 -yl)pyrimidin-2-yl]}amino«2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester (126.8 mg). MS (m/z): 733 [M+H]+ (3) (2R,4S)-4-{(3-C^ano-5-txifluoro piperidin-l-yl)pyriniidin-2-yl]}aiixino-2-et±Lyl-6-trifluorom 2H-quinoline-l-carboxylic acid ethyl ester (120 mg) is dissolved in ethanol (4 ml), and thereto is added 23NT aqueous sodium hydroxide solution (1 ml), and the mixture is stirred at room temperature for 3 hours. To the mixture are added 2N hydrochloric acid (1 ml) and ethyl acetate, and the mixture is separated. The organic layer is concentrated under reduced pressure, and the resulting residue is purified by silica gel column chromatograplry (hexane:eth3'l acetate = 7:3-»l:l) and by LC/MS (CAPCEL PAK MG II (Shiseido Co., Ltd.), watenmettLanol « 60:40—>methanol, 40 ml/min) to give (2R,4S)-4-{[5-(4-carboxypiperi(iin-l-yl)pyrimidin-2-yl]-(3-cyano-5- trifluorome1±iylbenz3d)}ajnino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H- CLAIMS 1. A compound of the formula (I): wherein R1 is a. hydrogen atom, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, an optionally substituted alkyl group, an optionally substituted alkanoyl group, a saturated or unsaturated monocyclic or bicyclic heterocj^clic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted), or a saturated or lansaturated monocj'clic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted),; R2 is a hydrogen atom or an optionally substituted alkyl group; R3 is a hydrogen atom or an optionally substituted alkyl group; R4 is an optionally substituted alkylene group; R5 is a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, wherein the heterocj^clic group is substituted b}' 1 to 5 substituents selected from the following groups, or said heterocyclic group is substituted by 1 to 5 substituents selected from the following groups and further by a halogen atom, an oxo and/or hydroxy group: cj'ano group, nitro group, carboxyl group, sulfo group, C3-10 alkyl group, substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, C3-10 alkoxy group, substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxycarbonyl group, optionally substituted carbamoyl group, optionally substituted carbamimidoyl group, optionally substituted alkylth-io group, optionally substituted alkylsulfinyl group, optionally substituted alkylsulfonyl group, optional^ substituted amino group, optionally substituted sulfamoyl group, optionally substituted alkanoyl group, a saturated or unsaturated monocyclic or bicyclic heterocycLic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted), a saturated or unsaturated monocyclic or bic3'clic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonyl group is optionally substituted); R6, R7, R8 and R9 are independently a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a cyano group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an optionally substituted alkylsulfonyloxy group or an optionally substituted amino group; or R6 and R7, or R7 and Rs, or R8 and R9 may combine at the ends to form an alkylene group which alkylene group may contain 1 to 3 heteroatoms selected independently from nitrogen, sulfur and oxygen atoms, and may have a substituent(s); and R10 is an aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the aromatic ring is optionally substituted), or a pharmaceutically acceptable salt thereof. 2. The compound of claim 1, wherein R5 is a saturated or unsaturated monocyclic or bicj^clic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, wherein the heterocyclic group is substituted by 1 to 5 substituents selected from the following groups, or said heterocyclic group is substituted by 1 to 5 substituents selected from the following groups along with halogen atom, oxo and/or hydroxy group: cyano group, nitro group, carboxyl group, sulfo group, C3-10 alkyl group, substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, C3-10 alkoxy group, substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxy carbonyl group, carbamoyl group, optionally substituted mono- or di-alkylcarbamoyl group, optionally substituted carbamimidoyl group, optionally substituted alkylthio group, optionally substituted alkylsulfinyl group, optional^ substituted alkylsulfonyl group, amino group, optionalty substituted mono- or di-alkylamino group, optionally substituted alkanoylamino group, optionally substituted alkoxycarbonylamino group, optionally substituted alkylsulfon3damino group, optionally substituted mono- or di-alkylcarbamoylamino group, a saturated or unsaturated monocyclic or bicyclic heterocyclic carbon3'lamino group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonylamino group is optionally substituted), sulfamoyl group, optionally substituted mono- or di-alkyl sulfamoyl group, optionally substituted alkanoyl group, a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocjrclic group is optionally substituted), a saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonyl group is optionally substituted); and R10 is an aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, which aromatic ring is optionally substituted by 1 to 4 substituents selected from the following groups: halogen - atom, carboxyl group, optionally substituted alkoxycarbon}^ group, carbamoyl group, optionally substituted mono- or di~alkylcarbamoyl group, optionally substituted alkyl group, optionally substituted alkoxy group, hydroxy group, nitro group, cyano group, amino group, optionally substituted mono- or di-alkylamino group, optionally substituted alkanoyl group, optionally substituted alkylthio group, and a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted). 3. The compound of claim 2, wherein the substituent(s) for substituted alkyl group, optionally substituted alkyl group, optionally substituted cycloalkyl group, optionally substituted alkenyl group, substituted alkoxy group, optionally substituted alkoxy group, optionally substituted cycloalkoxy group, optionally substituted alkoxycarbonj'l group, optionally substituted mono- or di-alkylcarbamoyl group? optionally substituted alkylthio group, optionally substituted alkylsulfinjd group, optionally substituted alkylsulfonyl group, optionally substituted mono- or di-alkylamino group, optionally substituted alkanoylamino group, optionally substituted alkoxycarbonylamino group, optionally substituted alkylsulfonylamino group, optionally substituted mono- or di-aJkylcarbamo3'lamino group, optionally substituted mono- or di-alkylsulfamo}?! group, optionally substituted alkanoyl group, optionally substituted alkylene group, a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonylamino group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic carbonylamino group is optionally substituted), a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heterocyclic group is optionally substituted), a saturated or unsaturated monoc3^clic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heteroc3'clic oxy group is optionally substituted), and a saturated or unsaturated monocyclic or bicyclic heterocyclic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms (the heteroc3'clic carbonyl group is optionally substituted) may be 1-5 groups selected from the following groups; halogen atom; cj'ano group; hydroxy group; nitro group; carboxyl group; oxo group; thioxo group; sulfo group; c3?-cloalkyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbon37"l group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkoxycarbonyl group optionally substituted by hydroxy group? halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, ph.enyl group or morpholinyl group; carbamoyl group; mono- or di-alkylcarbamoyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholn-tyl group; alkanoyl group optionally substituted by hydrox3^ group, halogen atom, carboxyl group, alkox3'pcarbonyl group, mono- or di-alk3"lamino group, phenyl group or morpholinyl group; alkoxy group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkanoyloxy group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkylthio group optionally substituted by hj'droxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkylsulfonyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; alkylsulfinyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbon}^ group, mono- or di-alkylamino group, phenyl group or morpholinyl group; mono- or di-alkylsulfamoyl group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbon34 group, mono- or di-alkylamino group, phenyl group or morpholinyl group; amino group; mono- or di-alkylamino group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; mono- or di-alkylsulfamoylamino group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; mono- or di-alkylureido group optionally substituted by hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, mono- or di-alkylamino group, phenyl group or morpholinyl group; and a group of the formulas: wherein X* and X^ are independently CH2» NH, O, S, SO or SO2; X2 and Xs are independently CH2, 0, S, SO or SO2; X« is NH, O, S, SO or S02; X6 and X7 are independently 0 or S; X8 is S or SO; and n, o, p, q and r are independently an integer of 1 to 4, wherein each group of the above formula is optionally substituted bj^ 1 to 3 substituents selected from the following groups: halogen atom, carboxyl group, hydroxy group, cyano group, oxo group, thioxo group, alkyi group, hydroxyalkyl group, alkoxycarbonylalkyl group, carboxyalkyl group, morpholinylalkyl group, phenylalkyl group, alkanoyl group, hydroxyalkanoyl group, alkoxyalkanoyl group, alkoxy group, phenylalkoxy group, alkoxycarbonyl group, benzyloxycarbonyl group, mono- or di-alkylamino group, mono- or di-alkylcarbamoyl group, mono- or di-alkylsulfamoyl group, alkylsulfonyl group and tetrazolyl group. 4. The compound of claim 3, wherein the "aromatic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a pherxyl, naphthyl, pyridyl, quinolyl, isoquinolyl, furyl, pyrimidinjd, triazolyl or thienyl group; the "saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a morpholinyl* thiomorpholinyl, piperazinyl, pyrrolidinyl, piperidinyl, hexahydroazepin3^1, pyrrolinyl, imidazolidinj^l, oxazolidinyl, tetrahydropyranjd, tetrahydrofuranyl, dioxolanyl, oxiranyl, pyrimidinyl, p3^ridyl, triazolyl, tetrazolyl, oxadiazolyl, dihydropyrimidinyl, pyrazinyl, thiazolyl, oxazolinyl, oxazolyl, pyridazinyl, imidazolinyl, imidazolyl, pyrazinyl, thienyl, pyrrofyl, furyl or dihydrooxazinyl group; the "saturated or unsaturated monocyclic or bicyclic heterocyclic oxy group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a morpholinyloxy, thiomorpholinyloxy piperazinyloxy, pyrrolidinyloxy, piperidinyloxy, hexahydroazepinyloxy, pyrrolinyloxy, imidazolidinyloxy, oxazolidinyloxy, tetrahydropyranyloxy, tetrahydrofuranyloxy, dioxolanyloxy, oxiranyloxy, pj^rimidinyloxy, pyridyloxy, triazolylox}^ tetrazolyloxy, oxadiazolyloxy, dihydrop3^rimidinyl-0x3^, pj^razinyloxy, thiazolylory, oxazolinyloxj% oxazolyloxy, pyridazinyloxy7 imidazolinyloxj^ imidazotyloxy, p3Taziri3J'loxy, thienylo?ry\ pyrrolyloxy. furyloxy or dihydrooxazinyloxj^ group; the "saturated or unsaturated monocyclic or bicyclic heteroc^^clic carbonyl group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a morpholinylcarbonyl, thiomorpholinylcarbonyl piperazinylcarbonyl, pyrrolidinylcarbonyl, piperidinylcarbonyl, hexahydroazepinylcarbonyl, pyrrolinylcarbon}^, imidazolidinylcarbonyl, oxazolidinylcarbonyl, tetrahydrop3^ranylcarbonyl, tetrahydrofuranylcarbonyl, dioxolanylcarbon3'l, oxiranylcarbonyl pyrimidin3'lcarbonyl> pyridylcarbonyl, triazolylcarbonyl, tetrazolylcarbonyl, oxadiazolylcarbon3rl? dihydropyrimidin3dcarbonyl, p3^razinylcarbonyl, thiazotylcarbon3?'l, oxazolinylcarbonyl, oxazolylcarbonyl, pyridazinyl-carbonyl, imidazolinylcarbonyl, imidazolylcarbonyl, pyxeizinylcarbonyl, thien3"lcarbon3^1, pyrrolylcarbonyl, furylcarbonyl or dihydrooxazinylcarbonyl group; and the "saturated or unsaturated monocyclic or bicyclic heterocyclic carbonylamino group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a morpholinylcarbon3?lamino, thiomorpholinylcarbonylamino piperazinylcarbonylamino, pyrrolidinyl-carbon37"lamino:, piperidinylcarbonylamino, hexahydroazepinylcarbonjd- amino, pyrrolinylcarbonylamino, imidazolidinylcarbonylamino, oxazolidirrylcarbonylamino, tetrahydropyxanylcarbonylamino, tetra- hydrofuranylcarbon34amino, dioxolanjdcarbonylamino, oxiran}'!- carbonylaxnino, p3Timidinylcarbon3damino, pyridylcarbonylamino, triazotyl- carbonylaxnino, , tetrazolylcarbonylamino, oxadiazolylcarbonylamino, dihydrop3^r imidinylcarbo^lamino, pyrazinylcarbonylarnino, thiazolyl- carbonylamino, oxazolinylcarbonylamino, oxazo Iylcarbon3rlamino, pyridazin^lcarbonylamino, imidazolinylcarbonylamino, iinidazolylcarbonyl-amino, pyrazin3dcarbon3^amino, thienylcarbonylamino, pyrrolylcarbonyl-amino, furylcarbon3damino or dihydrooxazinylcarbonylamino group. 5. The compound of claim 1> wherein R1 is a tiydrogen atom; an alkox3^cart>on3;rl group optionally substituted b3^ 1 to 5 substituents selected independently from cyano group, hydroxy group, carboxyl group, alkoxycar"bonyl group, alkoxy group (said alkox37 group is optionally substituted by 1 to 3 substituents selected independent^ from hydroxy group, amino group, mono- or di-alkylaraino group, halogen atom, carboxyl group, alkoxycarbonyl group, caxboxyalkoxy group and alkoxy car "bonylalkoxy group), alkylthio group, alkylsulfonyl group, alkenyl group, amino group, mono- or di-alkylamino group, tetrazofyl group, carbamoyl group, mono- or di-alkylcarbamoyl group (said mono- or di-alkylcarbamo3rl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group and alkoxycarbon34 group) , alkanoylaxnino group (said alkanoylamino group is optionally substituted b3^ 1 to 3 substituents selected independently from carbox34 group, alkoxycar"bon3rl group, hydroxy group and halogen atom), halogen atom, C3'cloalkyl group (said cycloalkyl group is optionalty substituted b3^ 1 to 3 substituents selected independently from Irydroxy groxip, amino : group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycar"bonyl group, carboxyalkyl group, alkox3?'carbonylalkyl group, carboxyaLkoxy group and alkoxycarbonylalkox3^ group), phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independent^ from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), morpholinyl group optionally substituted by oxo group, piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carbosyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), pyrrolidinyl group (said pyrrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkosycarbonylalkoxy group), and pyrimidinyl group (said pyrimidiiryl group is optionally substituted by 1 to 3 substituents selected independently from carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group); a carbamoyl group optionally substituted by alkoxy group; a dihydrooxazolyl group optionally substituted by 1 to 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; a dihydroimidazolyl group optionaUy substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; a dihydrooxazinyl group optionally substituted b}^ 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; mono- or di-alkylcarbamojd group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylainino group, morpholinjd group, pyridyl group, C3'cloalkyl group (said cycloaJLkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); an alkyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono-or di-alkylamino group, morphLolinyl group, pyridyl group, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from csrboxyl group, alkoxycarbonjd group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionalty substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); an alkanoyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxy^carbonjd group, alkoxy group, amino group, mono- or di-alkylamino group, morpholinyl group, pyridyl group, C3*cloalkyl group (said cycloaUkyl group is optionally substituted by 1 to 3 substituents selected independent^ from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbon3'l group, halogen atom, amino group and Itydroxy group); a morpholinylcarbonyl group ; a piperazinylcarbonyl group optionally substituted b}7" alkyl group, carboxyalkyl group or alkoxycarbon3'lalkyl group; a pyrrolidinylcarbon}^ group optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group; or a piperidinylcarbonyl grou.p optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbon}7! group, carboxyalkyl group and alkoxycarbonylalkyl group; R5 is a saturated or uxisaturated 5- to 8-membered heterocyclic group containing 1 to 4 hetero atoms selected independently from oxygen, sulfur and nitrogen atoms; wherein said heterocyclic group is substituted by 1 to 4 substituents selected from the following groups, or said heterocyclic gromp is substituted b3^ 1 to 4 substituents selected from the following groups along with a halogen atom, an oxo and/or hydroxy group: cyano group; nitro group; carboxyl group; sulfo group; cycloalkyl group optionally substituted b}^ carboxyl or alkoxycarbonyl group; C3-10 alkyl group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, tetrazolyl group, mono- or di-alkylcarbamoyl group, alkoxy group (said adkoxy group is optionally substituted by phenyl, carboxyl or hydroxy group), alkandyl group, alka_no3>loxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group optionally substituted by carboxyl or alkoxy group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, dioxolanyl group optionally substituted by alkyl group, pyrrolidinj^l group optionally substituted by alkcxxycarbonyl or carboxyl group, pyrrolidinyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperazinjd group optionally substituted by alkyl group, hexahydroazepinyl group, morpholinyl group, axid piperidinyloxy .group optionally substituted by alkyl group; alkenyl group optionally substituted by a group selected from cya^no group, hydroxy group, carboxyl group, benzyloxycarbonyl group, and tetrazolyl group; alkenyloxy group optionally substituted by carboxyl group; C3-10 alkoxy group; alkoxy group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, tetrazotyl group, carbamoyl group, mono- or di-alkylcarbamoyl group (said mono- or di-alkylcarbamoyl group is optionally substituted by carboxyl, alkoxycarbonyl or hydroxy group), alkoxy group (said alkoxy group is optionally substituted by carboxyl, formyl or hydroxy group), alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, aminosulfonyl group, amino group, mono- or di-alkylamino group substituted by carboxyl or alkoxy group, mono- or di-alkylsulfamojdamino group, mono- or di-alkylureido group optionally substituted by morplxolinyl group, cycloalkyl group optionally substituted by carboxyrnethyl group, oxiranyl group, phenyl group optionally substituted by alkoxy or carboxyl group, morpholinyl group, pyrrolidinyl group option-ally substituted by alkoxycarbonyl or carboxyl group, pyrrolidinyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, pyrrolidinyl group substituted by oxo group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidusyl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepinyl group, pyrimidinyl group, pyridyl group, dioxolanyl group optionally substituted by alkyl group, oxadiazofyl group optionalfy substituted, by ox:o group, oxathiadiazolyl group optionally substituted by oxo gro"up, pyrrolidinylcarbonyl group optionally substituted by carboxyl group, piperidinyloxy group optionally substituted by alkyl group, and morpholinylcarbonyl group; alkoxycarbonyl group optionally substituted by phenyl group; carbamoyl group; mono- or di-alkylcarbamo3>l group optionally substituted by a group selected from carboxyl group, morpholin3d group and alkoxy group; hj^droxycarbamimidoyl group; alkylthio group optionally substituted by a group selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamoyl group; alkylsulfinyl group; alkylsulfonyl group optionally'" substituted b}^ a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group and mono- or di- alkylcarbamoyl group; amino group; mono- or di-alkylamino group optionally substituted by a group selected from hydroxy group, carboxryl group, alkoxycarbonjd group, alkoxy group, mono- or di-alkylamino group and morpholinyl group; mono- or di-alkanoylamino group optionally substituted by a group selected from hydroxy group, alkoxy group, carboxyl group and amino group; mono- or di-alkylcarbamoylamino group optionally substituted by alkoxy group; morpholinjdcarbonylamino group; sulfamoyl group; mono- or di-alkylsulfamoyl group; alkanoyl group optionally substituted by a group selected from hydroxy group, carboxyl group, alkoxycarbcmyl group, alkoxy group, mono- or di-alkylamino group and morpholinyl group; or a group selected from the following groups: wherein X1 and X^ are independently CH2, NH, 0, S, SO or SO2; X^ and X5 are independently CH2, O, S, SO or S02; X* is NH, O, S, SO or S02; and n, o, p, q and r are independently an integer of 1 to 4, wherein each group of the above formuLa is optionally substituted by a substituent(s) selected from the following groups: carboxyl group, hydroxy group, cya.no group, oxo group, alkyl group, ■ hydroxyalkyl group, alkoxycarbonylalkyl group, carboxyalkyl group, morpholnrylalkyl group, phenylalkyl group, alkanoj^l group, hydroxyalkanoyl group, alkoxyslkanoyl group, alkoxy group, phenylalkoxy group, alkoxycarbonyl group, benayloxycarbonyl group, mono- or di-alkylamino group, mono- or di-alkylcarbamoyl group, mono- or di-alkylsulfamoyl group, alkylsulfonyl group and tetrazolyl group; R6, R7, R8 and R9 are independently a Itydrogen atom, a halogen atom, a hydroxy group, a nitro group, a cyano group, an alkyl group, an alkoxy group, or a mono- or di-alkylamino group, wherein said alkyl, alkoxy and mono- or di-alkylamino groups are optionally substituted by 1 to 6 substituents selected independently from halogen atom, hydroxy group, alkoxy group, alkylthio group, amino group, nitro group, c}^ano group, oxo group, carboxyl group, alkoxycaxbonyl group and mono- or di-alkylamino group; or R6 and R7, or R7 and R8, or R8 and R9 may combine at the ends to form an alkylene group which alkylene group may contain 1 to 3 heteroatoms selected independently from nitrogen, sulfur and o?cygen atoms; and R10 is an aromatic monocyclic ring optionally containing 1 to 3 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms; wherein the monocyclic aromatic ring is optionally substituted by 1 to 4 substituents selected independently from lialogen atom, carboxyl group, alkoxycarbonjd group, carbamoyl group, mono- or di-alkylcarbamoji. group, alkyl group, alkoxy group, hydroxy group, nitro group, cyano group, amino group, mono- or di-alkylamino group, alkanoyl group, alkylthio group, tetrazolji. group- and dihydrooxazolyl group, wherein the alkyl, alkoxy, mono- or di-alkylamino, mono- or di-alkylcarbamoyl, alkanoyl and alkylthio groups are optionally substituted by a substituent(s) selected independently from halogen atom, and hydroxy, alkoxy, amino, morpholinyl, piperidinyl, pyrrolidinyl, piperazinyl, alkylpiperazinyl and alkanoylpiperazinyl groups. 6. The compound of claim 5, wherein ttie "aromatic monocyclic ring optionally containing 1 to 3 heteroatoms sele cted independently from oxygen, sulfur and nitrogen atoms" is a phenyl gxoup, a pyridyl group, a pyrimidinyl group, a furyl group or a thienly group; and the "saturated or unsaturated' 5- to 8-membered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms" is a pyrimidinyl group, a pyridyl group, a triazolyl group, a tetrazolyl group, a oxadiazolyl group, a dihydropyrimidinyl group, a pyrazinyl group, a thiazolyl group, an oxazolyl gro~u.p, an imidazolyl group, a dihydrooxazin}^ group, a dihydropyrazmyl group or a pyrazolyl group. 7. The compound of claim 6, wherein Rx is a Irydrogen atom; an alkoxycarbonyl group optionally substituted by 1 to 5 siabstituents selected independently from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted, by l.to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), alkylthio group, alkylsulfonyl group, alkenyl group, amino group, mono- or di-alkylamino group, tetrazolyl group, carbamoyl group, mono- or di-alkylcarbamoyl group (said mono- or di-alkylcarbamoyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group and alkoxycarbonyl group) , alkanoylamino group (said alkanoylamino group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, hydroxy group and halogen atom), halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy giroup, amino group, mono- or di-alkylamino group, halogen atom, oxo groxip; carboxyl group, alkoxycaxbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group) „ phenyl group (said phenyl group is optionally substituted b}' 1 to 3 suibstituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), morpholinyl group optionally substituted by oxo group, piperidinyl group (said piperidinyl garoup is optionally substituted by 1 to 3 substituents selected independent^ from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, cjarboxyalkyl group, alkoxycarbonylalkyl group and carboxyalkoxy group, alkoxycarbonylaikoxy group), pyrrolidinyl group (said pyrrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from Ixydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkosy group), and pyrimidinyl group (said pyrimidinyl group is optionally substituted by 1 to 3 substituents selected independently from earboxyalkyl group, alkoxycarbonylalkyl group and carboxyalkoxy group, slkoxycarbonjdalkoxy group); dihydrooxazotyl group optionally substituted toy 1 to 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; or a mono- or di-alkylcarbamoyl group optiorrally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylamino group, morpholinyl group, pyridyl group, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl gxoup, alkoxycarbonyl group, halogen atom, amino group and hydroxy gromp) and phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); R2 is an alkyl group; R3 is a hydrogen atom; R4 is an alkylene group; R5 is a heterocyclic group selected from pyrimidinyl group, pjoidyl group, triazolyl group, tetrazolyl group, oxadiazolyl group, dihydropyrimidinyl group, p3'razin3'l group, thiazolyl group, oxazolyl groxip, imidazolyl group, dihydrooxazinyl group, pyrazolyl group and dihrydropyrazinyl group, wherein said heterocyclic group is substituted b3^ 1 to 4 substituents selected from the following groups, or 1 to 4 substituents selected from the following groups and oxo group: cj^ano group; nitro group; carboxyl group; sulfo group; C3-10 alkyl group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group , tetrazolyl group, mono- or di-alkylcarbamoyl group, alkoxy group (ssid alkoxy group is optionally substituted by phenyl, carboxyl or hydroxy group), alkano3rloxy group, alkylthio group, alkylsulfonyl group, aUkylsulfinyl group, amino group, mono- or di-alkylamino group optionally substituted by carboxyl or alkoxy group, mono- or di- alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholin3rl group, oxiranyl group, dioxolanyl group optionally substituted by alkyl group, pjirolidinyl group optionally substituted by alkox3'carbonyl or carboxyl group, pjOToliddnyl group optionally substituted by alkoxycarbonjdalkyl or carboxyaUkyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycairbonjdalkyl or carboxyalkyl group, piperazinyl group optionally subs-tituted by alkyl group, hexahydroazepinyl group, morpholinyl giroup, and piperidinjdoxy group optionally substituted by alkyl group; alkenyl group optionally substituted by a group selected from cyano group, hydroxy group, carboxyl group, benzyloxycarbonyl group, and tetrazofyl group; alkenyloxy group optionally substituted b3^ carbox37l group; C3-10 alkoxy group; alkoxy group substituted by a group selected from halogen atom, cyano group, trydroxy group, carboxyl group, alkoxycarbo nyl group, tetrazolyl group, carbamo3rl group, mono- or di-alkylcarbarxioyl group optionally substituted by hydroxy group, alkoxy group optionally substituted by carboxyl or hydroxy group, alkanoyloxy group, alkylthio group, alk3dsulfon3^1 group, alkylsulfinyl group, aminosulfonyl group, amino group, mono- or di-alkylamino group substituted by cazrboxyl or alkoxy group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, C3'cloalkyl group optionally substituted by carboxymethyl group, oxiranyl group, phenyl group optionally substituted by a_lkoxy or . carboxyl group, morpholinyl group, pyrrolidinyl group o ptionalfy substituted by alkoxycarbonyl or carboxyl group, pyrrolidin/yl group optionally substituted by alkoxycarbonylalkyl or carboxyalkyl group, pyrrolidinyl group substituted by oxo group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl. group optionally substituted by alkoxycarbonylalkyl or carfc>oxyalkyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepinyl group, pyrimidkiyl group, pyridyl group, dioxolanyl group optionally substituted by alkyl group, oxadiazolyl group optionally substituted by oxo group, oxathiadiazofyl group optionally substituted by oxo group, pyrrolidinylcarbonyl group optionally substituted by carboxjd group, piperidinyloxy group optionally substituted by alkyl group, and morpholmylcarbonyl group; alkoxycarbonyl group optionally substituted by phenyl group; carbamoyl group; mono- or di-alkylcarbamoyl group optionally substituted by a group selected from carboxyl group, morpholinyl group and alkoxy grroup; hydroxycarbamimidoyl group; alkylthio group optionally substituted by a group selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamo^l group; alkylsulfinyl group; alkylsulfonyl group optionalty substituted by a group selected from hydroxy group, carboxyl group and mono- or di-alkylcarbamoyl group; amino group; mono- or di-allcylamino group optionally substituted by a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group and morpholinyl group; alkanoylamino group optionally substituted by a group selected from hydroxy group, alkoxy group, carboxyl group and amino group; mono- or di-alkylureido group optional substituted b}^ alkoxy gromp; morpholinylcarbonjdamino group; sulfamoyl group; mono- or di-alkylsulfamoyl group; morpholinjd group optionally substituted by a group selected from oxo group and carboxyl group; optionally oxidized thiomorpholinyl group; piperazinyl group optionally substituted by a group selected from c}'ano group, alkyl group, hydroxyalkyl group, alkoxycarbonylslkyl group, carboxyalkyl group, alkanoyl group, hydroxyalkano}^ group, alkoxyalkanoyl group, benzyloxycarbonyl group, mono- or di-alkyl-carbamoyl group, mono- or di-alkylsulfamoyl group, alkylsulfonyl group and tetrazolyl group; piperidinyl group optionally substituted by a group selected from carboxyl group, bydroxy group, oxo group, alkyl group, hydroxyalkyl group, carboxj^alkyl group, alkanoyl group, alkoxy group, phenylaltcoxy group, alkox}rcarbon37l group and alkoxycarbo^'lalkyl group; pyrrolidinyl group optionally substituted by a group selected from oxo group, carboxyl group, alkano}^ group and mono- or di-alkylannino group; . pj^rrolinyl group optionally substituted by oxo group; hexahydrodiazepuiyl group optionally substituted by alkanoyl group; diazolidinyl group optionally substituted by oxo group; dioxolanyl group optionally substituted by alkyl group; pyridyl group optionally substituted by carboxyl group, hydroxy group or hydroxyalkyl group (said pyridyl group is optionally further oxidized); tetrazolyl group substituted by hydroxy group or alkyl group that is optionally substituted by morpholinyl group; dihydrooxadiazolyl group optionally substituted by oxo group; dihydroimidazolyl group; dihydrooxazolyl group; oxazolidinyl group optionally substituted by oxo group; tetrahydropyridyl group optionally substituted by benzyl group; pyrimidinj^l group; tetrahydropyranyl group; piperidinyloxy group optionally substituted by a group selected from alkyl group, carboxyl group, carboxyalkyl group and alkano3rl group; pyrrolidinyloxy group optionally substituted by a group selected from alkyl group, carboxyl group, carboxyalkyl group and alkanoyl group; * tetrahydropyranyloxy group; tetrahydrofuranyloxy group; optionally oxidized thianyloxy group; morpholinylcarbonyl group; piperazinylcarbonyl group optionally substituted by a group selected from alkanoyl group and alkyl group; and pyrrolidinylcarbonyl group; . R6 and R9 each are a itydrogen atom; R7 and R8 are independently a hydrogen atom, an alkyl group optionally substituted by halogen atom, an alkoxy group, a mono- or di-alkylamino group or halogen atom; or R7 and R8 combine at the ends to form an alkylenedioxy group; and Ri° is a phenyl or pyridyl group, which phenyl or pyridyl group is optionally substituted by 1 to 4 substituents selected from alkyl group optionally substituted by halogen atom, alkoxy group, hydroxy group, halogen atom, C3^ano group, amino group and mono- or di-alkylamino group. 8. The compound of claim 7, wherein R1 is an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independently from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group and alkoxycarbonyl group), alkenyl group, halogen atom, cycloalkyl group (said cj^cloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydrosy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), piperidinyl group (said piperidin}^ group is optionally substituted b\^ 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), and P3rrrolidinyl group (said pyrrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group); or a dihydrooxazolyl group optionally substituted b}' 1 or 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; R5 is a pyrimidinyl group, a pyridyl group, a triazolyl group, a tetrazolyl group, an oxadiazolyl group, a dihydropyrimidinyl group, a pyrazinyl group, a thiazolyl group, an oxazolyl group, a dibydrooxazinyl group, a pyrazolyl group or a dihj'dropyrazinyl group, said group being substituted by 1 to 4 substituents selected from the following groups: cyano group; nitro group; carboxyl group; sulfo group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group optionally substituted by carboxyl or hydroxy group, alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, aminp group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by alkoxycarbon3rl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperazinyl group optionally substituted by alkyl group, hexahr^droazepinyl group and morpholinyl group; alkenyl group optionally substituted by carboxyl group, cyano group or . benzyloxycarbonyl group; alkoxy group substituted bj^ a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group optionally substituted by carboxyl or hydroxy group, alkano3'loxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinjd group optionally substituted by alkoxycarbonyl or carboxyl group, piperazinyl group optionally substituted b3' alkyl group, hexahydroazepinyl group and morpholinyl group; alkoxycarbonyl group optionally substituted by phenyl group; mono- or di-alkylcarbamoyl group optionally substituted by carboxyl group; hydroxycarbamimidoyl group; alkylthio group; alkylsulfonyl group optionally substituted by carboxyl group; mono- or di-alkylamino group optionally substituted by hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group or morpholinyl group; mono- or di-alkylsulfamoyl group; morpholinyl group; optionally oxidized thiomorpholinyl group; piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; piperidinyl group optionally substituted by a group selected from carboxyl group, alkyl group and alkoxycarbonyl group; dioxolanyl group optionally substituted by alkyl group; tetrazolyl group optionally substituted by alkyl group, hydroxyalkyl group or morpholinylalkyl group; dihydrooxadiazolyl group optionally substituted by oxo group; pyrimidinyl group; or tetrahydropyranyl group; and R10 is a phenyl or pyridyl group, which phenyl or pyridyl group is optionally substituted by 1 to 4 substituents selected from alkyl group optionally substituted by halogen atom, alkoxy group, Itydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. 9. The compound of claim 1, wherein R1 is a hydrogen atom; an alkoxycarbonyl group optionally substituted by 1 to 5 substituents selected independently from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), alkylthio group, alkylsulfonyl group, alkenyl group, amino group, mono- or di-alkylamino group, tetrazolyl group, carbamoyl group, mono- or di-alkylcarbamoyl group (said mono- or di-alkylcarbamoyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyl group and alkoxycarbonyl group) , alkanoylamino group (said alkanoylamino group is optionally substituted by 1 to 3 substituents selected independently . from carboxyl group, alkoxycarbonyl group, hydroxy group and halogen atom), halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), phenyl group (said phenyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonylalkoxy group), morpholinyl group optionally substituted by oxo group, piperidinyl group (said piperidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group and carboxyalkoxy group, alkoxycarbonylalkoxy group), pyrrolidinyl group (said p3>rrolidinyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group,-amino group, mono- or di-alkylamino group, halogen atom, oxo group, carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group, carboxyalkoxy group and alkoxycarbonj'lalkoxy group), and pyrimidinyl group (said pj^rimidinyl group is optionally substituted by 1 to 3 substituents selected independently from carboxyalkyl group, alkoxycarbonylalkyl group and carboxyalkoxy group, alkoxycarbonjdalkoxy group); dihydrooxazolyl group optionally substituted b}r 1 to 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, alkyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hj^droxyalkyl group; or a mono- or di-alkylcarbamoyl group optionally substituted by 1 to 5 substituents selected independently from halogen atom, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, amino group, mono- or di-alkylamino group, morpholinyl group, pyridyl group, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independent^ from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group) and phen3*l group (said pherryl group is optionally substituted by 1 to 3 substituents selected independent^ from carboxyl group, alkoxycarbonyl group, halogen atom, amino group and hydroxy group); R2 is an alkyl group; R3is a hydrogen atom; R4 is an alkylene group; R5 is a group of the formula: wherein Ring A is a saturated or unsaturated 5- to 8-membered heterocyclic group containing 1 to 4 heteroatoms selected independently from oxygen, sulfur and nitrogen atoms, R11 is a group selected from the following groups: cyano group; nitro group; carboxyl group; sulfo group; alkyl group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarboryl group, alkoxy group (said alkoxy group is optionally substituted by phenyl, hydroxy or. carboxyl group), alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, -di-alkyldioxolanyl group, p3>rrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbon}?! or carboxyl group, piperazinyl group optionally substituted by alkyl group, hexahydroazepinyl group and morpholinyl group; alkenyl group optionally substituted by carboxyl group, cyano group or benzyloxycarbonyl group; alkoxy group substituted by a group selected from halogen atom, cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by phenyl, hydroxy or carboxyl group), alkanoyloxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted bj^ morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperidinyl group optionally substituted by alkoxycarbonyl or carboxyl group, piperazinyl group optional!}' substituted by alkyl group, hexahydroazepinyl group and morpholinyl group; alkoxycarbonyl group optionally substituted by phen}'! group; mono- or di-alkylcarbamoyl group optionally substituted bj^ carboxyl group; hydroxycarbamimidoyl group; alkylthio group; . alkylsulflnyl group; alkylsulfonyl group optionally substituted by carboxyl group; mono- or di-alkylamino group optionally substituted by hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, mono- or di-alkylamino group or morpholinyl group; mono- or di-alkylsulfamoyl group; morpholinjd group; optionally oxidized thiomorpholinjd group; piperazinyl group optionally substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; pyrrolidinyl group optionally substituted by carboxyl group, carboxyalkyl group, alkyl group, alkoxycarbonyl group or alkoxycarbonylalkyl group; piperidkryi group optionally substituted by carboxyl group, carboxyalkyl group, alkyl group, alkoxycarbonyl group or alkoxycarbonylalkyl group; dioxolanyl group optionally substituted by alkyl group; tetrazolyl group optionally substituted by alkyl group, hydroxyalkyl group or morpholinylalkyl group; dihydrooxadiazolyl group optionally substituted b}-7 oxo group; pyrxmidinyl group; or tetrahydropyranjd group; R6 and R9 each are a hydrogen atom; R7 and R8 are independently a hydrogen atom, an alkyl group optionally sbustituted by halogen atom, alkoxy group, or mono- or di-alkylamino group; or combine at the ends to form an alkylenedioxy group; and R10 is a phenyl or pyridj'l group, which phenyl or pyridyl group is optionally substituted by 1 to 4 substituents selected from alkyl group optionally substiuted by halogen atom, alkoxy group, hydroxy group, halogen atom, cyano group, amino group and mono- or di-alkylamino group. 10. The compound of claim 9, wherein Ring A is a pyrimidinyl group, a pyridyl group, a triazolyl group, a tetrazolyl group, an oxadiazolyl group, a dihydropyrimidinyl group, a pyrazinyl group, a thiazolyl group, an oxazolyl group, a dihydrooxazinyl group, an imidazolyl group, a pyrazofyl group, or a dihydrop3'razin3'l group. 11. The compound of claim 10, wherein Ring A is a pyrimidinyl group, a pyridyl group, a tetrazolyl group, an oxadiazolyl group, a pyrazinyl group, a thiazolyl group or an oxazolyl group; and R11 is a carboxyl group; a cyano group; a nitro group; an alkyl group substituted b3' a group selected from hydroxy group, cyano group, carbox3^1 group, alkoxycarbon3d group, alkoxy group, phenylalkoxy group, hydroxyalkoxy group, carboxyalkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by carboxyl group, piperidinyl group optionally substituted by carboxyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted by a group selected from hydroxy group, cyano group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, hydroxyalkoxy group, carboxyalkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono-• or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholi^l group, oxiranyl group, di-alkyldioxolanyl group, pyrrolidinyl group optionally substituted by carboxyl group, piperidinyl group optionally substituted by carboxyl group, piperazinyl group optionally substituted b3' alkyl group and morpholinyl group; an alkoxycarbonyl group; a h3>"droxycarbamiinidoyl group; alkylthio group; an alkylsulfonyl group optionally substituted by carboxyl group; a mono- or di-alkylamino group optionally substituted by hydroxy group, carboxyl group, alkoxy group or mono- or di-alkylamino group; a morpholinyl group; an optionally oxidized thiomorpholinyl group; a piperazinyl group optional!}' substituted b}' a group selected from alkyl group, alkano3^1 group and hydroxyalkanoyl group; a pyrrolidinyl group optionally substituted by carboxyl group, alkyl group carboxyalkyl group or alkoxycarbonyl group; a piperidinyl group optionally substituted by carboxyl group, alkyl group, carboxyalkyl group or alkoxycarbonyl group; a tetrazolyl group optionally substituted by alkyl group, hydroxyalkyl group, or morpholkrylalkyl group; an oxodihydrooxadiazolyl group; a pyrimidinyl group; or a tetrahydropyranyl group. 12. The compound of claim 11, wherein R1 is an alkoxycarbonyl group optionally substituted b3' 1 to 5 substituents selected independent^ from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group (said alkoxy group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group and alkoxycarbonyl group), alken}'! group, halogen atom, cycloalkyl group (said cycloalkyl group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), phenyl group (said phenyi group is optionally substituted by 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxy carbonjdalkyl group), piperidinyl group (said piperidinyl group is optionally substituted bj' 1 to 3 substituents selected independently from hydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbonylalkyl group), and pj'rrolidinyl group (said pyrrolidhryl group is optionally substituted by 1 to 3 substituents selected independently from Irydroxy group, halogen atom, carboxyl group, alkoxycarbonyl group, carboxyalkyl group and alkoxycarbon}4alkyl group); or a dihydrooxazolyl group optionally substituted by 1 or 2 substituents selected independently from carboxyl group, alkoxycarbonyl group, carboxyalkyl group, alkoxycarbonylalkyl group and hydroxyalkyl group; 1 Rao is a phenyl group substituted by 1 to 3 substituents selected from alkyl group optionally substituted b3' halogen atom, alkoxy group, halogen atom and cyano group; Ring A is a pyrimidinyl group, a pyridyl group, a tetrazolyl group, an oxadiazofyl group or a thiazolyl group; and Rn is a carboxyl group; a cyano group; a nitro group; an alkyl group substituted by a group selected from hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, carboxyalkoxy group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group,"mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionally substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted by a group selected from cyano group, hydroxy group, carboxyl group, alkoxycarbonyl group, alkoxy group, phenylalkoxy group, carboxyalkoxy" group, alkylthio group, alkylsulfonyl group, alkylsulfinyl group, amino group, mono- or di-alkylamino group, mono- or di-alkylsulfamoylamino group, mono- or di-alkylureido group optionalfy substituted by morpholinyl group, oxiranyl group, di-alkyldioxolanyl group, piperazinyl group optionally substituted by alkyl group and morpholinyl group; a hydroxycarbamimidoyl group; an alkylthio group; an alkylsulfonyl group optionally substituted b}' alkoxycarbonyl group; a mono-v or di-alkylamino group optionally substituted by hydroxy group, carboxyl group or alkoxy group; a morpholinyl group; optionally oxidized thiomorpholutyl group; a piperazinyl group optionalty substituted by a group selected from alkyl group, alkanoyl group and hydroxyalkanoyl group; a pyrrolidinyl group optionally substituted by carboxyl group, alkyl group carboxyalkyl group or alkoxycarbonyl group; a piperidinyl group optionally substituted by carboxyl group, alkyl group, carboxyalkyl group or alkoxycarbonyl group; a tetrazolyl group optionally substituted b}' alkyl group, hydroxy alkyl group, or morpholinylalkyl group; an oxodihydrooxadiazolyl group; a pjaimidktyl group; or a tetrahydropj^ranyl group. 13. The compound of claim 12, wherein R1 is an alkoxycarbonyl group optionally substituted by 1 or 5 substituents selected independently from carboxyl group, alkoxycarbonyl group, halogen atom, hydroxy group and cycloalkyl group; R10 is a phenyl group substituted by 1 to 3 substituents selected from cyano group, alkyl group optionally substituted b}" halogen atom and alkoxy group; Ring A is a pyrimidinyl group, a pyridyl group, a tetrazofyl group or an oxadiazolyl group; R11 is a carboxyl group; an alkyl group substituted by hydroxy group, carboxyl group, alkoxy group or alkylsulfonyl group; an alkenyl group optionally substituted by carboxyl group; an alkoxy group substituted bj' carboxyl group, cyano group, hydroxy group, alkoxy group, alkylthio group or alkylsulfonj^l group; a mono- or di-alkylamino group optionally substituted by carboxyl group or alkoxy group; a morpholinyl group; a piperidinyl group substituted by carboxyl group; or a tetrazolyl group substituted by hydroxyalkyl group; R7 is an alkyl group optional^ sbustituted b}' halogen atom, alkoxy group, or mono- or di-alkylamino group; and R8 is a hydrogen atom. 14. The compound of claim 13, wherein R1 is an ethoxycarbonyl group, a trfdroxyethoxycarbonyl group, a 2-fluoroethoxycarbonyl group, a 2,2-difluoroethoxycarbonyl group or a 2,2,2-trifluoroethoxycarbonyl group; R2 is an ethyl group; Rio is a phenyl group substituted by 1 to 2 substituents selected from cyano group, trifluoromethyl group and methoxy group; and R7 is a trifluoromethyl group or a methoxy group. 15. The compound of claim 13, wherein R1 is a carboxy(C2- ioalkoxy)carbonyl group or an aIkoxycarbonyl(C2-ioalkoxy)carbonyl group; R2 is an ethyl group; R10 is a phenyl group substituted by 1 to 2 substituents selected from cyano group, trifluoromethyl group and methoxy group; and R7 is a trifluoromethyl group or a methoxy group. 16. A compound selected from the following compounds or a pharmaceutically acceptable salt thereof. (2R,4S)-4-{[3,5-Bis(trifluoromefo^ yl]}ainino-2 -ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester; (2R,4S)-4-[[3,5-Bis(trffluorome1h^ amino}pyrimidin-2-yl)]amino-2-ethyl"6-trifluoromethyl-3,4-dihydro-2H- quinoline-1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben2yl]-[5-(2-metho^etho^)p5n±nidin- 2-yl]}amino-2-ethyl-6"trifluoromethyl-3,4-dihydro-2H-quinoline-l- carboxylic acid ethyl ester; (2R?4S)-4-{[3,5-Bis(trifluoromet3^^ 2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline»l-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(2-carboxyethyl)pyrimidin-2- yl]}amino-2-ethyl-6-txifluorometJiyl-3,4-dih3^dro-2H-quinoline-l-carboxylic acid ethyl ester; (2R,4S)-4-([3,5-Bis(trifluoromethyl)ben2yl]-{5-[2-(2.hydroxyethyl)-2H- tetrazol-5-yl]p3^riinidin-2-yl})amino-2-ethyl-6-trifluoromethyl-3,4-dihydro- 2H-quinoline-l -carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl^ yl]}ainino-2-eth3d-6-rnethox3^-3,4-dihydro-2H-qiiinoline-l»carboxylic acid ethyl ester; (2R,4S)-4-{(3,5-Dimethoxybenzyl)-[5-(m 2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester; (2Rr4S)-4-{(3,5-Dicyajaobenzyl)-[5-(morpholin-4-yl)pyrimidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2R?4S)-4-{(3-Cyanobenz}4)-[5-(morpholin-4-yl)pyrimidin-2-3d]}amino-2-ethyl-6-trifluorometh3d-3J4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2^4S*)-4-([3,5-Bis(trffluorome tetrazol-5-34]pyrimidin-2-yl})amino-2-ethyl-6-methox3^3>4-dih3^dro-2H-quinoline-1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trinuorometh3d)benz34]-[2-(2-hydroxyethyl)-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluorornethyl-3?4-dihydro-2H-quinoline-l-carboxylic acid eth3^1 ester; (2R?4S)-4-{[3,5-Bis(trifluorornethyl)benz34]-[2-(2-methanesulphonylethyl)-2H-tetrazol-5-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ettryl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(inorpholin-4-yl)pyrimidin-2-yl]}ainino-2-ethyl-6-trifluoroinethyl-3?4-dihydro-2H-quinoline-l-carbox3^1ic acid ethyl ester; (2R*?4S*)-4-{[3,5-Bis(1xifluoromethyl)benzyl]-[5-(morpholin-4-yl)pyrimidin 2-3d]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-h3'drox3>"ettiyl ester; (2R,4S)-4-{[3?5-Bis(trifluorornethyl)benzyl]-[5-(4-carboxypyperidin-l-3d)pyrimidin-2-yl]}amino-2-ethyl-6-methoxy-3,4-dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorometh34benzyl)-[5-(2-carboxyethyl)pyrimidin-2-3r'l]}amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-l- carboxylic acid ethyl ester; (2R,4S)-4-[[3,5-Bis(1xinuoro amino}pyrirnidin-2-3d)]ainino-2-ethyl-6-trifluororne1±iyl-3,4-dA quinoline-1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^l3-[5-(3-carboxypropoxy)p3?'rimidin- 2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid ethyl ester; (2R,4S)-4-([3?5-Bis(trifluoromethyl)benzyl]-{5-[3-(tetrazol-5-yl)- propoxy]pyrimidin-2-yl})amino-2-ethyl-6-triiluoromethyl-3,4-dihydro-2H- quinoline-1-carboxjdic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromet±^ 2-yl]}arnino-2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H-quinoline-l- carboxylic acid ethyl ester; (2R,4S)-4-{[3?5-Bis(txifluoromethy pyriinidin-2-yl]}ainino-2-ethyl-6-trifluorome1iiyl-3?4-dih 1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoroinethyl)benzyl]-[5-(2-carboxyethoxy)pyrirnidin-2- yl]}aniino-2-ethyl-6-trifluorornethyl-3,4-dihydro-2H-quinoline-l-caTbo^y-lic acid ethyl ester; (2R,4S)-4-{[3»5-Bis(1xifluoromethyl)benzyl]-[5-(4-carboxymethylpyperidin-l- yl)p3^rimidin-2-yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H- quinoline-l-carboxj^lic acid ethyl ester; (2R?4S)-4-{[3?5»Bis(trifluororneth3d)benzyl]-[5-(3-carboxypropoxy)pyridin-2- yll}ainino-2-ethyl-6-trifluoromethyl-3,4--dihydro-2H-quinoline-l-carboxylic acid ethyl ester; (2R,4S)-44[3,5-Bis(trifluoromethyl)ben^ 34]}ajTiino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-l-carbox3^1ic acid ethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethjdbenzyl)-[5-(4-carboxybutoxy}- pyrimidin-2-yl]}amino-2-ethyl-6-tr^ 1-carboxylic acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh3rl)benzyl]-[5-(3-carbox5^propo^)pyriinidin- 2-yl]}amino-2-eth3d-6-methox5^-3,4-dih\^dro-2H-quinoline-l-caTbo^ acid ethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benz34]-[5-(3-carboxypropoxy)pyrirnidin- 2-34]}amino-2-ethyl-6-dimethylainino-3,4-dihydro-2H-quinoline-l- carboxjdic acid ethyl ester; (2R?4S)-4-{[3,5-Bis(trmuoromethyl)benzyl]-[5-(4-carbox3^pyperidin-l- 3^)pyrimidin-2-yl]}amino-2-ethyl-6-trifluoroinethyl-3,4-dihydro-2H- quinoline-1-carboxylic acid 2,2,2-trifLuoroethyl ester; (2R>4S)-4-{[3,5-Bis(trifluorometh3^1)benzyl]-[5-(4-carboxyp3^eridin-l- yl)pyriinidin-2-yl]}ainino-2-ethyl-6-trifluorome1±Lyl-3?4-dihydro-2H quinoline-1-carboxtlic acid ethyl ester; (2R?4S)-4-{[3,5-Bis(trifluorometh3d)benzyl]-[5-(3-carboxypropoxy)p3rrirnidin- 2-yl]}ainino-2-ethyl-6-iTifluorornethyl-3J4-dihydro-2H-quinoline-l- carboxylic acid 2,2,2-trifluoroeth34 ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(3- carboxypropoxy)pyrimidin-2-3d]}arnino-2-ethyl-6-trifluorornethyl-3,4- dihydro-2H-quinoline-l-carboxylic acid 2,2,2-trifluoroethyl ester; (2R?4S)-4-{[3J5-Bis(trifluoromethyl)benzyl]-[5-(4-carboxypyperidin-l- yl)pyrimidin-2-yI]}amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H- quinoline-1-carboxylic acid 2-hydrox3'rethyl ester; (2R,4S)-4-{[3,5-Bis(trffluoromethyl)benzyl]-[5-(morpholin-4-34)pyrimidin-2- yl]}ajnino-2-eth3^1-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-carboxyethyl ester; (2RJ4S)-4-{[3,5-Bis(trifluorometh34)benzyl]-[5-(morpholin-4-yl)p3^rimidin-2- yl]}amino-2-ethyl-6-trifluorornethyl-3J4-dihydro-2H-quinoline--l-carboxylic acid 3-carbox3^prop34 ester; (2R,4S)-4-{[3,5-Bis(trffluorometh^ 3'l]}amino-2-ethyl-6-trifluorom acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carboxylic acid 2-carboxy-2~methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(morpholin-4-3d)p3Timidin-2- yl]}ajxiino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoUne-l-caxbox3^1ic acid 5-carbox3'pentyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^ 2-yl]}amino-2-ethyl-6»trifluorometiiyl-3,4-dJJaydro-2H-quinoUne-l- carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benzy^ 2-yl]}amino-2-eth3;"l-6-trifluorometh3^1-3,4-dihydro-2H-quinoline-1 - carboxylic acid 5-carboxypentyl ester; (2RJ4S)-4-{[3,5-Bis(trifluorometh3d)benzyl]-[5-(2-methox3-Tethox3r)p3^rimidm^ 2-yl]}ainino-2-eth3^-6-trifluorornethyl-3,4-dihydro-2H-quinoline-l- carboxjdic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)^^ 2-3d]}amino-2-ethyl-6-trifluoromethyl-3 f4-dihydro-2H-quinoline-1 - carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben2yl]-[5-(2-methoxyetihoxj^pyrm^ 2-yl]}amino-2-ethyl-6-tri£luoroinethyl-3>4-dihydro-2H-quinoline-l- carboxylic acid 4~carbox3>"butyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh3d)ben2yl]-[5-(3-cyariopropoxy)pyrimidin-2- 3d]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-carbox3'ethyl ester; and (2R,4S)-4-{[3f5-Bis(trifluorofhethyl)benzyl]-(5-dimet±iylaminopyrimidin-2 3d)}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-carboxyeth3'l ester. 17. A compound selected from the following compounds or a pharmaceutically acceptable salt thereof. (2R,4S)-4-{[3,5-Bis(trifluorom 2-yl]}amino-2-ethyl-6-trifluorometh^^ carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl^ 2-yl]}araino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l- carboxylic acid 4-carbox3>-butyl ester; (2R,4S)-4-{[3,5-Bis(triftuoromethyl)ben^^^^ 2-yl]}amino-2-ethyl-6-trifluoromethyl-354-dihydro-2H-quinoline-l- carboxylic acid 2-carboxy-2-methylpropyl ester; (2R?4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(2-methoxyethoxy)pyrimidin 2-yl]}ainino-2-ethyl-6-trifluoromethyl-3>4-dihydro-2H-quinoline-l- carboxylic acid 2-carboxy-2-methylprop3'l ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)benz34]-[5-(2-methoxyetho^)p3rrimidin- 2-yl]}ainino-2-ethyl-6-trifluoromethyl-3!4-dihydro-2H-quinoline-l- carboxylic acid 5-carboxypentyl ester; (2R,4S)-4-{[3?5-Bis(trifluoromethyl)benzyl]-[5-(3-cyanopropoxy)pyrimidin-2- yl]}aniino-2-eth3d-6-trifluorometh3'l-3,4-dihydro-2H-quinoline-l-carboxylic acid 3-carboxyprop34 ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^]-[5-(3-cyauiopropo3^)pyrimidin-2- yl]}amino-2-eth34-6-trifluorometh34-3,^ acid 4-carboxybutyl ester; (2R?4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(3-cyanopropoxy)pyrimidin-2- yl]}amino-2-e1±L3d-6-trifluoromethyl-3J4-dihydro-2H-quinoline-l-carboxylic acid 2-carbox3^-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben2^d]-[5-(3-cyanopropoxy)pyrimidin-2- yl]}amino-2-ethyl-6-trifluororneth34-3,4-dihydro-2H-quinoline-l-carboxylic acid 5-carbox3;ipentyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh3^)benzyl]-(5-dimethylaminopyrirnidin- yl)}ajxiino-2-eth3d-6-trifluoromethyl-3J4-dihydro-2H-quinoline-l-carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(trifluorom yl)}amino-2-ethyl-6-trifluoromethyl-3^ acid 4-carboxybutyl ester; (2R,4S)~4-{[3,5-Bis(trifluoromethyl)ben^ yl)}amino-2-ethyl-6-trifluoromethyl-3,4-dihfcydro-2H-quinoline-l-carbox5dic acid 2-carboxy-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluorome1Jiyl)ben2yl]-(5-dime&ylaininopyrirnidin-2- 3d)}amino-2-et±i3d-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 5-carboxypentyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylben^ 2-yl]}ainino-2-e1iiyl-6-tTifluorome1±i34-3?4-dihydro-2H-quinoline-1 - carboxylic acid 2-carbox3^ethyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethyfo^ 2-yl]}amino-2-etoyl-6-trifluororneth3?'l-3?4-dihydro-2H-quinoline-l- carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorornethylbenzyl)-[5-(morpholin-4-yl)pyriinidin- 2-34]}amino-2-ethyl-6-trifluorometh34--3,4-dihydro-2H-quinoline-l- carboxylic acid 4-carbox3>±>ut3'l ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(morpholin-4-3d)pyrimidm 2-3d]}arnino-2-ethyl-6-trifluorornethyl-3,4-dihydro-2H-quinoline-l- carboxylic acid 2-carbox3^-2-methylpropyl ester; (2R,4S)-4-{(3-C3^ano-5-trifluoromethylbenzyl)-[5-(2- methoxyethoxy)pyrimidin-2-3^1]}arnino-2-ethyl-6-trifluoromethyl-3,4- dihydro-2H-quinoline-l-carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{(3-C^ano-5-trifluoromethylbexizylj-[5-(2-metho^-ethoxy)pyrimidin-2-yl]}arnino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carboxylic acid 3-carbosypropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(2-rnethoxyethox3^)pyrimidin-2-yl]}arnino-2-ethyl-6-trifluorometh.34-3?4- dih3'dro-2H-quinoline-l-carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{(3-Cyano-5-trifluorometh3dben?yl)-[5-(2- methoxyethoxy)pyrimidin-2-yl]}amino-2-ethyl-6-trifluorome&yl-3?4^ dihydro-2H-quinoline-l-carboxylic acid 2-carboxy-2-methylprop3d ester; (2R,4S)-4-{[3,5-Bis(trifluorome^ 3d]}amino-2-ethyl-6-trifluoromethy^ acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben^l]-[5-(morphoUn-4-yl)pyridin-2- yl]}amino-2-ethyl-6-trifluoromethyl-3J4-dih3'pdro-2H-quinoline-l-carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{[3,5-Bis(trffluorometh34)benz3d]-[5'(morpholin-4-yl)pyridin-2^ yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trffluoromethy^ yl]}ainino-2-ethyl-6-trifluororneth3d-3,4-dih3^dro-2H-quinoline-l-carbo^ acid 2-carboxy-2-methylprop3'l ester; (2R,4S)-4-{[3?5-Bis(trinuoromethyl)benzyl]-[5-(2-hydroxyethoxy)pyridm yl]}ajnino-2-ethyl-6-trifluoroTnethyl-3,4-dih3^dro-2H-quinoline-l-carbo^lic acid 2-carboxy-2-methylprop3d ester; (2R?4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(2-methoxyethoxy)pyridin-^ yl]}aniino-2-ethyl-6-trifluorornethyl-3>4-dihydro-2H-quinoline-l-carbox3rlic acid 2-carboxyethyl ester; (2R.4S)-4-{[3,5-Bis(trifluorometh^^ yl]}arnino-2-ethylr6-trifluoromethyl-3,4-dihydro-2H-quinoline-l-carbo?cylic acid 3-carboxyprop3?*l ester; (2R,4S)-4-{[3,5-Bis(trifluoromethyl)ben2yl]-[5-(2-methox3^ethox3^)py yl]}ainino-2-ethyl-6-trifluoromethyl-3,4-dih3^dro-2H-quinoline-l-carboxylic acid 4-carboxybutyl ester; (2R?4S)-4-{[3,5-Bis(trmuorometh3d)benz3d]-[5-(2-methoxyethoxy)p3^ridin-2- 34]}amino-2-ethyl-6-trifluoromethyl-3J4-dih3^dro-2H-quinoline-l -carboxylic acid 2-carboxy-2-methylpropyl ester; (2R>4S)-4-{[3?5-Bis(trifluoromethyl)ben^yl]-[5-(3-cyanopropoxy)p^yridin-2- yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3?5-Bis(trifluoromethyl)benz54]-(5-dimeth3^aminopyridiri-2- yl)}amino-2-ethyl-6-trifluoromethyl-3?4-dihydro-2H-quinoline-1-carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh34)b^ yl)}amino~2-ethyl-6-trifluorometh3d-3,4-dih^ acid 3-carbo^propyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromethy^ 34)}aixiino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline- 1-carboxylic. acid 4-carboxybutyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh3^1)benz3^1]-(5-dimethylajninopyri^ 34)}arnino-2-ethyl-6-trifluoroine1±iyl-3J4-dihydro-2H-quinoline- 1-carboxylic acid 2-carboxy-2-rneth3dpropyl ester; (2R?4S)-4-{(3-Cyano-5-1rifluorometh3dbenzyl)-[5-(morpholin-4-34)p3^ridm yl]}amino-2-ethyl-6-trifluorometh34-3J4-dihydro-2H-quinoline--l-carbox34ic acid 2-carbox3^ethyl ester; (2R>4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(morphoUn-4-34)pyridin^ yl]}amino-2-ethyl-6-trifluoromethyl-3!,4-dihydro-2H-quinoline- 1-carboxylic acid 3-carboxypropyl ester; (2R,4S)-4-{(3-Cyajio-5-trifluorometh34benzyl)-[5-{morpholin-4-yl)pyridin-2- yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H--quinoline-l'"Carbox3dic acid 4-carboxybutyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(morpholin-4-yl)pyridin yl]}amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1 -carbp^lic acid 2-carbox3'-2~meth3'lpropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylben2^1)-[5-(2-metho^ethoxy)pyridm 2-34]}ajnino-2-eth3d-6-trifluorometh3rl-3,4-dih3rdro-2H-quinoline-l- carboxylic acid 2-carboxyethyl ester; (2R,4S)-4-{[3,5-Bis(trifluorome^ 3^1]}amino-2-ethyl-6-methoxy~3>4-dihydro-2H-quinoline-1-carboxylic acid 2-carbox3rettryl ester; (2R,4S)-4-{[3,5-Bis(trifluorome^^ yl]}ainino-2-eth3d-6-metiioxy-3,4-dihy^ acid 3- carboxypropyl ester; (2R)4S)-4-{[3,5-Bis(trifluoromethyl)benzyl]-[5-(morpholin-4-yl)pyr£inidin-2-yl]}amino-2-ethyl-6-methox3^-3,4-dih3^dro-2H-quinoline-1 -carboxylic acid 4-carboxybutyl ester; (2R,4S)-4-{[3>5-Bis(trmuoromethy^^ yl]}amino-2-ethyl-6-methoxy-3,4-dih3^dro-2H-quinoline-l-carboxylic acid 2-. carboxy-2-methylpropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluoromethylben23^1)-[5-(moi^holin-4-yl)pyrirnidin-2-yl]}ainino-2-ethyl-6-met±ioxy-3J4-dihydro-2H-quinoline-l-carbc>xylic acid 4-carboxybutyl ester; (2R,4S)-4-{(3-C3^ano-5-trifluorometh34benzyl)-[5-(morpholin-4-yl)pyrimidin 2-yl]}amino-2-eth3^1-6-methoxy-3,4-dihydro-2H-quinoline-l-carbc>x34ic acid 2-carboxy-2-meth3^1prop3d ester; (2R,4S)-4-{[3?5-Bis(trifluoromethyl)benzyl]-[5-(morpholin-4-3d)pyridin-2-yl]}amino-2-ethyl-6-methox3^-3,4-dihydro-2H-quinoline-l-carboxylic acid 2-carbox3^ethyl ester; (2R,4S)-4-{[3?5-Bis(trmuoromethyl)bens3rl]-[5-(morpholin-4-yl)pyridin-2-yl]}amino-2-eth34-6-methox3^3J4-dih3^dro-2H-quinoline-l -carboxylic acid 3-carbox3^propyl ester; (2R,4S)-4-{[3,5-Bis(trifluorometh3d)ben^]-[5-(morpholin-4-yl)pyridin-2-3d]}amino-2-ethyl-6-methox3*-3J4-dih3^dro-2H-quinoline-l-carboxylic acid 4-carboxybutyl ester; (2RJ4S)-4-{[3r5-Bis(trifluoromethyl)ben2yl]-[5-(morpholin-4-34)pyrldm^ yl]}amino-2-ethyl-6-methoxy-3J4-dihydro-2H-quinoline-l -carboxylic acid 2- carboxy-2-methylpropyl ester; (2R,4S)-4-{(3-Cyano-5-trifluo yl]}amino-2-eth3d-6-methoxy-3,4-dihydro-2H-quinoline-l-carboxylic acid 4- carbox\^butyl ester; (2R,4S)-4-{(3-Cyano-5-trifiuoromethyfo^ yl]}amino-2-ethyl-6-methoxy-3,4-dihydro-2H-quinoline- 1-carboxylic acid 2- carbox3^-2-methylpropyl ester; (2R,4S)-4-{[3,5-Bis(trifluoromefo^ yl]}amino-2-ethyl-6,7-ethylenediox3^-3,4-dihydro-2H-quinoline-l-carbox7ylic acid 2-carboxyethyl ester; and (2R,4S)-4-{(3-Cyano-5-trifluoromethylbenzyl)-[5-(2- methoxyethoxy)p3^rimidin-2-yl]}amino-2-ethyl-6,7-e1±Lylenedioxy-3,4 dihydro-2H-quinoline-l-carbosylic acid 2-carboxyethyl ester. 18. A process for preparing a tetrahydroquinoline derivative of the formula (I): wherein the S3'mbols Rif R2, R3, R4, R5, Ret R?? RS, R9 and Rio have the same meaning as defined in claim 1, which comprises condensing a compound of the formula (II): wherein each S3onbol has the same meaning as defined above with a compound of the formula (III): Rl0_R4-Z* (III) wherein Z1 is a leaving group and the other symbols have the same meaning as defined above. 19. A compound of the formula (II): wherein the symbols Ri, R2, R3, R5, R6> RT? RS and R9 have the same meaning as defined in claim 1, or a salt thereof. 20. A diastereomer mixture of the formula (XHI-a): wherein R15' is an optically active protecting group for amino group and the symbols R2, R3, R6, R7? RS and R^ have the same meaning as defined in claim 1, or a salt thereof. 21. A process for preparing a diastereomer mixture of the formula (XHI-a): wherein R15' is an optically active protecting group for amino group and the symbols R2, R3, R6, R7, Rs and R9 have the same meaning as defined in claim 1, which comprises reacting a compound of the formula (XV): wherein each sj'mbol has the same meaning as defined above with a compound of the formula (XIV-a): R3~=-NHR15' (XIV-a) wherein each symbol has the same meaning as defined above. 22. A process for preparing an optically active compound of the formula (XHI-b) wherein the symbols R2, R3, R&? R7, Rs and R9 have the same meaning as defined in claim 1, which comprises reacting a compound of the formula (XV): wherein each symbol has the same meaning as defined above with a compound of the formula (XlV-a): RS-^^NHRI* (xiv-a) wherein R15' is an optically active protecting group for amino group and R3 has the same meaning as defined above, resolving the resulting diastereomer mixture of the formula (XIII —a): wherein each symbol has the same meanirxg as defined above, and removing the optically active protecting group fox amino group. 23. The process of claim 21 or 22, wlierein a compound of the formula (XVIII): wherein the S3'mbols R2, R6, R7, R8 and R9 lxave the same meaning as defined in claim 1 is used in place of the compound (XV): wherein each symbol has the same meaning as defined above. 24. A pharmaceutical composition, which comprises as an active ingredient a compound according to any one of claims 1 to 17, or a pharrnaceutically acceptable salt thereof. 25. A method for prophylaxis or treatment of arteriosclerosis, peripheral vascular disease, dyslipidemia, hyperbetalipoproteinemia, hypoalphalipoproteinemia, hypercholestereinia, hypertriglyceridemia, familial-hypercholesteremia, cardiovascular diseases, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, restenosis after angioplasty, hypertension, cerebral infarction, cerebral stroke, diabetes, vascular complication of dia~betes, thrombotic diseases, obesity or endotoxemia, which comprises -administering an effective amount of a compound according to any one of claims 1 to 17, or a pharmaceutically acceptable salt thereof, to a patient in need thereof. 26. Use of a compound according to any one of claims 1 to 17, or a pharmaceutically acceptable salt thereof, in treatment of patients suffering from arteriosclerosis, peripheral vascular disease, dyslipidemia, hyperbetalipoproteinemia, hypoalphalipoproteinLemia, hypercholesteremia, hypertriglyceridemia, familial-hypercholesterernia, cardiovascular diseases, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, restenosis after angioplasty, hypertension, cerebral infarction, cerebral stroke, diabetes, vascular complication of diabetes, thrombotic diseases, obesity or endotoxemia. Dated this 28 day of September 2006

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3616-chenp-2006 complete specification as granted.pdf

3616-CHENP-2006 CORRESPONDENCE OTHERS.pdf

3616-CHENP-2006 CORRESPONDENCE PO.pdf

3616-CHENP-2006 FORM-1.pdf

3616-CHENP-2006 FORM-13.pdf

3616-CHENP-2006 FORM-2.pdf

3616-CHENP-2006 FORM-3.pdf

3616-CHENP-2006 PETITION.pdf

3616-chenp-2006-abstract.pdf

3616-chenp-2006-claims.pdf

3616-chenp-2006-correspondnece-others.pdf

3616-chenp-2006-description(complete).pdf

3616-chenp-2006-description(provisional).pdf

3616-chenp-2006-form 1.pdf

3616-chenp-2006-form 18.pdf

3616-chenp-2006-form 26.pdf

3616-chenp-2006-form 3.pdf

3616-chenp-2006-form 5.pdf

3616-chenp-2006-pct.pdf

3616-CHENP-2006.PDF