Title of Invention | LINEAR BASIC COMPOUNDS HAVING NK-2 ANTAGONIST ACTIVITY |
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Abstract | ABSTRACT 1173/CHENP/2004 Linear basic compounds having NK-2 antagonist activity Described herein are compounds of formula (I) useful an antagonists of tachykinins in general, and in particular of neurokin A. |
Full Text | LINEAR BASIC COMPOUNDS HAVING NK-2 ANTAGONIST ACTIVITY AND FORMULATIONS THEREOF Field of the invention The present invention relates to compounds antagonists of tachykinins in general, in particular of neurokinin A, and to their use in pharmaceutical formulations. State of the art Tachykinms is a family including at least three peptides, known as Substance V, Neurokinin A (NKA) e Neurokinin B (NKB). The research in the field of the tachykinins antagonist, mainly based on single or multle substitution of amino acids of the sequence of the peptidic agonists of Substance P and of the other tachykinins, lead to the discovery of nonzeptides containing one or more units of D-triptophan (Regoli et al., Pharmacol. 28,301 (1984)). However, the problems derived from the pharmacological use of high molecular weit pq>tides (multiple sites of enzymatic hydrolytic attack, poor bioavailability, rapid hepatic and renal excretion) induced to search the minimum peptidic fragment which is still capable of exerting an antagonist activity. These studies lead to the detection of adequately derivatised bicyclic and monocychc peptides, antagonist of neurokinin A (Patent Applications No. WO 9834949 and No. WO 200129066). Various compounds have been claimed as selective antagonists of Substance P, for instance in Patent Applications No. WO 9519966 andNo7wo'9845262;but, besides being selective for NKl receptor, these compounds have structural characteristics which are different from the compounds of the present invention, mainly the lack of a basic amino group. Among NKl antagonists, we can also mention those described in Patent Application No. WO 200014109; among these compounds, there is not even one alpha,alpha-disubstituted I amino acid, and the basic group, when present, is in positions that are very different from those in the compounds of the invention. Also in Patent No. EP 394 989 the compounds with NKl activity do not usually have a basic group and do hot exhibit an alpha,alpha-disubstituted amino acid. In Biorganic & Med. Ckem. (1994), 2 (2), 101-113 (S. Boile et; al.) compounds wiih NK2 activity are described, which contain an alpha,alpha-disubstituted phenylalanine (Phe)„but they do not exhibit the basic characteristics nor they can be associated to the structure described by the general formula (I). In Patent Application No. WO 9404494 NKl antagonists are described, which exhibit a disubstituted alpha,alpha-aimno acid whose structure do not correspond to the general formula (I), in particular for the presence -among other things - of a -0-CO- group in the place of XI. Summary of the invention It has been surprisingly found that the present non peptidic compomids of general formula (I) as defined hereinafter, show abetter behaviour in inhibiting the bonding of tachykinins onto the receptor NK2, and a better in vivo antagonist activity than that showed by the products disclosed in the above cited prior art patents. The present invention refers therefore to linear compounds of general formula (I) comprising an alfa,alfa-disubstituted amino acid and at least an amino group capable of giving basic characteristics to the compounds wherein: XI is a group selected fi-om -NR6-C0-, -CO- and -NR6-CS- RI is an aryl or aryl-alkyl or aryl-ethylene group containing firom 7 to 12 carbon atoms, wherein aryl indicates a group selected from the group consisting of pyridine, pyrrol, thiophene, benzene, naphthalene, imidazol, diphenyl, phenyl-thiopheae, and it can be possibly substituted by one or more groups independently chosen from the oup consisting of halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms (such as a trifluoromethylic group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a trifluoromethoxylic group), OH, -NHRIO, -N(R10)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -RSCONHRIO, -NHCORIO, and -nitro, wherein RIO is H or a linear or branched C1 -C6 alkyl chain, and R9 is a linear or branched C1 -C6 alkylene, chain; or the radical; possibly substituted by one or more substituents independently chosen from halogen, Cl-C6 Blkyl possibly substituted by not more than three fluorine atoms (such as a trifluoromethylic group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a triflucromethoxylic group), -OH, -fHR10, -N(R10)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -Ommmm. -R9CONHR10, -NHCORIO, and -nitro, wherein RIO is H or a linear or branched C1-C6 alkyl chain, and R9 is a linear or branched C1-C6 alkylene chain, and wherein D = O, S, CH2, 0-CH2 or N-R7, wherein R7 is selected from the group consistmg of H, a linear or branched C1-C6 alkyl chain, and acyl radical R8-C0, wherein R8 is selected from the group consisting of H and linear or branched C1-C6 alkyl chain; R6 is selected fromtiie group consisting of H and linear or branched C1-C6 alkyl chain; A and B are independently selected from the group consisting of linear or branched C1-C6 alkyl chain, aryl or arylalkyl chain wherein the aryl portion is selected from the group consisting of benzothiophene, indol, pyridine, pyrrol, benzofurane, thiophene, benzene, naphthalene, imidazol, diphenylcan be, possibly substitated by one or. more substituents independently chosen from halogen, C1-C6 alkyl chain possibly substituted by not more than three fluorine atoms (such as a trifluoromethylic group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a trifiuoromethoxylic group), -OH, -NHRIO, -N(R10)2, -SRlO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -CONHRIO, -R9C0NHR1Q, -NHCORIO, and -nitro, wherem RIO is H or a linear or branched C1-C6 alkyl chain, and R9 Is a linear or branched C1-C6 alkylene group, or A and B, together with the carbon atom to which they are bound, may form a group having general formxila (II): wherein the broken line indicates a possible double bond; n and m can independently be 0, 1 or 2; R13 and R14 are independently selected from the group consisting of H, C1-C6 alkyl chain, or they can be linked to form an aromatic group selected fix)m the group consisting of benzothiophene, indol, pyridine, pyrrol, benzofurane, thiophene, benzene, naphthalene, imidazol, and biphenyl, which can be possibly substituted by one or more substituents independently selected fro halogen, C1-C6 alkyl possibly substituted by not more than Ihree fluorine atoms (such as trifluoromethylic group), C1-C6 alkjdoxy chain possibly substituted by not more than three fluorine atoms (such as trifluoromethoxylic group), -OH, -NHRIO, -N(R10)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -CBMBHi, -R9CONHR10, -NHCORIO, and -nitro, wherein RIO is H or linear or branched C1-C6 alkyl chain, and R9 is a linear or branched C1-C6 alkylene chain; X2 is selected from the group consisting of -C0NR6- and -CH2>fR6-, wherein R6 is as described above; R2 is selected from the group consisting of an aryl-alkyl or aryl radical wherein the aryl portion is selected from the group consisting of benzothichene, indol, pyridine, pyrrol, benzofinane, thiophene, benzene, naphthalene, imidazol, and biphenyl, and it can be possibly substituted by one or more substituents independently selected from halogen, Cl-C6 alky] possibly substituted by not more than three fluorine atoms (such as a trifluoromethylic group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a trifluoromethoxjic group), -OH, -NHRIO, -N(RI0)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, R9CONHR10, -NHCORIO, and -nitro, wherein RIO is H or a linear or branched C1-C6 alkyl chain, and R9 is a linear or branched C1-C6 alkylene chain, R3 includes at least a basic amino group, and it is represented by the general formula; ~R4-X3-Rg wherein R4 is selected from the group consisting of: - C1-C6 alkylene, C5-C8 cycloalkylene, - an aliphatic heterocycie containing at least one atom selected from N, S and O, and possibly substituted by one or two C1-C6 aUcyl groups OT a -C0R15 group, in which R15 is selected from the group consisting of -NRnR12 and -ORll, wherein RIl and R12, independently from each other, are H or a Unear or branched C1 -C6 alkyl group; - aryl-alkyl or aryl wherein the aryl portion is selected from the group consisting of benzothiophene, indol, pyridine, pyrrol, benzofurane, thiophene, benzene, naphthalene, imidazol, and biphen>d, and it can be possibly substituted by one or more substituents independently selected from halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms {such as a group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a trifluoromethoxylic group), -OH, -fHR10, -N(R10)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -aOnOBB -R9CONHR10, -NHCORIO, and -nitro, wherem RIO is H or a linear or branched C1-C6 alkyl group, and R9 is a linear or branched C1-C6 alkylene group, X3 is a single bond or it is selcted from the group consisting of-CH2-, -CH2-CH2-, -CO-, - OCH2-CH2O-, -0- , -NH-CO-CH2-, and -NH-CO-; or -R4-X3- taken together are a group -CO-CH2- R5is: an aliphatic heterocycie selected from the group consisting of pyrrolidine, piperidine, morpholine, chinuclidine, diazepan, tetrahydropyran, l,4-dioxa-8-azaspiro[4,5]decane, possibly substituted by one or more substituents selected from the group consisting of C1 - C6 alkyl, hydroxymethyl, -OH, cyanomethyl, and C1-C6 alkyloxy; - an azetidine possibly substituted by a grotq) -(CH2)n-R17, wherem R17 is selected from the groi consisting of morpholine, piperidine, pyrrolidine, tetrahydropyran, and tetrabydrothiopyran; - a piperidine possibly C-substituted by a C1-C6 alkyl chain, substituted by a group X5-R18 wherein X5 is a bond or a group -C(Rn)(R12)-, -CO-, -C0CH2-, -CH2CH2-, and R18 is selected from the group consisting of morpholine, piperidine, pyrrolidine, tetrahydropyran, tetrabydrothiopyran, cyclohexane, dioxane, l,4-dioxa-spiro(4,5)decyl and an aromatic selected from the group consisting of thiophene, pyridine, furane, pyrrol, , thiadiazole, thiazole, and phenyl possibly substituted by one or more substituente selectee, from the group consisting of halogen, C1 -C6 alkyl possibly substituted by not more than three fluorine atoms, C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms, -OH, -NHRIO, -N(R10)2, and -SRIO wherein RIO, Rll and R12 are selected from H and linear or branched C1-C6 alkyl chain; - a piperazine possibly C-substituted by one or two C1-C6 alkyl groups, and possibly N-substituted by a group chosen from -SO2NRI 1R12,-CCH2)20(CH2)20H, -CH2CN, or by the group -X4-RI6 wherein X4 is a bond or it is selected from the group consisting of-CO-, -CH2-, -C0NR6-, -COCH2- and -CO-NR6-CH2-, and R16 is selected from the groxip consistii of pyrrolidine, morpholine, tefrahydropyran, tetrahydrofijrane, dioxane, thiophene, pyridine, phenyl, naphttiyl, diphenyl, pyrazol, oxazol, isoxazol and thiadiazol, possibly substituted by one or more groups selected from halogen, C1-C6 alkyl, C1-C6 alkyloxy, OH; and R6, Rll and R12 are as deiined above; - an amino group selected from the group consisting of -NRl 1R12, -NH(CH2)m-NR11R12, amino-tetrahydropyran, ftirylmethylamino, -NH(CH2)2O(CH2)20H, wherein m ranges from 3 to 6, and Rl 1 and RI2 are as defined above - an amino-cycloalkyl group possibly substituted on the ring by a group selected from OH, and NRl 1R12, wherein RI 1 and R12 are as defined above, -a cycloalkyi group possibly substituted on the ring by a group selected from NR11R12, wherein Rl 1 and Rl 2 are as defined above; - an aryl group selected from the group consisting of thiophene, pyridine, fiirane or phenyl possibly substituted by one or more substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkyloxy, and OH. Further object of the present invention are the 'retro-inverted' compounds of the present fonnida (I) compounds, i.e. the compounds of general formula (I) in which one or more amidic bonds are inverted. The presence of an alpha,alpha-disubstituted amino acid and the presence of at least one amino group in R3, which gives to the compounds a strong basicity, can be considered as a peculiar structural characteristic of the products belonging to the general formula (I). Further object of the present invention are the pharmaceuticaily acceptable salts of the compounds of general formula (I) with organic or inorganic acids selected from the group consisting of hydrochloric acid, sulphuric acid, phosphoric acid, acetic acid, trifluordacetic acid,oxalic acid, malonic acid, maleic acid, fumaric acid, succinic acid, tartaric acid ana citric acid. Furtiiennore, object of the present invention are the single enantiomers and diastereoisomers of the compounds of formula (I) or mixtures thereof, originating from the insertion into the structure of fonnula (I) of chiral residues or groups. Further object of the present invention are the pharmaceuticaJ formulations comprising the compounds of general formula (I) and the use of said compounds for prepaiii pharmaceutical formulations for the treatment of diseases in which neurokinin A plays a pathogenetic role. Detailed description of the invention Preferred compounds of the invention are the compounds of general formula (I), wherein the aminoacidic residue of general fonnula (III) is selected from the group consisting of aminoacidic residues of a,a-' disubstituted glycine-type selected from the group consisting of I-aminocyclohexane-I-carboxyhc acid (Ac6c), 1 -arainoc)lopentane-l -caihoxylic acid (Ac5c), 1 -aiiiinocyclopent-3-ene-l - carboxylic acid (Ac5c), 1-aminoisobutyrric acid, 1-aminoindane-i-carboxyUc acid (1-Aic), 2-arainoindane-2-caitioxyUc acid (2-Aic), 2-aminotetraline-2-caiboxylic acid (2-Atc), 2- methyl-2-ethylglycine, 2-methyl-2-isopropylglycine, 2-methyl-2-n-propylglycme, 2- methyI-2-(2-butyi) glycine, 2-methyJ-2-isobut5gIycine, 2-methyl-phenyIaIanine; and fee oflier groups are as defmed above. Preferred compounds according to the present invention are the compounds of formula (I) wherein: - Xlis a CO group Rl is an aryl or aryl-ethylene group containing from 7 to 12 carbon atoms, wherein aryl is a group selected from benzene, naphthalene, and biphenyl possibly substituted by one or more groups independently selected from halogen, CI-C6 alkyl possibly substituted by not more than three fluorine atoms (such as a trifluoromethylic group), C1-C6 alkyloxy possibly substituted by not more than three fluorine atoms (such as a trifluoromethoxylic group), -OH, -NHRIO, -N(RlQ)i, -SRlQ, -CONHRIQ, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -CONHRIO, -R9CONHR10, -NHCORIO. and -nitco, wherein RIO is H or a linear or branched C1-C6 alkyl chaiii, and R9 is a linear or braiKhed C1-C6 alkylene; possibly substituted by one or more substiluents independently selected from halogen, Cl-C6 alkyl possibly substituted by not more than three fluorine atoms (such as trifluoromethylic group), C1-C6 alityloxy possibly substituted by not more than liree fluorine atoms (such as trifluoromethoxylic group), -OH, -NHRIO, -N(R10)2, -SRIO, -CONHRIO, -CORIO, -COORIO, -R9COOR10, -OR9COOR10, -R9COR10, -taB8W» -R9CONHR10, -NHCORIO, and -nitro, wherein RIO is H or hnear or branched CI-C6 alkyl chain, and R9 is a linear or branched C1 -C6 alkylene chain, and wherein-D-= O,-S-oi-N-RT.wherein R7-is-selectedfroni-the group consisting of H, linear or branched C1-C6 alkyl chain, acyl radical R8-CO, wherein R8 is selected from the group consisting of H and lineai or branched C1 -C6 alkyl chain; - R6 is selected from the group consisting of H and linear or branched C1-C6 alkyl; - the amino acidic residue of general formula (III) s an a,a-disubstituted glycine-type residue selected from the group consisting of 1 -Lmjnocyclohexane-l-carboxylic (Ac6c), l-aminocyclopentane-l-carboxylic acid (Ac5c), I-aminoindane-l-carboxyHc acid (I-Aic), l-aminacyclopentan-3-ene 1- carboxylic acid (Ac5c), 2-methyI-pfaeny]alamne, 2-me&yl-2-ethy]-gHcme, R2 is a phenylmethyl group possibly substituted on the phenyl portion by one or two groups independently selected from the group consisting of halogen, C1-C6 alkyJ, C1-C6 aikyloxy, and OH; - X2 is selected from -C0NR6- and -CH2NR6; R3 includes at least one basic amino group and it is the following group; -R4" X3- Rs wherein - R4 is selected from the group consisting of a group -(CH2)n-, wherein n ranges from I to 3, a C5-C8 cycloalkylene group and an aliphatic heterocycle selected from piperidine, pyrrolidine or piperazine possibly substituted by one or two Cl-C6a(kyi chains; - X3 is a bond or it is selected from the group consisting of-CO-, -CH2-, -CH2-CH2-, -CO-CH:-,and-NH-CO-; - R5 is selected from the group consisting of: a) an aliphatic heterocycle selected from piperidine, pyrrolidine, moipholine, diazepan, tetrahydropyran, tetrahydrothiopyran, and l,4-dioxa-S-azaspiro[4,5]decane, possibly substituted by one or two groups selected from CI-CS alkyl, hydroxymethyl, cyanomethyl, CI-C6 aikyloxy, and OH; b) an azetidine possibly substituted by a -(CH2)n-Rl 7 group wherein RI7 is selected from the group cozjsisting of morpholine, piperidine, pyrrolidine, tetrahydropyran, and tetrahydrothiopyran; c) a piperidine, possibly C-substituted by a C1-C6 alkyl chain, substituted by a group X5-R]8, wherein X5 is a bond or it is selected from the group consisting of-C(Rn)(R12)-, -CO-, -CH2CH2-, and -COCH-; and R18 is selected from the group consisting of furane, morpholine, pyrrole, thiophene, tetrahydropyran, tetrahydrothiopyran, pyrrolidine, cyclohexane, cycJopentane, 1-3-dioxane, thiazole and l,4-dioxa-spiro(4,5)decyJ, possibly substituted by one or more groups selected from halogen, C1 -C6 alkyl, CI -C6 aikyloxy, -OH, -NHRIO, -N(R10)2, and -SRIO, wherein RIO, Rll and R12 are selected from H and linear or branched CI -C6 alkyl; d) a piperazine possibly C-substituted by one or two C1-C6 alkyl groups and possibly N-substituted by a group selected from -(CH2)20(CH3)20H, -CH2CN and a group X4-R16, wherein X4 is a bond or it is selected from the group consistiiig of-CH2-,-CH2-CH2-, and -COCH2-, and R16 is selected from the group consisting of pyridine, fiiiophene, tetrahydropyran, raoipholine, tetrahydrofurane, and 1,3-dioxane; e) an amino group selected from -NRnR12 and -NH-(CH2)m-NRllR12 wherein Rll, R12 and m are as defined above; f) an amino-cycloalkyi possibly substituted on the ring by a group selected from OH and -NR11R12, or a cycloalkyl possibly substituted by a groi NRUR12, wherein RU and R12 are as defined above; g) an heteroaromatic selected from pyridine and fliiazole. Amongst fiiese compoiaids particularly preferred are fee compounds wherein: XI is a-CO-group; Rl is an aromatic group selected from the group consisting of biphenyl, phenyl-ethylene, naphthyl, phenyl-thiophene, benzothiophene, benzofiirane, and indole possibly N- substituted by a C1-C6 alkyi group, which can be possibly substituted by one, two or three groups independently selected from the group consisting of halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms, C1-C6 alkyloxy, OH, NHRIO, and N(R10)2, wherein RIO is selected from H and C1-C6 alkyl; the amino acidic residue of general formula (III) is selected from the group consisting of 1- aminocyclohexane-1 -caiboxylic acid (Ac6c), 1 -aminocyclopentane-l -carboxylic acid (Ac5c), l-aminoindane-l-C3rboxylicacid(l-Aic), l-aininocyclopentan-3-enie 1-caiboxylic acid (Ac5c), 2-methyl-phenylalanine, and 2-methyl-2-ethyl-glycine; R6 is H; R2 is a phenyl-methyl group, having the phenyl group possibly substituted by a C1-C6 alkyl group; X2 is selected from -CONH- and CH2NH-; R3 includes at least one basic amino group having the following formula: "R- X3-R5 wherein: - R4 is selected from the group consisting of a group -(CH2)n wherein n ranges from 1 to 3, a C5-C8 cycloalkylene group selected from cyciopentylene and cyclohexylene, and an ilipfaatic heterocycle selected from piperidine, pyrrolidine and piperazine possibly iubstituted by one or two C1-C6 alkyl groups; - X3 is a bond or it is a group selected from -CO-, -CH2-, -CH2-CH2-, and -NH-CO-; - R5 is selected from: a) an aliphatic heterocycle selected from the group consisting of piperidine, pyrrolidine, rnoipholine, diazepan, tetrahydropyran, and l,4-dioxa-8-azaspiro[4,5]decane, possibly substituted by one or two groups selected from C1-C6 alkyl, C1-C6 alkyloxy, OH, and cyanomethyl; b) an azetidine substituted by a group -(CH2)n-R1 7, wherein Rl 7 is tetrahydropyran; c) a piperidine possibly C-suhstituted by a C1-C6 alkyl group, and substituted by a group X5-R18 wherein X5 is a bond or it is selected from the group consisting of-C(R11)(R12)-, -CO-, -CR2CH2-, and -COCH2-, and R18 is a group selected from thiophene, tetrahydropyran, tetrahydrothiopyran, pyrrolidine, cyclohexane, cyclopenfane, and 1-3-dioxane, possibly substituted by one or more groups selected from C1-C6 alkyl, -NHRIO, and -N(R10)2, wherein RIO, RI1 and R12 are selected from H and linear or branched Cl-C6 alkyl; d) a piperazine possibly C-substituted by one or two C1-C6 alkyl group, and possibly N-substituted by a group selected from -CH2CN and X4-R16, wherein X4 is a bond or it is selected from -CH2- and -COCH2-, and R16 is selected from the group consisting of pyridine, thiophene, tetrahydropyran, morpholine, tetrahydrofiirane, and 1,3-dioxane; e) an amino group selected from -NR11R12 and -NH-(CH2)m-NRllR12, wherein RU, R12 and m are as defined above; f) an amino-cyclohexane or a cyclohexane possibly substituted on the ring by the group -NR] 1R12, wherein Rl 1 and R12 are as defrned above; g) an heteroaromatic group represented by pyridine. Amonst these compounds more preferred are the present compounds of formula (I) wherein: XI is a-CO-group; Rl is an aromatic group selected from the group consisting of phenyl-ethylene, naphthyl, benzothiophene, and benzofurane, possibly substituted by one, two or three groups independently selected from halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms, C1-C6 alkyloxy, OH, NHRIO, and NCR10)2 wherein RIO is selected from H and C1-C6 alkyl; the amino acidic residue of general formula (III) is selected from 1-aminocyclohexane-l- carboxylic acid (Ac6c), and 1-aminocyclopentane-l-carboxylic acid (Ac5c); R6 is H; R2 is phenyl-methyl; X2is-CONH-; R3 includes at least one basic amino group and it is the following group; —R4 - X3- Rs wherein - R4 is selected from -(CH2)n- wherein n ranges from 1 to 3, and piperidine possibly substituted by a CI -C6 alkyl group; X3 is a bond or it is a group selected from -CO- and -CHj-; R5 is selected from: a) an aliphatic heterocycle selected from piperidine and tetrahydropyran, possibly substituted by one or more C1-C6 alkyl groups; b) a piperidine possibly C-substituted by a C1-C6 alkyl group, substituted by 3 group X5-Rl 8 wherein X5 is a bond or it is a group selected from -C(R11)(R12)- and -CO-, and Rl 8 is a group selected from tetrahydropjran, cyclohexane and 1-3-dioxane, possibly substituted by one or more groups selected from C1-C6 alkyl, -NHRIO, and -N(R10)2, wherein RIO, RU and Rl 2 are selected from Hand linear or branched CI-C6 alkyl; c) a piperazine possibly C-substituted by one or two C1-C6 alkyl groups, and possibly N-substituted by a group X4-R16 wherein X4 is -CHj-, and RI6 is selected from tetrahydropyran and 1,3-dioxane. Among the terms used for describing the present invention the following are preferred: - the term "halogen" refers to fluorine, chlorine, bromine or iodine; - the term "C1-C6 alkyl" refers to a group selected from methyl, ethyl, n-propyl, isopropyl, I n-butyl, ter-but) and, when possibly substituted by fluorine, trifluoromethyl; - the term "C1-C6 alkyloxy" refers to a group wherein the alkyl part is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, ter-butyl and, when possibly substituted by fluorine, trifluoromethyl; - the term "C1-C6 alkylene" refers to a group selected from methylene, ethylene, trimethylene, and tetramethylene; - the term "C5-C8 cycioalkylene" refers to a group selected from cyclobutylene, cyclopentylene, cyclohexylene, and cycloheptylene; - the tenn "cycloalkyl" refers to a group selected irom cyclobutane, cyclopentane and cyclohexane. The compounds of the present invention have shown an antagonist activity to the action of Substance P, Neurokinin A, and Neurokinin B; and they demonstrated particularly selective against the action of Neurokinin A. Thus the present compounds of formula (I) can be used for prepararing pharmaceutical formulations, possibly comprising pharmaceutically acceptable diluents and excipients commonly used in drug products, usefiil for the treatment and prevention of diseases in which tachykinins in general, and namely Neurokinin A, are involved as neuromodulators; as an example we can list the following diseases: respiratory pathologies, such as asthma, allergic rhinitis, and chronic obstructive bronchitis; ophthalmic diseases, such as conjunctivitis, skin diseases, such as allergic and contact dermatitis, and psoriasis, intestinal disordere, such as irritable colon, ulcerous colitis and Chron disease, gastric diseases, urinary diseases, such as cystitis and incontinence, erectile dysfimctions, diseases of the nervous central system, such as anxiety, depression and schizophreny, tumoural pathologies, autoimmunitary diseases or diseases related to AIDS, cardiovascular pathologies, neuritis, neuralgia and treatment of pain, in particular visceralgia, inflammatory processes, such as osteoarthritis or rheumatoid arthritis. The present compounds of formula (I), as defined above, can be prepared according to methods described in literature and well known to the person skilled in the art, such as by reactions of amidic condensation, substitution, addition or reductive amination. As an example the synthetic paths described in the general guidelines in the following reaction schemes can be followed by making the obvious and suitable changes according to the substituents. In the following schemes, imless otherwise clearly specified, the substituents are as defined above. For example, the compoimds of general formula (I) may be obtained according to the following Scheme 1 by reacting the activated carboxylic acid derivatives of general formula (IV) with the intermediate compound of general formula (V). Si:heme 1 In this case, as an example, Xi = CO. Again, as an example, the compounds of general fonnula (I) can be obtained as described in the following Scheme 2, according to the following sequence of reactions: a) formation of the oxazolinone of fomiula (VII) starting from activated carboxylic acid derivatives of formula (IV) and amino acids of fomiula (VI), with suitable activating and condensing agents; b) reaction of oxazolinone of formula (VTO with amines of fomiula (VIII) protected with a suitable protective group P, followed by deprotection by methods known to the person skilled in the art, to obtain the compounds of formula (IX); c) acylation, alkylation or reductive amination with suitable reagents to yield the final compounds of formula (I). Scheme 2 In this case, as an example, Xi = CO and n = 0,1, 2. The compounds of the present invention can occur in various isomeric forms, hi fact, whereas the configuration of the carbon linked to R5 is univocally prefixed by using during the synthesis the specific isomer of the amino acid derivative, fi-equently the other starting products can be constituted by mixture of stereo isomers of difficult separation. Therefore, the compounds of the present invention can be obtained as mixtures of iiiastereoisomeTS. These mixtures can be resolved by chromatography. The compounds of formula (I) can however be used as single enantiomers as well as mixtures of isomers. Some examples of the present compounds and of the preparation method thereof are provided in the following for illustrative and non limiting purposes of the present invention. Example 1 N°[N(benzo[b]thiophenyl-2-ylcarbonyl)-l-aminocyclopentane-l-carbonylJ-D- phenylalanine-N-[3(morphoIin-4-yl)propyl]amide la) to a solution of l-amino-cyclopentane-l-carboxylic acid (1 g, 7.66 mmol) in 30 ml of anhydrous dichloromethane (DCM) N,0-bis(trimethylsilyl)acetamide (BSA) (3.8 ml, 15.4 mmol) is added under magnetic stirring; after 15 min trimethylchlorosylane (TMSC1),(0.38 ml, 10 % of the BSA volume) is added. The amino acid is completely sylanised (the solution at the end of the addition is clear), and after about 2 hours of stiiring at room temperature benzo[b]thiophene-2-carbonyl chloride (7.66 mmol) dissolved in 10 ml of DCM is added to the reaction mixture. The reaction is kept for 12 hours under stirring at room temperature. The solution is concentrated under reduced pressure, then 50 ml of NaHCOs aq. IM are added, and is kept under stirring for 30'. Everything is transferred into a separatory funnel, then ethyl acetate (AcOEt) (50 ml) is added; die mixture is shaked and the organic phase is removed. The aqueous solution is acidified up to pH = 1 with HCi €N and washed with AcOEt (3 x 50 ml). The organic phases are collected together, transferred in a separatory funnel and washed with H2O and brine up to pH = 5-6. The organic phase is dried on anhydrous Na2S04, then brought to dryness. The isolated residue is crystallised from acetonitrile, thus obtaining 1.4 g (4.84 mmol, yield = 63%) of N"(benzo[fc]thiophene-2-carbonyl)-l-aminocyclopentane-I- carboxyhc acid. HPLC (method E): Rt = 14.04 min. lb) To a solution in anhydrous THF (25 ml) of the product coming from Example la) (500 mg, 1.73 mmol), l-ethyl-3-(3-dimethylaniinopropyl)carbodiimide hydrochloride (EDC) (2.08 mmol, 0.402 g) and diisopropylethylamide (DiPEA) (5.2 mmol, 0.89 ml) are added. The solution is kept under stirring for 2 hours at room temperature. The solvent is evaporated, and the residue is dissolved with AcOEt (50 ml); the organic phase is washed with NaHCOa IM (3 x 50 ml), HCl IM (3 x 50 ml), saturated aqueous solution of sodium chloride (3 x 50 ml). The organic solution is dried on anhydrous Na2S04 and then it is brought to dryness. 0.450 g of 2~(benzo[b]thiophen-2-yl)-4-cycIopentyl-l,3-oxazolin-5-one (1.66 mmol, yield = 96%) are obtained. HPLC (metiiod E): Rt = 21.86 min. Ic) To a solution in 15 ml of anhydrous THF of tert-butyloxycarbonyl-D-phenylalanine N-hydroxysuccinimmidyl ester (500 mg, 1.38 mmol), N-(3-aminopropyl)-morpholine (1.328 mmol, 0.201 ml) is added. The stirring is maintained for 90 min. The solvent is then evaporated, and the residue dissolved with AcOEt (50 ml); the organic phase is washed with NaHCOa IM (3 x 50 ml), HCl IM (3 x 50 ml), saturated aqueous solution of sodium chloride (3 x 50 ml). The solution dried on anhydrous Na2S04. Following the evaporation of the solvent, 474 mg of (ter-but}'loxycarbonyl-D-pheny'lalanine-N-[3(morpholin-4- yl)propyl] amide) (1.21 mmol, yield= 88%) are obtained. HPLC (method E); Rt = 10.35 min. 1 d) The product coming from Example 1 c) (0.474 g, 1.21 mmol) is dissolved m 50 ml of a solution of HCl 4N in dioxane. After 30' the solvent is evaporated, and the residue is dissolved and brought to dryness with toluene and with absolute ethanol. The so obtained solid is transferred into a separatory funnel with 50 ml of NaHCOa and 50 ml of CHCI3. After shaking, the organic phase is collected and the aqueous phase is washed with other 5 portions of CHCI3. All the organic phases are collected, then transferred into a separatory iimnel; one washing is made with a sodium chloride saturated solution. The organic phase is dried on Na3S04. The solvent is evaporated. 0.291 g (1 mmol, yield = 83%) of clear oil of D-phenylalanine-N-[3(morpholLn-4-yl)propyl]amide hydrochloride. le) To a soluticMi in a mixture of 10 ml of anhydrous CH3CN and 1 ml of anhydrous THF of the product coming from Example lb) (66.5 mg; 0.245 mmol), a solution of the product coming from Example Id) (72 mg, 0.247 mmol) in 5 ml of anhydrous CH3CN is added. The reaction is allowed to reflux for 48 hours. After removing the solvent at reduced pressiue, the residue is dissolved with AcOEt (50 ml), and the solution is transferred in a separatory funnel, and washed once with a sodium chloride saturated solution. The organic phase is dried on Na2S04 and the solvent evorated. 135 mg of the product are obtained, which is then purified by reverse phase chromatography, using a column Hibar Merck LiChrospher 100, RP-18e (5 }im), eluents = A: H2O + 0.1% TFA; B: CH3CN + 0.1% TEA; elution with a linear gradient from 10%B at 50%B in 40 min, flow 10 ml/min; UV detection ( X =230 nm). The fractions coiresponding to the peak of the product have been collected, concentrated to small volume at reduced pressure and lyophilised, yielding 0.124 mmol of N°[N"(ben2o[Z']thiophen-2-ylcarbony!)- l-aminocyclopentane-l-carbonyl]-D-phenylalanine-N-[3(morpholin-4-yl)propyl]ainide (yield = 51% after purification). MS (m/z): 563.3 (MH). HPLC (method E): Rt = 14.03 min. Example 2 (lR,3S)-acid-N{N°[N°(benzo[b]thiophen-2-yl-carbonyl)-l-aminocyclopentan-l-carboxy]- D-phenylalaniI}-3-aminocycIopentan-l-carboxylic-N-[(lS,2S)-2-aminocyclohexyl] amide 2a) To a solution of (lS,2S)-diaminocyclohexane (1.14 g, 10 mmol) in 50 ml of DCM, dibenzyl dicaibonate (2 g ,7 mmol) dissolved in 20 ml of DCM is added drop by drop. When the addition is over, the obtained precipitate is filtered and dried, obtaining 0.55 g of a white solid which is the starting diamine cyclohexane. The organic filtrate (80 ml) is extracted with HCI IN (3x10 ml) and the aqueous extract are collected, alkalinise to pH = 10 and extracted with DCM (3x10 ml). The collected organic extracts are dried on anhydrous Na2S04, then filtered and brought to dryness. The residue is dissolved in 3 ml of methanol, then ethy! acetate saturated of hydrochloric acid (EtOAc/HCl) (2 ml) is added and, subsequently, ethyl ether (20 ml) yielding a white precqiitate in suspension. This precipitate is filtered and dried thus obtaining 1.44 g of (1 S,2S)-N- monobenzylojcycaihonyldiaminocyclohexane hydrochloride (yield = 50,5 %). HPLC (E); Rt = 7.85 min. 2b) 360 mg (1.26 mmol) of the product coming from Example are dissolved in 10 ml of DMF and added with 0.296 g (1.29 mmol) of (lR,3S)-N-fer-butyloxycarbonyl-3-aminocycl(entan-3-carboxylic acid, 245 mg of EDC, 173 mg of HOBt and DiPEA until an alkaline reaction is achieved. The mixture is kept to react for 18 hours, then added with DCM (50 ml). The organic phase is washed with KHSO4 5% (3x50 ml), NaHCOj (3x50 ml), H2O (3x50 ml) and dried on anhydrous Na2S04. The organic solution is then filtered and brought to dryness yielding 0.610 g of a yellow solid, which is then dissolved in 5 ml of MeOH and added with 50 rril of EtiO. A white solid precipitates and, after filtration, 440 mg (yield = 68 %) are obtained. HPLC(E); Rt = 15.5 min. The residue is then dissolved in 10 ml of EtOAc and added wifh 20 ml of EtOAc/HCl; after 1 hour 100 ml of Et20 are added to the mixture, thus obtaining a white precipitate that, after filtration, gives 0.425 g of hydrochloride of (lR,3S)-3-aminocyclopentan-3-carboxylic-N-[(lS,2S)-2-N-(ben2yloxycarbonyl)aminocyclohexyI] amide acid. HPLC(E):Rt = 8.9min. 2c) 0.425 g of the product coming irom Example 2b) are dissolved in DMF (10 ml) and added with N°(tert-butyIoxycarbonyl)-D-pheny]alanine (0.312 g, 1.29 mmol), EDC (0.230 g, 1.29 mmol), HOBt (0.175 g, 1.29 mmol) and DiPEA until an alkaline reaction is achieved. The mixture is kept to react overnight, then 30 ml of DCM are added and the organic phase is washed with KHSO4 5% (3x50 ml), NaHCOs (3x50 ml), H2O (3x50 ml),. and dried on anhydrous Na2S04. After filtration and removal of the solvent, 531 mg of raw product are obtained from which, after grinding in EtsO, 470 mg of a white solid (yield = 83 %) are obtained. HPLC(E): Rt = 16.06 min. The release of the Boc groiq) with EtOAc/HCl and subsequent precipitation with EtiO (70 ml) allows the isolation of 410 mg of hydrochloride of (lR,3S)-N'-[D-phenyJalaniI]-3-aminocyclopentan-3-carboxylic-N-[(lS,2S)-2-N-(benzyloxycarbonyl) aminocyclohexyl] amide acid. HPLC(E) = 11.27 min. 2d) Into a 2 00 ml glass protected with a CaCh tube 1.29 g (10 mmol) of 1 -aminocyclobexan-l-carboxylic acid are suspended in 20 ml of DCM, and added with 5 ml of N,0-bis-(trimethylsilyI)-acetamide. The reaction mixture is kept under stirring for 2 hours until the amino acid derivative is completely dissolved. To the solution 1.8 g (0.92 mmol) of chloride of benzothiophene-2-carboxylic acid are added drop by drop in 20 ml of DCM, and the mixture is allowed to react for 1 hour at room temperature. The organic solution is then washed with water (5x50 ml), dried on anhydrous Na2S04, filtered, brought to dryness and grinded with Et20, thus yielding 2.60 g (yield = 90.2 %) of a white solid of N"(benzo[6]thiophen-2-yl-carbonyl)-l-aminocyclohexane-l-carboxylic acid. HPLC (method E): Rt = 17.7 min. 2e) To a solution in anhydrous THF (25 ml) of the product coming from Example 2d) (0.50 g. 1.67 mmol), EDC (2.08 mmol, 0.402 g) and DiPEA (5.2 mmol, 0.890 ml) are i added. The solution is maintained under stirring for 2 hours at room temperature. The solvent is then evaporated, the residue is dissolved in AcOEt (50 ml), the organic phase is washed with NaHCOs IM (3 x 50 ml), HCl IM (3 x 50 ml), sodium chloride saturated aqueous solution (3 x 50 ml). The organic solution is anhydrified on anhydrous Na2S04 and then brought to dryness. 0.450 g of 2-(benzo[i>]thiophen-2-yl)-4-cyclohexyl-oxazol-5-one (1.57 mmol, yield = 94 %) are obtained. HPLC (method E): Rt = 22.1 min. 2f) 0.176 g of the product coming from Example 2c), dissolved in 5 ml of anhydrous CH3CN, are added with 82 mg of the product coming from Example 2d) and with DiPEA until an alkaline reaction is achieved. The mixture is then heated to reflux for 18 hours. The reaction mixture is then diluted with DCM (20 ml ) and washed with KHSO4 5% (3x50 ml), NaHCOs (3x50 ml), H2O (3x50 ml), and dried on anhydrous Na2S04. The mixture is filtered, brout to dryness and grinded with Et20, thus obtaining 185 mg of a white solid. HPLC(E): Rt = 17.08 min. The so obtained solid product is dissolved in 12 ml of MeOH and 1 ml of acetic acid. The resulting solution is added with 250 mg of palladiumon carbon and insufflated with hydrogen for 2 hours imti], under HPLC at the above described conditions, the peak at Rt=I7.08 min disappears and a main peak at Rt = 11.78 min appeals. After filtration of the catalyst and removal of the solvent, the reaction mixture is then purified in 10 runs of preparative chromatography using a column Vydac Peptide&Protein (250 X 22 mm), lOi, eluting with H2O + 0,1% TFA (A) and CH3CN + 0,1 % TFA (B) (gradient 10% to 50% of B in 110 mm; flow 12 ml/min.)- The chromatographic flections which resulted pure fi-om HPLC analysis are collected and evaporated to yield a residue of 70 mg of (lR,3S)-acid-N'{N°[N°(benzo[fc]thiophen-2-yl- carbonyl)-l-aHiinDcyclope!itan-l-carboxy3-D-phenylalanil}-3-aminocyclopentan-l- carboxyhc-N-[(l S,2S)-2-aminocyclohexyl] amide. H-NMR (5, DMSO-dfi): 1.2-1.9 (m. 22H, CH2); 2.6 (m, IH, CH-CO-3Ac5c); 2.9-3.20 (m, 2H, (p)CH2-D-Phe); 3.85 (m, IH, CH-NH. 1,2 di-NHa-cyclohexane); 4.2 (m, IH. CH-NH- 3Ac5c); 4.45 (m, IH, (a)CH-D-Phe)); 7.1-7.25 (m, 5H, Carom-D-Phe); 7.45-7.85 (m, 8H, C(5)H-K:(6)H+_j2iCH-l,2di-NH2-cyclohexane+2CH-3Ac6c + NHs"" + NHCH-P- Phe); 7.90-8.02 (in, 2H, C(4)H+C(7)H); 8.3 (s, IH, C(3)H); 8.9 (s, IH, NH-lAc5c). MS-FAB: 644,3 (M+H)" }ffLe-(-me&od)H=-14TS-iiiiflr With analogous methods or by obvious changes for a skilled person, the following products have been prepared: Example 3 N{N°[N°(biphen-4-ylcarboxy)-l-aminocyclopentan-l-carboxy]-D-phenylalanyl}- (lR,3S)-3-aminocyclopentane-l-carboxyhc-acid-N-(ClS,2S)-2-aminocyclohexyl)amide trifluoroacetate salt MS-FAB: 664.32 (M+H)' HPLC (method E): Rt = 10.5 min. Example 4 - N{N°pj"(N-(methyl)indol-2-ylcarboxy)-l-aminocyclopentan-l-carboxy]-D- phenylalanyI}-(lR,3S)-3-aminocyclopentane-l-carboxyhc-acid-N-((lS,2S)-2- aminocyclohexyl) amide trifluoroacetate salt MS-FAB: 641.32 (M+Hf HPLC (method F): Rt = 4.8 min. Example 5 N'{N°[lS[°[4-(methyl)cynnamoyl]-l-aminocyclopentan-l-carboxy]-D-phenylalanyl}- (lR,3S>3-aminocyclopentane-l-carboxyiic-acid-K-((lS,2S)-2-aminocyclohexyl)amide trifluoroacetate salt MS-FAB: 628.4 (M+H)' HPLC (method F): Rt = 3.37 min. Example 6 N {N°[N°(ben2ofiiran-2-ylcarboxy)-1 -aminocyclopentan-1 -carboxyJ-D-phenylalanyl} - (lR,3S)-3-aniinocycIopentane-l-carboxylic-acid-N-((lS,2S)-2-aminocyclohexyl) amide trifluoroacetate salt MS-FAB: 628.3 (M+H) HPLC (method E): Rt = 9.25 min. Example 7 N"[N'(4-(methyl)cinnamoyl)-(R,S)l-aminoindane-l-carboxy]-D-phenylalanine amide-N- [ClS,3R)-3-(morpholin-4-yImethyl)cycIopentyl] MS-FAB: 635.2 (M+Hf HPLC (method E): Rt = 12.9 min. Example 8 7{N"fN"(bezo[*]thiophe□-2-yIcabonyl)-l-aminocyclopentaI■]-carboxy]-D- phenylalanyI}-(lR,3S)-3-ammocycIopentane-l-carboxylic-acid-N-((lS,2S)-2- dimethylaminocyclohexyl) amide hydrochloride salt MS-FAB: 572.3 QA+Hf HPLC (method E); Rt = 12.0 min. Example 9 N{N°[N"(benzo[2'Jthiophen-2-y!carbonyI)-l-aminocyc]opentan-]-carboxy]-rM-methyl- phenylalanyl}-(lR,3S)-3-amriiocyclopentane-l-carboxylic-acid-N-(lS,2S)-2-dimethyl aminocyclohexyl)amide hydrochloride salt MS-FAB: 686.3 (M+H) HPLC (method E): Rt = 12.1 min. Example 10 Nα(Nα(4-methyl-cimiainoyl)-l-aminocycIopentan-l-carboxy]-D-phenylalanyl}- (lR,3S)-3-aminocyclopentane-l-carboxylic-acid-N-((lS,2S)-2- dimethylammocyclohexyl)ainide hydrochloride salt MS-FAB: 656.3 (U+Hf HPLC (methodE): Rt= 11.9min. Example 11 N''{N"[N'*(beiizofuran-2-ylcarboxy)-l-aminocyclopentan-l-carboxy]-D-phenylalanyl}- (lR,3S)-3-ammocyclopentane-l-carboxylic-acid-N-((lS,2S)-2- dimethylaminocyclohexyl)amide hydrochloride salt MS-FAB: 656.3 (M+Hf HPLC (method E): Rt = 11.8 min. Example 12 N{N°[N"(biphen-4-ylcarbonyl)-l-aminocyclopentan-l-carboxy]-D-phenylalanyl}- (lR,3S)-3-aminocyclopentane-l-carboxylic-acid-N~((lS,2S)-2- dimethylaminocyclohexyl)amide hydrochloride salt MS-FAB: 692.4 (M+Hf HPLC (method E): Rt = 12.7 min. Example 13 Nα.{NαNα-(methyl)jndol-2-ylcarboxy)71 -ammocyclopentaii-1 -carboxy]-!!)- phenylaIanyl}-(lR,3S)-3-ammocyclopentane-l-carboxylic-acid-N-((lS,2S)-2- dimethylaminocyclohexyl)amide hydrochloride salt 'H-NMR (6, DMSO-dfi): 1.2-1.9 (m, 22H, CH2); 2.6 (m, IH, CH-CO-3Ac5c); 2.90-3.20 (m, 2H, (p)CIt-D-Phe); 2.75 (m, 6H, N(CH3)a); 3.8 (s, 3H, 1-(CH0 indole) 4.2 (m, IH, ai-NH-3Ac5c); 4.45 (m, IH, (a)CH -D-Phe); 7.10-7.25 (m, 5H, Crom-D-Phe); 7.45-7.85 (m, 6H, Cf5)H+Cf6>H+ NHCH-1.2di-NH7-cvclohexane+ NHCH- 3Ac6c+ IJN(CH3)2' + NHCH-D-Phe); 7.90-8.02 (m, 2H. C(4)H+C(7)H); 8.5 (s, IH, C(3)H); 8.9 (bs, IH, NH- lAc5c). MS-FAB: 669.3 (M+H)"" HPLC (method E): Rt= 12.2 min. Example 14 N'{N°[N"(benzo[i>]thiophen-2-ylcarbonyl)-(R)-a-methyl-a-ethylglycyl]-D- phenylalanyl)-(lRt3S)-3-ainino cycIopentane-l-carboxylic-acid-N-{ClS,2S)-2- aminocyclohexyl) amide trifluoroacetate salt MS-FAB: 632.2 (M+H)* HPLC (method F): Rt = 5.51 min. Example 15 Nα{Nα[Nα(4-methy]cini]amoy])-(R)-a-n) ethyl-a-ethylglycyl}-D-pheiiylalanyl}-(lR,3S)-3- amino cyc]opentane-l-carboxyJic-acid-N-((lS,2S)-2-aminocyc]ohexyl) amide trifluoroacetate saJt MS-FAB; 616.3 (M+H)* HPLC (method F): Rt = 5.58 min. Example 16 N'{N"[N"(biphenyM-carboxy)-1 -aminocyclopentan-l -carboxy]-R-3(4(methyi) phenyI)a!any!}-(IR,3S}-3-amJnocycIopentane-I-carboxylic-acid-N-((lS,2S)-2- aminocyclohexyl) amide hydrochloride salt MS-FAB: 678 (M+Ef HPLC (method E): Rt = 12.8 min. Example 17 methyl)phenyl)alanyl}-{iR,3S)-3-aininocyclopentane-l-carboxylic-acid-N-((lS,2S)-2- aminocyclohexyl)amide hydrochloride salt MS-FAB: 655 (M+Hf HPLC (method E): Rt = 12.2 min. Example 18 Nα{N°P(4-(methyl)cymiamoyl)-l-aminocyclopentan-l-carboxy]-R-3[4- methyl)phenyl]alanyl}-(lR,3S)-3-aminocyclopentane-l-carboxylic-acid-N-((lS,2S)-2- aminocyclohexyOamide hydrochloride salt MS-FAB: 642.2 (M+H) HPLC (method E): Rt = 12.0 min. Example 19 NαNαP(benzo[fe]thiophen-2-yI-caibonyl)-l-anainocyclohexan-i-carboxy]-D-phenyIaIaniiie- N- {3-[bis(n-buty])amino]propyI} anide Example 20 N'"(tenzo[Z']thiophen-2-yl-carbonyl)-l-aimnocyclohexan-l-carboxy]'D-phenylalaiime- N-[3(morphoIm-4-yl)propyl]ainide Example 21 3-cw-N{N°l>J°(benzo[*]thiophen-2-ylcarbonyl)-l-aminocyclofaexan-l-carboxy]-D- phenyIalaiiil}aminocyc]ohexan-l-carboxylicacid-N-((lR,2S)-2-aininocyciohexyl)aniide H-NMR (6, DMSO-de): 1.2-1.9 (ra, 26H, CH2); 2.3 (m, IH, CH-CO-3Ac6c); 2.8-3.15 (m, 2H, rp)CHrD-Phe): 3.55 (m, IH, Cg-NH 1,2 di-NHj-cyclohexane); 4.1 (m, IH, Qi-NH- 3Ac6c); 4.35 (m, IH, (a)CH -D-Phe); 7.05-7.18 (m, 5H, Carom-D-Pbe); 7.39-7.45 (m, 2H, C(5)H -1- C(6)H); 7.59-7.65 (m, 3H, HHCH); 7.89-7.96 (m, 2H, C(4)H+C(7)H); 8.3 (s, IH, C(3)H); 8.42 (s, lH,NH-IAc6c). MS-FAB; 672,45 (M+H) HPLC(method E); Rt = 12.7 min. Example 22 hP'{N°[N°(benzo[i)]thiophen-2-yicarbonyI)-l-aminocyclohexan-l-carboxy]-D- phenylalanyl} -3-c/j-ammocyclohexaii-1 -carboxylic-acid-N-(5-aminopentyl)-ainide trifluoroaeetate-salt- H-NMR (5, DMSO-dfi): 1.2-1.9 (m, 24H, -CH2-); 2.2 (m, IH, CH-CO-3Ac6c); 2.7 (m,2H, NH- CH2); 2.8-3.15 (m, 2H, (p)CH2-D-Phe); 3.0 (m, 2H, CHi-NH3: 4.1 (m, IH, CH-NH-3Ac6c); 4.35 (m, IH, (a)CH -D-Phe); 7.05-7.18 (m, 5H, Crrnn-D-Pbe); 7.59-7.65 (m, 3H, NHCH); 7.40-7.55 (m. 5H,C(5)H+C(6)H+ NHa"); 7.89-7.96 (m, 2H,C(4)H+C(7)H); 8.3 (s, IH, C(3)H), 8.42 (s, IH,NH-IAc6c). MS-FAB: 660.22 (M+H) HPLC (method E): Rt = 12.4 min. Example 23 N'[N"(ben2o[Z']thiophen-2-ylcaibonyl)-I-(R)-amino-indan-l-carboxy]-D-phenyIaIanine-N-[3 (moipholin-4-yl)propyl]amide Example 24 (beiizo[i']thiophen-2-yicarbonyl)-I-ammocycIopeatane-I-carboxy]-L-phenyIaIanine-N-[3(morpholm-4-yl)propyl]amide Example 25 (lR,3S)acid 3-{N°[N"(benzo[b]thiophen-2-ylcarbonyl)-l-aminocyclohexan-l- carboxy]-D-pheny]alanil}aminDcyc]opentane-l-carboxy]ic-N-()S,2R)-2- aminocyclohexyl) amide 'H-NMR (3, DMSO-dfi): 1.2-1.9 (m, 24H, CHj); 2.2 (m, IH, CH-CO-3Ac5c); 2.8-3.25 (m, 2H, (p)CH2-D-Phe); 4.0 (m, IH. CH-NH-3Ac5c); 4.25 (m, IH, CH-NH, 1,2 di-NH;-); 4.5 (m, IH, (a)CH -D-Phe);); 7.1-7.25 (m, 5H, Cnim-D-Phe); 7.45-7.55 (m, 2H, C(5)H+C(6)H); 7.6-7.75 (m, 3H,NHCH); 7.93-8.02 (m, 2H, C{4)H+C(7)H); 8.3 (s, IH, CC3)H); 8.42 (s, IH, NH-lAc6c). MS-FAB: 658.30 (M+H)"" HPLC (method E): Rt = 12.5 min. Example 26 acid-3-cis-N{N"[N'(benzo[&]thiophen-2-ylcarbonyl)-1 -aminocyclopentane-1 -carboxy]-L- phenylalanil} aminocycloliexane-l-carboxylic -N-(2-cis-aminocyclohexyl) amide Example 27 N'{N"[N"CbeTizo[6]thiophen-2-ylcarbonyl)-l-aminocyclohexane-l-carboxy]-D- phenylalanil} -(L-(4R)amino-proline-N-(IR,2R)-aminocyclohexyl) amide MS-FAB: 659.20 (M+Hf HPLC (method E): Rt ?= 11.4 min. Example 28 acid-3- cis-N'{N"(N°(ben2o{J]thiopIien-2-ylcarbonyI)-1 -aminocj/clohexan- ] -carboxy]-D- phenyla]anil}-aminocyclohexan-l-carboxylic--N-[(lS,2S)-2-aminocyclohexyl]amide MS-FAB: 672.24 (M+Uf HPLC (method E): Rt = 12.8 min. Example 29 acid-3-cis-N''{N"[N°(ben2o[b]]thiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy]-D- phenylalaml}aminocyclohexane-l-carboxylic-N-[(lS,2R)-2-dimethylaminocyclohexyl] amide Example 30 acid-3-cis-N{N"[N°(benzo[b]thiophen-2-yIcarbonyI)-I-aminocyciopentane-I-carboxy]-D-phenyIaIaiiil}aminocyclohexane-l-carboxylic-N-[(lS,2R)-aminocyclohexyl3 amide 1H-NMR (5, DMSO-dfi): 1.2-1.9 (m, 24H, CH2); 2.2 (m, IH, CH-CO-3Ac6c); 2.SO-3.20 (ra, 2H, (P)CH2-D-Phe); 3.75 (m, IH, CH-NH 1,2 di-NHi-cyclohexane); 4.2 {m, IH, CH- NH-3Ac6c); 4.45 (m. IH, (a)£H -D-Phe); 7.1-7.25 (ra, 5H, Carom-D-Phe); 7.40-7.50 (m, 3H, C(5)H+C(6)H+ NHCH-3Ac6c); 7.60-7.70 (m, 4H, NHCH-l,2di-NH2-cyclohexane + NHs"; 7.85 (IH, NHCH-D-Phe);7.90-8.02 (m, 2H, C(4)H+C(7)H); 8.25 (s, IH, C(3)H); 8.9(s,lH,NH-lAc5c). MS-FAB: 658.35 (U+Hf HPLC(method E): Rt = 12.0 min. Example 31 acid-3-cis-N''{N"P(benzo[6]thiophen-2-ylcarbonyI)-l-aininocyclopentan-l-carboxy]-D- phenylalanil}ainmocyclohexan-l-carboxylic-N-[(lS,2S)-aminocyclohexyl] amide MS-FAB: 658.30 (M+H)* HPLC(method E): Rt = 11.9 min. Example 32 N°[N'(benzo[Z>]thiophen-2-yIcarbonyl)-l-aminocyclopentane-l-carboxy]-D-phenylalanina amide-N-[(lS,3R)-3-(4-(methyl)piperaztn-l-yl)methyl)cyclopenthyl] Example 33 N"[N°(benzo[&]thiophen-2-ylcarbonyI)-l-aminocyclopentan-l-carboxy]-D-plienylalamne ainide-N-[(lS,3R)-3-(4-(methyl)piperazin-l-yl)carbon5d)cyclopentane Example 34 N°|>I°(beiJzo[/>]thiophen-2-ylcarbonyl)-D-a-methylphenylalanil]-D-phenylalaiune-N-[3- (morpholin-4-yl)propyl] amick Example 35 acid-3-cis-N"[N°(benzo[fe]thiophen-2-yIcarbonyl)-l-aminocyciohexan-l-carboxy]-D- pheiiylalanil)aminocyclohexaii-l-carboxylic-N-((lR,2S)-2-methylaminocyclohexyl)amide Example 36 Nα[Nα(benzo[/']thiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy]-D-phenylalanil}- L~(4R)amino-proIine-N-(-2-cis-aminocyclohexyl) amide .- . Example 37 (1R,3S) acid-3-Nα{Nα(benzo[b]thiophen-2-ylcaTbonyl)-l-amiiiocyclopentan-l- carboxy]-D-phenylalanil}aminocyclopentane-l-carboxylic-N-(2-cis-aminocycIohexyOamide 'H-NMR (5, DMSO-de): 1.2-1.9 (m, 22H, CH2); 2.2 (m, IH, ai-CO-3Ac5c); 2.70-3.25 (m, 2H, (P)£Ha-D-Phe); 4.0 (m, IH, CH-NH-3Ac5c); 4.2 (m, IH, CH-NH 1,2 di-NHi- cycIohexane_CH-NH-3Ac6c); 4.45 (m, IR, (a)Ca-D-Phe)),- 7.10-7.25 (m, 5H, Camm-D- Phe); 7.45-7.70 (m, 7H, C(5)H+C(6)H+NHCH-1,2 di-NH.-cYclohexane+ NHCH> 3Ac6cf NH3';7.85 (d, IH, NHCH-D-Phe);- 7.90-8.02 (m, 2H, C(4)H+C(7)H); 8.25 (s, IH, C(3)H); 8.9 (s, IH, NH-IAc5c). MS-FAB: 644.3 (M+H)"" HPLC(inethod E): Rt = 11.8 min. Example 38 (lS,3R)-l-N{N"[N°(benzo(fc]thiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy]-D- phenylalanil}-3-{[lS-((2S)-aminocyclohexyI)amino]methyl}aiiiinocyclopentaiie Example 39 acid-3-cis-N(N°[N°(ben2;o[*}thiophen-2-y]carbonyl)-l-ammocycIcentan-]-carboxy]-D- phenylalami} aminocyclohexan-l-carboxylic-N-({lR,2S)-2-diinethylammocyciohexyl) amide Example 40 (1R,3S) acid-3-N{N'[N°(ben2o[Zj]thiophen-2-ylcarbonyl)-l-aminocyclohexan-l-carboxy]- D-phenylalaiiil}aininocyclopentan-l-carboxylic-N-((lR,2R)2-aminocyclohexyl) amide Example 4 Biphenyl-4-carboxylic acid, {l-[l-(3-morpholin-4-yl-propylcarbamoyl)-2-(R)-phenyl- ethylcarbamoyl]-cyclopentyl}-amide Example 42 Benzofiiraii-2-carboxylic acid, {l-[l-(3-moipbolin-4-yi-propylcarbamoyl)-2-(R)-phenyl- ethylcarbamoyl]-cyclopentyl} -amide Example 43 Ben2o[Zj]thiophene-2-carboxylic acid, methyl-{l-[l-(3-morpholin-4-yI-propylcarbamoyI)- 2(R)-phenyI-ethylcarbamoyl]-cyclohexyI}-arQide Example 44 l-P-{3,4-dichlorophenyl)-acryloylamino]-cyclopentanecarboxylic acid, [l-(3-morpholiji- 4-yl-propylcarbamoyl)-2-(R)-phenyl-ethyl]-amide Example 45 Ben2o[6]thiophene-2-carboxyIic acid {l-[IJ!-(3-moipholin-4-yl-propylcarbamoyl>2- phenyl-ethylcarbamoyl]-cyclopent-3-enyl}-amide MS m/z: 561.3 (M+H). HPLC (method C) Rt = 12.16 min. Example 46 Benzo[Z)]thiophen-2-caTboxylic acid, [l-(l-aminomethyl-2-(R)-phenyl-ethylcarbamoyl)- cyclohexyl]-amide Example 47 1-Methyl-li/-indoIe-2-carboxylic acid, {l-[l-(3-mQrpholiri-4-yl-propylcaibamoyl)-2-(R.)- phenyl-ethylcarbamoy!] -cyclopentyl} -amide Example 48 Ben2o[i]thiophene-2-caiboxylic acid (1 - {1 -[3-(2,6-dimethyl-morpholin-4-yl)- propylcarbamoyI]-2-(R)-phenyl-ethylcarbamoyl}-cyclohexyl)-amide MS (m/z); 605.4 (Mlf). HPLC (method B): Rt = 4.57 min. Example 49 lif-indoI-2-carboxylic acid, {1 -[ 1 -(3-moipholm-4-yl-propylcarbamoyl)-2-(R)-phenyl- ethyicarbamoyl] -cyclopentyl} -amide Example 50 l-[3-(3,4-dibromophenyl)-acryloylamino]-cyclopentanecaiboxylic acid [l-(3-morpholin-4- yI-propyIcarbamoyl)-2-(R)-phenyl-ethyl]-amide Example 51 5-phenyl-thiophene-2-caiboxylic acid, {l-[I-(3-morpholin-4-yl-propylcarbamoyl)-2-(R)- phenyl-ethylcaibamoyl]-cyclopentyl}-araide Example 52 Ben2o[6Jthiophen-2-carboxylic acid, (l-{l(R)-[3-(4-methyl-[l,4]diazepan-l-yl)- propylcarbamoyl]-2-phenylethyl carbamoyl}-cyclopentylj-araide TFA salt 52a) To a suspension of 1-amino-l-cyclopentancarboxyIic acid (19.2 g, 149 mmol) in 500 ml of anhydrous CH2CI2, is added, under magnetic stirring, N,0- bis(trimethylsilyl)acetamide (BSA) (54 g, 268 mmol, containing 5% of TMSCl). After about 1 hour under stirring at room temperature, to this solution benzo[6]thiophene-2- carbonylchloride (29.2 g, 149 mmol) dissolved in 200 ml of CH2CI2 is added in about 2 hours; the reaction mixture is kept under stirring for further 3 hours. The solution is then evaporated under reduced pressure, and the residue is treated with 200 ml of aqueous K2CO3 5% for 15 min, then extracted with AcOEt (2 x 100 ml). The aqueous phase is then acidified with aqueous HCl 37% until complete precipitation of a white solid, which is extracted with. AcOEt (2 x 200inl) and dried on anhydrous Na2S04. The organic phase is filtered and evaporated, thus obtaining l-[(ben2o[fe]thiophene-2-carbonyl)-aTmno]-cyclopentanecarboxylic acid (38.7 g, 134 mmol). HPLC (method A): Rt = 3.51 min. Wi analogous procedures the following intermediate products have also been obtained: l-[(6-Bromo-benzo[fc]thiophene-2-carbonyl)-amino]-cycIopentanecarboxyiic acid HPLC (method A): Rt = 4.08 min. l-[(6-Bromo-naphthalene-2-carbonyl)-amino]-cyclopentanecarboxyUcacid HPLC (method A): Rt = 4.03 min. 1 -(3-(E)-73-ToiyI-acry!oyIanuno)-cycIopentanecarboxyIic acid HPLC (method A): Rt = 3.47 min. l-[(5-Chloro-benzofuran-2-carbonyl)-aniino3-cyclopentanecarboxylicacid HPLC (method A): Rt = 3.74 min. 52b) To a solution in anhydrous THF (500 ml) of the product coming from Example 52a) (16 g, 55 mmol), EDC.HCl (12.7 g, 66 mmol) and diisopropylethylamine (30 ml) are added under magnetic stirring at room temperature. The reaction mixture is kept under stirring for 4 hours, then the solvent is evaporated to dryness, and the residue Js dissolved in AcOEt (1000 ml) and washed with NaHCOs 10% (3 x 300 ml), citric acid 10% (3 x 300 ml), H2O (3 X 500 ml), then dried on Na2S04 and brought to dryness, thus obtaining a whitish solid of 2-benzo[63thiophen-2-yl-3-oxa-l-azaspiro[4.4]-nou-l-en-4-one (13 g, 47.9 mmol). HPLC (A): Rt = 4.97 min. With analogous procedures the following intermediate products have also been obtained: 2-(6-Bromo-benzo[&]thiophen-2-yl)-3-oxa-l-aza-spiro[4.4]-non-l-en-4-one, HPLC(method A): Rt = 5.55 min. 2-(6-Bromo-naphthalen-2-yl)-3-oxa-l-aza-spiro[4.4]-non-l-en-4-one, HPLC (method A): Rt= 5.65 min. 2-(5-Ciiloro-benzofuran-2-yl)-3-oxa-l-a2a-spiro[4.4]non-l-en-4H one, HPLC (method A): Rt = 4.97 win. 52c) To a solution in anhydrous DMF (100 ml) of Z-D-phenylalanine (5 g, 16.7 mmol) HOBt (2.34 g, 17.6 mmol) and EDC.HCl (8.73 g, 17.55 mmol) are added under magnetic stirring. After iO nun 3-aminopropanol (1.25 g, 16.72 mmol) dissolved in DMF (60 ml) is added to the solution, and the reaction mixture is kept at room temperature for 12 hours. The mixture is then diluted with AcOEt (200 ml) and extracted with KHSO4 (5% solution, 200 ml) and with NaHCOa (saturated solution, 2O0 ml). The organic phase, dried on Na2S04, filtered and brought to dryness, is then washed with ethyl ether and the white solid in suspension is filtered to give the desired product (5.15 g, 14.5 mmol). HPLC (method B): Rt = 3.48 min. The product coming from the previous reaction, is deprotected by hydrogenation (H2, Pd/C 10%) according to a procedure known to any person skilled in the art, to give a white solid of 2(R)-amino-A'-(3-hydroxypropyl)-3-phenyl-propionamide (2.91 g, 14.5 mmol), which is used directly in the subsequent reaction. 52d) To the product coming from step 52b) (1 g, 3.7 mmol) dissolved in anhydrous DMF (40 ml), the intermediate described in fwfcTl! g, 5.6 mmol) is added, and the reaction is kept at room temperature under magnetic stirring for 24 hours. Then the mixture is diluted with AcOEt (150 ml) and the organic phase is washed with distilled water (3 x 50 ml) and a saturated solution of NaHCOa (2 x 50 ml), then dried on anhydrous Na2S04 and brought to dryness to give a white solid of benzo[&]thiophene-2-carboxylic acid il-[l(R)-(3-hydroxypropylcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyc]opentyl}-amide (1.51 g, 3 mmol). HPLC (method A): Rt = 3.73 min. 52e) The so obtained product (1.2 g, 2.44 mmol), without further purification, is dissolved m AcOEt (30 ml). To this solution, maintained at 0° C wifli an ice bath, an aqueous solution of NaBr (0.5 M, 5.35 ml, 2.68 mmol), 2,2,6,6-tetrameth>-l-piperidinyloxy (TEMPO, 3.4 mg, 0.022 mmol) is added and, drop by drop, aqueous NaClO (1-83 M, 1.55 mi). The biphasic mixture is kept at 0°C under stirring for fiirther 20 min, then the organic phase is separated and the aqueous phase is extracted with AcOEt (20 ml). The organic fractions are collected and washed with a buffered solution of KI (20 ml), 10% solution of Na2S203 (20 ml) and NaHCOs (5%, 20 ml); they are then dried and evaporated to give a product, which is purified by flash chromatography (EtOAc/hexane, 80/20) to yield 0.82 g of a white solid of 4-[2(R)-({l-[(Benzo[b]thiophene-2-carbonyl)-amino]-cyclopentanecarbonyl}-amino)-3-phenyl-propionyiamino]-propanal. HPLC (method B): Rt = 3.99 min. The so obtained aldehyde (100 mg, 0.203 mmol) is dissolved m methanol (5 ml) and added with l-methyl-[l,4]dia2epan (115 mg, 1.01 mmol) and glacial acetic acid (0.2 ml). After the solution has been stirred for 15 min, Na(CN)BH3 (20 mg, 0.32 mmol) is added to the solution. After 12 hours the solvent is evaporated under reduced pressure and the raw product is dissolved in HCI IM. The acid extract is washed with AcOEt (10 ml) and brought up to alkaline pH by adding solid NaHCOs, then it is extracted with AcOEt (2 x 25 nol). The organic phase is evaporated, then purified by means of preparative HPLC (colonna; Combi HT™ (SB C18, 5pm, lOOA, 21 x 50 mm), MeUiod: H2OH-0.1%TFA/ MeCN+0.1% TFA, 95/5>5/95 in 10 min, flow = 40 ml/min, X.=220, 270 nm) to yield benzo[6]thiophene-2-carboxylic acid (l-{l-[3-(4-meflijd-[l,4]diazepan-l-yl)- propylcarbamoyl]-2-(R)-phenylethylcarbamoyl}-cyc!opentyl)-amide TFA salt (40 mg, 0.067 mmol). MS (m/z): 590.5 (MH). HPLC (method A): Rt = 3.05 min. With analogous methods the following products have also been prepared; Example 53 Benzo/2']tbiopIiene-2-carboxylic acid (1 - (l(R)-[3-(4-methoxy-piperidin-l -yl)- propylcarbamoyl]-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide TFA salt MS (m/2): 591.3 (MH. HPLC (method A): Rt = 3.64 min. Example 54 Benzo[i']thiophene-2-carboxylic acid (l-{l-(R)-[3-(4-hydroxy-piperidin-l-yl)- propylcart)amoyl]-2-phenylethyl carbamo3d}-cyclopentyl)-amide. MS (m/z): 577.3 (MH. HPLC (method A): Rt = 3.31 min. Example 55 Benzo[&]thiophene-2-carboxylic acid (1 - {1 (R)-t3-(1,4-dioxa-8-a2a-spiro[4.5]dec-8-yl)- piopyIcaitamoyJ]-2-pheny!-ethy]carbamoyI}-cycIopentyl)-amide TFA salt MS (m/z): 619.3 (MH*). HPLC (method A): Rt = 3.68 min. Example 56 Benzo[5]£hiophene-2-carboxyIic acid (]-{i(R)-[3-(3,5-c:>-dimethyIpiperazin-I-y])-3-oxo- propylcarbamoyl]-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide TFA salt 56a) Boc-D-phenylalanine O-succinimidoester (5 g, 16.56 mmol) is dissolved in CH3CN (60 mi) and added to a soJution of p-ajamne (2.08 g, 16.56 mmol) and TEA (4.61 ml) in 60 ml of water. After 30' min the organic solvent is evaporated and the aqueous residue, acidified by adding HCI, is extracted with AcOEt (3 x 100 ml). The organic extract is washed with water, dried and brought to dryness to give a colourless oil {4.19 g, 12.08 mmol). HPLC (B): Rt = 3.19 min. The so obtained product is deprotected under standard conditions (HCl, dioxane) and the so obtained amine (2.9 g, 12 mmol) is used, without further purification steps, in the reaction with the intnnediate product described in Example 52b), in the presence of stoichiometric DiPEA, in the conditions above described, to yield 3-[2(R)-({l- [ (Ben2o[Z)]thiophene-2-carbonyl)-amino]-cyclopentanecarbonyl} -amino)-3-phenyl- propionylaminoj-propionic acid (5.17 g, 10.2 mmol). HPLC (B): Rt = 3.98 min. 56b) The so obtained acid (100 mg, 0.2 mmol) is caused to react with 2,6-cis- dimethylpiperazine by a standard method for the formation of the amidic bond (EDC, HOBt, CH2CI2). The raw product of the reaction is purified by preparative HPLC (same conditions of Example 52) to yield benzo[fc]thiophene-2-carboxyhc acid (l-{l(R)-[3-(3,5- cw-dimethyl-piperazin-1 -yl)-3-oxo-propylcarbamoyl] -2-phenyl-ethyl carbamoyl} - cyclopentyl)-ajnide TFA salt (25 mg, 0.035 mmol). MS (m/z): 604.2 (MH. HPLC (method A): Rt = 3.36 min. With analogous methods, starting from suitable intemiediate products as described in Example 52b) and using the obtained suitable amines when necessary, the following products have been prepared according to methods known to the skilled person: Example 57 BeDzo[i)]thiophene-2-carboxylic acid (l-{l(R)-[3-oxo-3-(4-pyridin-2-5d-piperazin-l-5)- propylcaTbamoyl]-2-phenyl-ethyIcarbamoyl}-cyclopentyl)-amide MS (m/z): 653.3 (MH*). HPLC (method A): Rt = 3.40 min. Example 58 6-Bromo-naphthalene-2-cari30xylic acid (l-{l(R)-[3-oxo-3-(4-pyridin-2-yl-piperazin-l- yl)-propylcarbamoyl]-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide TFA salt MS (m/z): 725 (MH, monoisotopic). HPLC (method A): Rt = 3.76 min. Example 59 6-Bromo-benzo[]thiophene-2-carboxylic acid (l-{l(R)-[3-oxo-3-(4-pyridin-2-yl- piperazin-l-yl)-propylcarbamoyI]-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide MS (m/z): 731 (MH*, monoisotopic). HPLC (method A): Rt = 3.73 min. Example 60 ienzo[&]thiophene-2-carboxyiic acid [l-(l(R)-{3-oxo-3-[4-(tetrahydro-pyran-4-ylmethyl)- ipeTa2in-l-yl]-propylcarbamoyl}-2-phenyl-ethylcarbamoyl)-cyclopentyl]-amideTFAsalt 4S (m/z): 674 (MH*] HPLC (method A): Rt = 3.43 miD. example 61 3enzo[&]thiophene-2-carboxylic acid [1 -(1 (R)- {3-oxo-3-[4-(tetrahydro-pyran-4-yl)- )iperazin-l-yl]-propylcarbamoyl}-2-phenyi-ethylcarbamoyi)-cyclopentyl]-amideTFAsalt vis (m/z): 660.3 (Uit). HPLC (method A): Rt = 3.40 min. 5:xample 62 3eazo[ij3thiophene-2-carboxyIic acid (l-{l(R)-[3-(4-[I,3]dioxan-5-ylmeth5-pipera2in-I- /I)-3-oxo-propyIcarbamoylj-2-phenyi-ethylcarbamoyl}-cycIopentyl)-amideTFAsalt MS (m/z): 676.2 (MH. HPLC (method A): Rt = 3.43 min. Example 63 Benzo[Z>]thiophene-2-caTboxylic acid [l-(l(R)-{[l-(l-amino-cyclopentanecarbonyl)- piperidin-4-ylmethyl]-carbamoyl} -2-phenyI-e&y] carbamoy])-cyclopentyl]-afflide MS (m/z): 644.3 (MH. HPLC (method A): Rt = 3.55 min. Example 64 Benzo[&]thiophene-2-carboxylic acid [l-(l(R)-{3-oxo-3-[4-(telrahydro-furan-2(R)- yhnethyl)-piperazin-l-yl]-propylcarbamoyl)-2-phenyl-ethyIcarbamoyl)-cyclopentyl]- amide TFA salt MS (m/z): 660.2 (Mit). HPLC (memod A): Rt = 3.68 mjn. Example 65 Benzo[&]thiophene-2-carboxylic acid (l-{l(R)-[3-(4-cyanomethyl-piperazin-I-yl)-3-oxo- propylcarbamoyl] -2-phenyl-ethylcarbamoyi} -cyclopentyI)-amide MS (m/z): 615.1 (MH. HPLC (method A): Rt = 3.79 min. Example 66 Ben2o[J]thiophene-2-carboxyiic acid {i-[2-phenyl-I(R)-(I-pyridin-2-ylmethyI-piperidin- 4-ylcarbamoyl)-ethylcarbamoyl]-cyclopentyl}-amide TFA salt. 66a) Z-D-phenylalanina (3.28 g, 11 mmol) is caused to react with N-Boc-(4- amino)piperidine hydrochloride (2.6 g, 11 mmol) xinder the usual conditions for peptidic coupling (HOBt, EDC, DIPEA, CH2C12) as described in Example 56b). The so obtained adduct (5 g, 10.3 mmol), after a simple extractive processing, is hydrogenated in the presence of Pd/C as the catalyst, so to obtain 4-(2(R)-amino-3-phenyl-propionylamino)- piperidine-1-carboxylic'acid tert-hutyl ester (3.21g, 9.27 mmol). HPLC (method B): Rt = 3.22 nun. With analogous procedures the following inteimidiates have also been obtained: 4-[(2(R>ainino-3-phenyl-propionylamino)-raethyI]-piperidme-l-carfaox>1icacidtert-butyl ester 4-[2-(2(R)-amino-3-phenyl-propionylamino)-ethyl]-piperidine-l-carboxylicacid/er/-butyl ester (in this case, the N-Boc-(4-aminoethyl)piperidine obtained stating from the corresponding alcohol by obvious reaction for a skilled person, has been used). 66b) The compound obtained as in Example 66a') (1-69 a. 4.87 mmoD is reacted vith DMF at room temperature for 24 hours with the oxazoiinone described in example 52b') (1.29 g. 4.8 mmol). The so obtained intermediate (2.9 g. 4.7 mmol, ■IPLC (B): Rt = 4.85 min"). after a simple extractive working, is dsprotected by eaction with TFA in CHCU, to yield benzorf)"|thiophene-2-carboxvlic acid il-t2-henvl-l(R)-fpiperidin-4-vlcarbamovl')-etliylcarbamoyl]-cyciopentvll-amide TFA ah. MS (miz): 519.2 (MHV HPLC (method AV Rt 3.29 iTiin. With analogous methods the following compounds have been prepKed: benzo[jthiophene-2-carboxyhc acid (1 - {2-phenyI-l (R)-[(piperidin-4-yI-methyi)- carbaraoylj-ethylcarbamoyl}-cyclopentyl)-amide TFA saU MS (m/2): 533.3 (MIT). HPLC (method A): Rt = 3.29 min. ben2o[6]thiophene-2-carboxyIicacid {l-[2-pfaenyl-l(R)-(2-piperidin-4-yl-ethylcarbamoyl) -efhyIcarbamoyl]-cyclopentyl}-amide TFA salt MS (m/z); 547.3 (MIT*). HPLC (method A): Rt = 3.39 min. 66c) 200 mg (0.31 mmol) of benzo[i]thiophene-2-caTboxylic acid {l-[2-phenyI-l(R)- (piperidin-4-yIcaibamoyl)-ethylcarbamoyl]-cyclopentyl}-amide are used for the reaction of I reductive amination with pyridine 2-carboxaldehyde (64 mg, 0.6 mmol), to yield, after purification by preparative HPLC according to the method already described in the previous Examples, the desired product ben2o[b]thiophene-2-carboxyiic acid (l-[2- pheny]-l(R)-(l-pyiidin-2-ylmefhyI-piperidin-4'yicaibamoyl)-ethylcarbamoyI]- cyloopentyl)-amide TFA salt (120 mg, 0.16 mmol). VIS (m/z); 610.3 (MH+]. HPLC (method A): Rt = 3.58 min. In analogy to what described in Example 66c), the reaction in DMF, at room temperature and for times ranging from 12 to 48 hours, of the intermediate products described in Example 66a) with oxazoHnones described in Example 52h), and the reaction of the intermediate products described in Example 66a) with l-(3-(E)-p-Tolyl-acryloylamino)-cyclopentanecaiboxylic acid described in Example 52a) under conditions of peptidic coupling, gives, after deprotection of the amino groups, intermediates analogous to those described in Example 66b). Such intermediates are alkylated under conditions which are widely reported in the literahne and well known to any person skilled in the art, such as: - aldehyde or ketone, cyanoborohydride supported on resine in anhydrous CH2CI2 - aldehyde or ketone, Na(AcO)3BH, in CH2CI2 or THF - alkyl halide, KI, DiPEA in DMF, or under the conditions described abovein Example 52d). With the synthetic procedure described in Example 66 the following products have been prepared: Example 61 Benzo[i']thiophene-2-carboxylicacid(l-{2-phenyl-l(R)-[l-(tetrahydro-pyran-4-ylmethyi)- piperidin-4-ylcarbamoyl]-ethylcaihamoyl}-cyclopentyl)-amide TFA salt MS (m/z): 617.3 (Mlt). HPLC (method A): Rt = 3.44 min. Example 68 Benzo[fc]thiophene-2-carboxyIic acid [l-(2-phenyl-l(R)-{l-[2~(tetrahydro-pyran-4-yl)- ethyl]-piperidin-4-y]carbamoyJ}-ethylcarbamoyI)-cycJopentyJ]-amide TFA salt MS (m/z): 631.3 (MH+). HPLC (method A): Rt = 3.57 min. Example 69 6-Bromo-benzo[]thiophene-2-carboxyiic acid [l-(2-phenyl-I(R)-{[l-(tetrahydro-pyran-4- ytmefliyl>piperidin-4-y]methyI]-carbamoyl}-e:thylcarbamoyl)-cyclopentyl]-amide TFA salt MS (m/z); 709 (MlT, isotopjc pattern of Br). HPLC (method A): Rt = 3.S2 min. 'HNMR(400 MHZ): (5, DMS0-d6) 1.12-2.13 (m, 17 H); 2.17-2.30 (m, IH); 2.74-3.00 (m, 5H), 3.02-3.38 (m, 5H); 3.44-3.57 (m, 2H); 3.80-3.93 (m, 2H); 4.39-4.50 (m, IH); 7.U-7.24 (m, SH); 7.55-7.66 (m, 2H); 7.S5-7.92 (m, IH); 7.93-7.9S (m, IH); S.30 (s, IH); 8.34-8.38 (m, IH); 8.97 (s, IH); 8.78 and 9.01 (2 broad signal, IH total). Example 70 thiophene-2-carboxyhc acid (l-{l-(R)-[(l-isopTOpyl-piperidi3i-4-yhnethyl)- carbamoyl]-2-phenyl-ethyIcarbamoyl}-cyclopentyl)~amide IMS (m/z); 575.3 (MH). HPLC (method A): Rt = 3.56 mm. Example 71 Benzo[i]thiophene-2-carboxylic acid [l-(2-phenyM(R)-{[l-(tetrahydro-pyran-4- ylmethyl)-piperidin-4-ylmethyI]-carbamoyl}-ethylcarbamoyl)-cyclopeDtyl]-amide 4S (m/z): 631.3 (MH.HPLC (method A)=Rt = 3.51 min. H NMR (500 MHz): (6, DMS0-d6) amongst the others 0.99-1.14 (m, 4H); 2.18-2.29 (m, IH), 2.65-2.75 (m, 2H); 2.78-3.02 (m, 3H); 3.75-3.85 (m, 2H); 4.41-4.50 (m, IH); 7.09- 7.23 (m, 5H); 7.43-7.52 (m, 3H); 7.86 (d, IH, J=8.6); 7.94-8.07 (m, 2H); 8.30 (s, IH); 8.89 Cs, IH). Example 72 6-Bromo-naphthalene-2-carboxylic acid [l-(2-phenyl-l(R)-{[l-(tetrahydro-pyran'4- ylmethyl)-piperidin-4-ylmethyI]-carbamoyI}-ethylcarbamoyl)-cyclopentyl]-amide MS (m/z); 703.3 (MH, isotopic pattern of Br). HPLC (method A): Rt = 3.88 min. *H NMR (600 MHz): (5, DMS0-d6) 0.90-1.11 (m, 4H); 1.18-1.29 (m, IH); 1.38-1.73 (m, 12H); 1.74-1.82 (m, IH); 1.87-1.91 (m, 2H); 1.92-1.99 (m, IH); 2.27-2.34 (m, IH); 2.50- 2.56 (m, 2H); 2.81-2.89 (m, 2H); 2.94-3.02 (m, IH); 3.16-3.28 (m, 3H); 3.75-3.83 (m, 2H); 4.44-4.50 (m, IH); 7.11-7.21 (m, 5H); 7.46 ft IH, J=5.77 Hz); 7.71-7.75 (m, IH); 7.82(d, IH, J=8.65 Hz); 7.98-8.04 (m, 3H); 8.29-8.31 (m, IH); 8.53 (s, IH); 8.83 (s, IH). Example 73 Benzo[;?]thiophene-2-carboxylic acid [l-(2-phenyl-I(R)-{[l-(tetrahydro-pyran-4-yI)- piperidin-4-ylmethyl]-carbamoyl)-ethylcarbamoyl)-cyclopentyl]-amide MS (m/z): 614.4 (MH*). HPLC (method A): Rt = 3.46 min. Example 74 1 -(3-E--Tolyl-acryloylaniino)-cyclopentanecaiboxyiic acid (2-phenyl-l (R)- {[I - (tetrahydro-pyran-4-yhnethyI)-piperidin-4-yhnethyl]-carbamoyl}-ethyl)-amideTFAsalt MS (m/z): 615.4 (MH). HPLC (method A): Rt = 3.56 min. H NMR (400 MHz); (5, DMSO-d6) amongst the others 1.13-1.25 (in, 2H); 2.15-2.23 (m, IH); 2.34 (s, 3H); 3.80-3.87 (m. 2H); 4.36-4.44 (2 m, IH total); 6.68 and 6.69 (2 d, IH total J=15.8I for both); 7.13-7.30 (m, 7H); 7.375 and 7.38 (2 d, 1 H total, J=15.81 for both); 7.45-7.51 (m, 2H); 7.66 and 7.73 (2 t, 1 H total, J=5.8 Hz for both); 7.82 and 7.83 (2 d, IH total, J=S.67 for both); 8.54 and 8.55 (2 s, IH total); 8.80 and 8.97 (2 broad signal, IH total). Example 75 Benzo[b]thiophene-2-carboxylic acid [l-(2-phenyl-l(R)-{2-[l-(tetrahydro-pyran-4-ylnieihyl)-piperidm-4-yl]-ethylcarbajnoyl}-ethylcarbanioyl)-cycIopentyl]-ainideTFA salt MS (m/z): 645.5 (MH*), HPLC (method A): Rt = 3.63 min. Example 76 6-Bromo-naphthalene-2-carboxyIic acid (l-{I(R)-[(I-ethy!-piperidin-4-yImethyI)-carbamoyl]-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide MS (m/z): 633.4 (MH", con isotopic pattern of Br). HPLC (method A): Rt = 3.86 min. Example 77 Benzo[6]thiophene-2-carboxylic acid [I-(2-phenyl-l(R)-{2-[l-(tetrahydro-pyran-4-yl)-pjperidin-4-yI]-ethyIcarbamoy!}-eth5lcarbamoyl)-cyciopenty]]-amideTFA salt MS (m/z): 631.4 (Mif). HPLC (method A): Rt = 3.53 min. Example 78 Benzo[&]thiophene-2-carboxylic acid {l-[2-phenyl-l(R)-({l-[2-(tetrahydro-pyran-4-yl)-ethyl]-piperidin-4-ylmethy!} -carbarn oyl)-ethylcarbamoyl3-cyc]opentyl) -amide MS im/z): 645.3 (MH. HPLC (method A): Rt = 3M min. Example 79 Benzo[6]thiophene-2-carboxylic acid (l-{l(R)-[(l-cyclohexylmethyl-piperidin-4-ylmethyl)-carbamoylj-2-phenyl-ethylcarbamoyl}-cyclopentyl)-amide MS (m/z): 629.3 (MH*). HPLC (method A): Rt = 4.11 min. Example 80 6-Bromo-naphthalene-2-carboxylic acid [l-(2-phenyl-l(R)-{[l-(tetrahydro-pyran-4-yl)-piperidin-4-ylmethyl]-carbamoyl} -ethylcarbamoyl)-cyclopentyl]-amide MS (m/z): 689.3 (MH*, isotopic pattern of Br). HPLC (method A): Rt = 3.83 min. Example 81 Benzo[2i]ftiiophene-2-carboxylic acid [l-(2-pheDy]-l(R)-{[l-(tetrahydro-thiopyran-4-yl)-p!peridin-4-ylmethyl]-carbanioyl}-ethyicarbamoyl)-cyclopentyl]-amide TFA salt MS (m/z): 633.5 (MH*). HPLC (method A): Rt = 3.79 min. Example 82 acid [l-(2-phenyl-l(R)-{[l-(tetrahydro-lhiopyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl>cyclopentyl]-amide MS (m/z): 647.3 (MH+). HPLC (method A): Rt = 3.91 min. Example 83 l-((E)-3-p-Tolyl-acryloylamino)-cyclopentanecarboxylic acid {2-phenyl-I(R)-[(l-thiophen-2-ylmethyl-piperidi3i-4-ylmethyl)-carbaraoyl]-ethyl}-amide TFA salt MS (m/z): 613.3 (Mit). HPLC (method A): Rt = 3.82 min. Example 84 6-Bromo-naphthalene-2-carboxylic acid (]-{2-phenyl-I(R)-[2-(l-pyn-olidiii-2(S)-ylmethyl-piperidiii-4-yI)-ethylcarbamoyI]-ethylcarbamoyI}-cycIopeiityl)-ainide TFA salt MS (m/z); 702 (MH*", isotopic pattern of Bi). HPLC (method A): Rt = 3.55 min. Example 85 6-Bromo-naphthalene-2-carboxylic acid (l-{2-phenyI-l(R)-[(piperidin-4-yhnethyl) carbamoyl]-ethy]carbamoyl}-cycIopentyl)-amide MS (m/z): 605 (MH, isotopic pattern of Br). HPLC (method A): Rt = 3.71 min. Example 86 l-{3-J?-Toiyl-acryloylamino)-cyclopentanecarboxylic acid (2-phenyl-l(R)-{2-[l- (tetrahydro-pyran-4-ylmethyI)-piperidin-4-yl]-ethyIcarbamoyl}-ethyI)-amide TFA salt MS (m/z): 628.4 (MlT). HPLC (method A): Rt = 3.60 min. Example 87 Benzo[6]thiophene-2-carboxyiic acid (l-{l(R)-[2-(l-cyanQmethyl-piperiditt-4-yl)-ethylcarbamoyl3-2-phenyl-ethykaTbamo>d}-cyclopentyl)-amide TFA salt MS (m/z); 586.3 (MlT). HPLC (method A): Rt = 3.60 min. Example 88 Benzo[6jthiophene-2-carboxylic acid (]-{l(R)-[(l-[l,3]diox3n-5-ylmethyl-piperidin-4-/Imethyl)-carbamoyl]-2-phenyI-etiiylcarbamoyI}-cyclopentyl)-amide TFA salt vis (m/z): 633.3 (MH+). HPLC (method A); Rt = 3.50 mm. Example 89 5-Bromo-naphthalene-2-carboxylic acid (l-{l(R)-[(i-tl,3]dioxan-5'ylmethyl-piperidin-4 lmethyl)-carbamoyl]-2-phenyI-ethylcarbamoyI}-cyclopentyl)-amide fS (m/z): 705.3 (MH+), isotopic pattern of Br). HPLC (method A): Rt = 3.62 min. Example 90 Benzo[i]thiophene-2-carboxyllic acid (l-{l(R)-[(l-[l,3]dioxan-2-ylmethyl-piperidin-4-yLmethyl)-carbamoyl] -2-phenyl-ethylcarbamoyl} -cyclopentyI)-amide MS (m/z): 633.4 (MH+). HPLC (method A): Rt = 3.66 min. Example 91 5-Chloro-beiizofuran-2-cart)Qxylic acid (l-{l(R)-|;(l-[l,3]dioxan-5-ylmethyl-piperidin-4-y]methy])-carbamoylj-2-phenyi-ethyJcarbamoyl}-cyc]openty!)-amide MS (m/z): 651.3 (Mlf, isotopic pattem of CI). HPLC (method A): Rt = 3.73 min. Example 92 5-Chloro-ben2oftiran-2-carbQxylic acid [l-(2-phenyl-l{R)-{[l-(tetrahydro-pyran-4-yl)-piperidin-4-ylmethyl]-carbamoyl} -ethyl carbamoyl)-cyclopentyl]-amide MS (m/z): 635.3 (MlT, isotopic pattem of CI). HPLC (method A): Rt = 3.70 min. Example 93 5-Chloro-ben2ofiiran-2-carboxylic acid [I-(2-phenyl-l(R)-{[l-(tetrahydro-thiopyran-4-yl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide MS (m/z): 651.3 (MHT, isotopic pattern of CI). HPLC (method A): Rt = 3.98 min. Example 94 Benzo[&]thiophene-2-carboxylic acid [I-(l(R>benzyl-2-{2-[l-(thiophen-2->d-acetyl)-piperidin-4-ylJ-thy]amiDo}-ethy]carbamoyJ)-cycIopenty]]-amide TFA salt 94a) l-trityI-2-(R)-benzyl-l,2-ethylendiamine. To a suspension of 24 gof D-phenylalaninamide in DMF (200 ml) 41.0 g ditrityl chloride are added under stirring at room temperature and, after 1 hour, 80 ml of TEA diluted in 100 ml of DMF are also added. Stirring is maintained for 10 hours, then the solvent is evaporated, the residue is dissolved in ethyl acetate and washed with NaCI aq. 10%, citric acid aq. 10% and again with NaCl aq. 10%. After drying and evaporation, the residue is then dissolved in 200 ml of DMF. To th eso obtamed solution 2000 ml of distilled water are added drop by drop. A precipitate is obtained, which is first brought to dryness then dissolved in 200 ml of THF and this solution is added, drop by drop, in 20 min at 0°C, xmder stimng and xmder nitrogen atmosphere, to a solution of 400 ml of LiAlHt 0.62 M in THF. The mixture is heated and maintained under reflux for 4 hours. After the mixture has been brought to 0°C, 15 ml of distilled water, 15 ml of NaOH aq. 15% and 45 ml of water are added in this order. By filtration of the so obtained precipitate, l-trityl-2-(R)-benzyl-1,2-ethyIendiamine is obtained. 94b) To a solution of l-trityl-2-(R)-benzy!-l,2-ethylendianiine coming from Example 94a) (21.6 g, 55 nunol) in anhydrous CH2CI2 (300 ml) and TEA (8.4 ml, 60.5 mmol) maintained at 0°C, 2-mtrobenzensolphonylcbloride (12.2 g, 55 mmol) is added in small poftions. Once the addition is over, the mixture is kept under stirring at room temperature for 4 hours more, then it is washed witti NaCl aq, 15% (150 ml), NaHCOs aq. 5% (150 ml) and again with NaCl aq. 15% (150 ml). The organic phase dried and evaporated at reduced temperature yield a solid product, which is then dissolved in 150 ml of CH3CN, cooled at 0°C and treated with an excess of HCl in dioxane. After 2 hours at room temperature the solvent is evaporated to dryness, and the solid residue is dissolved in ethyl ether and filtered to yield a white solid of A-(2(R)-Amino-3-phen)i-propyl)-2-nitro-benzenesulphonamide hydrochloride. HPLC (method A): Rt = 2.70 min. 94c) The oxazolinone described in Example 52b) (407 mg, 1.5 mmol) and the intermediate 94b) described above (670 mg, 1.5 mmol) are dissolved in DMF (8 ml), added wdth TEA (0.64 ml, 4.5 mmol) and maintained at 80°C under stirring for 2 hours. The residue obtained from evaporation of the solvent is dissolved with AcOEt (30 ml) and washed with HCl IM (10 ml), NaHCOs (5%, 10 ml), and NaCl aq. 15% (10 ml). The so obtained raw product is purified by flash chromatography (AcOEt/hexane 1/1) to give 0.5 g (0.8 mmol) of the intermediate benzo[b]thiophene-2-carboxylic acid {1 -[ 1 (R)-benzyl-2-(2-nitro-benzenesulphonylamino)-ethylcarbamoyl]-cyclopentyl}-amide. HPLC (method B): 4.74 mm. 94d) 1.2 g (3.36 mmol, 3 mmol/g of loading) of triphenylphosphinic resin are maintained to swell for 30 min in CH2CI2 (25 ml) under balancing stirring; to the suspension the intermediate described in Example 94c) (0.5 g, 0.84 mmol), N-Boc-4-hydroxyethyi-piperidine (600 mg, 2.52 mmol) and tert-butyl-diazodicarboxylate (600 mg, 2-52 mmol) are added. After 16 hours xmder stirring the resin is removed by filtration and the solution is brought to small volume (10 ml). 5 ml of trifluoroacetic acid are added under stirring. After 1 hour the solution is brought to dryness, the residue is dissolved with AcOEt (30 ml) and the solution washed with Na2C03 aq. 5% (15 ml) e NaCI aq. 15% (10 ml), dried and evaporated. Ben2o[b']thiophene-2-carboxylic acid (1-{1 (R)-ben2yl-2-[(2-nitro-benzenesulphonyl)-(2-piperidin-4-yI-ethyl)-aniino]-ethylcarbamoyi}-cyclopentyl)-amide is obtained as a foamy solid (553 mg, 0.77 mmol). HPLC (method A): Rt = 4.20 min 95e) The product coming ftom the previous step (60 mg, 0,084 mmol) is dissolved in CH2CI2 (2 ml) and to this solution 60μl of TEA and 13.5 \J1 of thiophen-2-yl-acethyl chloride are added. The magnetic stimng is maintained for 12 houre, then the solvent is evaporated and the residue, dissolved with AcOEt (10 ml), is washed with NaiCOs aq. 5% (2x5 ml). The raw product obtamed from evaporation of the solvent (60 mg, 0.07 mmol), is dissolved in DMF (3 ml) and treated with diazabicyclotmdecene (DBU, 32 mg, 0.21 mmol) and 2-mercaptcethanol (17 mg, 0.21 mmol) for 12 hours. The residue obtained from evaporation of the solvent at reduced pressure is washed with ethyl ether and purified by preparative HPLC yielding 10 mg (0.013 mmol) of benzo[&]thiophene-2-carboxylic acid [l-(l(R)-benzyl-2-{2-[l-(thiophen-2-yl-acetyl)-piperidin-4-yl]-ethylamino}- ethylcarbamoyl)-cyclopentyl]-anude TFA salt as white lyophilic product. MS (m/z): 657.3 (MH*). HPLC (method A): Rt = 4.12 min. Example 95 Ben2o[J!']thiophene-2-carboxylic acid [l-(l(R)-{2-[(l-amino-cyclohexanecarbonyl)- aminoj-ethylcarbamoyl} -2-phenyl-ethylcarbamoyl)-cyclopentyl]-amide [2-(2(R)-Amino-3-pheny]-propionylamino)-ethyl]-carbamic acid tert-hutyl ester (200 mg, 0.65 mmol), obtained by coupling of "N-Boc-ethylendiamine and Z-D-phenylalanine succinimidoester followed by hydrogenation, is added to a solution of 2-benzo[/)]thiophen- 2-yl-3-oxa-l-a2aspiro[4.4]-noh-l-en-4-one (176 mg, 0.65 mmol) in DMF and maintained under magnetic stirring at room temperature for 48 hours. The so obtained product is deprotected (HCl, dioxane), acylated with l-Boc-amino-l-cyclohexancarboxylic acid (156 mg, 0.65 mmol), by standard activation as described above, then again deprotected (HCl, dioxane). The raw product obtained from extractive work up is purified by flash chromatography (eluent: CHCla/MeOH 9:1) to give ben2o[&]thiophene-2-carboxyiic acid [l-(l(R)-{2-[(l-aniino-cyclohexanecarbonyl)-amino]-ethylcarbamoyl}-2-phenyl- ethylcarbamoyl)-cyclopenty]]-araide (160 mg, 0.27 mmol). MS (m/z): 604.3 (MH+). HPLC (method A): Rt = 3.58 min. With analogous methods the following products have been prepared; Example 96 Benzo[b]thiophene-2-carboxylic acid [l-(l(R)-{[l-(l-amino-cyclohexanecarbonyl)- piperidin-4-ylmethyl]-carbamoyl}-2-phenyl-ethylcarbarnoyl)-cyclopentyI]-amide TFA salt . Example 97 6-Bromo-naphthalene-2-carboxylic acid [l-(l(R)-{[l-(l-amino-cyclohexanecarbonyl)-piperidiii-4-ylmethyl]-carbamoyl}-2-phenyl-ethylcaihamoyl)-cyclopentyl]-amide MS (m/z): 730.2 (MH", isotopic pattern of Br). HPLC (method A): Rt = 4.00 min. Example 98 6-Bromo-naphthalene-2-carboxylic acid [l-(2-phenyl-l(R)-{2-[l-(pyrrolidine-2(S)-caihonyl)-piperidin-4-yl]-ethylcarbamoyl}-ethylcarbamoyI)-cyclopentyl]-amide MS (m/z); 716.3 (MH", isotopic pattern of Br). HPLC (method A): Rt = 3.95 min. Example 99 6-Bromo-naphthalene-2-carboxyiic acid [l-(2-phenyl-l(R)-{2-[l-(pyrrolidine-2(R)-carbonyl)-piperidin-4-yl]-ethylcarbamoyl}-ethylcaTbamoyl)-cyclopentyl]-amide MS (m/z): 716.3 (MH, isotopic pattern of Br). HPLC (method A): Rt = 3.97 mm. Example 100 Benzo[Z)]thiophene-2-carboxylic acid [l-(2-phenyl-l(R)-{2-[4-(thiophen-2-5-acetyl> piperazin-1-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cycIopentyl]-amide. Analogously to Example 95) 4-[2-(2(R)-amino-3-phenyl-propionylamino)-ethyl]-piperazine-1-carboxylic acid teri-huty\ ester (obtained starting from Z-D-phenylalanine and N-Boc-4-hydroxyethylpiperazine by reactions and coupling widely described in literature and in part already reported in previous examples) (100 mg, 0.26 mmol) and 2-benzo[fe]thiophen-2-yl-3HDxa-l-a2aspiro[4.4]-non-I-en-4-one (72 mg, 0.26 mmol) are caused to react in DMF to yield a product which is deprotected and subsequently acylated with thiophen-2-yI-ace±yl chloride in CH2CI2 (as described in Example 94 and purified by flash chromatography using AcOEt as the eluent 69 mg (0.10 mmol) of benzo[&]thiophene-2-carboxylic acid [l-(2-phenyl-l(R>{2-[4-(thiophen-2-yl-acetyl)-piperazin-l-yl]-ethylcarbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide are so obtained. MS (m/z): 672.3 (MH. HPLC (method A): Rt = 3.87 min. Example 101 Ben2o[Z)]thiophene-2-carboxyiic acid [l-(2-phenyl-l(R.)-{2-[4-(tetrahydro-pyran-4-ylmethyl)-piperazin-l-yl]-ethylcarbamoyl}-ethyIcarbamoyl)-cyclopentyl]-amideTFAsalt The compound of the title is obtained by a procedure analogous to that described in Example 100, but carrying out a reductive amination with tetrahydropyranyl 4-carboxyaldehyde in place of an acylation step with thiophen-2-yl-acethy] chloride, MS (m/z): 646.2 (MlT). HPLC (method A): Rt = 3.24 min. Example 102 5-Chloro-benzofuran-2-carboxyIic acid {l-[li?-(3-morpholin-4-yl-propylcarbamoyl)-2-piienyl-ethylcarbamoyl]-cyc!opentyl}-amide 196 mg of 5-ch]orobenzofuran-2-carboxylic acid are suspended in 12 ml of anhydrous CH2CI2, in nitrogen atmosphere. 100 l of oxalyl chloride and one drop of DMF are then added. The stiuing is maintained until the reaction is fmished. The solvent is then evaporated and the residue is brought to dryness in a hard vacuum. 87 mg of the so obtained acyUc chloride are added to a mixture of 132 mg of 1 -amino-cyclopentanecarboxylic acid [l(R)-(3-moipholin-4-yI-propylcarbamoyl)-2-phenyl-ethyl]-amide £»is-hydrochloride, 200 \H of TEA and 10 ml of anhydrous CH2CI2 under magnetic stirring. Once the reaction is over, the solvent is evaporated and the residue is dissolved with a mixture of ethyl acetate and K2CO3 aq. 10%, by vigorously stirring. After separation of the organic phase, washings with basic water, drying on anhydrous Na2S04, filtration and evaporation of the solvent, 134 mg of a residue are obtained, which are theft purified by flash chromatography, eluting with increasing amounts of methanol in.ethyl acetate until MeOH/AcOH = 1/6 v/V, so to obtain the desired amide. MS (m/z): 581.3 (MlT). HPLC (method C): Rt = 13.14 min. With analogous procedure the following compounds have been prepared: Example 103 5-Chloro-benzo[&]thiophene-2-carboxylic acid {l-[li!-(3-moipholin-4-yl- propylcarbamoyl)-2-phenyl-ethyl carbamoyl] -cyclopentyl} -amide MS (m/z): 597.3 (M+H. HPLC (method C): Rt = 13.80 min. Example 104 5-Bromo-benzofLiran-2-carboxylic acid {l-[li?-(3-morpholin-4-yl-propylcarb3moyI)-2-phenyl-ethyl carbamoyl]-cyclopentyl} -amide MS m/z: 625.2 (M+H*, monoisotopic). HPLC (method C): Rt = 13.41 min. Example 105 6-Chloro-benzo[fe]duophene-2-caihoxylic acid {l-[lii-(3-morpholin-4-yl- propylcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyclopentyl}-amide MS m/z; 597.3 (M+H. HPLC (mefliod Q: Rt= 13.58 min. Example 106 6-Methoxy-ben2o[i>]thiophene-2-carboxylic acid {l-[lJ;-(3-moipholin-4-yl- propylcarbamoyl)-2-phenyI-ethylcarbamoyi]-cyclopentyl}-amide MS m/z: 593.3 (M+H. HPLC (method C): Rt= 12.62min. Example 107 4-Chloro-ben2o[Z7]thiophene-2-carboxylic acid {l-[li?-(3-moipholiii-4-yl- propylcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyclopent)1}-amide MS m/z: 597.3 (M+H. HPLC (method C): Rt = 13.79 min. Example 108 6-Bromo-benzo[i]thiophene-2-caitK>xyIic acid {l-[lii-(3-morphohn-4-yl- propylcarbamoyl)-2-phenyl-ethylcarbamoy!]-cyclopentyl}-amide MS m/z: 641.3 (M+H*, monoisotopic). HPLC (method C): Rt = 13.86 min. Example 109 6-Bromo-benzo[i]thiophene-2-carboxyUc acid {l-[lif-(3-moipholin-4-yl- propylcarbamoyI)-2-phenyl-ethylcarbamoyl]-cycIohexyl}-amide MS m/z: 655.2 (M+Vt, monoisotopic). HPLC (method C): Rt = 14.63 min. Example HO 5-Fluoro-l-methyl-l/f-indo]e-2-carboxylic acid {l-[li;-(3-morpholin-4-yl- propylcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyclopentyl}-amide MS m/z: 578.3 (M+H. HPLC (method C): Rt = 13.18 min. Example 111 6-CMoro-l-methyl-1/f -indole-2-carboxyiic acid {l-[li?-(3-morpholin-4-yl- propylcarbamoyl)-2-phenyl-etfaylcarbamoyl]-cyclopentyl}-amide MS m/z: 594.3 (M+H). HPLC (method C): Rt = 14.03 min. Example 112 7-Methyi-benzo[i]thiophene-2-carboxylic acid" {l-[lJ?-(3-morpholm-4-yl- propyIcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyclopentyl}-amide MS m/z: 577.3 (M+H*). HPLC (method C): Rt = 13.26 min. Example 113 5 -Methyl-ben2ofuran-2-carboxylic acid {1 -[ lR-(3 -morpholin-4-yl-prQpylcarbamoyl>2-phenyl-ethylcarbamoyl]-cyclopentyl}-amide MSm/z: 561.3 (M+}f). HPLC (method C):Rt = 13.01 min. Example 114 l,5-D2methyl-]i/-indo]e-2-carboxylic acid {i-[lR -(3-morpho]in-4-yl-propylcarbanioyJ)-2-phenyl-ethylcarbamoyl]-cyclopentyl} -amide MS m/z: 574.3 (M+H. HPLC (method D): Rt = 13.62 min. Example 115 6-Amino-benzo[Z»]thiophene-2-carboxylic acid {l-[l -(3-moipholin-4-yl- prqpylcarbamoyl)-2-phenyl-ethylcarbamoyl]-cyc]opentyl}-amide MS m/z: 578.2 (M+H. HPLC (method D): Rt = 8.62 min. Example 116 6,7-Dichloro-benzo[6]thiophene-2-carboxyIic acid {I-[l-fl -(3~morpfaolin-4-yi-propylcarbamoyl)-2-phenyl-ethylcarbamoyI]-cyclopentyl}-amide MS m/z: 631.3 (M+lT). HPLC (method C): Rt = 14.57 min. Example 117 6-Iodo-naphthalene-2-carboxyUc acid [l-(2-pfaenyl-lii-{[l-(tetrahydro-pyran-4-yImethyl)-piperidin-4-ylmethyl]-carbainoyJ} -ethylcarbamoyO-cyclopentyl]-amide 118a) 18.0 g of 4-tetrahydropyrancarboxylic acid are introduced in a 250 ml flask with a calcium chloride tube, and dissolved in 130 ml of CH2CI2. Under magnetic stirring, 15 ml of oxalyl chloride and 3 drops of DMF are added successively. The solution, that regularly degasses, is kept under magnetic stirring for 16 hours. After evaporation of ihe solvent, the residue is dried in hard vacuxim at room temperature, dissolved in 100 ml of CH2CI2 and put in a bath of ice and water, maintaining a vigorous magnetic stirring. A solution of 21.75 g of ethyl 4-piperiduicarboxylate in 30 ml of CH2CI2 containing 15.35 g of TEA is added to the mixture by means of a dripping funnel. During the addition, that lasts 3 hours, a clear suspension fomis. The reaction mixture is left to stand overnight, then CH2CI2 is evaporated and the residue is brought to diyness in hard vacuum. The residue is dissolved in 110 ml of ammonia aq. 25%, then methanol is added until complete solubilisation. Methanol is refluxed until the ester disappears (samples are taken, evaporated and analised by IH-NMR). The solution is brought to small volume and extracted 25 times with 100 ml of chlorofomi to give, after evaporation of the solvent, 21.4 g of raw diamide. 14.79 g of the so obtained diamide are added in portions to 175 ml of a solution IM of borane in THF. The addition lasts about 1 hour and it is carried out under a nitrogen flow, so that the temperature does not exceed 35°C. Once the addition is completed, the reaction mixture is heated to reflux and the reflux is maintained for 11 hours. In a bath of ice and water, 130 ml of a solution 4M of HCl in 1,4-dioxane, previously diluted wiHi 100 ml of methanol, are added drop by drop to the solution obtained as above. The the reaction mixture is heated to reflux, and the eflux is maintained for 12 hours before cooling at 0- 4°C. By filtration 7.95 g of C-[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-y3]-methylaniiae ibw-hydrochloride are recovered. From mother liquor, by dilution to doubled volume with diethyl ether, fiirther 1.85 g of the desired product are recovered. IH-NMR (200 MHz, DMSO-dg), • (ppm); 1.09-1.33 (m, 2H); 1.51-2.20 (m. 8H); 2.59- 3.08 (m, 6H); 3.09-3.58 (m, 4H); 3.76-3.91 (m, 2H); 8.18 (br, 3H); 10.20 (bf, IH). Analogously, the following amines have also been prepared: C-[ 1 -{4-Metiiyl-tetrahydro-pyran-4-ylmetiiyI)-piperidin-4-yl] -mefh>4amine MS (m/z): 227 (MfT) 'H NMR (200MH2): (5, CDCb) 0.94 (s, 3H); 1.08-1.69 (m, 9H); 2.10 (s, 2H); 2.10-2.30 (m, 2H); 2.48-2.59 (m, 2H); 2.67-2.83 (m, 2H); 3.47-3.79 (m. 4H). C-14-Methyl-l-(4- n)ethvl-tetrahydro-pvran-4-vJmethyl)-piperidin-4-yl]-methyIamine MS (m/z): 227.3 (Mif) C-[4-Methyl-l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yi]-methyiamine MS (m/z): 241.2 (MH llTb) Starting from the amine obtained in Example IHa), by a pe5>tidic synthesis using Boc, under the operative conditions well known to a skilled person, by reacting flie above said amine wifli Boc-D-phenylalanine 0-succinimidoester, deprotecting, reacting with N- Boc l-amino-l-cyclopentancarboxylic acid and deprotecting, the compound l-amino- cyclopenlanecarboxylic acid (2-phenyI-li;-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4~ 3methyl]-carbamoyl}-ethyl)-amide is obtained. This compound is caused to react with the chloride of 6-iodonaphthalen-2-carboxylic acid, by a procedure analogous to that described in Example 102), thus obtaining the final product 6-iodo-naphthalene-2-caTboxylic acid [i-(2-phenyI-iii-{[l-(tetrahydro-pyr3n-4- yimethyI)-piperidin-4-y]methyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide. MS m/z: 751.3 (M+H. HPLC (method D): Rt = 14.00 min. Analogously to that described in Example 117), by reaction of the corresponding carboxylic acids activated with 1-amino-cycIopentanecarboxyiic acid (2-phenyl-Ii?-{[l- (tetrahydro-pyTan-4-ylmethyI)-piperidin-4-yimethyl]-carbamoyl}-ethyl)-amide, the following compounds have been obtained: Example 118 6-Methoxy-naphthalene-2-carboxylic acid [ 1 -(2-phenyl-l i?- {[ 1 -(tetrahy dro-pyran-4-ylmethyI)-piperidin-4-yImethyl]-carbamoyi}-ethyIcarbamoyl)-cycIopentyi]-ainide MS m/z: 655.2 (M+H. HPLC (method D): Rt = 12.42 min. IH-NMR (DMSO-d6). 5 (amongst the others): 0.94-1.07 (m, 4H); 1.42-1.72 (m, 12H); 1.74-1.81 (m, IH); 1.89-2.00 (m, 3H); 2.24-2.33 (m, IH); 2.55-2.63 (m, 2H); 2.82-2.90 (m, 2H); 2.94-3.01 (m, IH); 3.74-3.83 (m, 2H); 3.91 (s, 3H); 4.42-4.49 (m, IH); 7.I0-7.2I (m, 5H); 7.23-7.27 (m, IH); 7.38-7.41 (m, IH); 7.51 (t, J = 5.7 Hz, IH); 7.79 (d, J = 8.6, IH); 7.86-7.97 (m, 3H); 8.45 (s, IH); 8.69 (s, IH). Example 119 6-Bromo-benzoftiran-2-carboxylic acid [ 1 -(2-phenyl-1 J?- ([ 1 -{tetrahydro-pyran-4-y!methyl)-piperidin-4-ylmetfayl]-carbamoyl)-ethylcarbamoyl)-cyclopentyl]-amide MS m/z: 693.5 (M+H, monoisotopic). HPLC (method D): Rt = 13.1S min. IH-NMR (DMS0-d6). 5 (amongst the others): 0.97-1.12 (m, 4H); 1.39-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m, 2H); 2.79-2.92 (m, 2H); 2.95-3.03 (m. IH); 3.77-3.85 (m, 2H); 4.40-4.48 (m, IH); 7.10-7.22 (m, 5H); 7.45 (t, J = 5.7 Hz, IH); 7.54 (dd, J = 1.7 and 8.4Hz, IH); 7.67 (d, J = 0.8Hz, IH) 7.79 (d, J = S.4, IH); 7.S5 (d, J = S.6H2, IH): 7.95 (s ,br, lU); 8.85 (s, IH). Example 120 6-Chlorq-benzoftu'an-2-carboxylic acid [l-(2-phenyl-lii-{[l-(tetrahydro-pyran-4-yimethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyI]-aniide MS m/z: 649.3 (M+H*). HPLC (method D): Rt = 13.00 min. IH-NMR (DMSO-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m," 2H); 2.79-2.92 (m, 2H); 2.95-3.03 (m, IH); 3.77-3.85 (m, 2H); 4.40-4.48 (m, IH); 7.10-7.22 (m, 5H); 7.42 (dd, J = 1.8 and S.4Hz, IH); 7.46 (t, J = 5.8 Hz, IH); 7.66 (d, J = 0.9Hz,. IH) 7.81-7.86 (m, 2H); 8.84 (s, IH). Example 121 5-Fluoro-benzofuran-2-carboxylic acid [I-{2-phenyl-li;-{[l-(tetrahydro-pyraD-4-yImethyl)-piperidin-4-yliiiethyi]-carbamoyl}-ethylcarbainoyI)-cyclopentyl]-amide MS m/z: 633.5 (M+H. HPLC (method D); Rt = 12.10 min. IH-NMR (DMS0-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m, 2H); 2.78-2.93 (m, 2H); 2.95-3.03 (m, IH); 3.75-3.85 (m, 2H); 4.40-4.48 (m, IH); 7.10-7.22 (m, 5H); 7.32 -7.37 (m, IH); 7.46 (t, J = 5.8 Hz, IH); 7.60-7.66 (m, 2H); 7.71 (dd, J = 4.1 and 9.0Hz, IH) 7.83 (d, J = S.6H2. IH); 8.S4 {s, IH). Example 122 5-Chloro-ben2oiuran-2-carboxylic acid [l-(2-phenyl-lJ?-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yImethyl]-carbamoyl} -ethy]carbamo5d)-cyciopentyl]-amide MS m/z: 649.5 (M+ff*). HPLC (method D): Rt = 12.78 min. IH-NMR (DMSO-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m, 2H); 2.78-2.93 (m, 2H); 2.95-3.03 (m. IH); 3.75-3.85 (m, 2H); 4.40-4.48 (m, IH); 7.10-7.22 (m, 5H); 7.46 (t, J = 5.8 Hz, IH); 7.50-7.53 (m, IH); 7.61 (s, br, IH); 7.71 (d, J = 8.8Hz, IH) 7.85 (d, J = 8.6Hz, IH); 7.92 (d, J =2.2, IH); 8.87 (s, IH). Example 123 5-Bromo-benzofurari-2-carboxylic acid [l-(2-phen5d-li?-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmetiiyi]-cafbamoyl}-etliykarbamoyl)-cyclopentyl]-amide MS m/z: 693,5 (M+H, monoisotopic). HPLC (method D): Rt = 13.14 min. IH-NMR (DMS0-d6). • (amongst the others): 0.97-1.12 (m, 4H|; 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m, 2H); 2.78-2.93 (m, 2H); 2.95-3.03 (m, IH); 3.75-3.84 (m,.2H); 4.40-4.48 (m, IH); 7.11-7.21 (m, 5H); 7.44 (t, J = 5.8 Hz, IH); 7.58-7.69 (m, 3H) 7.85 (d, J = 8.6Hz, IH); 8.06 (d, J =2.0, IH); 8.87 (s, IH). Example 124 7-/ert-ButyI~benzofi]ran-2-carboxyIic acid [l-(2-phenyi-l-ff-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl} -ethylcarbamoyl)-cyclopentylj-amide MS m/z: 671.6 (M+H*). HPLC (method D): Rt = 15.16 min. Example 125 6-Methyl-benzofuran-2-carboxylic acid [ I -(2-phenyl- IR'{[1 -(tetrahydro-pyran-4-ylinethyI)-piperidm-4-ylmethyl]-carbamoyl} -ethylcarbamoyl)-cyclopentyl] -amide MS ra/z: 629.5 (M+H. HPLC (method D): Rt = 12.69 min. Example 126 5-Methyl-beii2ofiiran-2-carboxylic acid [l-(2-phenyl-li;-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyI]-carbamoyI}-ethylcarbamoyl)-cycIopentyl]-amide MS m/z: 629.5 (M+H*). HPLC (method D): Rt = 12.66 min. IH-NMR (DMS0-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.44 (s, 3H) 2.63-2.71 (m, 2H); 2.78-2.93 (m, 2H); 2.95-3.03 (m, IH); 3.75-3.84 (m, 2H); 4.40-4.48 (m, IH); 7.11-7.21 (m, 5H); 7.29-7.33 (m, IH) 7.49 (t, J = 5.7 Hz, IH); 7.53-7.60 (m, 3H); 7.86 (d, J = 8.5Hz, IH); 8.76 (s, IH). Example 127 5-Iodo-benzofhraii-2-carboxyhc acid [l'(2-pheny]-lii-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yIi2iethyl]-carbamoyl}-ethylcarbamoyl)-cycIopentyl]-amide MS m/z: 741.5 (M+tf). HPLC (method D): Rt = 13.42 min. IH-NMR (DMSO-d6). ■ (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.89-1.96 (m, IH); 1.97-2.04 (m, 2H); 2.21-2.29 (m, IH); 2.63-2.71 (m, 2H); 2.78-2.93 (m, 2H); 2.95-3.03 (m, IH); 3.75-3.84 (ra, 2H); 4.40-4.48 (m, IH); 7.11-7.21 (m, 5H); 7.43 (t, J = 5.8 Hz, IH); 7.53 (d, J = 8.7 Hz, IH) 7.58 (s, IH); 7.76 (dd, J = 1.8 and 8.7 Hz, IH); 7.86 (d, J = 8.6Hz, IH); 8.22 (d, J =1.7, IH); 8.88 (s, IH). Example 128 5-/e-rr-ButyI-benzoi\iran-2-carboxylic acid [ 1 -(2-phenyl-1 J?- {[ l-(tetrahydro-pyran-4-ylmethyI)-piperidin-4-ybnethyl]-carbamoyl}-etfayIcarbamoyl)-cyclopentyl]-amide MS m/z; 671.5 (M+H. HPLC (method D): Rt = 14.90 min. Example 129 6-Iodo-benzo[i]thiophene-2-carboxyIic acid [l-(2-phenyl-lJ?-{[l-(tetrahydro-p3Tan-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl3-aniide MS m/z; 757.2 (M+lO. HPLC (method D): Rt = 13.85 min." Example 130 6-Chloro-ben2o[6]thiophene-2-carboxylic acid [i-(2-phenyl-lR-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethyIcarbamoyl)-cyclqpentyl]-amide MS mfz: 665A (M+H. HPLC (mefliod D): Rt = 13.32 min. IH-NMR (DMS0-d6). • (amongst the others): 0.97-1.12 (ra, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.87-1.94 (m, IH); 2.17-2.28 (m, IH); 2.65-2.71 (m, 2H); 2.79-2.87 (m. IH); 2.88-2.99 (m, 2H); 3.31-3,20 (m, IH); 3.76-3.84 (m, 2H); 4.42-4.49 (m, IH); 7.10-7.21 (m, 5H); 7.44 (t, J = 5.8Hz, IH); 7.49 (dd, J = 2.0 and 8.5, IH), 7.85 (d, J = 8.6 Hz, IH); 8.00 (d, J = 8.5 Hz, IH); 8.22 (d, J = 1.9 Hz, IH); 8.28 (s, IH); 8.93 (s, IH). Example 131 7-Bromo-benzo[&]thiophene-2-carboxylic acid [l-(2-phenyl-li!-{[l-(tetrahydro-pyran-4-yImethyI)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoy])-cyclopentyl]-ainide MS m/z: 709.4 (M+H, monoisotopic). HPLC (method D): Rt = 13.12 min. Example 132 7-Iodo-benzo[&]thiophene-2-carboxylic acid [l-(2-phenyl-l/?-{[l-(tetrahydro-pyran-4-yImethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide MS m/z; 757.4 (M+H. HPLC (method D): Rt = 13.38 min. Example 133 6-Trifluoromethyl-benzo[fe]thiophene-2-c3rboxylic acid [I-(2-phenyl-Iif-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yImethyI]-carbamoy]}-ethylcarbamoyI)-cyclopentyl]-amide MS mJz: 699.5 (M+H. HPLC (method D): Rt = 13.88 min. Example 134 7-Methyl-benzo[]thiophen6-2-carboxylic acid [l-(2-phenyl-li!-{[l-(tetrahydro-pyran-4-ylmethyI)-piperidin-4-ylmethyl3-carbamoyl}-ethylcarbamoyI)-cyclopentyl]-amide MS m/z: 645.5 (M+H). HPLC (method D): Rt 12.83 min. IH-NMR (DMS0-d6). - (amongst the othere); 0.98-1.12 (m, 4H); 1.36-1.82 (m, I4H); 1.87-1.95 (m, IH); J.95-2.06 (m, 2H); 2.19-2.29 (m, IH); 2.53 (s, 3H); 2.67-2.74 (m, 2H); 2.80-2.94 (m, 2H); 3.15-3.28 (m, 3H); 3.76-3.83 (m, 2H); 4.41-4.48 (m, IH); 7.10-7.23 (m, 5H); 7.29-7.33 (m, IH); 7.37-7.41 (m, IH); 7.44 (t, J = 5.7 Hz, IH); 7.86-7.8 (m, IH); 7.86 (d, J = 8.6 Hz, IH); 8.31 (s, IH); 8.86 (s, IH). Example 135 6-Meth6xy-benzo[6]thiophene-2-carhoxylic acid [I-(2-phenyi-l-([l-(tetrahydro-pyran-4-yhnethyl>piperidin-4-ylmethyl]-carbamoyI}-ethylcarbamoy])-cyclopentyI]-amide MS m/z: 661.5 (M+H. HPLC (method D): Rt = 12.32 min. Example 136 7-Trifiuoromethy!-benzo[&]thiophene-2-carboxylic acid [I-(2-pheiiyl-li?-{[l-(tetrahydro-pyran-4-yIiiiethyI)-piperidm-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-aniide MS m/z: 699.5 (M+H. HPLC (method D): Rt = 13.31 nun. Example 137 7-Chloro-benzo[Z»]thiophene-2-carboxylic acid [l-(2-phenyl-li;-{[l-(tetrahydro-pyran-4-ylniethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-aiiiide MS m/z: 665.4 (M+H. HPLC (method D): Rt = 12.99 min. Example 138 5-Methyl-ben2o[fr]thiophene-2-carboxylic acid [l-(2-phenyI-li?-{[l-(tetrahydro-pyran-4-ylmethyI)-piperidin-4-ylmethyl3-carbamoyl}-ethylcarbamoyl)~cyclopentyl]-amide MS m/z: 645.5 (M.+lt). HPLC (method D): Rt = 13.03 min. IH-NMR (DMSO-d6). • (amongst the others): 1.00-1.11 (m, 4H); 1.43-1.80 (m, 13H); 1.87-1.94 (m, IH); 1.95-2.04 (m, 2H); 2.18-2.28 (m, IH); 2.44 (s, 3H); 2.66-2.73 (m, 2H); 2.80-2.87 (m, IH); 2.90-3.00 (m, 2H); 3.14-3.27 (m, 3H); 3.75-3.84 (m, 2H); 4.41-4.50 (m, IH); 7.10-7.21 (m, 5H); 7.29-7.33 (m, IH); 7.47 (t, J = 5.8 Hz, IH); 7.75 (s, IH); 7.84 (d, J = 8.6 Hz, IH); 7.87-7.91 (m, IH); 8.19 (s, IH); 8.83 (s, IH). Example 139 6-MethyJ-ben2of6]thiophene-2-caiiboxylic acid [I-(2-phenyl-!-ff-{[l-(tetrahydro-pyran-4-ylmethyI)-piperidin-4-ylmethyl]-carbamoyl} -ethylcarbamoyl)-cycIopentyI] -amide MS m/z: 645.5 (M-t-H. HPLC (method D): Rt = 13.02 min. IH-NMR (DMSO-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.87-1.94 (m, IH); 2.17-2.28 (m, IH); 2.45 (s, 3H); 2.67-2.73 (m, 2H); 2.79-2.87 (m, IH); 2.88-2.99 (m, 2H); 3.31-3.20 (m, IH); 3.76-3.84 (m, 2H); 4.42-4.49 (m, IH); 7.10-7.21 (m, 5H); 7.28 (d, J = 8.2 Hz, IH): 7.47 (t, J = 5.6Hz, IH); 7.78-7.88 (m, 3H); S.22 (d, J = 1.9 Hz, IH); S.22 (s, IH); S.SO (s, IH). Example 140 Ben2ofuran-2-carboxyIic acid [l-(2-phenyl-l -{[li;-(tetrahydro-pyran-4-yimethyI)-pjperidin-4-ylmethy]] -carbamoyl} -ethyl carbamoy!)-cyclopentyl3-amide Example 141 6-Fluoro-benzo[i]thiophene-2-carboxyIic acid [l-(2-phenyl-l-{[li?-(tetrahydro-pyTan-4-ylmethyl)-piperidin-4-yhnethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide MS m/z: 649.3 (M+H. HPLC (method D): Rt = 12.51 min. IH-NMR (DMS0-d6). • (amongst the others): 0.97-1.12 (m, 4H); 1.42-1.73 (m, 12H); 1.74-1.81 (m, IH); 1.87-1.94 (m, IH); 2.17-2.28 (m, IH); 2.45 (s, 3H); 2.67-2.73 (m, 2H); 2.79-2.87 (m, IH); 2.88-3.00 (m, 2H); 3.31-3.20 (m, IH); 3.76-3.84 {m, 2H); 4.42-4.49 (m, IH); 7.10-7.21 (m. 5H); 7.34 (m, IH); 7.47 (t, J = 5.8Hz, IH); 7.84 (d, J = 8.6, IH); 7.95- 7.98 (ra, IH); 8.00-8.04 (m, IH); 8.27 (s, IH); 8.89 (s, IH). Example 142 l-MethyI-17/-indole -2-carboxylic acid [l-(2-phenyl-l-{[li;-{tetrahydro-pyran-4- ylmelhyl)-piperidin-4-ylmeth3]-carbamoyl}-ethylcarbaiiioyl)-cyclopentyl]-aniide Example 143 7-Chloro-l-methj4-li/-indole -2-carboxylic acid [Iif-(2-phenyl-l-{[l-(tetrahydro-pyraii-4- ylinethyl)-piperidin-4-ylinetiiyl]-carbamoyI}-ethylcarbamoyl)-cyclopentyl]-amide Example 144 5-Chloro-3-me1hyl-benzDfuiaii-2-caiboxylic acid [ii?-(2-phenyl-l-{[l-(tetraiiydTo-pyran- 4-yhnethy])-piperidiii-4-ylmethyi]-carbainoyl}-ethylcarbamoyl)-cyclopentyI]-amide Example 145 6-Diethyl amino-benzofliran-2-carboxylic acid [ 1 -(2-phenyl-1 - {[ 1 i?-(tetrahydro-pyran-4- ylmethyI)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyi]-aniide MS m/zi 686.4 (M+H. HPLC (method D): Rt = 8.76 mm. Example 146 5-Methoxy-benzofiiran-2-carboxyIic acid [l-(2-phenyl-l-{[li!-(tetrahydro- pyran-4-ylmethyl)-piperidiii-4-ylmethyl]-carbamoyl}-ethylcarbainoyl)-cyclopentyl]-amide MS m/z: 645.5 (M+H. HPLC (method D): Rt = U .98 min. Example 147 ' 5-DiethyIamino-benzofiiran-2-caiboxylic acid [l-(2-phenyl-l-{[li2-(tetrahydro-pyran-4- yImethyI)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-ainide MS m/z: 686.6 (M+H. HPLC (method D): Rt = 8.58 min. Example 148 3,5,6-Trimethyl-benzofuran-2-carboxylic acid [l-(2-phenyl-l-{[li?-(tetrahydro-pyTan-4- ylmethyl)-piperidiii-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopeiityi]-amide Example 149 ■Naphthalene-2-carboxylic acid [l-(2-phenyl-l-{[]ii-(tetrahydro-pyran-4-ylmethyl)- piperidiii-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopenty]]-amide MS m/z: 639.5 (M+H. HPLC (method D): Rt = 13.14 min. Example ISO 5-Bromo-naphthalene-2-carboxylic acid [l-(2-phenyl-l-{[lii-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-aniide MS m/z: 703.4 (M+H, monoisotopic). HPLC (method D): Rt = 13.53 min. Example 151 Naphthalene-2-carboxyIic acid [l-(2-phenyl-l-R-{[l-(tetrahydro-pyran-4-ykDethyl)-piperidin-4-ylmethyl]-carbamoyl} -ethyl carbamoyl)-cyclopentyl]-amide MS m/z: 625.5 (U+it). HPLC (method D) Rt = 12.29 min. IH-NMR (DMS0-d6). 5 (amongst the others): 0.94-1.07 (m, 4H); 1.43-1.72 (m, 12H); 1.76-1.83 (m, IH); 1.90-2.00 (m, 3H}; 2.25-2.34 (m, IH); 2.55-2.63 (m, 2H); 2.82-2.90 (m, 2H); 2.94-3.01 (m, IH); 3.74-3.83 (m, 2H); 3.91 (s, 3H); 4.42-4.49 (m, IH); 7.10-7.21 (m, 5H); 7.23-7.27 (m, IH); 7.52 (t, J = 5.7 Hz, IH); 7.58-7.67 (m, 2H); 7.80 (d, J = 8.6, IH); 7.95-8.06 (m, 4H); 8.53 (s, IH); 8.78 (s, IH). By analogous procedure to that described in Example 117, the following compounds have moreover been prepared: Example 152 Benzo[6]thiophene-2-carboxylic acid [l-(2-phenyM(R)-{[l-{tetrahydro-pyran-4-yImethyl)-azetidin-3-ylmethyl]-carbamoyl)-ethyIcarbamoyi)-cyclopentyl]-amide, by using ethyl 3-azetidincarboxylate in place of ethyl 4-piperidincarboxylate. MS (m/z): 603.3 (MH*). HPLC (method A): Rt = 3.63 mm. Example 153 6-Bromo-naphthalene-2-caTboxylic acid [l-{l(R)-{[l-(4-methyl-tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl] -carbamoyl} -2-phenyl-ethyIcarbamoyl)-cyclopent543-amide, by using C-[l-(4-Methyl-tetrahydro-pyTan-4-yImethyl)-piperidin-4-yl]-methylamine prepared as described in Example 117a). MS (m/z): 617.4 (MH*, isotopic pattem of Br). HPLC (method A): Rt = 4.01 min. Example 154 6-Bromo-naphthalene-2-carboxylic acid [ 1 -(1 (R)-{[ 1 -(5-ethyl-[l,3]dioxan-5-yhnethyl)-piperidin-4-ylmethyl]-carbamoyl}-2-phenyl-ethylcarbamoyl)-cyclopentyl]-amide, by using 5-ethyl-[l,3]dioxane-5 carboxylic acid in place of 4-tetrahydropyrancarboxylic acid. Example 155 6-Bromo-naphthalene-2-carboxyHc acid [l-(l(R)-{[4-methyl-l-(4-raethyl-tetrahydro-pyraii-4-ylmethyl)-piperidm-4-ylmethyI]-carbamoyl}-2-phenyl-ethylcarbamoyi)-cyclopentyl]-amide, by using C-[4-methyl-l-(4-methyl-tetrahydro-pyran-4-ylmethyl)-piperidiii-4-yl]-methylamine prepared as described in Example 117a). Example 156 6-Bromo-naphthalene-2-carboxylic acid [1 -(1 (R)- {[4-metiiyl-l -(tetrahydro-pyran-4-ylmethyI)-piperidin-4-ylmethyI3-carbamoyl}-2-phenyl-ethylcarbamoyl)-cyclopentyl]-amide, by using C-[4-methyl-l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yl]-methylamine prepared as described in Example 117a). MS (m/z): 717.4 (MH^, isotopic pattern of Br). HPLC (method A): Rt = 4.16 min. HPLC methods Mobile phase: A = H2O + 0.1%TFA; B =MeCN +0.1% TFA METHOD A Column; Zorbax™ SB-18, 3.5μm lOOA (50 x 4.6 mm) Gradient: irom A/B = 95/5 to AB = 5/95 in 6.5 min +1 min isocratic Flow rate: 3 ml/min X=220, 270 nm. METHOD B Column: Platinum'™ RP-I8. 3 m, lOOA (33 x 7 mm) Gradient: from A/B = 95/5 to ATB = 5/95 in 6.5 min +1 min isocratic Flow rate: 3 ml/min X=220,270 run. METHOD C Column: Jupiter™ CI 8, 5μm (250 x 4.6 mm) Gradient: irom A/B = 85/15 to A/B = 5/95 in 20 min Flow rate: I ml/min λ=210nm. METHOD D Column: Symmetry™ 300 018, 5 μm (250 x 4.6 mm) Gradient: from A/B = 85/15 to A/B = 5/95 in 20 mm Flow rate: 1 ral/min X.=210mn. METHOD E Column; Protein & Peptide Vydac™ CI 8 (250 x 4.6 mm) Gradient: from A/B = 80/20 to A/B = 20/80 in 25 min + A/B = 20/80 for 10 min Flow rate: 1 ml/min ^=230 nm. METHOD F Column: Inertsil ODS-3 (GL Sciences), 3 pm (50 x 3 mm) (250x4.6 mm) Gradient: from A/B = 80/20 to A/B = 30/70 in 9 min Flow rate: 0.8 ml/min ^=230 mn. List of Abbreviations In the present description the following abbreviations have been used: Ac5c, aminocyclopentanecarboxylic;Ac6c, aminocyclohexanecarboxylic; AcOEt, ethyl acetate; Boc, N-/erf-butyioxycarbonyI;BSA,N,0-bis(trimethyisilyi)acetamide; DCM, dichloromethane; DIPEA, N,N-diisopropylethylamine; DMF, N,N-dimethylfonnamidfi; EDO, l-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride; EtOAc, ethyl acetate; HOBt, l-hydroxybenzotriazole; TEA, trietfaylamine; TEMPO, 2,2,6,6-tetramethyI- 1-piperidinyloxy; TFA, trifluoroacetic acid; THF, tetrahydrofuran; TMSCl, trimethylsilylchioride; Z, N-benzyloxycarbonyl. The evaluation of the antagonist activity on NK-2 receptors has been assessed by binding and iimctional tests according to that already described in literature in relation to NK-2 antagonists. In particular, the affinity of the present compounds for the human NK-2 receptor has been assessed by a binding test using Chinese hamster ovary (CHO) cell membranes transfected with NK-2 receptor of hxmian ileum together with ['^^I]NKA (Am^sham, aspecific activity 2000 Ci/mmol) radiobinder at the concentration of 100 pM in competition studies. The test substances have been tested within a concentration range from 0.01 nM to 10 nM. At the end of the incubation time (30 min, 20°C) the samples have been filtered and radioactivity has been determined using a gamma-counter. The data shown in the following Table I have been obtained for some compounds of general formula (I) and refer to the afEinity values of human NK-2 receptor: The present compounds of formula (I) can be handled according to the common pharmacopoeial techniques in order to prepare formulations suitable for oral, intranasal, parentheral, sublingual, inhalatory, transdermic, local or rectal use according to the data known in literature for this kind of products; these formulations comprise oral fomiulations, such as tablets, capsules, powders, granulated preparations, and oral solutions or suspensions, formulations for sublingual administration, for intranasal administration, aerosol formulations, implantations, formulations for subcutaneous, intramuscular, intravenous, intraocular-and rectal administration. Xhe effectiva doses, are 0.1 to 50 mg/kg of body weight. For humans the effective dose may preferably range from 0.5 to 4000 jng/day, in particular from 2.5 to 1000 mg according to the age of patients and to the type of treatment. The treatment is performed by administering to the patient the required amoimt 1 to 4 times-per-day for periods of time up to 2 weeks or in any case until remission of symFjtoms; for chronic pathologies, administration can be prolonged for significantly longer periods of time according to the physician judgement Thanks to their high antagonist activity to tachykinins NK-2 receptor, the present compounds are useful in tbetreatment of diseases in which Neurokinine A plays a pathogenetic role, and namely in the following pathologies: - chronic obstructive respiratory pathologies, such as asflima and allergic rhinitis, cough, bronchitis; - ophtahnic pathologies, such as conjunctivitis or vitreoretinopathy; - skin problems such as allergic and contact dennatitis, atopic dermatitis, eczema, itch, psoriasis, bums, in particular solar bums; - intestinal disorders, such as irritable colon, ulcerous colitis, Crohn disease, diarrhoea; - gastric diseases, such as nausea or emesis; - urinary pathologies, such as prostatitis, spinal reflex bladder, urinary incontinence, cystitis, urethritis, nephritis, erectile dysiunctions; - tumoral pathologies, autommunitary diseases or diseases associated to AIDS; - pathologies of the nervous central system, such as anxiety, depression, schizophreny, dementia, epilepsy, Parkinson's syndrome, Alzheimer's diseases, drugs and alcohol addiction, alcoholistn, Huntington's chorea, neurodegenerative diseases and somatic disorders, such as stress; - treatment of pain, in particular visceralgia, neuritis, neuralgia; - cardiovascular diseases, such as hypertension, edemas, thrombosis, angina, vascular spasmus; - inflammatory, such as arthritis, rheumatoid arthritis. WE CLAIM: 1. Linear compounds of general formula (I) comprising an alfa-alfa-disubstituted amine acid and at least an amino group capable of giving basic characteristics to the compounds wherein: XI is a-CO- group; Ri is an aromatic group selected from the group consisting of biphenyl, phenyl-ethylene, naphthyl, phenyl-thiophene, benzothiophene, benzofurane, and indole possibly N- substituted by a CI -C6 alkyl group, which can be possibly sutetituted by one, two or three groups independently selected irom the group consisting of halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms, C1-C6 alkyloxy, OH, NHRIO, and N{R10)2, wherein RIO is selected from H and C1-C6 alkyl; R6 is H; the aminoacidic residue of general formula (III) is an a,a-disubstituted glycine-type residue selected from the group consisting of 1-aminocyclohexane-1-carboxylic (Ac6c), l-aminocyclopentane-l-caiboxylic acid (Ac5c), l-aminoirdane-l-carboxy)ic acid (l-Aic), l-aminocyclopenlan-3-ene 1- carboxylic acid (Ac5c), 2-melhyl-phenylalanine, 2-methyl-2-ethyI-glycine, R2 is a phenyl-methyl group having the phenyl group possibly substituted by a CI-C6 alky] group," X2 is selected from -CONH- and CH2NH-; R3 includes at least one basic amino groiqj having the following formula: ~R4 - X3-RS wherein: - R4 is selectwJ from the group consisting of a group - - R5 is selected from: a) an aliphatic heterocycle selected from the group consisting of piperidine, pyrrolidine, morpholine, diazepan, tetrahydropyran, and l,4-dioxa-8~azaspiro[4,5]decane, possibly substituted by one or two groups selected from CI-C6 alkyl, CI-C6 alkyloxy, OH, and cyanomethyl; b) an azetidine substituted by a group -(CH2)n-1^17» wherein R17 is tetrahydropyran; c) a piperidine possibly C-substituted by a C1-C6 alkyl group, and substituted by a group X5-R] 8 wherein X5 is a bond or it is selected from the group consisting of-C(R11 )CR12)-, -CO, -CH2CH2-, and -COCH2-, and RI8 is a group selected from fluophene, tetrahydropyran, tetrahydrotiiiopyran, pyrrolidine, cyclohexane, cyciopentane, and 1-3-dioxane, possibly substituted by one or more group selected from C1-C6 alkyl, -NHRIO, and -N(R10)2, wherein RIO, Rl 1 and R12 are selected from H and linear or branched Cl-C6 alkyl; d) a piperazijie possibly C-substituted by one or two CI -C6 alkyl group, and possibly N-substituted by a group selected from -CH2CN and X4-R16, wherein X4 is a bond or it is selected from -CH2- and -COCH2-, and R16 is selected from the group consisting of pyridine, thiophene, tetrahydropyran, moipholine, tetrahydrofurnane, and 1,3-dioxane; e) an amino group selected from -NRllRH and -NH-(CH2)m-NRUR12, wherein RU and R12 as defined above and m ranges from 3 to 6; f) an amino-cyclohexane or a cyclohexane possibly substituted on the ring by the groui NRnR12, wherein Rll and Rl 2 are as defined above; g) an heteroaromatic group represented by pyridine. 2. The compounds of general formula (I) according to claim 1, wherein: XI is a -CO- group; RI is an aromatic group selected from the group consisting of phenyl-ethylene, naphthyl, benzothiophene, and benzofurane, possibly substituted by one, two or three groups independently selected from halogen, C1-C6 alkyl possibly substituted by not more than three fluorine atoms, C1-C6 alkyloxy, OH, NHRIO, and N(R10)2 wherein RIO is selected from H and C1 -C6 alkyl; the amino acidic residue of general formula (m) is selected from 1 -aminocyclohexane-1 - carboxylic acid (Ac6c), and 1-aminocyclopentane-l-caiboxylic acid (Ac5c); R6 is H; R2 is phenyl-methyl; X2is-C0NHs R3 includes at least one basic amino group and it is the following group: ~ R4 - X3- R5 wherein - R4 is selected from -(CH2) wherein n ranges from 1 to 3, and piperidine possibly substituted by a C1-C6 alkyl group; X3 is a bond or it is a group selected from -CO- and -CH2-; R5 is selected from: a) an aliphatic heterocycle selected from piperidine and tetrahydropyran, pcwsJbly substituted by one or more C1-C6 alkyl groups; b) a piperidine possibly C-substituted by a C1-C6 alkyl group, substituted by a group X5-Rl 8 wherein X5 is a bond or it is a group selected from -C(R11)(R12)- and -CO-, and R18 is a group selected from tetrahydropyran, cyclohexane and 1-3-dioxane, possibly substituted by one or more groups selected from C1-C6 alkyl, -NHRIO, and -N(R10)2, wherein RIO, RI1 and RI2 are selected from H and linear or branched C1-C6 alkyl; c) a piperazine possibly C-substiluted by one or two C1-C6 alkyl groups, and possibly N-substituted by a group X4-R16 wherein X4 is -CH2-, and R16 is selected from tetrahydropyran and 1 ,3-diotane. 3. Th compounds of general formula (0 according to claim 1, wherein the ^id compounds are defined by the following fonnulas: Nα[Nα(benzo[fe]thiophenyl-2-ylcarbonyl)-l-aminocyclopentane-l-caTt>onyl]-D- phenylalanine-N-[3(moipholin-4-yl)propyl]amide (1 R,3 S)-acid-hr{N'^°(benzo[b]thiophen-2-yl -caibonyl)-1 -aminocyc!opentan-l -carboxy ] - D-phenyiatanil}-3-aminocyclopentan-l-caiboxyHc-N-[(lS,2S)-2-aminocyclohexyI] amide hr{N"[N"(biphen-4-ylcarboxy)-l--aininocyclopentan-l-caiboxy]-D-phenylalanil}-(lR,3S)- 3-aminocyclopentane-]-carboxylic-acid-N-((lS,2S)-2-aminocyclohexyl)amide trifluoroacetate salt >P'{N"[N'XN-(methyl)indol-2-yicaiboxy)-l-aminocyclopentan-l-<:arboxy> phenyIa]anyl}-(lR,3S)-3-aminocyclopentane-l-carboxylic-acid-N-({lS,2S)-2-amino cyclohexy!)amide trifluoroacetate salt N^{N"[N'[4-(methyl)cyimamoyI]-1 -aminocyclopentan- i -carboxy]-D-phenyIa!anyl} - (lR,3S)-3-aminocyclopentane-1 -carboxylic-acid-N-(( 1 S,2S)-2-aminocyclohexyl)am!de Irifluoroacetate salt N^{N'[N*'(benzoftjran-2-ylcarboxy)-!-aminocyciopentan-!-carboxy]-D-phenyialanyI}- (1 R,3 S)-3 -aminocyclopentane-1 -caiboxyIic-acid-N-(( 1 S,2S)-2-aminocyclohexy 1) amide trifluoroacetate salt N"[N"(4-(metiiyl)cinnamoyl)-(R,S) I -aminoindane-1 -carboxy ]-D-pheiiyIa!anine amide-N- [(lS,3R)-3-(moipholin-4-ylmethyl)cyc!openty!] Nα{NαEN"(benzo[bthiophen-2-ylcarbonyl)-I-aminocyclopentan-l-carboxy]-D- pheny}alanyl}-(lR,3S)-3-aminocyclopeniane-l-caiboxylic-acid-N-((lS,2S)-2- dimethylaminocyclohexyi)amide hydrochloride salt N^{N*tN"(ben2o[5]thiophen-2-ylcarbonyl)-l-aminocyclopenlan-l-caTboxy]-D-4-methyl- phenylalanyl}-(lR,3S)-3-aminocyclopentane-l-carboxyIic~acid-N-(lS,2S)-2-dimethyl aminocyclohexyl)amide hydrochloride salt N^IN^tN^t^-methyl-cinnamoyO-I-aminocycIopentan-I-caiboxyJ-D-phCTylalanyl}- C1 R,3 S)-3-aminocy clopentane-1 -caiboxylic-acid-N~((l S,2S)-2- dimetfiylaminocyclohexyl)amide hydrochloride salt {N'αI°(benzofur-2-ylcarboxy)-l-aminocyclopentan-l-carboxy]-D-phenylalanyI}- (lR,3S)-3-ammocyclopentane-l-carboxy!ic-acid-N-C(IS 2-2- dimethy!aminocyclohexyl)amide hydrochloride salt Nα{Nα[Nα(biphen4-y]carbonyl)-l-aminocyc!opentan-I-carboxy]-D-phenylalanyl}- (1 R,3S)-3-aminocyclopentane- l-cajboxylic-acid-N-C(l S,2S)-2- dimethylaminocyclohexyl)aiiiide hydrochloride salt K'{N'^[N"(N-(methyI)indo]-2-ylcarboxy)-l-aminocycIopei]tan-l-carboxy]-D- pheny lalanyl} -(1 R,3 S)-3-aminocyclopentane-1 -carboxyIic-acid-N-(( 1 S,2S)-2- diinethyiaininocyclohexyl)aniide hydrochloride salt >r{N°[N"(benzo[fe]thiophen-2-ylcarbonyl)-CR)-a-methy!-a-ethylglycyl]-D- phenylalanyl} -(lR,3S)-3-amino cyclopentane-1 -carboxy!ic-acid-N-((l S,2S)-2- aminocyclohexy!) amide trifluoroacetate salt N^{N"[N"(4-methyIciraiarnoyl)-(R)-a-metityl-a--ethyIglycyl]-D-phenyIalanyl}.(lR,3S)-3- amino cyciopentane-l-carboxy1ic-acid-N-((lS,2S)-2-aminocyclohexyl) amide trifluoroacetate salt >r{N"fN"(biphenyl-4-carboxy)-l -aminocyclopentan-1 -carboxy]-R-3(4(methyl) pheny!)alanyl}-(lR,3S)-3-aminocyclDpentane-l-carboxylic-acid-N-((lS,2S)-2- aminocyclohexyl)amide hydrochloride salt N^{N"[hr'(N-(methyl)indol-2-ylcarboxy)-l-aminocyc]opentan-l-caTboxy]-R-3-(4- inelhyl)phenyl)alanyl}-(lR,3S)-3-aminocyc! aminocyc!ohexyl)amide hydrochloride salt Nα{Nα[Nα(4-(methyl)cynnamoyl)-l-aminocyclopentan-l-carboxy]-R-3[4- methyl)phenyl]alanyI}-(lR,3S)-3-aminocyclopentane-I-carboxylic-acid-N-((]S,2S)-2- aminocyclohexyl)amide hydrochloride salt N"[N"{benzo[fc]ti]iophen-2-yl-carbonyl)-1 -aminocyclohexan-1 -caiboxy]-D-phenyla!anine- N- (3 -[bis(n-butyl)amino]propyl} amide N°[>r^(benzo[6]thiophen-2-yl-carbonyl)-l-aminocyclohexan-l-caiboxy]-D-phenylaianine- N-p(moipholin -4-yl)pn^yl]amide acid-3-c£s-N^{N"[N"(benzo[i]thiophen-2-ylcarbonyl)-l-aminocyclohexan-l-carboxy]-D- phenyialamI}aminocyc(ohexan-l-cart>oxylic-N-{(lR,2S)-2-aminocycIohexyI)amide N^{N"[N'\benzo[fc]thiophen-2-ylcarbonyl)-1 -aminocyclohexan-1 -carboxy]-D- phenylalanyl}-3-cts-aminocyclohexan-l-carboxylic-acid-N-(5-aininopentyl)-amide trifluoroacetate salt Nα[NαCbenzo[6]thiophen-2-ylcaibonyl)-l-(R)-amino-idane-l-caroxy]-D-phenylalanine- N-[3Cmoipholin-4-yl)propyl amide Nα[Nα(benzo[6]thiophen-2-ylcarbonyl)-l-aminocyclopentane-l-carboxy]-L- phenylalanme-N-f3(moipholin'4-yl)pr{^yl Jamide (!R,3S) acid-3-N^{N"fN"(benzo[6]thiophen-2-ylcarbonyl> 1 -aminocyclohexan-! - carboxy]-D-phenylalanil}aminocyclopentane-l-cari)OxyHc-N-(lS,2R)-2-ammocyclohexyI) henylalanil} aminocyclohexan-1-carboxylic -N-(2-cis-ammocycIohexyl) amide >r{N"[N"(benzo[6]thiophen-2-ylcarbonyl)-l-aminocyclohexan-l-carboxy]-D- phenylalanil} -(L-(4R)amino-proHne-N-ClR,2R)-aminocyclohexyl) amide acJd-3- cis-N''{>r[N"(benzo[fe]th!ophen-2-ylcarbonyl)-1 -aminocyclohexan-1 -carboxy]-D- phenylalanil}-aminocyclohexan-l-carboxylic--N-[(lS,2S)-2-aminocycIohexyl]amide acid-3-cis-N^{N"[N"(benzo[d]ttiiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy3-D- phenyIaIaniI}aminocyclohexan-l-carboxylic-N-[(lS,2R)-2-dimethy!aminocycIohexyl] amide acid-3-cis-{N"[N"α(benzo[fe]thiophen-2-ylcarbonyl)-1 -aminocyclopentan-1 -carboxy]-D- phenylalanil} aminocyclohexan-1 -carboxylic-N- [(1 S,2R)-aminocycIohexyl] amide acido-3-cis->r'{N'^[N"(benzo[i>]thiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy]- D-phenyIaianil)aminocyclohexan-l-carboxyHc-N-{(IS,2S)-aminocycIohexyI] amide N"fN'Cbenzo[6]thiophen-2-ylcarbonyl)-l-aminocyciopentano-l-carboxy]-D-phenylaIaiiiiia amide-N-Kl S,3R)-3-(4-(methyl)piperazin-1 -yl)melhyl)cyclopentyl) N"[N'*(ben2X)[bthiophen-2-yIcarbonyl)- l-aminocyclopentan-1 -carboxyj-D-phenylaianina amide-N-[(lS,3R)-3-(4-(methyl)piperazin-l-y!)carbonyi)cycIopentane N"[N"Cben2o[i)fliiophen-2-ylcaibony1)-D-a-mediylphenyIalanil]-D-phenyla!anina-N-[3- (moipholin-4-yl)propyl]ami acid-3-cis-N"[N'*(benzo[6]Aiophen-2-yIcaibony!)-l-aminocyclohexan-l-carboxy]-D- phenyla!anil}aminocyclohexan-l-caiboxylic-N-((lR,2S)-2-methylaminocyclohexyl)amide Nα[Nα(benhze[b]2-ylcarbonyl)-l-aminocyc!opentan-l~carboxy]-D-phenylalaniI}- L-(4R)araino-proIina-N-(-2-cis-aminocyclohexyf) amide (IR,3S)aci-Nα{Nα0'enzo[6]1hiophen-2-ylcarbnyI)-l-aminocyclopentan-l- carboxy]-D-pheny lalanil} aminocyclopentane-1 -caroxylic-N-(2-cis- aminocyclohexyl)anude (lS,3R.)-i-N{Nα[Nαbenzo[bthiophen-2-ylcarbonyl)-l-aminocyclopentan-l-carboxy]-D- phenyIa!anil}-3-{[lS-((2S)-aminocyclohexyl)amino}methyl}aminocyclopentane acid-3-cis-N{N"[N"(benzethiophen-2-yIcarbonyl)-l-aminocyclopentan-l-carboxy]-D- phenylalanil} aniinocyclohexan-l-carboxy]ic-N-((IR,2S)-2-dimethy1amino(^c!ohexyI) amide (lR,3S)acid-3-N{N°[N^(benzof6]thiophen-2-ylcarbonyl)-l-aminoco'clohexan-l-carboxy]- D-phenylalanil}amiiiocyclopentan-l-carboxylic-N-((lR,2R)2-aminocyclohexyl) amide Biphenyl-4-carboxylic acid, {1 -[ 1 -(3-moipholin-4-yl-propylcarbamoyl)-2-(R)-phenyI- ethylcarbamoyl] -cyclopentyl} -amide Benzofiiran-2-carboxylic acid, {l-[l-(3-mo!pholin-4-yl-propylcarbainoyl)-2-(R)-phenyl- ethylcarbamoylj-cyclopentyl} -amide Benzo[63thiophene-2-carboxylicacid, methyl-{l-[l-(3-moipholin-4-y!-propylcarbainoyl)- 2(R)-phenyl-ethylcai1>amoyl]-cycIohexyl}-amide l-[3-(3,4-dichlorpphenyl)-aciyloylamino}- 4-yl-propylcarbamoyl)-2-(R)-phenyl-ethyl]-amide Benzo[i»]thiophene-2-carboxylicacid {l-Ilff-(3-inorpholin-4-yl-propylcarbamoyl>-2- phenyl-elliyIcarbainoyl]-cyclopent-3-enyl}-amide l-Methyl-l^-indole-2-carboxylicoacido, {l-[l-(3-morpholin-4-yl-propylcarbainoyI)-2- (R)-phenyl-ethylcartjamoyl]-cyclopentyl}-aiiiide Benzo[&]thi(^hene-2-carboxylic acid (l-{l-[3-(2,6-dimethyl-moipholin-4-yl)- propylcarbamoyl]-2-(R)-phenyl-ethylcarbamoyl} -cyclohexyl)-amide lH-indoIe-2-carboxylicacid, {l-[l-(3-moipholin-4-yI-propylcarbainoy!>2-(R)-phenyl- ethylcarbamoyl]-cyclopentyl} -amide l-[3-(3,4-dibrom6phenyl)-acryloylamino]-cyclopentanecaTboxylic acid|l-(3-moipholin-4- yi-propylcarbamoyl)-2-(R)-phenyI-etiiyl]-amide 5-pheny!-thiophene-2-carboxylicacid, {l-[l-(3-morpholin-4-yl-propyicarbamoy!)-2-(R)- phenyl-etlcarbamoyl]h-cyclopenfyI} -amide Benzo[6]thiophene-2-carboxyiic acid, (l-{l(RH3-('*-mettiyl-[l,4]diazepan-i-yl)- propylcarbamoy!]-2-phenylethyl caibamoyl}-cyclopentyl)-amide TFA salt Benzo/fe]fliiophene-2-carboxylic acid fl-{l(R)-[3-(4-methoxy-piperidin-l-yl)- propylcart)amoyl]-2-phenyl-ethylcarbamoyl}-cycIopentyl)-amide TFA salt Ben/;o[6]thiophene-2-cari)oxy!icacid(!-{l-(RH3-(4-hydroxy-piperidin-I-yI)-propylcarbainoyI]-2-pheny!ethylcari)ainoyl}-cyclopentyi)-amide. Benzo[i»]fliiophene-2-cart>oxylicacid(l-{l(R)-[3-(l,4-dioxa-8-a2a-spiro[4.5]dec-8-yl)-propylcarbamoyl]-2-phenyI-ethylcarbainoyl}-cyclopentyl)-amide TFA salt Benzo[i]thiophene-2-caTbQxyIicacid(l-{lCR)-t3-(3,5-cM-dimethylpiperazin-l-y!)-3-oxo-propylcarbainoyl]-2-phenyl-ethylcarbamoy!)-cycJqpentyl)-amide TFA salt Benzo[6]thiophene-2-caTboxyiicacid(l-{lCR)-[3-oxo-3-(4-pyridin-2-yl-piperazin-l-yl)-propylcarbamoyl]-2-phenyl-ethylcaibanioyI}-cyclopentyl)-3mide 6-Bromo-n^hthalene-2-carboxylicacid(l-{I(RH3-oxo-3-(4-pyridin-2-yl-piperazin-l-yl)-propylcaibamoyl]-2-phenyl-ethy!carbainoyI}-cyclopentyl)-amide TFA salt 6-Bromo~benzo[fr]tiiiophene-2-carboxylic acid (l-{l(R)-[3-oxo~3-(4-pyTidm-2-yl-piperazin-1 -yl)-pTopyicarbamoyi]-2-phenyl-ethylcarbainoyl} -cyc!opentyi)-amide Ben7;o[i)]aiiophene-2-carboxyHcacid []-(l(R)-{3-oxo-3-[4-(tetrahydro-pyian-4-ylmethyl)-pipera2in-l-yI]-propylcaii)amoyl}-2-pbeny]-etfiylcaibamoyI)-cyclopenty?j-amide TFA salt Benzo[6]thiophene~2-caTboxy!ic acid [l-(l(R)-{3-oxo-3-[4-(tetrahydro-pyran-4-y1)-piperaz!n-l-yl]-propy]cari)amoyl}-2-phenyl-etiiylcaibamoyl)-cyclopentyl]-amide TFA salt Beiizo[fe]tliiophene-2-cari>oxylicacid(l-{l(RH3-(4-[l,31dioxan-5-ylmethy!-piperazin-I-yl)-3-oxo-propylcaibamoyI]-2-phenyl-ethylcarbamoyl}-cycloopentyl)-anMde TFA salt Benzo[6}thiophene-2-carboxylic acid [l-(l(R)-{[l-(l-amino-cyclopentanecarbonyl)-piperidin-4-y!methyl]-carbamoyl}-2-pheny!-ethyIcaibamoyl)-cyclopentyi]-amide Benzo[&]fliiophene-2-caiboxylic acid [l-(l(R)-{3-oxo-3-[4-(tetrahydro-furan-2(R)-ylmethyl)-piperazin-1 -yl]-propylcaibamoyI} -2-phe!iyl-ethylcaibamoyl)-cyclopenlyl] -amide TFA salt Benzo[63thiophene-2-caiboxylicacid{l-(l(R)-[3-{4-cyanomethyl-piperazin-l-yl)-3-oxo-propyIcarbainoy!]-2-phenyI-ethylcaibamoy]} -cyclopentyl)-amide Benzo[&]thiophene-2-carboxylicacid{l-[2-phenyl-I(R>-(l-pyridir-2-ylmethyl-piperidin-4-ylcaibamoy1)-ethylcarbamoyI]-cyciopenty!}-amide TFA salt. Benzo|;fc]Uiiophene-2-caiboxylic acid [l-(2-phenyl-l(R)-{l-[2-(tetiahydro-pyran-4.y!)-ethyl]-piperidin-4-ylcarbamoyl)-ethylcarbamoyl)-cycIopentyl]-amide TFA salt 6-Bromo-n^hthalene-2-carboxylic acid (l-{l(R)-[(l-ethyl-piperidin-4-ylmethyl)-carbamoyl3-2-phenyl-ethylcarbamoyI}-cycIopentyl)-amide Benzo[6]thiophene-2-carboxylic acid {1 -[2-phenyl-1 (R)-( {1 -[2-(tetrahydro-pyTan-4-yl)-ethyl]-piperidin-4-ylmethyi} -carbamoyl)-ethylcarbamoyl]-cycIopentyI J-amide Benzo[6]thiophene-2-carboxyiic acid (1 -{1 (R)-[(l -cyclohexylmethyl-piperidin-4-ylmethyl)-carbamoyl]-2-phenyl-ethy]carbamoyl}-cycIopentyl)-amide Benzo[ft]thiophene-2-carboxylic acid [ 1 -(2-phenyM(R)-{[I-(tetrahydro-thiop3Tan-4-y])-piperidin-4-ylmethyl]-carbamoy1}-ethylcarbainoyl)-cyclopentyI]-ainide TFA salt Benzo[i»]thiophene-2-carboxylic acid [I-(2-phenyi-I(R)-{[l-(tetrahydro-lhiopyran-4-ylmethyl)-piperidin-4-yImethyl]-carbamoyl}-ethylcarbamoyI)-cyclc^ntyl}-amide I-((E)-3-p-Tolyl-acryloylamino)-cyctopentanecarboxylic acid {2-phenyl-](R)-[(l-thiophen-2-ylinethyl-pjperidin-4-ylmethyi)-caibamoyl]-etiiyl}-amide TFA salt 6-Broino-naphthalene-2-carboxylicacid(l-{2-phenyl-l(R)-[2-(l-pyrrolidin-2(S)-ylnieihyl-piperidin-4-yl)-ethy]caibamoyl]-ethyIcarbamoyl}-cycIopentyl)-amide TFA salt 6-Bromo-naphthalene-2-carboxylicacid(l-{2-phenyI-l(R)-[(piperidin-4-ylmethyl)-caibamoyl] -ethylcaibamoyl} -cyclopentyl)-amide l-(3-p-Tolyl-acryloylainino)-cycIopentanecarboxylicacid(2-phenyl-l(R)-{2-[l-(tetrahydro-pyran-4-y!methyl)-piperidin-4-yl]-ethyIcarbainoyl}-ethyl)-ainide TTA salt Benzo[i]fliiophene-2-carboxylic acid (1 -{l(R)-[2-(l-cyanomethyl-piperidin-4-yl)-ethylcarbamoyl]-2-phenyl-ettiylcart)amoyl}-cyciopentyl)-amide TFA salt Benzo[ft]thiophene-2-carboxylic acid (1 -{1 (R)-[(l -[ 1,3]dioxan-5-ylmethyl-piperidin-4-ylinethyl)-carbamoyl]-2-phenyl-ethylcaibamoyl}-cyclopentyl)-ainide TFA salt Benzo[fe]thiophene-2-caiboxylicacid (l-{l(RH(l-[l,3]dioxan-2-ylmethyl-piperidin-4-ylinethyl)-carbamoyl]-2-phenyl-ethylcaibamoyl} -cyclopentyl)-ainide 5-Chloro-benzoiuran-2-carboxyIicac!d [l-(2-phenyl-l(R)-{[l-(tetrahydro-pyran-4-yl)-piperidin-4-ylmethyl]-carbamoyl} -efliylcarbamoyl)-cyclopentyl] -amide 5-Chloro-benzofiiran-2-caiboxylic acid [l-(2-phenyl-l(R)-{[l-(tetrahydn)-thiopyran-4-yl)-piperidin-4-ylmethyl]-carbamoyl}-efliy!carbamoyl)-cyclopentyi]-amide Benzo[fr]thiopheiie-2-caii>oxylicacid [l-{l(R)-ben^I-2-{2-[l-(thiopheii-2-yl-acetyI)-piperidin-4-yl]-ethylamino}-ethylcarbamoyl)-cycl(^ntyl]-amide TFA salt Benzo[t]thiophene-2-carboxylic acid [i-(l(R)-{[l-(l-amino-cyclohexanecaibonyl)-piperidin-4-ylmethyl]-carbamoyl}-2-phenyI-ethylcarbamoyl)-cyc!opentyl]-amide TFA salt 6-Broino-naphthalene-2-carboxylicacid[l-(2-phenyl-l(R)-{2-[l-(pyrroIidine-2(S)-carbonyl)-piperidin-4-yl]-ethylcarbamoyl}-ethylcarbamoy!)-cyclopentyl]-amide 6-Bromo-naphthalene-2-carboxylic actd [l-(2-phenyl-l(R)-{2-[l-(pyrrolidme-2(R)-cariKmyO-piperidin-4-yI]-ethyIcaibanioyl}-etfiyIcarbamoyI)-cyciopentyi]-ainide Benzo[fe]thiopbene-2-caii)OxyHc acid [l-(2-pheny!-I (R)-{2-[4-(thiophen-2-yI-acetyl)-piperazin-l-yl3-ethylcarbainoy1}-ethylcaibamoyl)-cyclopentyl]-atnide. 5-ChIoro-benzofuran-2-carfao3cyJic acid {I-[iyf-(3-moiphoIin-4-yI-propyIcarbainoyJ)-2- 6,7-Dichloro-benzo[6]thiophene-2-carboxylic acid {1-[1^ -(3-moipholiii-4-yl-propylcarbamoyl)-2-phenyl-ethylcaibamoyi]-cyclopentyI}-aniide 5-rert-ButyI-benzofiiran-2-carboxyHc acid [l-(2-phenyl-IJ?-{[l-(tetrahydro-pyraii-4-y!methyl)-piperidin-4-ylmethyl]-carbamoyl} -ethylcarbamoyl)-cyclopentyl]-amide 6-Iodo-benzo[6]ihiophene-2-carboxyiic acid n-(2-phenyl-li!-{[l-CtetrahydrD-pyran-4-y lniethy!)-p!peridin-4-y Imethyll-carbamoyl} -ethylcarbanioyl)-cyclopentyl] -amide 7-Brorao-benzo[i']lhiophene-2-carboxyHc acid [l-(2-pheiiyl-iJ?-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yImethyI]-caibainoyI} -ethylcarbamoyl)-cyclopentyl] -amide 7-Iodo-benzo[b]thiophene-2-carboxyHc acid [l-(2-phenyl-l^-{[l-(tetrahydTo-pyran-4-ylmethy])-piperidin-4-ylmethyl]-carbamoyl} -eihylcarbamoyl)-cyclopeniyl]-amide 7-Methy1-benzo[6]thiophene-2-carboxyIic acid [l-(2-phenyl-lfl-{[l.(tetrahydn>-pyran-4-ylniethyl)-piperidin-4-yImethyl]-carbamoyl}-ethylcaTbamoy])-cycIopenty!]-amide 7-Trifluoromethyl-benzo[fc]diiophene-2-carboxylicacid[l-cycIopentyl]-amide 7-Chloro-l-methyl-14H-indole -2-carboxylic acid [lfl-C2-phenyI-I-{[l-(tetrahydro-pyraii-4-yimethyl)-piperidin-4-ylmethyl]-carbamoyI}-ethylcarbamoyl)-cycIopentyl]-amide 5-Chloro-3-methyl-beiizofuran-2-caiboxylicacid [lJi-(2-phenyl-l-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmetiiyl]-carbamoyl) -ethylcarbamoyl)-cyc]opentyl]-amide 5-Methoxy-benzoftiran-2-carboxyIicacid [l-(2-phenyl-l-{[lA-(tetrahydro-pyran-4~ ylmethyl)-piperidin-4.ylmethyl]-caibamoyl} -ethylcaTbamoyl)-cyclopentyl]-amide 3,5,6-TrimethyI-benzofiifan-2-carboxylic acid [l-(2-phenyl-l-{[lii-(tetrahydro-pyran-4-ylmethy))-piperi din-4-y lmethyl]-carbamoyl} -ethylcarbamoy l)-cyclopenQ'l]-amide 5-Bromo-naphthalene-2-carboxylic acid [l-(2-phenyl-l-{[1R]-(tetrahydro-pynin-4-ylmediyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyI)-cyclopentyl]-amide Naphthalene-2-carboxylic acid [l-(2-phenyl-lfl-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethy]carbamoyl)-cyclopentyI]-amide Benzo[6]1hiophene-2-carboxylic acid [ 1 -(2-phenyl-1 (R)-{[I-Ctetrahydro-pyran-4- ylmethyJ)-azetidin-3-ylmethyl]-carbamoyl} -etfiylcarbamoyl)-cyclopentyI]-amide, 4. The compounds of general foimula (1) according to claims 1 and 2, wherein the said^ compounds are defined by the following formulas: ] Benzo[i]lhiophene-2-carboxylic acid(l-{2-phenyl-l(R)-[l-(tetrahydro-pyran-4-ylmethyi; piperidin-4-ylcarbamoyl]-ethylcaibamoyl}-cyclopentyl)-amide TFA salt Benzob])hene-2-carboxylic acid [l-(l(R)-{2-[(l-amino-cyclohexanecaibonyl)- amino]-ethylcaibamoyl}-2-phenyl-ethyIcaibamoy!)-cyclopentyI]-amide 6-Bromo-benzo[i}thiophene-2-carboxylic acid [l-(2-phenyI-l(R)-{[l-(tetrahydro-pyran-4- ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcaTbamoyl)-cyclopentyl]-amideTFA salt Benzo[6]thiophene-2-carboxylic acid(l-{l-(R.)-[(I-isopropyI-piperidin-4-ylmethyl)- carbamoyl]-2-phenyI-ethylcarbamoyl}-cycIopentyl)-amide Benzo[Z']tfjiophene-2-carboxylic acid [l-(2-phenyl-l(R)-{[l-(tetrahydro-pyran-4- ylmethyl)-piperidin-4-ylmethyl]-carbamoyl} -ethylcarbamoy!)-cyclopentyl]-amide 6-Bromo-naphthalene-2-carboxyHc acid [l-(2-phenyl-l(R)-{[l-(tetrahydro-pyran-4- ylmethyl)-pipen'din-4-yImefhyI]-carf>amoyI}-elhyIcarbamoy()-cyclopentyIJ-amide Benzo[fc]fliiophene-2-carix)xyUc acid [l piperidin-4-ylmethyl]-carbamoyl) -ethylcart>amoyl)-cyclopentyl]-amide 1 -(3-E-p-Tolyl-acryloylamino)-cyclopentanecarboxyUc acid (2-phenyl-1 CR)-{E 1 - (tetTabydro-pyran-4-ylmethyl)-piperidin-4-ylmeftyI]-carbamoyl}-elhyI)-amide TFA sail Benzo[d]tfiiophene-2-carboxylic acid [l-(2-phenyl-l(R)-{2-[i-(tetrahydro-pyTan-4- ylmethyl)-piperidin-4-yl]-etiiylcaibamoyl}-ethylcarbamoyl)-cyclopentyl]-ainideTFAsalt Benzo[i]thiophene-2-caiboxylic acid [l-(2-phenyl-l(R>{2-[l-(tetrahydrD-pyran-4-yl)- piperidin-4-y!]-elfty!carbamoyl}-ethylcaibamoyl)-cyclopentyl]-amideTFAsaK 6-BromD-n^hthaIene-2-carboxyIicacid[l-(2-phenyI-l(R)-{[l-(tetrahydro-pyran-4-y])- piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide 6-Bromo-naphflialene-2-carboxylic acid (1- {1 (R)-[(l-[ 13]dioxan-5-ylmethyl-piperidin-4- y!methyl)-caibamoyl]-2-phenyl-ethylcarbamoyl} -cycIopen^I)-amide 5-Ch]OTo-ben2oftiran-2-caiboxylic acid (l-{l(R)-[{l-[l,3]dioxan-5-ybnelhyl-piperidin-4- ylmethyl)-carbamoyl]-2-pheny]-ediylcatbamoyl}-cyclopentyl)-amide 6-Brorao-n^htha!ene-2-carboxylic acid [ 1 -(1 (R)-{[1 -(.1 -amino-cyclohexanecarbony])-piperidin-4-ylmetbyl]-carbamoyl}-2-phenyl-ethylcarbamoyl)-cycIopeiityl]-amide 6-Iodo-naphthalene-2-carboxylicacid[l-(2-pbenyJ-!H-([l-(tetrahydro-pyran-4-y]methy])-piperidin-4-ylmethyl]carbamoyl}-ethylcarbamoyl)-cyclopentyl]-amide 6-Methoxy-naphthalene-2-carboxyIicacid [l-(2-phenyI-l^-{[l-(tetrahydro-pyran-4-yimethyl)-piperidin-4-ylmethy!]-carbajiioyt}-ethy]carbamoyl)-cyclopentyl]-amide 6-Bromo-benzoftuan-2-caiboxylic acid [l-(2-pheny]-lJ?-{[l-(tetrahydro-pyran-4-yImethy])-piperidin-4-y]metbyl]-carbainoyI}-efl»y]caTbainoy])-cyclopentyl]-amide 6-Chloro-benzofuran-2-carboxylic acid [l-(2-phenyl-li?-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyI}-etbylcarbamoyI)-cycIopentyl]-amide 5-Fluoro-benzoftiraii-2-carboxylic acid [l-(2-phenyI-l/i-{[i-{tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl]-carbamoyl} -efliylcarbamoyi)-cyclopentyl]-ainide 5-CbIoro-l«nzolwan-2-cariJoxy]ic acid [l-(2-pheny]-lJ?-{[l-(tetrahydro-pyTan-4-y]methyl)-piperidin-4-ylinethyI]-carbamoyl} -ethylcarbanioyl)-cyclopentyl]-am!de 5-Bromo-benzoiuran-2H:arboxyIic acid [I-(2-phenyI-Ifl-{[l-(tetrahydro-pyTan-4-ylmethyl)-piperidin-4-yImethyl]-carbainoyl}-ethylcaibamoyl)-cyclopentyl]-amide 7-lert-Butyl-benzoftiran-2-cart>oxylic acid [l-(2-pbenyI-l^-{[l-(tetrahydro-pyraii-4-yIinetfiyI)-piperidin-4-ylnietf3yl J-carbamoy]} -etby]carbamoy])-cyc]openlyl]-aniide 6-MethyI-benzoiuran-2-carboxyHc acid [l-(2-phenyl-lJ?-{[l-(tetrahydro-pyTan-4-ylmeliiyl)-piperidin-4-ylinethy IJ-carbamoyl} -ethylcaibamoyO-cycIopentylj-amide 5-Melhyl-benzofiiran-2-carboxylic acid [l-(2-phenyI-lft-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-ylmethyl3-carbamoyl} -ethylcarba3noyl)-cyclopentyI3-ainide 5-Iodo-benzofia-an-2-carboxy!icacid [1 -(2-phenyl-lJ?-{[l-(letrahydrD-pyran-4-yJinelby!)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbanioyl)-cyclopentyl]-ainide 6-Chloro-benzo[ft]thiophene-2-carboxy}ic acid [l-(2-phenyl-lJ?-{[l-(tetiahydro-pyran-4-ylmethyl)-piperidin-4-ylmetiiyl]-carbamoyI}-ediylcarbamoyl)-cycIopentyI]-amide 6-Trifluoromethyl-benzo[i]thiophene-2-carboxy!icacid[l-(2-phenyl-Ii?-{[l-(tetrahydro-pyran-4-ylmethyl)-piperidin-4-yJmeIbyl]-caibfflnoyI}-elby]caibamoyJ)- 6-MethyI-b6nzo[b]thiophene-2-carbeoxylic acid[l-(2-phenyi-IR-{[l-(tetraydro-pyran-4- yImethyl)-piperidin-4-yimethyJ]-carbainoyI}-ethylcarbamoyl)-cyclopen^r]-ainide 6-Fluoro-benzo[63thiophene-2-carboxylic acid [l-(2-phenyl-l-(Ili!-(tetrahydro-pyTan-4- ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-ethylcarbamoyl)-cyc]opeiityl]-aniide 6-IMefliylamino-benzofiu"an-2-carboxylic acid [l-(2-phenyl-l-{n^-(tetrahydro-pyran-4- yIm^hyl)-piperidin-4-ylmetbyl]-carbamoy]}-ethylcarbamoyl)-cyc}c^nQ'l]-amide 5-Diethylamtno-benzofiiran~2-carboxylic acid [l-(2^henyI-l-{[Ii?-(tetrahydro-pyTan-4- ylmethyl)-piperidin-4-ylinethyl]-caibamoyl)-ethy!caibamoyl)-cyclopentyl]-amide N^hthalene-2-carboxylic acid [l-(2-pheiiyl-l-{[li?-(tetrahydio-pyTan-4-ylmethyl)- piperidin-4-ylmethyl]-carbamoyll-ethylcarbainoyl)-cyclopen1yl]-ainide 6-Bromo-napbtba]ene-2-carboxylic acid [3-(l(R)-{[l-(4-methyl-teti:abydro-pyran -4- ylmethyJ)-piperidin-4-ylmeUiyl]-c^bamoyl}-2-phenyI-ethylcarbainoyl)-cyclopentyI]- amide 6-Broino-n^hthalene-2-carboxylicacid[l-(l(R)-{[l-(5-ethyl-[l,3]dioxan-5-ylmetbyl)- piperidin-4-y!methyl]-carbamoyl)-2-phenyl-etbylcarbamoyl)-cyclopenty!l-amide, 6-Broino-tiapbthalene-2-carboxylic acid [ 1 -(1 (R> {[4-methyl-1 -(4-methyl-tetrahydro- pyran-4-ylmethyl)-piperidin-4-ylmefl»yl]-carbamoyl} -2-phenyl-etfiylcaibamoyl)- cycIopentyI]-ainide, 6-Bromo-napththalene-2-carboxylic acid [l-(l(R)-{[4-methyl-l-(tetrahydro-pyran-4- ylmethyl)-piperidin-4-ylmethyl]-carbamoyl}-2-pbenyl-ethylcaibainoyl)-cyclopentyl]- amide. |
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1173-chenp-2004 claims duplicate.pdf
1173-chenp-2004 correspondence others.pdf
1173-chenp-2004 correspondence po.pdf
1173-chenp-2004 description (complete) duplicate.pdf
1173-chenp-2004 description (complete).pdf
1173-chenp-2004 pct search report.pdf
Patent Number | 224427 | ||||||||||||||||||||||||||||||||||||
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Indian Patent Application Number | 1173/CHENP/2004 | ||||||||||||||||||||||||||||||||||||
PG Journal Number | 49/2008 | ||||||||||||||||||||||||||||||||||||
Publication Date | 05-Dec-2008 | ||||||||||||||||||||||||||||||||||||
Grant Date | 15-Oct-2008 | ||||||||||||||||||||||||||||||||||||
Date of Filing | 27-May-2004 | ||||||||||||||||||||||||||||||||||||
Name of Patentee | MALESCI ISTITUTO FARMACOBIOLOGICO S.P.A. | ||||||||||||||||||||||||||||||||||||
Applicant Address | VIA LUNGO I'EMA 7, LOC, PONTE A EMA, 50012 BAGNO A RIPOLI, | ||||||||||||||||||||||||||||||||||||
Inventors:
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PCT International Classification Number | CO7K5/062 | ||||||||||||||||||||||||||||||||||||
PCT International Application Number | PCT/EP02/12022 | ||||||||||||||||||||||||||||||||||||
PCT International Filing date | 2002-10-28 | ||||||||||||||||||||||||||||||||||||
PCT Conventions:
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