| Title of Invention | N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS PDFG RECEPTOR INHIBITORS |
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| Abstract | The invention is directed to : N-Substituted tricyclic 3-aminopyrazole derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical composition comprising the compounds of the presentinvention and to methods for treating conditions such as tumors and other cell proliferative disorders. |
| Full Text | N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS PDFG RECEPTOR INHIBITORS Cross Reference The present international application claims priority under from co- pending U.S. Patent Application Serial No. 60/380,735, filed May 15, 2002, which is incorporated herein by reference in its entirety and for all purposes. Field of the Invention This invention relates to a novel series of N-substituted tricyclic 3- aminopyrazole compounds and the use of such compounds to treat cell proliferative disorders, such as tumors, restenosis, rheumatoid arthritis, diabetic retinopathy, and the like. More particularly, the compounds are inhibitors of the PDGF receptor tyrosine kinase. Background of the Invention Accumulating evidence supports the concept that loss of growth control of cancer cells involves perturbation of signaling pathways that in the normal cell are controlled by growth regulatory factors. Platelet-derived growth factor (PDGF) is a connective tissue cell mitogen that has been implicated in i tumorigenesis (Ostman and Heldin, Adv. Can. Res., 80:1-38, 2001, and references therein) as well as a principal player in the complex process of angiogenesis that is critical for tumor growth. PDGF exerts its cellular effects through binding to its specific receptor, PDGF-R. PDGF-R is a transmembrane receptor tyrosine kinase (RTK). It consists of two isozymes a and β. Each of these receptors has an extracellular part featuring five immunoglobulin-like domains and an intracellular part with a tyrosine kinase domain. Both a and p-containing receptors have been associated with mitogenic activity, stimulating edge ruffling and loss of stress fibers. Only the p-containing receptors has been associated with chemotaxis and actin reorganization (Heldin, C-H, EMBO Journal 11:4251-4259,1992). Binding of PDGF to PDGF-R results in dimerization of the two subunits of the PDGF-R receptors, thereby allowing autophosphorylation of each subunit on specific tyrosine residues in the cytoplasmic domain. The autophosphorylation leads to increased kinase activity and produces docking sites for a large number of signaling molecules with SH2 domains, such as Grb2/Sos1, PLC-gamma, GAP, PI-3 kinase and Src. (Heldin et al., Biochem. Biophys. Acta 1378:F79-113, 1998, and references therein). Upon binding to PDGF-R, these SH2 domain-containing signaling molecules initiate signal transduction pathways that are involved in different cellular responses such as cell proliferation, cell mobility, cell permeability or apoptosis. PDGF has several important cellular effects in vivo. It regulates cell growth, differentiation, and migration during embryonal development, and plays a possible role in neuroprotection and regeneration. It also stimulates wound healing in adults. In addition, PDGF also has specialized functions in the vascular system as well as in the homeostasis of connective tissue (Ostman and Heldin, Adv. Can. Res., 80:1-38, 2001, and references therein). Overactivity of PDGF has been implicated in the pathogenesis of a number of serious diseases, including cancers (glioma, lung, breast, colorectal, prostate, gastric and esophageal, leukemias and lymphomas), and other cell proliferative disorders, such as atherosclerosis, transplantation-induced vasculopathies, neointima formation, lung fibrosis, restenosis, pulmonary fibrosis, glomerulonephritis, glomerulosclerosis, congenital multicystic renal dysplasia, kidney fibrosis, and rheumatoid arthritis (Ostman A, Heldin CH., Adv. Cancer Res, 80:1-38, 2001, and references therein). A considerable body of direct and indirect experimental evidence showed that sustained tumor growth and metastasis are angiogenesis- dependent (see e.g., Hanahan, Science, 277:48-50, 1997). Angiogenesis is the development of new vasculature from preexisting blood vessels and/or circulating endothelial stem cells (see i.e.. Springer et al., 1998). Angiogenesis plays a vital role in many physiological processes, such as embryogenesis, wound healing and menstruation. Angiogenesis also appears to be important in certain pathological events, such as solid tumor growth and metastasis, arthritis, psoriasis and diabetic retinopathy (Hanahan and Folkman, Cell, 86(3):353-364,1996;). Anti-angiogenic therapy is currently being studied as a way to interfere with tumor growth. Indeed, numerous studies in animal models have demonstrated striking effects in tumor growth inhibition by targeting angiogenic growth factors such as vascular endothelial growth factor (VEGF), acidic and basic fibroblast growth factor (aFGF, bFGF) and PDGF. The receptors for VEGF and PDGF belong to one super family of receptor tyrosine kinases. Therefore, in addition to their role in treating other cell proliferative disorders, clinically useful PDGF-R tyrosine kinase inhibitors are useful for antiangiogenic therapy and to control tumor cell proliferation. Small molecule inhibitors of the receptor tyrosine kinase constitute a novel class of drugs with large potential (Druker and Lydon, J. Clin. Invest., 105:3-7, 2000, and references therein). Since 1995, a number of small molecule inhibitors for PDGF receptor autophosphorylation have been characterized. Some examples are listed below. JP 06087834 (Zimmermann) discloses N-phenyl-2-pyrimidine-amine derivatives which have tumor inhibitory activity and are useful for treating tumors in warm-blooded animals including human beings. Derivatives of this group of compounds, compound CGP53716 (Buchdunger et al., PNAS, 92:2558-2562,1995) and compound STI-571 (Buchdunger et al., Cancer Res, 56:100-4,1996), have been shown to inhibit PDGF-R autophosphorylation. JP 11158149 (Kubo et al.) discloses quinoline derivatives for the treatmenl diseases such as tumors and diabetic retinopathy. Derivatives of this group of compounds, compound Ki6783 (Yagi et al., Exp. Cell Res. 243:285-292, 1997) and compound Ki6896 (Yagi et al., Gen. Pharmacol. 31:765-773, 1998), have been shown inhibit PDGF-R autophosphorylation. US5932580 (Levitzki et al.) discloses PDGF receptor kinase inhibitory compounds of the quinoxaline family including Tyrphostin, ATP-cbmpetitive inhibitors of the receptor kinase. US5409930 (Spada, et al.) discloses bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. Compound RPR101511A, a derivative of this group of compound, has been shown to inhibit PDGF-R autophosphorylation (Bilder et al., Circulation. 99(25):3292-9.1999). US 5563173 (Yatsu, et al.) discloses a method of inhibiting the proliferation of smooth muscle cells by sodium butyrate, which inhibits PDGF-R kinase activity. US5476851 (Myers, et al.) discloses Pyrazolo[3,4-g]quinoxaline compounds, as PDGF receptor protein tyrosine kinase inhibitors. Compound SU-6668, an ATP competitive inhibitor, has been shown to inhibit PDGF-R autophosphorylation (Laird, et al., Cancer Res. 60:4152-4160, 2000]. WO01/79198 (Reich et al.) discloses amino-pyrazole compounds of the following formula that modulate and/or inhibit the activity of protein kinases. WO0212242 (Fancelli et al.) discloses bicyclo-pyrazole compounds that are useful for treating diseases linked to disregulated protein kinases. Up to now, STI-571 (GLEEVEC) is the only compound to reach market with significant PDGFR activity, although it is not a selective antagonist of this enzyme. Therefore, PDGF-R remains an extremely attractive target for the design of potent and selective small molecule inhibitors that will represent an important new class of therapeutic agents for the treatment of tumors and other cell proliferative disorders. References to a number of substituted tricyclic pyrazole derivatives include those disclosing use as: inhibitors of tyrosine kinase activity (WO 99/17769, WO 99/17770); cyclin dependent kinases inhibitors (WO 99/54308); selective estrogen receptor modulators (WO 00/07996); analgesics (U.S. 4,420,476); prophylaxis and therapy of diseases caused by rhinoviruses (U.S. 4,220,776; U.S. 4,140,785); analgesics / anti-inflammatory activity (U.S. 3,928,378; Schenone, Silvia et al. Farmaco (2000), 55(5), 383-388 ); cyan couplers for photographic dye (EP 0620489, JP 8022109); quinolines and naphthyridines as drugs (JP 6092963); and immunomodulators (JP 6100561); and hypoglycemic agents (Reddy, R. Raja et al., Indian Journal of Heterocyclic Chemistry (1998), 7(3), 189-192). Summary of the Invention The present invention provides N-substituted tricyclic 3-aminopyrazole derivatives as inhibitors of the PDGF receptor (PDGF-R) tyrosine kinase and the use of such compounds to treat cell proliferative disorders or disorders related to (i.e., associated with or implicating with) platelet-derived growth factor receptor (PDGF-R) such as such as tumors, restenosis, rheumatoid arthritis, diabetic retinopathy, and the like. Illustrative of the invention is a pharmaceutical composition comprising a pharmaceuticaly acceptable carrier and any of the compounds of Formulae (I) and (II). Another illustration of the invention is a process for making a pharmaceutical composition comprising mixing any of the compounds of Formulae (I) and (II) and a pharmaceutically acceptable carrier. Another illustration of the present invention is a pharmaceutical composition prepared by mixing any of the compounds of Formulae (I) and (II) and a pharmaceutically acceptable carrier. The present invention is further related to the use of a compound of Formulae (I) and (II) for the treatment of a PDGF-R related disorder or a cell proliferative disorder in a subject comprising administering to the subject a therapeutically effective amount of a compound of Formulae (I) and (II). The disorder related to PDGF-R or a cell proliferative disorder is selected from neoplastic and other cell proliferative disorders. Preferably, said neoplastic disorder is a cancer selected from a glioma cancer, a lung cancer, a breast cancer, a colorectal cancer, a prostate cancer, a gastric cancer, an esophageal cancer, a colon cancer, a pancreatic cancer, an ovarian cancer, a melanoma, a myelodiys plasia, a multiple myeloma, a leukemia and a lymphoma, and said other cell proliferative disorder is selected from atherosclerosis, transplantation- induced vasculopathies, neointima formation, lung fibrosis, macular degeneration, restenosis, pulmonary fibrosis, glomerulonephritis, glomerulosclerosis, congenital multicystic renal dysplasia, kidney fibrosis, rheumatoid arthritis and diabetic retinopathy. The invention is directed to a method of inhibiting the onset of a disorder related to PDGF-R or a cell proliferative disorder in a subject comprising administering to the subject a prophylactically effective amount of a compound of Formulae (I) and (II). The invention further includes a combination therapy in treating or inhibiting the onset of a disorder related to PDGF-R or a cell proliferative disorder in a subject. The combination therapy comprises administering to the subject a therapeutically or prophylactically effective amount, respectively, of a compound of the invention and one or more other anti-cell proliferation therapies including, but not limited to, chemotherapy, radiation therapy, gene therapy and immunotherapy. The present invention also provides a method for the treatment of a cell proliferative disorder, preferably restenosis, intimal hyperplasia, inflammation, or atherosclerosis in vessel walls, comprising the controlled delivery, by release from an intraluminal medical device, of a compound of the invention in therapeutic effective amounts. The present invention further provides a method of treating a cell proliferative disorder in a subject, preferably, a neoplastic disorder selected from a glioma cancer, a lung cancer, a breast cancer, a colorectal cancer, a prostate cancer, a gastric cancer, an esophageal cancer, a colon cancer, a pancreatic cancer, an ovarian cancer, a melanoma, a myelodysplasia, a multiple myeloma, a leukemia and a lymphoma, comprising administering to the subject a therapeutic effective amount of a compound of the invention conjugated to a targeting agent. The present invention futher provides a method for reducing or inhibiting the kinase activity of PDGF-R or c-Abl in a cell comprising the step of contacting the cell with a compound of Formulae (I) or (II). The present invention also provides a method of inhibiting the kinase activity of PDGF-R or c-Abl in a subject comprising the step of administering a compound of Formula (I) or (II) to the subject. The present invention further provides a method of inhibiting cell proliferation in a cell comprising the step of contacting the cell with a compound of Formulae (I) or (II). The present invention further provides a method of identifying novel PDGF-R kinase inhibitors. The method comprises the steps of: (a) determining a three-dimensional structure of the compound of Fomulae (I) or (II) in the absence or presence of a polypeptide comprising the PDGF-R kinase catalytic domain; (b) analyzing the three-dimensional structure for the compound alone or for the intermolecular interaction between said compound and PDGF-R; (c) selecting a compound that mimics the structure for the compound alone or incorporates the predictive interaction; (d) synthesizing said designed compound; and (e) determining the ability of the molecule to bind and inhibit PDGF-R kinase activity. The present invention further provides a method of identifying novel c-Abl kinase inhibitors. The method comprises the steps of: (a) determining a three-dimensional structure of the compound of Formulae (I) or (II) in the absence or presence of a polypeptide comprising the c-Abl kinase catalytic domain; (b) analyzing the three-dimensional structure for the compound alone or for the intermolecular interaction between said compound and c-Abl; (c) selecting a compound that mimics the structure for the compound alone or incorporates the predictive interaction; (d) synthesizing said designed compound; and (e) determining the ability of the molecule to bind and inhibit c-Abl kinase activity. The present invention is further directed to processes for the preparation of compounds of Formula (I) and compounds of Formula (II) Other features and advantages of the invention will be apparent from the following detailed description of the invention thereof, and from the claims. Detailed Description of the Invention The present invention relates to novel N-substituted tricyclic 3- aminopyrazole derivatives, their synthesis and the use of said compounds for the treatment and / or prevention of PDGF-R related disorders, such as tumors, restenosis, rheumatoid arthritis, diabetic retinopathy, and the like. 1. Formula (I) n is an integer from 1 to 4; 15 R1 is selected from the group consisting of hydrogen, lower alkyl, -OH, alkoxy, -oxo, -NH2, -NH(alkyl) and -N(alkyl)2; 0 —• is selected from the group consisting of an aryl, a five to six membered monocyclic heteroaryl, a nine to ten membered benzo-fused heteroaryl, a nine to ten membered benzo-fused heterocycloalkyl group, and a 20 nine to ten membered benzo-fused cycloalkyl group; wherein the benzo-fused heteroaryl, benzo-fused heterocycloalkyl or benzo-fused cycloalkyl group is attached to the molecule such that the phenyl ring is bound directly to the •S-x—A1—(5) R is selected from the group consisting of ' ^-^ , and -X-A1-Y-A2; wherein, X and Y are each independently absent or selected froiYi the group consisting of -O-, -NH-, -N(alkyl)-, -S-, -SO-. -S02-, -OC(=0), -C(=0)0-, -NHC(=0)-, -N(alkyl)C(=0)-, -C(=0)NH-, -C(=0)N(alkyl)-. -OC(=0)0-, -NHC(=0)0-, -OC(=0)NH-, -N(alkyt)C(=0)0-, -OC(=0)N(alkyl)-? -NHC(=0)NH-, -NHC(=0)N(alkyl)-, -N(alkyl)C(=0)NH-. -N(alkyl)C(=0)N(alkyl)-, -NHSOr, -SO2NH-, -N(alkyl)S02- and -S02N(alkyl)-; A1 is absent or selected from alkyl or alkenyl; A2 is selected from alkyl, alkenyl, or H; wherein, when A1 or A2 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from halogen, cyano, hydroxy, alkoxy, thio, halogenated alkoxy, -OC(=0)alkyl, -OC(=0)Oalkyl, amino, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, dialkylamino. -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalky1, -N(alkyl)C(=0)NH2, -OC(=0)NHalkyl. -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl. -NHS02alkyl, -N(alkyl)S02alkyl. thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; v--/ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitrot cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl. -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl. -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; q is an integer from 0 to 4; R3 is selected from the group consisting of halogen, hydroxy, amino, thio, nitro, cyano, alky!, halogenated alkyl, alkoxy, halogenated alkyloxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)a!kyl, or dialkylarnino, -NHC(=0)NH2, -NHC(=0)NHalkyl. -N(alkyl)C(=0)NHalkyl. -OC(=0)NHalkyl. -NHC(=O)0alkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl. -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2> -N(alkyl)C(=0)N(alkyl)2 and -OC(=0)N(alkyl)2; provided that the sum of p and q is an integer from 0 to 4; L1 is absent or selected from the group consisting of alkyl; ^-^ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof, useful for the treatment of a PDGF-R related disorders. is selected form the group consisting of a five or six membered heteroaryl. In 0 another embodiment of the present invention N—• is selected from the group consisting of a nine or ten membered benzo-fused heteroaryl, a nine or ten membered benzo-fused cycloalkyl, and a nine or ten membered benzo-fused heterocycloalkyl. In a preferred embodiment of the present invention R1 is selected from the group consisting of hydrogen, hydroxy, methyl, and oxo, preferably R1 is hydrogen or methyl. In an embodiment of the present invention n is an integer from 1 to 2. In another embodiment of the present invention p is 0 and q is an integer from 0 to 2. In yet another embodiment of the present invention p is an integer from 1 to 2 and q is an integer from 0 to 1. , i-X A1 (S) In an embodiment of the present invention, R is ' v~' 1 (5) wherein X, A and ^-^ are as defined herein. Preferably, X is O. In another embodiment of the present invention, X is O and is a heterocycloalkyl or heteroaryl, wherein the heterocycloalkyl or heteroaryl is optionally substituted with one to three substituents independently selected from halogen, alkoxy, hydroxy, amino, alkylamino or dialkylamino. In another embodiment of the present invention, R2 is -X-A1-Y-A2 wherein X, A1, Y, A2 are as defined herein. Preferably, X and Y are each independently absent or O. In an embodiment of the present invention, R3 is selected from the group consisting of alkoxy, halogen, amino, dialkylamino, lower alkyl, and hydroxy. Preferably, R3 is lower alkyl or lower alkoxy. In an embodiment of the present invention L1 is a lower alkyl, preferably methylene. In another embodiment of the present invention L1 is absent. (5) A preferred embodiment of the present invention,v—' is aryl, heteroaryl, (B) cycloalkyl, or herterocycloalkyl. Preferably v—' is aryl or heteroaryl. In an embodiment of the present invention is a compound of Formula (B) wherein n, R1, p, R2, q, R3, L1 and ^-^ are as defined herein for Formula (I), or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salt thereof. Another preferred embodiment of the present invention is,a compound of formula (I) wherein n is an integer from 1 to 2; R1 is hydrogen; 0 v—' is selected from the group consisting of phenyl, a five to six membered heteroaryl and a nine to ten membered benzo-fused heterocycloalkyl group; wherein the nine to ten membered benzo-fused heterocycloalkyl group is attached to the molecule such that the phenyl ring is bound 0 directly to the portion of the molecule; preferably, ^— is selected from the group consisting of phenyl, thienyl and 1,3-benzodioxolyl; 14 p is an integer from 0 to 2; R2 is selected from the group consisting of di(lower alkyl)amino-alkoxy, lower •l-O—A1 (B) alkyl-alkoxy, hydroxy substituted alkoxy and ' ^-^ ; wherein A1 is selected from the group consisting of lower alkyl; wherein 5 the lower alkyl is optionally substituted with one to two substituents independently selected from hydroxy, amino, alkylamino or dialkylamino; and wherein ^~s is selected from the group consisting of a five or six membered heteroaryl and a five or six membered heterocycloalkyl; wherein the heteroaryl or heterocycloalkyl is optionally substituted with 10 one to two substituents independently selected from halogen, lower alkyl, lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino; preferably, R2 is selected from the group consisting of 3-dimethylamino- propoxy, 3-methoxy-propoxy, 2,3-dihydroxy-n-propoxy, 3-hydroxy- propoxy, 2-hydroxy-3-pyrrolidin-1-yl-propoxy and 3-(4-methyl-piperazin- 15 1-yl-propoxy; q is an integer from 0 to 2; R3 is selected from the group consisting of lower alkyl and lower alkoxy, and halogen; preferably, R3 is selected from the group consisting of methyl, methoxy, ethoxy. 20 L1 is absent or lower alkyl, preferably, L1 is absent or CH2; v 'P is selected from the group consisting of phenyl and a five or six membered heteroaryl group; wherein the phenyl or heteroaryl group is optionally substituted with one to two substituents independently selected from halogen, lower alkyl, lower alkoxy or benzyloxy; 25 preferably, v 'P is selected from the group consisting of phenyl and pyridyl; wherein the phenyl is optionally substituted with one to two substituents independently selected from fluoro, chloro, methyl, methoxy or benzyloxy; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salt thereof. 5 Another embodiment of the present invention is a compound of Formula (I) wherein R1 is selected from the group consisting of hydrogen and lower alkyl; preferably R1 is selected from hydrogen or methyl; 0 ^—' is selected from the group consisting of phenyl, a five to six 10 membered heteroaryl and a nine to ten membered benzo-fused heteroaryl; wherein the phenyl, five to six membered heteroaryl or nine to ten membered benzo-fused heteroaryl is optionally substituted with one to two substituents independently selected from halogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy or lower alkoxy-lower alkoxy; preferably 0 15 ^— is selected from the group consisting of phenyl, 3,5-dimethoxyphenyl, 4,5-diethoxyphenyl, 4,5-di(trifluoromethoxy)-phenyl, 4,5-di(methoxyethoxy)- phenyl, 4,5-di(methoxypropoxy)-phenyl, 4,5-di(isopropoxy)-phenylI 4,5- di(difluoromethoxy)-phenyl, 4-chloro-5-methoxy-pheny1, 4-methoxyethoxy-5- ethoxy-phenyl, pyridyl, pyrimidinyl, furyl, 5-chloro-thienyl, 3-ethoxy-thienyl, 20 isoxazolyl, 3-methyl-isoxazolyl, 2-methyl-8-ethoxy-benzoxazolyl, benzothienyl, L1 is absent or selected from lower alkyl, preferably L1 is absent or selected from methyl or ethyl; c v 'P is selected from the group consisting of aryl, cycloalkyl and a five to six membered heteroaryl; wherein the aryl or heteroaryl group is 25 optionally substituted with one to two substituents independently selected from halogen, lower alkyl, hydroxy substituted lower alkyl, lower alkoxy, aminosulfonyl, (lower alkyl)amino, di(lower alkyl)amino, di(lower alkyl)amino- alkoxycarbonyl, lower alkoxycarbonyl, heterocycloalkyl- 16 loweralkylaminocarbonyl, di(lower alkyl)amino-lower alkylaminocarbonyl or heteroaryl-loweralkylaminocarbonyl; wherein the heteroaryl or heterocycloalkyl portion of the heterocycloalkyl-loweralkylaminocarbonyl or heteroaryl- loweralkylaminocarbonyl substituent is optionally substituted with a substituted selected from lower alkyl, hydroxy or hydroxy substituted lower alkyl; preferably v 'P is selected from the group consisting of phenyl, benzyl, phenylethyl, cyclohexyl, cyclohexyl-methyl, 3-hydroxy- cyclohexyl, 4-hydroxy-cyclohexyl, 2-fluorobenzyl, 2-chlorobenzyl, 3- chlorobenzyl, 2,3-dichlorobenzyl, 2,6-dichlorobenzyl, 2-fluorophenylethyl, 3- fluorophenyl, 3-bromophenyl, 3-chlorophenyl, 2-methylbenzyl, 3-methylbenzyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-hydroxymethylphenyl, 2-hydroxymethyl- benzyl, 3-chloro-4-fIuoro-benzyl, 2-aminosulfonyl-benzyl, 2-aminosulfonyl- phenyl, 3-aminosulfonyl-phenyl, 4-aminosulfonyl-phenyl, 3-dimethylamino- phenyl, 3-(dimethylamino-ethylaminocarbonyl)-phenyl, 3-ethoxycarbonyl- phenyl, 3-(2-pyrrolidin-1-yl-ethylaminocarbonyl)-phenyl, 3-(2-pyrrolidin-1-yl-n- propylaminocabronyl)-phenyl, 3-(dimethylamino-ethylaminocarbonyl)-phenyl, 3- (2-imidazol-1-yl-ethylaminocarbonyl-phenyl,3-(2-(1-methyl-imida'zol-2-yl)- ethylaminocarbonyl)-phenyl, 3-[3-(hydroxymethyl-pyrrolidin-1-yl-propyl)- aminocarbonyl]-phenyl, pyridyl-methyl, pyridyl-ethyl, pyrimidinyl-methyl and 3- methyl-imidazolyl-methyl; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salt thereof. 1 .b. Preparation of Compounds of Formula (I) The present invention is further directed to a process for the preparation of compounds of Formula (I) Formula (I) wherein, n is an integer from 1 to 4; R1 is selected from the group consisting of hydrogen, lower alkyl, -OH, alkoxy, -oxo, -NH2, -NH(alkyl) and -N(alkyl)2; 0 v-— is selected from the group consisting of an aryl, a five to six membered monocyclic heteroaryl, a nine to ten membered benzo-fused heteroaryl, a nine to ten membered benzo-fused heterocycloalkyl group, and a nine to ten membered benzo-fused cycloalkyl group; wherein the benzo-fused heteroaryl, benzo-fused heterocycloalkyl or benzo-fused cycloalkyl group is attached to the molecule: such that the phenyl ring is bound directly to the i-X A1 (B) R is selected from the group consisting of ? v-y , and -X-A1-Y-A2; wherein, X and Y are each independently absent or selected from the group consisting of -O-, -NH-, -N(alkyl)-, -S-. -SO-, -S02-, -OC(=0), -C(=0)0-. -NHC(=0)-, -N(alkyl)C(=0)-, -C(=0)NH-. -C(=0)N(alkyl)-, -0C(=0)0-, -NHC(=0)0-t -OC(=0)NH-, -N(alkyl)C(=0)0-, -OC(=0)N(alkyl)-,' -NHC(=0)NH-, -NHC(=0)N(alkyl)-, -N(alkyl)C(=0)NH-. -N(alkyl)C(=0)N(alkyl)-. -NHSO2-, -SO2NH-, -N(alkyl)S02- and -S02N(alkyl)-; A1 is absent or selected from alkyl or alkenyl; A2 is selected from alkyl, alkenyl, or H; wherein, when A1 or A2 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from halogen, cyano, hydroxy, alkoxy, thio, halogenated alkoxy, -OC(=0)alkyl, -OC(=0)Oalkyl, amino, alkylamino, -NHC(=0)alkyl, -N(alky1)C(=0)alkyl, dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl. -N(alkyl)C(=0)NH2, -OC(=0)NHalkyl, -NHC(=0)Oalkyl. -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl. halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2. -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; © ^-^ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substjtuents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2. -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -0C(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2. -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; q is an integer from 0 to 4; R3 is selected from the group consisting of halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkyloxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(^0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl. thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 and -0C(=0)N(alkyl)2; provided that the sum of p and q is an integer from 0 to 4; L1 is absent or selected from the group consisting of alkyl; v--/ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocydoalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocydoalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof; comprising reacting the compound of formula (S5) with a compound of formula (S6), in an aprotic solvent, to yield the corresponding compound of forrnula (S3); wherein Formula A-3 is attached on the b3 side of Formula A-3 to the L2 ring of formula (II), and B1, B2 and B3are independently (i) -CH- optionally substituted with alkyl, aryl, alkoxy, or halogen, (ii) -S-; (iii) -0-; or (iv) -N-; provided that no more than one of B1, B2 or B3 is -S-or -0-, and, provided that when one of B1, B2 or B3 is -S-or -0-, then the adjacent ring members are not -S-or -0-; R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2t -OC(=0)NHalkyl, -SO^alkyl, thio and thioalkyl; L2 is a linking group selected from the group consisting of: -(CH2)i4-, -CH(R100h -C(=R100)-, -C(R100)2-, -0-, -0(CH2)^-, -OCH(R100)-, -OC(R10V, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alky1)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; wherein R100is selected from: alkyl, hydroxy, aryl, alkoxy, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH; provided that when L2 is -ChbCrV, neither R6 nor R7 is -CH2-(C=0)NHalkyl, -CH2-(C=0)N(alkyl)2 or -CH2C(=0)Oalkyl; provided that when L2 is -OCH(R100)-, R100 is alkoxy, and ^— is phenyl, R5 is not-C(=0)NH-NH2; and provided that when L2 is -O- or -S-, neither R6 nor R7 is -CH3; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyl)-. -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH, -NHC(=0)0-, -NHS02-, -0-, -0C(=0), -OC(=0)N(alkyt)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2> -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; v—y is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine, to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -0C(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02aikyl, 5 -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl. -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten 10 membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents 15 independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. 20 -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. 25 In formula (II), "the L2 ring of formula (II)" refers to the ring of Formula (II) containing the L2 substituent. The v>—' ring of Formula (II) is attached to the L ring of formula (II) such that the point of attachment for the v—- ring is the second and third carbon 10 2.a Embodiments of Formula (II) 2.a.1 Further emobidments of the present invention include compounds of Formula II wherein E, L2, R6, R7. R4, L3 H, and (R5)r vary as set forth below 15 individually and combinations of the variations thereof. An embodiment of the present invention includes compounds of Formula (II) wherein: (£ —' is selected from the group consisting of Formulae A-1, A-2 and A-3: wherein R8 is H or lower alkyl; -NHC(=0)N(alkyl)2, -NHC(=0)NH2. -NHC(=0)NHalkyl. -NHC(=O)0alkyl, -NHS02alkyl, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl and thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: i R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, hydroxy, -NHC(=0)alkyl, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, and thioalkyl. A embodiment of the present invention includes compounds of Formula (II) wherein: R9 is independently selected from the group consisting of: alkoxy, alkyl, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, hydroxy and -NHC(=0)alkyl. A embodiment of the present invention includes compounds of Formula (II) wherein: R9 is independently selected from the group consisting of: methoxy, ethoxy, isopropoxy, methyl, amino, cyano, N,N-dimethyi-amino, bromo, chloro, fluoro, trifluoromethyl, trifluoromethoxy, hydroxy and N-(1-oxo-ethyl)-amino. An embodiment of the present invention includes compounds of Formulae (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)-, -(CH2)M-, -CFKR100)-, -C(=R100)-, -C(R100)2-, -0-, -0(CH2)M-, -OCH(R100)-, -OC(R1°V, -S-, -NH-, -N(lower alkyl)-, -N(COalkyt)-, -N(aryl)-, -N(C02alkylK -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i^-, -CH(R100)-, -C(=R100)-. -C(R100)2-. -0-, -0(CH2)i-»-. -OCH(R20°K -OC(R100)2-. -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; wherein R200is selected from: alkyl, hydroxy, aryl, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)-M-, -CH(R100)-. -C(=R100)-. -C(R1(xy, -0-, -0(CH2)^-, -OCH(R100)-, -OC(R100)2-. -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -NKSO^Ikyl) and -N(S02aryl)-. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)1-4-, -CH(R100K -C(=R100)-, -C(R10V , -0(CH2)i-r, -OCH(R100)-, -OC(R100)2-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-. -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)-, -(CH2)W-, -CH(R100)-, -C(=R100h -C(R100)2-, -0(CH2)^-, -OCH(R200)-, -OC(R10V. -NH-. -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; wherein R200 is selected from: alkyl, hydroxy, aryl, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100)-I -C(=R100)-, -C(R1°V, -0-, -0(CH2)^-, -OCH(R100)-. -OC(R100)r. -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is - CH2CH2-, neither R6 nor R7 is -CH2-(C=0)NHalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100K -C(=R100)-, -C(R10V, -0-. -0(CH2)n-, -OCH(R100)-, -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyi)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is - CH2CH2-. neither R6 nor R7 is -CH2-(C=0)NHalkyl or -CH2-(C=0)N(alkyl)2. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100h -C(=R100)-. -C(R10V, -0-, -0(CH2)^-, -OCH(R100)-, -OC(R1°V, -S-, -NH-, -N(lower alkyl)-. -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is - CH2CH2-, neither R6 nor R7 is -CH2C(=0)Oalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)M-, -CH(R100h -C(=R100h -C(R10V, -0-, -0(CH2)i-r. -OCH(R100)-. -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -IM(aryl)-, -N(C02alky1)-. -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is - CH2CH2-, neither R6 nor R7 is -CH2-(C=0)NHalkyl, -CH2-(C=0)N(alkyl)2 or -CH2C(=0)Oalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)M-, -CH(R100)-. -C(=R100)-, -C(R10V, -O-, -0(CH2)i-r, -OCH(R100)-, -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-,-N(aryl)-,-N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is -OCH(R100)-, R100 is alkoxy, and V-^ is phenyl, R5 is not -C(=0)NH-NH2. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(Chfe)^-, -CH(R100)-, -C(=R100)-, -C(R100)2-, -0-, -0(CH2)^-, -OCH(R100)-, -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2is -O-. neither R6 nor R7 is -CH3. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i^-, -CFKR100)-, -C(=R100h -C(R100)2-, -0-, -0(CH2)i-4-, -OCH(R100)-1 -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkylh -N(S02alkyl) and -N(S02aryl>-; provided that when L2is -S-, neither R6 nor R7 is -CH3. An embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i^-, -CH(R100)-, -C(=R100)-, -C(R100)2-, -0-, -0(CH2)i-r. -OCH(R100)-, -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-,-N(aryl)-,-N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is -O- or -S-, neither R6 nor R7 is -CH3. A embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100)-, -C(=R100)-. -C(R10V . -0-, -0(CH2)M-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-. A embodiment of the present invention includes compounds of Formula (II) wherein: L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100)-. -C(=R100h -C(R100)2-, -0-, and -0(CH2)^-. A embodiment of the present invention includes compounds of Formula (II). wherein: R100 is selected from: alkyl, hydroxy, aryl, oxo or =N(OH). A embodiment of the present invention includes compounds of Formula (II) wherein: R100is selected from: alkyl, hydroxy, aryl, or oxo. An embodiment of the present invention includes compounds of Formulae (II) wherein: R100 is selected from: methyl, hydroxy, phenyl, oxo or =N(OH). A embodiment of the present invention includes compounds of Formulae (II) wherein: R100 is selected from: methyl, hydroxy, phenyl, or oxo. An embodiment of the present invention includes compounds of Formula (II) wherein: R10 is independently selected from the group consisting of An embodiment of the present invention includes compounds of Formula (II): wherein X1 and Y1 are each independently absent or selected from the group consisting of: -C(=0)NH-. -C(=0)0-, -NH-, -NHC(=0)-, -NHC(=0)NH, -NHC(=0)0-, -NHSO2-, -O-, -OC(=0), -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -SO2- and -S02NH-. An embodiment of the present invention includes compounds of Formula (II): wherein X1 and Y1 are each independently absent or selected from the group consisting of: -NH-, -0-, -S02- and -S02NH-. An embodiment of the present invention includes compoiinds of Formula (II), wherein X1 and Y1 are each independently absent or -0-. An embodiment of the present invention includes compounds of Formula (II), wherein X1 is absent or -O-. An embodiment of the present invention includes compounds of Formula (II), wherein Y1 is absent. An embodiment of the present invention includes compounds of Formula » (II), wherein: A20 is absent or alkyl; and wherein when A20 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2l-N(alkyl)C(=0)NH2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl. -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)N An embodiment of the present invention includes compounds of Formula (II) wherein: A20 is absent or alkyl; and wherein when A20 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy, -NHC(=0)NH2, -NHS02alkyl, -S02alkyl or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: A20 is absent or selected from methyl, ethyl, propyl or isopropyl; wherein methyl, ethyl, propyl or isopropyl are optionally substituted with one or more groups independently selected from: alkoxy, dialkylamino or hydroxy. An embodiment of the present invention includes compounds of Formula (II) wherein: A20 is absent or selected from methyl, ethyl, propyl or isopropyl; wherein methyl, ethyl, propyl or isopropyl are optionally substituted with one or more groups independently selected from methoxy, dimethyl-amino or hydroxy. An embodiment of the present invention includes compounds of Formula (II) wherein: A21 is selected from alkyl, alkenyl, or H; and wherein when A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy. alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NH2, -N(alkyt)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: A21 is selected from alkyl, alkenyl, or H; and wherein when A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy, -NHC(=0)NH2, -NHS02alkyl or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein A21 is H. An embodiment of the present invention includes compounds on-ormuia (II) wherein v—y is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl. -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl. -N(alkyl)C(=0)OalkyI, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alky1)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2. 5 An embodiment of the present invention includes compounds of Formula (II) wherein © v~-' is selected from the group consisting of aryl, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents 10 independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl. ordialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, 15 -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2. An embodiment of the present invention includes compounds of Formula 20 (II) wherein N—' is selected from the group consisting of phenyl, imidazolyl, pyrrolidinyl, piperidinyl and morpholinyl optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, 25 alkylamino, -NHC(=0)alkyl. -N(alkyl)C(=0)alkyl, or dialkylarnino, -NHC(=0)NH2, -NHC(=0)NHalkyl. -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -SOzalkyl. halogenated -S02alkyl, -NHC(=0)N(alkyl)2, 30 -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2. An embodiment of the present invention includes compounds of Formula (II) wherein © x—"^ is selected from the group consisting of phenyl, imidazolyl, pyrrolidinyl, piperidinyl and morpholinyl optionally substituted with one or more 5 substituents independently selected from halogen, hydroxy, amino, nitro, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, i dialkylamino, -NHS02alkyl or -S02alky1. An embodiment of the present invention includes compounds of Formula 10 (II) wherein ® x—' is selected from the group consisting of phenyl, imidazolyl, pyrrolidinyl, piperidinyl and morpholinyl optionally substituted with one or more substituents independently selected from chloro, fluoro, hydroxy or alkyl. 15 An embodiment of the present invention includes compounds of Formula (II) wherein R9 and R10are independently selected from the group consisting1 of: 1- piperidinyl, 2-(pyrrolidin-1-yl)-ethoxy, 2,3-dihydroxy-propoxy, 2-hydroxy- 3-pyrrolidin-1-yl-propoxy, 3-(4-methyl-piperazin-1-yl)-propoxy, 3-(/V,rV- 20 dimethyl-amino)-propoxy, 3-hydroxy-propoxy, 3-imidazol-1-yl-propoxy, 3-methoxy-propoxy, 3-morpholin-4-yl-propoxy, 3-pyrrolidin-1 -yl-2- hydroxy-propoxy, 3-pyrrolidin-1 -yl-propoxy, 4-methyl-piperazin-1 -yl, amino, benzyl, benzyloxy, bromo, chloro, cyano, ethoxy, fluoro, H, hydroxy, isopropoxy, methoxy, methyl, A/-(1-oxo-ethyl)-amino, and N,N- 25 dimethyl-amino. An embodiment of the present invention includes compounds of Formula (II) wherein R6 and R7 are independently selected from the group consisting of: 30 (a) H; pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl. -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=0)NH(C1.2o)alkyl, or -C(=O)N(C1.20alkyl)2, wherein said -C(=0)NH(Ci-2o)alkyl, may be optionally substituted with one or more 5 groups independently selected from: -OH, -Oalkyl, -NH2, i-NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(atkyl)2, and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups 10 independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)i.3aryl or -C(=0)NHaryl, wherein said -C(=0)NHaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2l -NHalkyl, -N(alkyl)2, 15 heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1-pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, 20 -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH20H, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2l -NHalkyl, -N(alkyl)2l halogen or nitrile; 25 (p) -C(=S)NH2; (q) -C(=S)NHalkyl; (r) -C(=S)N(alkyl)2; (s) -S02NH2; (t) -S02NHalkyl; 30 (u) -S02N(alkyl)2; (v) -P(=0)(OCH3)2; and (w) -P(=0)(OCH2CH3)2; from: -OH, -Oalkyl, -NH2. -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or-OC(=0)alkyl; (I) -C(=O)NH(CH2CH2O-)1.i0 terminating with -H, methyl, ethyl, benzyl,-CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1- pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or-C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(C1.20)alkyl. or -C(=O)N(C1.20alkyl)2, wherein said -C(=O)NH(Ci.20)alkyl, may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH. -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)i.3aryl or -C(=0)NHaryl, wherein said -C(=0)NHaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1-pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl, or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; i (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of Formula (II) wherein R6 and R7 are independently selected from the group consisting of: (a) H; OH OH HO^^x^COjH HO^^-v^COzH (b) rk provided that R4 is not ^ ; (c) -CH2- substituted with one group selected from: -H, -methyl, -Oalkyl, -CH2OH. -CH(CH3)OH. -0(C=0)alkyl, -(C=0)0H, -C(=0)Oalkyl, -C(=0)Oaryl, -C(=0)Oheteroaryl, -(C=0)NH2, -(C=0)NHalkyl, -(C=0)N(alkyl)2, -C(=0)alkyl, -phenyl-OCH3 or -phenyl-0C(=0)alkyl; (f) -C(=0)alkyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -Oalkylaryl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, or -OC(=0)alkyl; (g) -C(=0)aryl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2. -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (h) -C(=0)(CH2)i^C(=0)- terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkyl0C(=O)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl or -N(alkyl>2; (i) -C(=0)0(CH2CH20-)i.io terminating with H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyloptionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -C(=0)OH. -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)Oaryl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. halogen, nitrile, or -OC(=0)alkyl; (I) -C(=0)NH(CH2CH20-)1.io terminating with -H, methyl, ethyl, benzyl,-CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1- pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl. -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or-C(=0)alkyl; (m) -C(=0)NH(Ci.2o)alkyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2. -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl>2, halogen or nitrile; (n) -C(=0)NHaryl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. halogen, nitrile, or -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1-pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH20H, -CH2CH2OCH3, -CH2CH2OCH2CH3l -CH2CH2OC(=0)alkyl, or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of Formula (II) wherein R6 and R7 are independently selected from the group consisting bf: (c) -CH2- substituted with one group selected from: -H, -methyl, -Oalkyl, -CH2OH, -CH(CH3)OH, -0(C=0)alkyl, -C(=0)Oalkyl, -(C=0)NH2, -C(=0)alkyl or -phenyl-OC(=0)alkyl; (f) -C(=0)alkyl optionally substituted with one or more groups 5 independently selected from: -OH, -Oalkyl, -Oalkyl-phenyl or -OC(=0)alkyl; (g) -C(=0)phenyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2. -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, chloro, fluoro,, nitrile, or 10 -OC(=0)alkyl; (h) -C(=0)(CH2)i.6C(=0)- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or pyrrolidinyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -Oalkyl; (i) -C(=O)O(CH2CH2O-)1.10 terminating with H or benzyl; 15 (j) -C(=0)Oalkyloptionally substituted with one or more -Oalkyl groups; (k) -C(=0)Ophenyl optionally substituted with one or more groups i independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, chloro, fluoro, nitrile, or -OC(=0)alkyl; 20 (I) -C(=0)NH(CH2CH20-)i.io terminating with -H; (m) -C(=0)NH(d-2o)alkyl optionally substituted with one or more groups independently selected from: -NH2, -NHalkyl, -N(alkyl)2, pyrrolidinyl, morpholinyl, -NHC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)phenyl or -C(=0)Oalkyl; and, wherein the phenyl portion of said -NHC(=0)phenyl 25 may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NHphenyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, 30 heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, chloro, fluoro, nitrile, or -OC(=0)alkyl; (o) -C(=O)NHCH2CH2NH(CH2CH2NH-)0-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1 -pyrrolidinyl, -CH2CH2-1 -piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl, and -C(=0)phenyl; wherein the phenyl portion of said -C(=0)phenyl may be optionally substituted 5 with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen and nitrile; (p) -C(=S)NH2; (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; 10 provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of Formula (II) wherein 15 R6 and R7 are independently selected from the group consisting of: (j) -C(=0)Oalkyloptionally substituted with one or more -Oalkyl groups; (k) -C(=0)Ophenyl optionally substituted with one or more gr6ups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, chloro. fluoro, nitrite, and -OC(=0)alkyl; (I) -C(=O)NH(CH2CH2O~)1.10 terminating with -H; (m) -C(=0)NH(Ci.2o)alkyl optionally substituted with one or more groups independently selected from: -NH2, -NHalkyl, -N(alkyl)2, pyrrolidinyl, morpholinyl, -NHC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)phenyl or -C(=0)Oalkyl; and, wherein the phenyl portion of said -NHC(=0)phenyl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2. -NHalkyl, -N(alkyl)2, halogen and nitrile; (n) -C(=0)NHphenyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, chloro, fluoro, nitrile, and -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o.3 terminating with -CH2CH20H and -C(=0)phenyl; wherein the phenyl portion of said -C(=0)phenyl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2. -NHalkyl, -N(alkyl)2, halogen and nitrile; (p) -C(=S)NH2; (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of Formula (II) wherein R6 and R7 are independently selected from the group consisting of: (a) H; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of 5 Formulae (II) wherein R6 and R7 are independently selected from the group consisting of: H, provided that R is not /> 1-methoxy-1-oxo-ethyl, 1-methyl-ethoxy-carbonyl, 1-oxo-butoxy-methyl, 1-oxo-ethoxy-methyl, 1-oxo-ethyl, 1-oxo-propyl, 2-(1 -oxo-ethoxy)-1 -oxo-ethyl, 2-(2-methoxy-1 -oxo-ethoxy)-1 -oxo-ethyl, 2-(2-methyl-1 -oxo-propoxy)-1 -oxo-ethyl, 2-amino-2-oxo-ethyl, 2,2-dimethyl-1 -oxo-propoxy-methyl, 2-ethoxy2-oxo-ethyl, 2-methoxy-2-oxo-ethyl, 2,6-difluoro-benzoyl, 2-[2-(2-hydroxy-ethoxy)-ethoxy]-ethoxy-carbonyl, 2-benzyloxy-1 -oxo-ethyl, 2-benzyloxy-ethoxy-carbonyl, 2-chloro-phenoxy-carbonyl, 2-fluoro-benzoyl, 2-hydroxy-1 -oxo-ethyl, 2-hydroxy-ethyl, 2-hydroxy-propyl, 2-methoxy-1-oxo-ethyl, 2-methoxy-ethoxy-carbonyl, 2-methyl-1-oxo-propyl, 2-oxo-propyl, 3-(A/,A/-diethyl amino)-1,3-dioxo-propyl, 3-1 H-pyrrolidin-1 -yl-1,3-dioxo-propyl, 3-ethoxy-1,3-dioxo-propyl, 3-1 H-pyrrolidin-1 -yl-1,3-dioxo-propyl, 4-(1-oxo-ethoxy)-benzyl, 4-amino-1,4-dioxo-n-butyl, 4-ethoxy-1,4-dioxo-n-butyl, 4-hydroxy-1,4-dioxo-n-butyl, 4-methoxy-1,4-dioxo-n-butyl, 4-chloro-benzoyl, 4-chloro-phenoxy-carbonyl, 4-fluoro-benzoyl, 4-fluoro-phenoxy-carbonyl, 4-methoxy-benzoyl, 5-(A/-methyl-amino)-1,5-dioxo-pentyl, 5-methoxy-1,5-dioxo-pentyl, benzoyl, diethoxy-phosphinyl, ethoxy-carbonyl, methoxy-carbonyl, methoxy-methyl, methyl, A/-(2-ethoxy-2-oxo-ethyl)-amino-carbonyl, A/-(2-1 H-pyrrolidin-1 -yl-ethyl)-amino-carbonyl, A/-(2-amino-ethyl)-amino-carbonyl, A/-(2-morpholin-4-yl-ethyl)-amino-carbonyl, A/-(3-ethoxy-3-oxo-propyl)-amino-carbonyl, A/-(3-fluoro-phenyl)-amino-carbonyl, A/-(pentadecyl)-amino-carbonyl, /V,A/-dimethyl-amino-sulfonyl, A/-[2-(2-methenyl-1-oxo-propoxy)-ethyl]-amino-carbonyl, A/-[2-(3-methyl-1 -methoxy-1 -oxo)-n-butyl]-amino-carbonyl, A/-[2-(4-methyl-1-methoxy-1-oxo)-pentyl]-amino-carbonyl, /V-[2-(/V,/v A/-[2-(/V-methyl-amino)-ethyl]-amino-carbonyl, W-[2-[2-(2-hydroxy-ethoxy)-ethoxy]-ethyl]-amino-carbonyl, A/-[2-[A/-(1-oxo-ethyl)-amino]-ethyl]-amino-ca rbonyl, A/-[2-[A/-(2-hydroxy-benzoyl)-amino]-ethyl]-amino-carbonyl, AA-[2-[A/-(2-hydroxy-ethyl)-amino]-ethyl]-amino-ca rbonyl, A/-[2-[A/-(2-methyl-1-oxo-propyl)-amino]-ethyl]-amino-carbonyl, A/-methyl-amino-carbonyl, /V-methyl-amino-thiocarbonyl, and phenoxy-carbonyl, provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. An embodiment of the present invention includes compounds of Formula (II) wherein L3 is absent or is a linking group selected from the group consisting of methylene, ethylene, carbonyl or -SO2-. A embodiment of the present invention includes compounds of Formula (II) wherein L3 is absent or is a linking group selected from the group consisting of methylene, ethylene or carbonyl. An embodiment of the present invention includes compounds of Formula (II) wherein © N-—' is selected from the group consisting of an aryl, a cycloalkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine1 to ten membered benzo-fused heterocycloalkyl. A embodiment of the present invention includes compounds of Formula (II) wherein © v— is selected from the group consisting of an aryl, a cycloalkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl and a nine to ten membered benzo-fused heterocycloalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein © v--' is selected from the group consisting of phenyl, cyclohexyl, furyl, imidazolyl, isoxazolyl, pyridyl, pyrimidinyl, indolyl, indazolyl, piperidinyl, morpholinyl, indanyl, 2,3-dihydro-1 H-indolyl and benzodioxolyl. A embodiment of the present invention includes compounds of Formula (II) wherein R5 is independently selected from the group consisting of: alkyl, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated thioalkyl, hydroxy, hydroxy alkyl, -NHC(=0)NH2, -NHS02alkyl, nitro, -S02alkyl, 4-v—B10-TF) -S02NH2, thio, thioalkyl, > ^^, and —V—B10—W—B20 A embodiment of the present invention includes compounds of Formula (II) wherein R5 is independently selected from the group consisting of: alkyl, alkyloxy, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated thioalkyl, hydroxy, .|_v—B10-(F) ■ hydroxy alkyl, nitro, -S02NH2, thioalkyl, p ^-^ , and —V— B10—W—B20. An embodiment of the present invention includes compounds of Formula (II) wherein R5 is independently selected from the group consisting of: methyl, ethyl, isopropyl, t-butyl, methoxy, ethoxy, -C(=0)NH2, -C(=0)Omethyl, -C(=0)Oethyl, -C(=0)OH, cyano, dimethyl-amino, bromo, chloro, fluoro, trifluoromethyl, trifluoromethoxy, thio-trifluoromethyl, hydroxy, hydroxymethyl, hydroxyethyl, nitro, -S02NH2, thiomethyl -§-V—B10-^ a^ _v_Bio_w_B20 An embodiment of the present invention includes compounds of Formula (II): wherein V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -NH-, -NHC(=0)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -0-, -0C(=0), -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, and -S02NH-. An embodiment of the present invention includes compounds of Formula (II): wherein V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=6)0-, -NH-, -O- and -S02-. An embodiment of the present invention includes compounds of Formula (II) wherein V is absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -NH-, -O- and -S02-. An embodiment of the present invention includes compounds of Formula (II) wherein V is absent or selected from the group consisting of: -C(=0)NH-, -C(=0)0-, -NH-, -O- and -S02-. An embodiment of the present invention includes compounds of Formula (II) wherein W is absent. An embodiment of the present invention includes compounds of Formula (II) wherein: B10 is absent or alkyl; and wherein when B10 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alky1)C(=0)NH2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, rN(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl. -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: B10 is absent or alkyl; and wherein when B10 is alkyl, the alkyl may be optionally substituted, with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy -NHC(=0)NH2, -NHS02alkyl, -S02alkyl or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: B10 is absent or selected from methyl or ethyl, ; wherein methyl or ethyl are optionally substituted with one or more groups independently selected from dialkylamino or hydroxy. An embodiment of the present invention includes compounds of Formula (II) wherein: B10 is absent or selected from methyl or ethyl, ; wherein methyl or ethyl are optionally substituted with one or more groups independently selected from dimethyl-amino or hydroxy. An embodiment of the present invention includes compounds of Formula (II) wherein: B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2l -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl. -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy. hydroxy, -NHC(=0)NH2, -NHS02alkyl or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: B20 is absent or H. An embodiment of the present invention includes compounds of Formula (II) wherein: vV is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents independently selected from alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=9)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl. nitro, -OC(=0)N(alkyl)2l -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: v-^ is selected from the group consisting of phenyl, imidazolyl, pyridinyl, pyrimidinyl, pyrrolidinyl, morpholinyl, piperazinyl and piperidinyl optionally substituted with one or more substituents independently selected from alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalky1, -NHS02alkyl, nitro, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: v_y is selected from the group consisting of phenyl, imidazolyl, pyridinyl, pyrimidinyl, pyrrolidinyl, morpholinyl, piperazinyl and piperidinyl optionally substituted with one or more substituents independently selected from alkoxy, alkyl, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, heteroaryl, hydroxy, hydroxy alkyl, -NHC(=0)NH2, -NHS02alkyl, nitro or-S02alkyl. An embodiment of the present invention includes compounds of Formula (II) wherein: is selected from the group consisting of phenyl, imidazolyl, pyridinyl, pyrimidinyl, pyrrolidinyl, morpholinyl, piperazinyl and piperidinyl optionally substituted with one or more substituents independently selected from methoxy, ethoxy, methyl, ethyl, bromo, chloro, fluoro, trifluoromethyi, pyridinyl, hydroxy or hydroxymethyl. A embodiment of the present invention includes compounds of Formula (II) wherein: N>--_-/ is selected from the group consisting of: 1-(3-methoxy- phenyl)-(S*)ethyl; 2-(3-bromo)-pyridyl; 2-(3-methyl)-pyridyl; 2-(3-methyl- 5-bromo)-pyridyl; 2-(4,6-dimethyl)-pyridyl; 2-(4-bromo)-pyridyl; 2- (piperidin-l-yl)-ethyl; 2,2-difluoro-1,3-benzodioxol-4-yl; 2,3-dichloro- benzyl; 2,3-dichloro-phenyl; 2,3-dihydro-1H-indol-1-yl; 2,3-dimethoxy- benzyl; 2,4,6-trifluoro-phenyl; 2,4-dichloro-phenyl; 2,4-difluoro-benzyl; 2,4-dimethoxy-phenyl; 2,4-dimethoxy-phenyl; 2,5-dichloroLbenzyl; 2,5- dichloro-phenyl; 2,5-difluoro-benzyl; 2,5-difluoro-phenyl; 2,5-dimethoxy- benzyl; 2,5-dimethoxy-phenyl; 2,6-dichloro-benzyl; 2,6-difluoro-benzyl; 2.6-difluoro-phenyl; 2-bromo-3-fluoro-phenyl; 2-bromo-benzyl; 2-bromo- phenyl; 2-chloro-benzyl; 2-chlorophenyl; 2-ethyl-phenyl; 2-fluoro-benzyl; 2-fluoro-phenyl; 2-furyl; 2-isopropyl-phenyl; 2-methoxy-benzyl; 2- methoxy-phenyl; 2-methyl-benzyl; 2-methyl-phenyl; 2-morpholin-4-yl- ethyl; 2-pyridyl; 2-pyridyl-methyl; 2-trifluoromethoxy-benzyl; 2- trifluoromethoxy-phenyl; 2-trifluoromethyl-4-bromo-phenyli 2- trifluoromethyl-benzyl; 2-trifluoromethyi-phenyl; 3-(1 -hydroxy-ethyl)- phenyl; 3-(2,4-dimethoxy)-pyridyl; 3-(2-chloro)-pyridyl; 3-(2-hydroxy- ethyl-amino-carbonyl)-phenyl;3-(4-methoxy)-pyridyl; 3-(4-methyl- piperazinyl-carbonyl)-phenyl; 3-(4-trifluoromethyl)-pyridyl; 3-(amino- carbonyl)-phenyl; 3-(amino-sulfonyl)-pheny(; 3-(ethoxy-carbony!)-phenyl; 3-(methoxy-carbonyl)-phenyl; 3-(trifluoromethyl-thio)-phenyl; 3,4,5- trimethoxy-phenyl; 3,4-dichloro-benzyl; 3,4-dichloro-phenyl; 3,4-difluoro- benzyl; 3,4-dimethoxy-phenyl; 3,4-dimethyl-benzyl; 3,4-methylenedioxy- phenyl; 3,5-di(tert-buty!)-phenyl; 3,5-di(trifluoromethyl)-phenyl; 3,5- dichloro-benzyl; 3,5-dichloro-phenyl; 3,5-difluoro-phenyl; 3,5-dimethoxy- phenyl; 3,5-dimethyl-phenyl; 3-[/V-(3-pyrrolidin-1 -yl-propyl)-amino- i carbonyl]-phenyl; 3-benzyloxy-phenyl; 3-bromo-phenyl; 3-carboxy- phenyl; 3-chloro-4-fluoro-phenyl; 3-chloro-4-methoxy-phenyl; 3-chloro-4- methyl-benzyl; 3-chloro-benzyl; 3-chloro-phenyl; 3-cyano-phenyl; 3- ethoxy-phenyl; 3-ethyl-phenyl; 3-fluoro-benzyl; 3-fluoro-phenyl; 3- hydroxymethyl-phenyl; 3-hydroxy-phenyl; 3-isopropoxy-phenyl; 3- methoxy-5-trifluoromethyl-phenyl; 3-methoxy-benzyl; 3-methyl-benzyl; 3- methyl-phenyl; 3-methylthio-phenyl; 3-pyridyl; 3-pyridyl-methyl; 3- trifluoromethoxy-phenyl; 3-trifluoromethyl-phenyl; 4-(4-methyl-piperazin- 1-yl)-phenyl; 4-(ethoxy-carbonyl)-phenyl; 4-(/V,/N/-dimethyl-amino)-phenyl; 4-(piperidin-4-yl-sulfonyl)-phenyl; 4-benzyloxy-phenyl; 4-bromo-phenyl; 4-chloro-3-methyl-benzyl; 4-chloro-phenyl; 4-cyano-phenyl; 4- dimethylamino-phenyl; 4-fluoro-3-chloro-phenyl; 4-fluoro-3-nitro-phenyl; 4-fluoro-3-trifluoromethyl-phenyl; 4-fluoro-benzyl; 4-fluoro-phenyl; 4- methoxy-benzyl;4-methyl-3-[A/-[4-(3-pyridyl)-pyrimidin-2-yl]amino]- phenyl; 4-methyl-benzyl; 4-methyl-phenyl; 4-trifluoromethoxy-phenyl; 4- trifluoromethyl-phenyl; 5-(phenyl)-isoxazol-3-yl-methyl; 5-bromo-2,3- dihydro-1 H-indo!-1-yl; 5-chloro-2-methoxy-phenyl; 5-ch!oro-2-methyl- -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; provided that when L2 is -O-, neither R6 nor R7 is -CH3; R100 is selected from: alky), hydroxy, aryl, oxo or =N(OH); 5 R10 is independently selected from the group consisting of 4x'-A*-© -IT*"-® 4*'-® HD » » * » -X'-A^-Y^A21, -X'-A^-A21, -X1-A21, -A20-A21 and -A21, wherein 10 X1 and Y1 are each independently absent or selected from the group consisting of: -NH-, -O-, -S02- and -SO2NH-; A20 is absent or alkyl; wherein when A20 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, 15 alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, 20 -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; A21 is selected from alkyl, alkenyl, or H; wherein when A21 is alkyl or alkenyl, the alkyl or alkenyl may be 25 optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2l 30 -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2. -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(-0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thioorthioalkyl; and © x— is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkyiamino, -NHC(=0)alkyl. -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2> -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl. -OC(=0)NHa»kyl. -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl. thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2> -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; (c) -CH2- substituted with one group selected from: -H, -methyl, -Oalkyl, -CH2OH, -CH(CH3)OH, -0(C=0)alkyl, -(C=0)OH, -C(=0)Oalkyl, -C(=0)Oaryl, -C(=0)Oheteroaryl. -(C=0)NH2, -(C=0)NHalkyl, -(C=0)N(alkyl)2, -C(=0)alkyl, -phenyl-OCH3 or -phenyl-0C(=0)alkyl; (d) -C(=O)(CH2CH2O-)i.i0 terminating with H; (e) -C(=0)CH20(CH2CH20-)i-io terminating with H; (f) -C(=0)alkyl optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -Oalkylaryl, -NH2l -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. or -OC(=0)alkyl; (g) -C(=0)(CH2)i.3aryl or -C(=0)aryl, wherein said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (h) -C(=0)(CH2)i-6C(=0)-terminating with methyl, ethyl,-OH,-Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl or -N(alkyl)2; (i) -C(=O)O(CH2CH2O-)1.10 terminating with H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyloptionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2l heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -C(=0)OH. -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or-C(=0)N(alkyl)2; (k) -C(=0)0(CH2)i.3aryl or -C(=0)Oaryl, wherein said -C(=0)Oaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -0C(=0)alkyl; (I) -C(=O)NH(CH2CH2O-)1.10 terminating with -H, methyl, ethyl, benzyl,-CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1- pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=0)NH(Ci^o)alkyl, or -C(=O)N(C1.20alkyl)2l wherein said -C(=0)NH(Ci.2o)alkyl, may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)1.3aryl or -C(=0)NHaryl, wherein said -C(=0)NHaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. halogen, nitrile, or -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1-pyrrolidinyl, -CH2CH2-1 -piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; (q) -C(=S)NHalkyl; (r) -C(=S)N(alkyl)2; (s) -S02NH2; (t) -S02NHalkyl; (u) -S02N(alkyl)2; (v) -P(=0)(OCH3)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent; L3 is absent or is a linking group selected from the group consisting of methylene, ethylene, carbonyl or-S02-; v—' is selected from the group consisting of an aryl, a cycloalkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated thioalkyl, hydroxy, hydroxy alkyl, -NHC(=0)NH2, -NHS02alkyl, nitro. -S02alkyl, -SO2NH2, thio, thioalkyl, "* ^^, and —V—B10—W—B20; wherein V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-. -NH-, -NHC(=0)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -O-, -OC(=0). -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, and -S02NH-; B10 is absent or alkyl; wherein when B10 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2l -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl. -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents independently selected from alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl. -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. -OC(R100)2-, -S-, -NH-, -Nflower alkyl)-. -N(COalkyl)-,-N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; R100is selected from: alkyl, hydroxy, aryl, oxo or =N(OH); 5 R10 is independently selected from the group consisting of 4*'-*K2). -HKs), i-®. _X-_A*_Y,_A„. —X1—A20—A21 and —X1—A21, wherein X1 and Y1 are each independently absent or -0-; 10 A20 is absent or alkyl; wherein when A20 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy, -NHC(=0)NH2, -NHS02alkyl, -S02alkyl orthioalkyl; 15 A21 is selected from alkyl, alkenyl, or H; wherein when A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy, -NHC(=0)NH2, -NHS02alkyl or 20 thioalkyl; and v— is selected from the group consisting of aryl, heteroaryl and heterocycloalkyl optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, 25 -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl. -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl. -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or 30 -OC(=0)N(alkyl)2; pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=0)NH(Ci.2o)alkyl, or -C(=O)N(C1.20alkyl)2l wherein said -C(=0)NH(Ci-2o)alkyl, may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrite; (n) -C(=0)NH(CH2)i-3aryl or -C(=0)NHaryl, wherein said -C(=0)NHaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=O)NHCH2CH2NH(CH2CH2NH-)0.3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1 -pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1-piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl, or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent; L3 is absent or is a linking group selected from the group consisting of methylene, ethylene or carbonyl; —' is selected from the group consisting of an aryl, a cycloalkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of. alky], alkyloxy, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated thioalkyl, hydroxy, 4-V-B10 B10—W—B20; wherein V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-f -NH-, -O- and -S02-; B10 is absent or alkyl; wherein when B10 is alkyl, the alkyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy -NHC(=0)NH2, -NHS02alkyl, -S02alkyl or thioalkyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, dialkylamino, halogen, halogenated alkoxy, hydroxy, -NHC(=0)NH2, -NHS02alkyl or thioalkyl; and v~^ is selected from the group consisting of phenyl, imidazolyl, pyridinyl, pyrimidinyl, pyrrolidinyl, morpholinyl, piperazinyl and piperidinyl optionally substituted with one or more substituents independently selected from alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -SC^alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2.-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2. -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl. thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. R100 is selected from the group consisting of: H and alkyl; RBand Rc are independently selected from the group consisting of: alkoxy; and R5is selected from the group consisting of: alkoxy and halogen; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof. A preferred embodiment of the present invention includes compounds of Formula (ll-AA) wherein R100 is selected from the group consisting of: H, methyl, ethyl; RB and Rc are independently selected from the grdup consisting of: methoxy and ethoxy; and R5 is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, bromo, and fluoro. The present invention is further directed to compounds of Formula (II- Rcis-0(CH2)3OH; R100 is selected from the group consisting of: H and alkyl; RB is selected from the group consisting of: alkoxy; and R5is selected from the group consisting of: alkoxy and halogen; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. A preferred embodiment of the present invention includes compounds of Formula (ll-BB) wherein R100 is selected from the group consisting of: H, methyl, ethyl; RB is selected from the group consisting of: methoxy and ethoxy; and R5is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, bromo, and fluoro. wherein R100 is selected from the group consisting of: H and alkyl; RB and Rc are independently selected from the group consisting of: alkoxy; and R5is selected from the group consisting of: alkyl, cyano, hydroxy, alkoxy and halogen; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. A preferred embodiment of the present invention includes compounds of Formula (ll-CC) wherein R100 is selected from the group consisting of: H, methyl, ethyl; RBand Rc are independently selected from the group consisting of: methoxy and ethoxy; and R5is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, methyl, cyano and hydroxy. Rc is -0(CH2)3OH; R100 is selected from the group consisting of: H and alkyl; RB is selected from the group consisting of: alkoxy; and R5is selected from the group consisting of: alkyl, cyano, hydroxy, alkoxy and halogen; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. i A preferred embodiment of the present invention includes compounds of Formula (ll-DD) wherein R100 is selected from the group consisting of: H, methyl, and ethyl; RB is selected from the group consisting of: methoxy and ethoxy; and R5 is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, methyl, cyano and hydroxy. The present invention is further directed to compounds of Formula R10 is independently selected from the group consisting of —-— x1 A22 CG ) $ W and-X'-A^-Y'-A21; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyl)-, -C(=0)N(alky1)-, -C(=0)NH-. -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-. -N(alkyl)C(=0)0-, -N(alkyl)S02-. -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=O)0alkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl. -0C(=0)alkyl, -OC(=0)N(alkyl)2> -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; — is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle^ heteroaryl, heterocycloalkyl, nine'to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano. alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; s is an integer from 0 to 2; m is an integer from 0 to 4; provided that the sum of m and s is an integer from 0to4; R6 and R7 are independently selected from the group consisting of: (a) H; OH QH H0^^\^CO2H HO^/k^C02H HO*"V° HO^'Y0 (b) rk- provided that R4 is not J^ ; (c) -CH2- substituted with one group selected from: -H, -methyl, -Oalkyl, -CH2OH, -CH(CH3)OH, -0(C=0)alkyl, -(C=0)OH, -C(=0)Oalkyl, -C(=0)Oaryl, -C(=0)Oheteroaryl, -(C=0)NH2, -(C=0)NHalkyl, -(C=0)N(alkyl)2, -C(=0)alkyl, -phenyl-0CH3 or -phenyl-OC(=0)alkyl; (d) -C(=O)(CH2CH2O-)i-i0 terminating with H, methyl, ethyl, or benzyl; (e) -C(=0)CH20(CH2CH20-)i.io terminating with H, methyl, ethyl, or benzyl; (f) -C(=0)alkyl, or -C(=0)(C3-6)cycloalkyl, wherein said -C(=0)alkyl, and -C(=0)(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -Oalkylaryl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, or -OC(=0)alkyl; (g) -C(=0)(CH2)i.3aryl, -C(=0)aryl, -C(=0)(CH2)i.3heteroaryl, or -C(=0)heteroaryl, wherein said -C(=0)(CH2)1.3aryl, -C(=0)aryl, -C(=0)(CH2)i.3heteroaryl, and -C(=0)heteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -0C(=0)alkyl; (h) -C(=0)(CH2)^C(=0)-terminating with methyl, ethyl,-OH,-Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(=O)O(CH2CH2O-)1.10 terminating with H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyl, or -C(=0)0(C3-6)cycloalkyl, wherein said -C(=0)Oalkyl, and -C(=0)0(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. -OC(=0)alkyl, -C(=O)0H, -C(=0)Oalkyl, -C -C(=0)N(alkyl)2; (k) -C(=O)0(CH2)1.3aryl, -C(=0)Oaryl, -C(=0)O(CH2)i-3rieter6aryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i.3heteroaryl, or-C(=0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl>2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrite, or-OC(=0)alkyl; (I) -C(=O)NH(CH2CH2O-),.10 terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2. -CH2CH2-1- pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or-C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(Ci.20)alkyl, -C(=0)NH(C3.6)cycloalkyl. or -C(=0)N(alkyl)2, wherein said -C(=O)NH(C1.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2. heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl. -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or-C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)1.3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)i-3heteroaryl, or -C(=0)NHheteroaryl, wherein said -C(=0)NH(CH2)i-3aryl, -C(=0)NHaryl. -C(=0)NH(CH2)i.3heteroaryl, and -C(=0)NHheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, —' is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, aralkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino. -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2l -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2, thio, thioalkyl, > ^^, and —V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -O-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independehtly selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0,)alkyl, -N(alkyl)C(=0)N(alkyl)2> -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl. -NHC(=0)N(alkyl)2f -NHC(=0)NH2, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioatkyl; and (J) v_/ is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(^0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2> -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. Further embodiments of the invention include compounds of Formula II- FF wherein L2, R4, R6, R7, L3 H, and (R5)r vary as set forth in section 2.a.1 above for Formula II and combinations of the variations thereof. In a preferred embodiment, the present invention is further directed to compounds of Formula (ll-GG): wherein Formula A-1-c is attached on the a6 side to adjacent carbons on the d'or d2 side of Formula A-1; wherein R8 is H or alkyl; wherein Formula A-2 is attached on the b2 side of Formula A-2 to the L2 ring of Formula (ll-GG), and A1, A2, A3, A4 are (i) -N-; or (ii) -C- substituted with H or alkoxy, wherein the alkoxy may be optionally further substituted with alkoxy on a terminal carbon or up to 3 halogen atoms on a terminal carbon; provided that at least one and no more than two qf A1, A2, A3, A4 wherein Formula A-3 is attached on the b3 side of Formula A-3 to the L2 ring of Formula (ll-GG), and B1, B2 and B3 are independently (i) -CH- optionally substituted with alkyl, aryl, alkoxy, or halogen, (ii) -S-; (iii) -0-; or (iv) -N-; provided that no more than one of B1, B2 or B3 is -S-or -0-, and, provided that when one of B1, B2 or B3 is -S-or -0-, then the adjacent ring members are not -S-or -O-; R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oaikyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2. -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; L2 is a linking group selected from the group consisting of: -(CH2)i-4-, -CH(R100)-, -C(=R100h -C(R100)r . -0-, -0(CH2)i-r. -OCH(R100)-, -OC(R100)r. -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; wherein R100 is selected from: alkyl, hydroxy, aryl, alkoxy, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH; provided that when L2 is -OCH(R100)-, R100 is alkoxy, and V-^ jS phenyl, R5 is not-C(=0)NH-NH2; R10 is independently selected from the group consisting of -I— X1 A22 (7) $ W and-X1-A20-Y1-A21; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyl)-, -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-f -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -0C(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halbgen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl. -N(alkyl)C(=0)Oalkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; v—' is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -0C(=O)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -SOjalkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; s is an integer from 0 to 2; (T m is an integer from 0 to 4; provided that when N—- is not substituted with Formulae A-1-a, A-1-b or A-1-c, the sum of m and s is an integer from 0 0 to 4, and when —- is substituted with one of Formulae A-1-a, A-1-b, or A-1-c, the sum of m and s is an integer from 0 to 2; Rs and R7 are independently selected from the group consisting of: (a) H; OH OH HOV^^N>C°2H HCV/k^COjH Hcr^f° HO**' Y° (b) ik provided that R4 is not N*" (c) alkyl (d) -C(=0)alkylOH; and (e) -C(=0)CH2Oalkoxy; v—' is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, aralkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2)-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2l -NHC(=0)NH2, -NHC(=0)NHalkyl, -NI^C(=0)Oallcyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2l thio, thioalkyl, * ^-^, and —V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-. -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -0-, -0C(=0), -OG(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl. -N(alkyl)C(=0)N(alkyl)2t -N(alkyl)C(=0)NH2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2. -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and v-^ is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, i hydroxy alkyl, -N(alkyl)C(=0)alkyl. -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2l -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof. Further embodiments of the invention include compounds of Formula II- GG wherein E, L2, R4, L3 H, and (R5)r vary as set forth in section 2.a.1 above for Formula II, and R6 and R7 vary as set forth below, and combinations of the aforementioned variations of E, L2, R4, L3 H, (R5)r, R6 and R7 wherein Formula A-2 is attached on the b2 side of Formula A-2 to the L2 ring of formula (ll-HH), and A1, A2, A3, A4 are (i) -N-; or (ii) -C- substituted with H or alkoxy, wherein the alkoxy may be optionally further substituted with alkoxy on a terminal carbon or up to 3 halogen atoms on a terminal carbon; provided that at least one and no more than two of A1, A2, A3, A4 wherein Formula A-3 is attached on the b side of Formula A-3 to the L2 ring of formula (ll-HH), and B\ B2 and B3 are independently (i) -CH- optionally substituted with alkyl, aryl, alkoxy, or halogen, (ii)-S-; (iii^-O-; or(iv) -N-; provided that no more than one of B1, B2 or B3 is -S-or -0-, and, provided that when one of B1, B2 or B3 is -S-or -0-, then the adjacent ring members are not *S-or -0-; R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2. -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyl)-, -C(=0)N(alkyl)-( -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)SO?-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-. -OC(=0)0-, -S-, -SO-, -SO2-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyt)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; © N—' is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NH0(=O)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl. -OC(=0)NHalkyl. -NHC(=0)Oalkyl. -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; s is an integer from 0 to 2; c? m is an integer from 0 to 4; provided that when x—■ is not substituted with Formulae A-1-a, A-1-b or A-1-c, the sum of m and s is an integer from 0 (T to 4, and when x—' is substituted with one of Formulae A-1 -a, A-1 -b, or A-1-c, the sum of m and s is an integer from 0 to 2; -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2. heterocycloalkyl, -NHC(=0)alkyl. -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (h) -C(=0)(CH2)i^C(=0)- terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(=O)O(CH2CH2O-)1.10 terminating with H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyl, or -C(=0)0(C3^)cycloalkyl. wherein said -C(=0)Oalkyl, and -C(=0)0(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl. -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i.3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2)1.3aryl, -C(=0)Oaryl, -C(=0)O(CH2)i.3heteroaryl, or -C(=0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl. -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl. -NHC(=0)alkyl, -NHS02alkyl. halogen, nitrile, or -OC(=0)alkyl; (I) -C(=0)NH(CH2CH20-)i.io terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CHr1- pyrrolidinyl, -C^CH^I-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or-0(=O)alkyl; (m) -C(=0)NH2, -C(=0)NH(Ci.2o)alkyl. -C(=0)NH(C36)cycloalkyl, or -C(=0)N(alkyl)2, wherein said -C(=O)NH(Ci.20)alkyl, -C^OJNHtCs-ejcycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl. -NH2, -NHalkyl, -N(alkyl)2. heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; L is absent or is a linking group selected from the group consisting of alkyldiyl, carbonyl or -S02-; ©• x—' is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, aralkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated SOralkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyt,-N(alkyl)C(=0)N(alkyl)2l-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, .£_v B10-T?) -S02NH2, thio,thioalkyl. 5 ^-y, and—V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)SOr. -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-. -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl, alkenyl, or H; i wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(a'lkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2> -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl. -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyr, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl>2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl. -NHC(=0)alkyl, -NHC(=0)N(a!kyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alky1, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. Further embodiments of the invention include compounds of Formula II- HH wherein E, R4, R6, R7, L3 H, and (R5)r vary as set forth in section 2.a.1 above for Formula II, and L2 varies as set forth below, and combinations of the aforementioned variations of E, L2. R*. R6, Rr. L3 H, (R5)r In a preferred embodiment of the invention are compounds of Formula ll-HH, wherein L2 is a linking group selected from the group consisting of: -(CH2)-, -CH(CH3)-, -CH(CH2CH3)-. In a preferred embodiment, the present invention is further directed to 5 compounds of Formula (ll-JJ): -C(=0)(CH2)i.3heteroaryl, and -C(=0)heteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or-OC(=0)alkyl; (h) -C(=0)(CH2)1.6C(=0)-terminating with methyl, ethyl,-OH,-Oalkyl, -NH2, -NHalkyl. -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl. -N(alkyl)2, or heterocycloalkyl; (i) -C(=0)0(CH2CH20-)1.10 terminating with H, methyl, ethyl, or benzyl; 0) -C(=0)Oa)kyl, or-C(=0)0(C36)cycloalkyl. wherein said -C(=0)Oalkyl, and -C(=0)0(C3^)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl>2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl. -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2),.3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i.3heteroaryl, or -C(=0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl. -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. halogen, nitrile, or -0C(=0)alkyl; (I) -C(=0)NH(CH2CH20-)i_io terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1- pyrrolidinyl, -CH2CH2-1-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1- piperazinyl, -CH2CH2-1-(4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(C1.20)alkyl, -C(=0)NH(C3^)cycloalkyl. or -C(=0)N(alkyl)2, wherein said -C(=O)NH(C1.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, and -C(=0)N(alkyl)2rnay be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl. -C(=0)OH. -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or-C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally -NHC(=0)NH, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -0C(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl.may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2l -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl. -NHC(=0)N(alkyl)2> -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl. -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; ^s is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl. thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; m is an integer from 0 to 4; provided that when v—' is not substituted with Formulae A-1-a, A-1-b or A-1-c, the sum of m and s is an integer from 0 (? to 4, and when x—' is substituted with one of Formulae A-1-a, A-1-b, or A-1-c, the sum of m and s is an integer from 0 to 2; L? is absent or is a linking group selected from the group consisting of alkyldiyl, carbonyl or -S02-; v—y is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, aralkyl, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated SOralkyf, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)SO?alkyl, -NHC(=0)alkyl. -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl. -NHS02alkyl. nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, 4-v—B10-^F) -S02NH2, thio, thioalkyl, ' ^^, and —V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-. -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-. -NH-. -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)O, -NHS02-, -0-, -OC(=0). -OC(=0)N(alkyl)-, -OC(=0)NH-, -0C(=O)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NH2l -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl. -OC(=0)N(alkyl)2l -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl. heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2. -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2l -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2l -OC(=0)NHalkyl, -S02alky1, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof; comprising wherein Formula A-3 is attached on the b3 side of Formula A-3 to the L2 ring of 10 formula (II), and B1, B2 and B3 are independently (i) -CH- optionally substituted with alkyl, aryl, alkoxy, or halogen, (ii) -S-; (iii) -0-; or (iv) -N-; provided that no more than one of B1, B2 or B3 is -S-or -0-, and, provided that when one of B1, B2 or B3 is -S-or -O-, then the adjacent ring members are not -S-or -0-; 15 R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, 20 -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl. -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -0C(=0)N(alkyl)2> -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; 25 L2 is a linking group selected from the group consisting of: -(CH2)i^-, -CH(R100)-, -C(=R100)-, -C(R100)2-, -0-, -0(CH2)^-, -OCH(R100)-, -OC(R100)2-, -S-, -NH-, -N(lower alkyl)-, -N(COalkyl)-, -N(aryl)-, -N(C02alkyl)-, -N(CONHalkyl)-, -N(S02alkyl) and -N(S02aryl)-; wherein R100is selected from: alkyl, hydroxy, aryl, alkoxy, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH; R10 is independently selected from the group consisting of —-— x1 A2Q CG) $ W and-X1-A20-Y1-A21; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyl)-, -C(=0)N(alkyl)-. -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-. -NHC(=0)NH, -NHC(=0)0-, -NHSCV, -0-, -OC(=0). -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -SOzNH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2l -NHC(=0)NH2, -NHC(=0)NHalkyi, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2. -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; —y is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl. halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; s is an integer from 0 to 2; m is an integer from 0 to 4; provided that when x—- is not substituted with Formulae A-1-a, A-1-b or A-1-c, the sum of m and s is an integer from 0 to 4, and when v—' is substituted with one of Formulae A-1 -a, A-1-b, or A-1 -c, the sum of m and s is an integer from 0 to 2; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof; reacting a compound of formula (T1) with 1,1'-thiocarbonyldiimidazole, in the presence of a base, in an aprotic solvent, to yield the corresponding compound of formula (T5). The present invention is further directed to a process for the preparation of compounds of formula (T3) R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2. -NHC(=0)NH2, -NHC(=0)NHalkyl. -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2l ' -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; N~^ is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl. -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alky!)2, -N(alkyl)C(=0)N(alkyl)2 or -0C(=0)N(alkyl)2; s is an integer from 0 to 2; m is an integer from 0 to 4; provided that when v—' is not substituted with Formulae A-1-a, A-1-b or A-1-c, the sum of m and s is an integer from 0 (T to 4, and when x—' is substituted with one of Formulae A-1 -a, A-1-b, or A-1-c, the sum of m and s is an integer from 0 to 2; L3 is absent or is a linking group selected from the group consisting of alkyldiyl, carbonyl or -S02-; ^-^ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, aralkyl, a heteroaryl , a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, a nine to ten membered benzo-fused heteroaryl, and a nine to ten membered benzo-fused heterocycloalkyl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2l -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NhC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2, thio, thioalkyl, *~" ~K-^, and —V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -0-, -OC(=0). -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-. -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl. -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2l -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2l -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and ^~y is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, i halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2> -NHC(=0)NH2> -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2. -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof; comprising Unless otherwise noted, the term "alkyl" as used herein, whether used alone or as part of a substituent group, includes straight and branched chains having 1 to 10 carbon atoms, or any number within this range. For example, alkyl radicals include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec- butyl, f-butyl, n-pentyl, 3-(2-methyl)butyl, 2-pentyl, 2-methylbutyl, neopentyl, n- hexyl, 2-hexyl, 2-methylpentyl, and the like. Unless otherwise noted, lower alkyl shall include straight and branched chains having 1 to 4 carbon atoms, or any number within this range. Unless otherwise noted, the terms "alkoxy" or "alkyloxy" are used synonymously herein, and as used herein, whether used alone or as part of a substituent group, denotes an oxygen ether radical of the above described straight or branched chain alkyl groups. For example, alkoxy radicals include methoxy, ethoxy, n-propoxy, sec-butoxy, f-butoxy, n-hexyloxy and the like. Specific placement of the oxygen atom in relation to the alkyl portion is specified in the following manner, "-Oalkyl" or "-alkylO-", to describe -OCH3 and -CH20- respectively (wherein alkyl is methyl for purposes of the example). Unless otherwise stated, "aryl," employed alone or in combination with other terms (e.g., aryloxy, arylthioxy, arylalkyl), shall mean an aromatic ring 1K7 structure comprising carbon atoms, for example, phenyl, naphthyl, fluorenyl, and the like. As used herein, unless otherwise noted, "aralkyl" shall mean any lower > alkyl group substituted with an aryl group such as phenyl, naphthyl and the like, far example, benzyl, phenylethyl, phenylpropyl, naphthylmethyl, and the like. Unless otherwise noted, the term cycloalkyl' as used herein, whether used alone or as part of a substituent group, shall mean any stable 3-10 i membered, saturated ring system, for example cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl. Unless otherwise noted, the term "partially unsaturated carbocycle" as used herein, whether used alone or as part of a substituent group, shall mean > any stable 5-10 membered, partially unstaturated ring system, wherein the carbocycle contains, at least one unsaturated bond, for example cyclopentenyl, cyclohexenyl, cycloheptenyl, and" the like. Unless otherwise noted, the term "heteroaryl group" as used herein, i whether used alone or as part of a substituent group, shall denote any five to ten membered monocyclic or bicyclic aromatic ring structure which containing carbon atoms and at least one heteroatom selected from the group consisting of O, N and S, optionally containing one to four additional heteroatoms independently selected from the group consisting of O, N and S. The > heteroaryl group may be attached at any heteroatom or carbon atom of the ring such that the result is a stable structure. Examples of suitable heteroaryl groups include, but are not limited to, pyrrolyl, furyl, thienyl, oxazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, triazolyl, thiadiazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, pyranyl, furazanyl, indolizinyl, indolyl, isoindolinyl, ) indazolyl, benzofuryl, benzothienyl, benzimidazolyl, benzthiazolyl, purinyl, quinolizinyl, quinolinyl, isoquinolinyl, isothiazolyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, naphthyridinyl, pteridinyl, and the like. As used herein, the term 'heterocycloalkyl" shall denote any five to ten membered monocyclic or bicyclic, saturated or partially unsaturated ring structure containing C atoms and at least one heteroatom selected from the group consisting of O, N and S, optionally containing one to founadditional heteroatoms independently selected from the group consisting of O, N and S. The monocyclic or bicyclic heteroalkyl group may be attached at any heteroatom or carbon atom of the ring such that the result is a stable structure. Examples of suitable monocyclic or bicyclic heteroalkyl groups include, but are not limited to, pyrrolinyl, pyrrolidinyl, dioxolanyl, imidazolinyl, imidazolidinyl, pyrazolinyl, pyrazolidinyl, piperidinyl, dioxanyl, morpholinyl, dithianyl, thiomorpholinyl, piperazinyl, trithianyl, indolinyl, chromenyl, 1,3- methylenedioxypheny! (equivalent to benzofused dioxolyl), 1,4- ethylenedioxyphenyl (equivalent to benzofused dioxanyl), 2,3-dihydrobenzofuryl, and the like. As used herein, unless otherwise noted, the term "benzo-fiised heteroaryl" shall mean a bicyclic ring structure wherein one of the rings is phenyl and the other is a five to six membered heteroaryl. The benzo-fused heteroaryls are a subset of heteroaryls. Suitable example include, but are not limited to, indolyl, isoindolyl, benzofuryl, benzothienyl, indazolyl, benzthiazolyl, quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, pteridinyi, and the like. As used herein, unless otherwise noted, the term "benzo-fused heterocycloalkyl" shall mean a bicyclic ring structure wherein one of the rings is phenyl and the other is a five to six membered heterocycloalkyl. The benzo- fused heterocycloalkyls are a subset of the heterocycloalkyl groups. Suitable examples include, but are not limited to, 1,3-benzodioxolyl (also kpown as 1,3- methylenedioxyphenyl), indolinyl, 1,4-benzodioxolanyl (also known as 1,4- ethylenedioxyphenyl), benzodihydrofuranyl, benzotetrahydropyranyl, i benzodihydrothiophene and the like. As used herein, unless otherwise noted, the term "benzo-fused cycloalkyl" shall mean a bicyclic ring structure wherein one of the rings is phenyl and the other is a three to eight membered cycloalkyl. Suitable examples include, but are not limited to indanyl, 1,2,3,4-tetrahydronaphthyl, 6,7,8,9,-tetrahydro-5H-benzocycloheptenyl, 5,6,7,8,9,10-hexahydro- benzocyclooctenyl, and the like. As used herein, the term "linking group" is intended to refer to a divalent radical derived by, for example, the removal of at least one hydrogen atom from each of two different atoms, or the removal of two hydrogen atoms from a single atom, such that the two monovalent radical centers, or the single divalent radical center, form bonds with different atoms. As used herein, the term "alkyldiyl" shall include straight and branched chain of 1 to 10 carbon atoms, or any number within this range, divalent or monovalent hydrocarbon radicals derived by the removal of one hydrogen atom from each of two different carbon atoms, or by the removal of two hydrogen atoms from a single carbon atom. Examples include methyldiyl (also referred to herein as methylene), and ethyldiyls (also referred to herein as ethylene), such as ethan-1,1-diyl, and ethan-1,2-diyl. In general, IUPAC nomenclature rules are used throughout this disclosure. Nomenclature for radical substituents is derived by first indicating the functionality having the point of attachment with a hyphen, followed by the adjacent functionality toward the terminal portion of the side chain, as in: -(Ci.io)alkyl-C(0)NH-(Ci-io)alkyl-Phenyl , or, when a lead hyphen is not used, by describing the terminal portion of the side chain first, followed by the adjacent functionality toward the point of attachment, as in: phenyl-(Ci.io)alkylamido(Cii0)alkyl, or phenylalkylamidoalkyl Where the are two point of attachment, for example in a linking group, or a ring member, the two points of attachment are indicated with a lead hyphen and a final hypen. For example, the points of attachment of a linking group having two monvalent radical centers would be indicated as -(CH2)2- or -0(CH2)2- and the like; and the points of attachment of a linking group having a single divalent radical center would be indicated as -NH- or -N(C=0 alkyl)- and the like. Points of attachment for an aromatic ring member would be indicated as -N-., -S-br-CH- and the like, for example. Where the phrase "terminating with" is used, the point of attachment for the terminal substitucnt is indicated by the second dash. For example, for the phrase "-C{-0)-(CH2CH20-)i-io terminating with -H. methyl, ethyl, or benzyl" the point of attachment for the selected terminal substituent is the terminal oxygen, for example, -C(=0)-(CH2CH2OH) or -C(=0)- (CH*CH20CH2CH2OCH2CHoOCH3). When a particular group is "substituted" (e.g., phenyl, aryl, heteroalkyl, heteroaryl), that group may have one or more substituents, preferably from one to five substituents, more preferably from one to three substituents, most preferably from one to two substituents, independently selected from the list of substituents. With reference to substituents, the term "independently" means that when more than one of such substituents is possible, such substituents may be the same or different from each other. It is intended that the definition of any substituent or variable at a particular location in a molecule be independent of its definitions elsewhere in that molecule. It is understood that substituents and substitution patterns on the 4-9 4 compounds of this invention can be selected by one of ordinary skill in the art to provide compounds that are chemically stable and that can be readily synthesized by techniques known in the art as well as those methods set forth herein. 5 Compounds exemplified in the present invention were named according to nomenclature well known in the art, either using Autonom Version 2.2 (brand of nomenclature software provided in the ChemDraw Ultra® 7.0.1 Office Suite marketed by CambridgeSoft.com) 10 i ' Abbreviations used in the specification, particularly the Schemes and Examples, are as follows: Aq. = Aqueous ATP = Adenosine triphosphate DBU = 2,2'-Diazabicycloundecane DCM = Dichloromethane DME = Dimethoxyethylene DMF = N,N-Dimethylformamide DMSO = Dimethylsulfoxide DTT = Dithiothreitol j EtOAc = Ethyl acetate i HPLC ';;■!.. = High Pressure Liquid Chromatography | IprOH I = Isopropyl alcohol MeOH = Methanol PBS = Phosphate buffer saline PLC = Phospholipase C RAR = Rat aortic ring Sat. = Saturated SMGS = Smooth muscle growth supplement TFA = Trifluoroacetic Acid THF = Tetrahydrofuran TLC = Thin Layer Chromatography Tris HCI or = Tris[hydroxymethyl]aminomethyl hydrochloride Tris-CI i ■ ! , : i ■! I1 The compounds of the present invention may be prepared by any number of processes as described generally below and more specifically as described in the Examples which follow herein. During any of the processes for preparation of the compounds of the present invention described herein, it may be necessary and/or desirable to protect sensitive or reactive groups on any of the molecules concerned (for example hydroxy, amino, thio, oxo or carboxy groups). This may be achieved by means of conventional protecting groups, such as those described in Protective Groups in Organic Chemistry, ed. J.F.W. McOmie, Plenum Press, 1973; and T.W Greene & P.G.M. Wuts, Protective Groups in Organic Synthesis. John Wiley & Sons, 1991. The protecting groups may be removed at a convenient subsequen stage using methods known from the art. wherein R1, R2, R3, p, q, and n are as described herein for Formula (I) Compounds of the formula (S1) are either known or commercially available compounds or compounds which may be prepared from known compounds by known chemistry. Aromatic ketones may be prepared by the Friedel-Crafts reaction (See Practical Organic Chemistry by Vogel, Third Edition, pp724-749). For example, Friedel-Crafts acylation of substituted aryl propanoic acids of formula (S1a), or their derivatives will yield substituted indan-1-ones of formula (S1b), as described One skilled in the art will recognize that for the preparation of the compounds of the instant invention, the starting materials, i.e., compounds of Formula (S1), supra are known compounds or are compounds which may be prepared according to known methods, for example, as outlined above. Starting compounds of Formula (S1) wherein n is selected from 2 to 4, are similarly known compounds, or may similarly be prepared according to known methods or by modification of the above noted examplary procedures. Method A Compounds of Formula (I) may be prepared according to the process outlined in Method A. Accordingly, a compound of Formula (S1), a known compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (S2), a known compound or compound prepared by known methods, at a temperature in the range of about - 78 to about 100°C, in an aprotic organic solvent such as THF, dioxane, DMF, and the like, in the presence of a base such as lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, to yield the corresponding compound of Formula (S3). The compound of Formula (S3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (I). Examples of p-ketothioamide cyclization (S3 to I) with hydrazine forms anilinopyrrazoles similar to those described in the second step of Method A above, have been reported in literature (For example, see M. Suesse and S. John, J. Prakt. Chem.; (1986). 328(4), 635-9). Additionally, some 3 ketothioamides are reported in the literatures, for example Wesolowska et al.. Pol. J. Chem. (2001), 75(3), 387^00; Hansen, et al., J. Mol. Struct. (1996). 378(1). 45-59; Augustin. et al.. J. Prakt. Chem. (1979). 321(2). 205-14; Schoe etal., Rocz. Chem. (1971). 45(1). 73-60. ) Method B Compounds of Formula (I) may alternatively be prepared according to the process outlined in Method B. Accordingly, a compound of Formula (S1), a known compound or compound prepared by known methods, is reacted with a compound of Formula (S4) (1,1'- thiocarbonyldiimidazole). at a reduced temperature in the range of abGut -78°C to about 0°C, in an aprotic organic solvent such as THF. dioxane, DMF, and the like, in the presence of a strong base such as sodium hydride, lithium bis(trimethylsilyt) amide, sodium bis(trimethylsilyl)amide. lithium diisopropylamide, and the like, to yield the corresponding compound of Formula (S5). The compound of Formula (S5) is reacted with a suitably substituted compound of Formula (S6), a known compound or compound prepared by known methods, in an aprotic organic solvent such as THF, dioxane, methylene chloride, chloroform, DMF. and the like, to yield the corresponding compound of Formula (S3). The compound of Formula (S3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (I). The present invention is further directed to a process for the preparation of a compound of Formula (I), as decribed in more detail in method B above. In one embodiment of the present invention the invention relates to a process for the preparation of a compound of Formula (S5), using Method B above. In another embodiment the invention relates to a process for the preparation of a compound of Formula (S3), using the process outlined in Method B above. More particularly, the compound of Formula (S1), a known compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (S2), a known compound or compound prepared by known methods, at a temperature in the range of about 0 to about 120°C, in an aprotic organic solvent such as THF, DMF, and the like, in the presence of sodium hydride, to yield the corresponding compound of Formula (S3). The compound of Formula (S3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (I). Accordingly, a compound of Formula (S1), a known compound or compound prepared by known methods, is reacted with carbon disulfide and methyl iodide, in the presence of a base such as sodium hydride, lithium bis(trimethylsilyl) amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, in an aprotic organic solvent such THF, DMF, and the like, at an elevated temperature in the range of about 25° to about 100°C, to yield the corresponding compound of Formula (S7). Some compounds of Formula (S7) are known, for example as disclosea in Villemin et al., Synthesis (1991), (4), 301-3; Augustin, et al., J. Prakt. Chem. (1979), 321(2), 215-25; and in WIPO publication WO 95/07893. The compound of Formula (S7) is reacted with a suitably substituted compound of Formula (S6), a known compound or compound prepared by known methods, in an aprotic organic solvent such as THF, DMF, and the like, at an elevated temperature in the range of about 25° to about 15b°C, in the presence of a catalytic amount of an acid such as acetic acid, sulfuric acid, p- toluene sulfonic acid, and the like, to yield the corresponding compound of Formula (S8). The compound of Formula (S8) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (I). Method E Compounds of Formula (I) may alternatively be prepared according to the process outlined in Method E. Accordingly, a compound of Formula (S1), a known compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (S2), a known compound or compound prepared by known methods, in the presence of methyl iodide and a base such as DBU, NaH, lithium bis(trimethylsilyl) amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, in an aprotic organic solvent such as acetonitrile, THF, DMF, and the like, at an elevated temperature in the range of about 0 to about 100°C, to yield the corresponding compound of Formula (S8). The compound of Formula (S8) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (I). Accordingly, a compound of Formula (T1), a known compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (T2), a known compound or compound prepared by known methods, at a temperature in the range of about - 78 to about 100°C, in an aprotic organic solvent such as THF, dioxane. DMF, and the like, in the presence of a base such as lithium bis(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, to yield the corresponding compound of Formula (T3). Compoud of Formula (T1) where L2 containing oxygen, sulfur or nitrogen atom can also be prepared by known methods (For example, see A. R. Deshpande, et al., Synthetic Communications , (1990), 20(6), 809-816; W-S. Li, etal., Tetrahedron Letters, (2002), 43, 1923-1925; C. Brian, et al., Tetrahedron, (1987), 43(1), 69-76; H. Winfvoid, et al., Chemie. (1970), 10(9), 343: C. Mukerjee, et al., Synletters, (2002), (2), 325-327; T. Sugasawa, et al., J. Org. Chem., (1979), 44(4), 578-586:S; and Torii, et al., J. Org. Chem.,(1978), 43(14), 2882-2885.) The compound of Formula (T3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (Ma). Examples of p-ketothioamide cyclization (T3 to Ha) with hydrazine forms anilinopyrrazoles similar to those described in the second step of Method F above, have been reported in literature (For example, see M. Suesse and S. John, J. Prakt. Chem.; (1986), 328(4), 635-9). Additionally, some ketothioamides are reported in the literatures, for example Wesolowska et al., Pol. J. Chem. (2001), 75(3), 387-400; Hansen, et al., J. Mol. Struct. (1996), 378(1), 45-59; Augustin, et al., J. Prakt. Chem. (1979), 321(2), 205-14; Schoen et al., Rocz. Chem. (1971). 45(1), 73-60. Accordingly, a compound of Formula (T1), a known compound or compound prepared by known methods, is reacted with a compound of Formula (T4) (1,1'- thiocarbonyldiimidazole), at a reduced temperature in the range of about -78°C to about 0°C, in an aprotic organic solvent such as THF dioxane, DMF, and the like, in the presence of a strong base such as sodium hydride, lithium bis(trimethylsilyl) amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, to yield the corresponding compound of Formula (T5). The compound of Formula (T5) is reacted with a suitably substituted compound of Formula (T6), a known compound or compound prepared by known methods, in an aprotic organic solvent such as THF, dioxane, methylene chloride, chloroform, DMF, and the like, to yield the corresponding compound of Formula (T3). The compound of Formula (T3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (Ma). The present invention is further directed to a process for the preparation of a compound of Formula (lla), as decribed in more detail in method G above. In one embodiment of the present invention the invention relates to a process for the preparation of a compound of Formula (T5), using Method G above. In another embodiment the invention relates to a process for the preparation of a compound of Formula (T3), using the process outlined in Method G above. More particularly, the compound of Formula (T1), a knowri compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (T2), a known compound or compound prepared by known methods, at a temperature in the range of about 0 to about 120°C, in an aprotic organic solvent such as THF, DMF, and the like, in the presence of sodium hydride, to yield the corresponding compound of Formula (T3). The compound of Formula (T3) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (lla). Method ICompounds of Formula (II), of the structure (lla), may alternatively be prepared according to the process outlined in Method I. Accordingly, a compound of Formula (T1), a known compound or compound prepared by known methods, is reacted with carbon disulfide and methyl iodide, in the presence of a base such as sodium hydride, lithium bis(trimethylsilyl) amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, in an aprotic organic solvent such THF, DMF, and the like, at an elevated temperature in the range of about 25° to about 100°C, to yield the corresponding compound of Formula (T7). The compound of Formula (T7) is reacted with a suitably substituted compound of Formula (T6), a known compound or compound prepared by known methods, in an aprotic organic solvent such as THF, DMF, and the like, at an elevated temperature in the range of about 25° to about 1509C, in the presence of a catalytic amount of an acid such as acetic acid, sulfuric acid, p- toluene sulfonic acid, and the like, to yield the corresponding compound of Formula (T8). The compound of Formula (T8) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (Ila). Method J Compounds of Formula (II), of the structure (lla), may alternatively be prepared according to the process outlined in Method J. Accordingly, a compound of Formula (T1), a known compound or compound prepared by known methods, is reacted with a suitably substituted compound of Formula (T2), a known compound or compound prepared by known methods, in the presence of methyl iodide and a base such as DBU, NaH, lithium bis(trimethylsilyl) amide, sodium bis(trimethylsilyl)amide, lithium diisopropylamide, and the like, in an aprotic organic solvent such as acetonitrile, THF, DMF, and the like, at an elevated temperature in the range of about 0 to about 100°C, to yield the corresponding compound of Formula (T8). The compound of Formula (T8) is reacted with hydrazine, preferably in the presence of about one equivalent of an acid such as acetic acid, hydrochloric acid, and the like, at an elevated temperature, preferably at about reflux temperature, to yield the corresponding compound of Formula (Ila). The present invention includes compounds of Formula (II) wherein one of R6orR7 is present and other than hydrogen (i.e., compounds of formula (lib), (lie), (lid), (lid), (lie), (llf), (llg), (llh), (llj). (Ilk). (Mm) (lln), (llo), (lip). (Ilq), (Mr) and (Ms) as defined in more detail below). Said compounds are potentially prodrugs of compounds of Formulae (I) and (II). The present invention further includes process for the preparation of said compounds of formula (lib), (lie), (lid), (lid), (lie), (llf), (llg), (llh). (Ilj), (Ilk), (Mm) (lln). (Ho), (lip), (llq), (Mr) and (lis). As prodrugs, compounds of Formula (II) wherein one of R6 or R7 is present and other than hydrogen are believed to be absorbed in vivo and then metabolized or hydrolyzed to the corresponding compounds of Formulae (I) or (II). The compounds of formula (II) wherein one of R6 or R7 is present and other than hydrogen may further have intrinsic biological activity similar to the parent compounds of Formula (I) and / or (II). Method L Compounds of formula (lib) and (lie) wherein one of R6 or R7 is selected from the group consisting of paragraph (c) of Formula (II) may be prepared according to the process outlined in Method L. Accordingly, a suitably substituted compound of Formula (Ila) is reacted 3 with a suitably substituted alkylating agent, a compound of formula (T9), a known compound, for example methyl iodide, dimethyl sulfate, chloromethylpivalate, ethylene oxide, and the like, or compound prepared by known methods, for example as halide, mesylate, tosylate, epoxide and triflate, and the like, at a temperature in a range of -70° to 100°C, in an aprotic solvent such as THF, DMF, and the like; in the presence of a base, such as potassium carbonate, cesium carbonate, pyridine, triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (Mb) and (lie). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (lib) and (lie). Method M Compounds of formula (lid) and (lie) wherein one of R6 or R7 is selected from the group consisting of consisting of paragraphs (d), (e), (f), (g), (h) and (hh) of Formula (II) may be prepared according to the process outlined in Method M. Accordingly, a suitably substituted compound of Formula (lla) is reacted with a suitable acylating agent, a compound of formula (T11) or (T12), a known compound or compound prepared by known methods, for example, acetyl chloride, isobutyryl chloride, succinic anhydride, methoxylacetylchloride, benzyloxylacetylchloride, benzoyl chloride, and the like, at a temperature in a range of about between about-70° and about 100°C, in an aprotjc solvent, such as THF, DMF, pyridine and the like, in the presence of base, such as pyridine, triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (lid) and (lie). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (lid) and (Me). Method N Compounds of formula (lid) and (lie), wherein one of R6 or R7 is selected from the group consisting of paragraphs (d), (e), (f), (g), (h) and (hh) of Formula (II) may alternatively be prepared according to the process outlined in Method Accordingly, a suitably substituted compound of formula (lla), is reacted with a suitably substituted carboxilc acid, a compound of formula (T13), a known compound or compound prepared by known methods, for example, 3- oxo-3-pyrrolidin-1-propionic acid, and the like, at a temperature in a range of i between about -70° and about 100°C, in an aprotic solvent such as THF, DMF, and the like, in the presence of base, such as triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (lid) and (He). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two corresponding regioisomers, compounds of formula (IIf) and (llg). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (llf) and (i"g). Method P Compounds of formula (llh) and (llj), wherein one of R6 or R7 is selected from the group consisting of paragraphs (I), (m), (n) and (o) of Formula (II) may be prepared according to the process outlined in Method P. Accordingly, a suitably substituted compound of Formula (lla) is reacted 5 with a suitably substituted aryl chloroformate, a compound of formula (T15), a known compound or compound prepared by known methods, for example, phenyl chloroformate, 4-nitrophenyl chloroformate, and the like, at a temperature in a range of between about -70° and about 100°C, in an aprotic solvent, such as THF, DMF, DCM, and the like, in the presence of base such as pyridine, triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (T16) and (T17). Compounds of formula (T16) and (T17) are separated by silica gel column chromatography or reverse column chromatography. The compounds of formula (T16) and (T17), separately, are reacted with a suitably substituted amine, a compound of formula (T18), a known compound or compound prepared by known methods, for example, 1-methyl-1-ethyl-1,2- diamine, propylamine, 3-(morpholin-4-yl)-1 -propylamine, and the like, in an aprotic solvent such as DMF, DMSO, THF, and the like, at the temperature in a range of between about -70° and about 100°C to yield the corresponding compounds of formula (llh) and (llj). Alternatively, the compounds of formula (T16) and (T17) as a mixture are reacted with a suitably substituted amine, a compound of formula (T18), to yield a mixture of compounds of formula (llh) and (llj). Jhe compounds of formula i (llh) and (llj) are then separated by known methods, for example by silica gel column chromatography or reverse phase column. Both sequences give the desired compounds of formula (llh) and (IN). Preparation of a library of compounds is achieved more efficiently by reacting the compounds of formula (T16) and (T17) separately than by reacting a mixture of compounds of formula (T16) and (T17) followed by separation. Accordingly, a suitably substituted compound of Formula (lla) is reacted with a suitably substituted isocyanate, a compound of formula (T19) or a suitably substituted thioisocyanate, a compound of formula (T20), for example, phenylisocyanate, methylisocyanate, methylthioisocyanate, and the like, at a temperature in a range of between about -20° and about 100°C, in an aprotic solvent, such as THF, DMF, DCM, and the like, in the presence of base, such as pyridine, triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (Ilk) ahd (llm). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (Ilk) and (llm). One skilled in the art will recognize that when the compound of formula (lla) is reacted with an isocyanate, then the corresponding compounds of formula (Ilk) and (llm) will have R6 or R7 substituents of -C(0)NHR Similarly, when the compound of formula (lla) is reacted with an thioisocyanate, then the corresponding compounds of formula (Ilk) and (llm) will have R6 / or R7 substituent of -C(S)NHR""'. Method R Compounds of formula (lln) and (llo), wherein one of R6 or R7 is selected from the group consisting of paragraphs (s), (t) and (u) of Formula (II) may be prepared according to the process outlined in Method R. Accordingly, a suitably substituted compound of Formula flla) is reacted with a suitably substituted sulfamoyl chloride, a compound of formula (T21), a known compound, for example, dimethylsulfamoyl chloride, ethylsulfamoyl chloride, and the like, or a compound prepared by known methods, at a temperature in a range of between about -20° and about 100°C, in an aprotic solvent, such as THF, DMF, DCM, and the like, in the presence of base, such as pyridine, triethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (lln) and (Ho). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (lln) and (Ho). One skilled in the art will recognize that when the compound of formula (lla) is reacted with an sulfamyl, then the corresponding compounds of formula (llo) and (lip) will have R6 or R7 substituents of-S02NHR",m and -S02N(Rnm)2. Accordingly, a suitably substituted compound of Formula (Ha) is reacted with a suitably alkyl chlorophosphate, a compound of formula (T22), a known compound, for example, dimethylchlorophosphate, diethylchlorophosphate, and the like, or a compound prepared by known methods, at a temperature in a range of between about -20° and about 100°C, in an aprotic solvent, such as THF, DMF, DCM, and the like, in the presence of base, such as pyridine, tnethylamine, diisopropylethylamine, and the like, to yield a mixture of the corresponding regioisomers, compounds of formula (lip) and (llq). The ratio of the two regioisomers is dependent on the base and solvent used. Preferably, the two regioisomers are separated by silica gel column chromatography or reverse phase column chromatography to yield compounds of formula (lip) and (llq). One skilled in the art will recognize that when the compound of formula (Ila) is reacted with a dialkyl chlorophosphate, then the corresponding Compounds of formula (T24) and (T25) are seprated by silica gel column chromatography or reverse phase column chromatography. The compounds of formula (T24) and (T25), separately are reacted with 5 a suitably substituted amine, a compound of formula (T26), a known compound or compound prepared by known methods, for example, piperidine, morpholine. Dimethylamine, pyrrolidine and the like, in an aprotic solvent such as DMF, DMSO, THF, and the like, at the temperature in a range of between about -70° and about 100°C to yield the corresponding compounds of formula (Mr) and nO (lis). Alternatively, the compounds of formula (T24) and (T25) as a mixture are reacted with a suitably substituted amine, a compound of formula (T26), to yield a mixture of compounds of formula (Mr) and (lis). The compounds of formula 15 (Mr) and (lis) are then separated by known methods, for example by silica gel column chromatography or reverse phase column. Both sequences give the desired compounds of formula (llr) and (lis). Preparation of a library of compounds is achieved more efficiently by reacting 20 the compounds of formula (T24) and (T25) separately than by reacting a mixture of compounds of formula (T24) and (T25) followed by separation.. N-Glucuronide Synthesis To varying degrees the compounds of this invention may undergo the in 25 vivo N-glucuronidation by various endogenous isozymes of the UDP- glucuronosyltransferase family (Chiu, S-HL; Huskey, S-EW; 1996ASPETN- glucuronidation of xenobiotics symposium: Species differences in N- glucuronidation, Drug Metabolism and Disposition 1998, 26(9): 838-847). 30 One skilled in the art will understand that in vivo metabolites of compounds of Formulae (I) and (II) may be readily reverted to compounds of Formulae (1) and (II) by action of endogenous p-glucuronidase. The scientific literature details that tumor tissue generally contains elevated levels of endogenous p-glucuronidase. By action of endogenous ^-glucuronidase, the in situ re-generation of compounds of Formulae (I) and (II) can be accomplished. In this way, the ability of the compounds of the present invention to be reversibly glucuronidated allows for the targeting of the present compounds to tumor tissue (Sperker, B; Backman, JT; Kroemer, HK, The role of p- glucuronidase in drug disposition and drug targeting in humans, Clin. Pharmacokinet., 1997, 33(1): 18-31). Furthermore, reversible glucuronidation of the present compounds may also be recognized by one skilled in the art as a potential method for the detoxification of compounds of Formulae (I) and (II) (Caldwell, J; The significance of phase II conjugation reactions in drug disposition and toxicity, Life Sci, 1979, 24: 571-578), thus allowing the N-glucuronide metabolites formed to serve as a potential non-toxic reservoir for compounds of Formulae (I) and (II) which can then be readily unmasked to fully biologically active compounds of Formulae (I) and (II) in situ by tumor associated p- glucuronidase. Usually, the glucuronidated compounds will have a ^-configuration about the anomeric carbon atom, especially if the glucuronide is produced by well- established enzymatic methods known to persons skilled in the art (Luukkanen, L; Kilpelaeinen, I; Kangas, H; Ottoila, P; Elovaara, E; Taskinen, J, Enzyme- Assisted Synthesis and Structural Characterization of Nitrocatechol Glucuronides, Bioconjugate Chemistry (1999), 10(1), 150-154). The N-glucuronides may also be prepared by direct synthesis by reacting compounds of Formulae (I) and (II) with suitably protected glucuronosyl halides by synthetic methodology know to persons skilled in the art (Upadhyaya, Pramod; Mclntee, Edward J.; Hecht, Stephen S., Preparation of Pyridine-N-glucuronides of Tobacco-Specific Nitrosamines., Chemical Research in Toxicology (2001), 14(5). 555-561). One skilled in the art will recognize that the GLU A, GLU B and GLU C derivatives of the compounds of Formulae (I) andi(ll) may be prepared by known methods, by adapting the procedures cited above. For epcample, if one or more of the Z groups are hydroxy, the hydroxy group may be reacted according to known methods with an alkyl halide, to forrr the corresponding -O-alkyl substituent; with CI-C(0)-alkyl or CI-C(0)-aryl to form the corresponding -C(0)-alkyl or -C(0)-aryl substituent; with Cl-C(0)0- alkyl or CI-C(0)0-aryl to form the corresponding -C(0)0-alkyl or -C(0)0-aryl substituent; or with C(0)N(alkyl) or C(0)C(aryl) to form the corresponding - OC(0)N(alkyl) or -OC(0)N(aryl) substituent. If one or more of the Z groups is amino, the amino group may be reacted according to known methods with HC(0)-alkyl or HC(0)-aryl to form the corresponding -NHCHb-alkyl or -NHCH2-aryl substituent; with CI-C(0)-alkyl or CI-C(0)-aryl to form the corresponding -NHC(0)-alkyl or -NHC(0)aryl substituent; with C(0)N-alkyl or C(0)N-aryl to form the corresponding - NHC(0)NH-alkyl or -NHC(0)NH-aryl substituent; with CI-C(0)0-alkyl or Cl- C(0)0-aryl to form the corresponding -NHC(0)0-alkyl or -NHC(0)0-aryl substituent; or with CI-SC>2-alkyl or CI-SO?-aryl to form the corresponding - NHSOralkyl or -NHSOraryl substituent. One skilled in the art will further recognize that if the Z group is an alkyl amino or aryl amino group, similar chemistry may be preformed to yield corresponding substituents where the N group bound directly to the A or B ring remains substituted with tlpie alkyl or aryl group. If one or more of the Z groups is thio, the thio group may be reacted according to known methods with an alkyl halide to form the corresponding alkyl thio substituent. If one or more of the Z groups is alkylthio, the alkylthio group may be reacted according to known methods to form the corresponding alkyl sulfonyl substituent. If one or more of the Z groups is carboxy, the carboxy group may be reacted according to known methods to form the corresponding -C(0)CI group, which in turn may be further reacted to form the desired R2 and / or R3 substituents. If one or more of the Z groups is -C(0)CI, the -C(0)CI group may be reacted according to known methods with an alkoxy to form the corresponding - C(0)0-alkyl substituent; with -NH(alkyl) or N(alkyl)2 to form the corresponding - C(Q)NH(alkyl) or-C(0)N(alkyl)2 substituent If one or more of the Z groups is a halogen such as iodine or bromine, the halogen may be reacted according to known methods with B(OH)2-alkyl, B(OH)2-aryl or B(OH)2-heteroaryl to displace the halogen with the corresponding -alkyl, -aryl or-heteroaryl group. Alternatively, if one or more of the Z groups is a halogen such as iodine or bromine, the halogen may be reacted according to known methods with an alkylamine, a dialkylamine, an arylamine, a heteroarylamine or a heterocycloalkylamine to displace the halogen with the corresponding -NH- alkyl, -N(alkyl)2, -N-aryl, -NH-heteroaryl or -NH-heterocycloalkyl group. Alternatively, if one or more of the Z groups is a halogen such as iodine or bromine, the halogen may he reacted according to known methods with HO- alkyl, HO-aryl, HO-heteroaryl or HO-heterocycloa|kyl to displace the halogen with the corresponding -O-alkyl, -O-aryl, -O-heteroaryl or -O-heterocycloalkyl group. Alternatively, if one or more of the Z groups is a halogen such as iodine or bromine, the halogen may be reacted according to known methods with HS- alkyl, HS-aryl, HS-heteroaryl or HS-heterocycloalkyl to displace the halogen with the corresponding -S-alkyl, -S-aryl, -S-heteroaryl or -S-heterocycloalkyl group. If one or more of the Z groups is -0-S02-aryl or -OS02-alkyl, the -O- S02aryl or -OSOralkylgroup may be reacted according to known methods with an alkyl amine, a dialkylamine an aryl amine or a heteroarylamino to form the corresponding -NH(alkyl), -N(alkyl)2, -NH(aryl) or -NH(heteroaryl) group. Alternatively, If one or more of the Z groups is -0-SC>2-aryl or -OSOr alkyl, the -0-S02aryl or -OS02-alkylgroup may be reacted according to known methods to displace the -0-S02 group with a halogen such as Br or I, to form a reactive intermediate which can then be further reacted to form the desired substituent. If one or more of the Z groups is -S-alkyl, -S-aryl, -S-heteroaryl or -S- heterocycloalkyl, the S may be oxidized according to known methods to form the corresponding -SC>2-alkyl, -S02-aryl, -S 62-heteroaryl or -S02- heterocycloalkyl substituent. If one or more of the Z groups contains a terminal unsaturated bond, the Z group may be reacted according to known methods to form the corresponding epoxide, which in turn may be reacted with a substituted amine such as an alkylamino, a dialkylamine, an arylamine, a heteroarylamine, a 1 i- heterocycloslkylamine, or a cyclic amine (such as, piperidine, moipholine, imidazole, and the like), to form the corresponding -CH(OH)CH2-NH-alkyl, - CH(OH)CH2-N(alkyl)2, -CH(OH)CH2-NH-aryl, -CH(OH)CH2-NH-heteroaryl, - CH(OH)CH2-NH-heterocycloa1kyl or -CH(OH)CH2-(cyclic amine bound through the N atom) substituent. One skilled in the art will further recognize transformation or reactions similar to those described above may be employed in (or applied to) the preparation of compounds of formula (II). More particularly, the processes G? described above for the introduction of R2 and/or R3 groups on the v—' and / G) or x-—-^ rings may be used to incorporate R5, R9 and/or R10 substituents onto 0 © the v—' and N-—y rings on the compounds of formula (II). One skilled in the art will recognize that compounds of Formula (I) wherein R1 is oxo (=0) may be converted according to known methods to form compounds of Formula (I) wherein R1 is hydroxy (by reduction) or converted to intermediate compounds wherein R1 is =NHOH (by reacting with NH4OH). The intermediate compounds wherein R1 is =NH0H may then be reduced according to known methods to the corresponding amine, which may then be further optionally functionalized to the corresponding substituted amine. Compounds of Formula (I) wherein R1 is hydroxy may be converted according to known methods to form intermediate compounds wherein R1 is -O- S02-aryl or -0-S02-alkyl by reacting the intermediate compound with the corresponding CI-S02-aryl or CI-S02-alkyl reagent. The -0-S02-aryl or -O- S02-alkyl R1 group may then be further optionally reacted according to known methods to form an amine (by reacting with NaN3| followed by reduction). Alternatively, compounds of Formula (I) wherein R1 is hydroxy may be converted according to known methods to form compounds of Formula (I) wherein R1 is -O-alkyl by reacting with the corresponding alkyl halide. Compounds of Formula (I) wherein R1 is amine or alkyl amine may be reacted according to known methods to form compounds of Formula (I) wherein R1 is -NH-CH2-alkyl or-NH-(CH2-alkyl)2 by reacting with HC(0)-alkyl. One skilled in the art will further recognize that transformation or reactions similar to those described above may be employed in (or applied to) the preparatton of compounds of formula (II). More particularly, the processes described above for the introduction and optional conversion of R1 groups in the compounds of formula (I) may be similarly applied to the preparation of compounds of formula (II), wherein such transformations are appropriate in the preparation of desired L2 groups. One skilled in the art will further recognize that the above examples for the inclusion of desired substituent groups into the compounds of Formula (I) and / or compounds of formula (II) are not intended to be all inclusive, but rather are intended to provide examples of known chemistry for the incorporation of representative substituents. Additional substituents groups not i i specifically described herein may be incorporated into the compounds of Formula (I) and / or compounds of formula (II) by known methods. wherein, n is an integer from 1 to 4; R1 is selected from the group consisting of hydrogen, lower alkyl, -OH, alkoxy, -oxo. - NH2, -NH(alkyl) and -N(alkyl)2; X and Y are each independently absent or selected from the group consisting of -0-, - NH-, -N(alkyl)-, -S-, -SO-, -S02-. -OC(=0). -C( ^0)0-, -NHC(=0)-, -N(alkyl)C(=0)-, -C(=0)NH-, -C(=0)N(alkyl)-, -0C(=-0)0-, -NHC(=0)0-, -OCX=0)NH-, -N(alkyl)C(=0)0-, -OC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)N(alkylV, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)N(alkyl)-, -NHS02-, -S02NH-, -N(alkyl)S02- and -S02N(alkyl)-; ^Y 1 7 V^ A is absent or selected from alkyl or alkenyl; A is selected from alkyl, alkenkj^br H; wherein, when A or A is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from halogen, cyano, hydroxy, alkoxy, thio, halogenated alkoxy. -OC(:=0)alkyl, -OC(=0)Oalkyl, amino, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, dialkylarnino, -NHC(=0)NH2. - NHC(0)NHalkyl, -N(alkyl)C(=0)NHalkyl. -K(alkyl)C(=0)NH2, -OC(=0)NHalkyl, - NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, - N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; (5) v—/ is selected from the group consisting of an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio. nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, - N(alkyl)C(=0)alkyl, or dialkylarnino, -NHC(=0)NH2, -NHC(K))NHalkyl, - N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, - NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; q is an integer from 0 to 4; R3 is selected from the group consisting of halogen, hydroxy, amino, thk>, hitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkyloxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylarnino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)$alkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 and -0C(=0)N(alkyl)2; provided that the sum of p and q is an integer from 0 to 4; L1 is absent; (5) v--/ is aryl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. v-V •. 3. The compound as in claim 1 wherein - / n is an integer from 1 to 2; R is hydrogen; * 0 ^— is phenyl; p is an integer from 0 to 2; R is selected from the group consisting of di(lower alkyl)amino-alkoxy, lower alkyl- i-o—A1—(5) alkoxy, hydroxy substituted alkoxy and ^ v-x ; wherein A1 is selected from the group consisting of lower alkyl; wherein the lower alkyl is optionally substituted with one to two substitucnts independently selected from (5) hydroxy, amino, alkylamino or dialkylamino; and wherein ^-^ is selected from the group consisting of a five or six membered heteroaryl and a five or six membered heterocycloalkyl; wherein the heteroaryl or heterocycloalkyl is optionally substituted with one to two substituents independently selected from halogen, lower alkyl, lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino; q is an integer from 0 to 2; R3 is selected from the group consisting of lower alkyl and lower alkoxy, and halogen; benzyloxy; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceuticallyacceptable salt thereof. 4. The compound as claimed in claim 1 wherein n is an integer from 1 to 2; R1 is hydrogen; 0. ^— is phenyl; p is an integer from 0 to 2; R2 is selected from the group consisting of 3-dimethylamino-propoxy, 3-methoxy- propoxy, 2,3-dihydroxy-n-propoxy, 3-hydroxy-propoxy, 2-hydroxy-3-pyrrolidin-l-yl- propoxy and 3-(4-methyl-piperazin-l-yl-propoxy; q is an integer from 0 to 2; R3 is selected from the group consisting of methyl, methoxy, ethoxy; C' * 'P is phenyl wherein the phenyl is optionally substituted with one to two substituents independently selected from fluoro, chloro, methyl, methoxy or benzyloxy; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salt thereof. 5. The compound as claimed in claim 1 wherein (A , ,M} ^— is phenyl; p is an integer from 0 to 2; R is selected from the group consisting of heterocycloalkyl, benzyloxy, di(lower alkyl)amino-lower alkoxy, lower alkoxy-lower alkoxy, heteroaryl-lower alkoxy, heterocycloalkyl-lower alkoxy and lower alkoxy; wherein the heterocycloalkyl, whether alone or as part of a substituent group is optionally substituted with a substiuent selected from lower alkyl or hydroxy; wherein the lower alkoxy, whether alone or as part of a subtituent group is optionally substituted with one to two hydroxy; q is an integer from 0 to 2; R3 is selected from the group consisting of hydroxy, lower alkoxy, lower alkyl, halogen, amino, (lower alkyl)amino and di(lower alkyl)amino; 0(?q v 'P is phenyl; wherein the phenyl is optionally substituted with one to three substituents independently selected from hydroxy, carboxy, halogen, lower alkyl, hydroxy substituted lower alkyl, lower alkoxy, lower alkoxycarbonyl, trifluoromethyl, trifiuoromethoxy, lower alkylamino, di(lower alkyl)amino, cyano, nitro, aminocarbonyl, lower alkylaminocarbonyl, di(lower alkyl)aminocarbonyl, (hydroxy substituted lower alkyl)-aminocarbonyl, (heteroaryl-lower alkyl)-aminocarbonyl, lower alkyl-thio, trifluoromethylthio, aralkyloxy, heterocycloalkyl, lower alkyl substituted heterocycloalkyl or heterocycloalkyl-sulfonyl; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptttble C salt thereof. , v^\^ %^ ~* 6. The compound as claimed in claim 5, wherein 0 — is phenyl; R1 is selected from the group consisting of hydrogen, hydroxy, oxo and methyl; p is an integer from 0 to 2; R2 is selected from the group consisting of piperidinyl, 4-methyl-piperizin-l-yl, 3-(4- methyl-piperazin-l-yl)-propoxy, 3-dimethylamino-propoxy, 3-methoxy-propoxy, 3- morpholin-1-yl-propoxy, 3-pyrrolidin-lyl-propoxy, 3-imidazol-l-yl-propoxy, 2,3- dihydroxy-propoxy, 3-hydroxy-propoxy, 2-hydroxy-3-pyrrolidin-l-yl-propoxy, and benzyloxy; q is an integer from 0 to 2; R3 is selected from the group consisting of hydroxy, methoxy, ethoxy, isopropoxy, methyl, bromo, fluoro, chloro, amino and dimethylamino; v yP is selected from the group consisting of phenyl, 4-chlorophenyl, 3- chlorophenyl, 2-chlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 2- bromophenyl, 3-bromophenyl, 4-bromophenyl, 2-methylphenyl, 3-methylphenyl, 4- J methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 2-isopropylphenyl, 2-methoxyDhet^j^l-' methoxyphenyl, 4-methoxyphenyl, 3-methoxycarbonylphenyl, 3-ethoxycafDbnylphenyl, 4-ethoxycarbonylphenyl, 3-hydroxyphenyl, 3-cyanophenyl, 4-cyanophenyl, 3- carboxyphenyl, 2-trifluoromethylphenyl, 3-trifluoromethylphenyl, 4- trifluoromethylphenyl, 2-trifluoromethoxyphenyl, 3-trifluoromethoxyphenyl, 4- trifluoromethoxyphenyl, 3-hydroxymethyl-phenyl, 3-(l-hydroxyethyl)phenyl, 3- methylthiophenyl, 3-trifluoromethylthiophenyl, 3-benzyloxy-phenyl, 4-benzyloxyphenyl, 4-methylaminophenyl, 4-dimethylaminophenyl, 3-aminocarbonylphenyl, 2,5- difluorophenyl, 3,4-difluorophenyl, 3,5-difluorophenyl, 2,4-dichlorophenyl, 2,5- dichlorophenyl. 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,5-dichlorophenyl, 3,5- dimethylphenyl, 2,4-dimethoxyphenyl, 2,5-dimethoxyphenyl, 3,4-dimethoxyphenyl, 3,5- dimethoxyphenyl, 3,5-di(trifluoromethyl)-phenyl, 3,5-di(tert-butyl)-phenyl, 3-chloro-4- fluoro-phenyl, 3-chloro-4-methoxy-phenyl, 4-chloro-3-methyl-phenyl, 5-chloro-2- methyl-phenyl, 5-chloro-2-methoxy-phenyl, 4-bromo-2-trifluoromethyl-phenyl, 4-fluoro- 3-trifluoromethyl-phenyl, 4-fluoro-3-nitro-phenyl, 3,4,5-trimethoxyphenyl, 4-(4-methyl- piperidin-l-yl)-phenyl, 4-(piperidine-4-sulfonyl)-phenyl, 3-(2-hydroxy- ethylaminocarbonyl)-phenyl, and 3-(3-pyrrolidn-1 -yl-propylaminocarbonyl)-phenyl; or an optical isomer, enantiomer, diastereomer, racemate or pharmaceutically acceptable salt thereof. A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(-0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; ^^ is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, are optionally substituted with one or more substituents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (h) -C(=0)(CH2)i-6C(=0)- terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(=O)O(CH2CH2O-)M0 terminating with H, methyl, ethyl, or benzyl; 0') -C(=0)Oalkyl, or -C(=0)0(C3.6)cycloalkyl, wherein said -C(=0)Oalkyl, and -C(=0)0(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(==0)alkyl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)I.3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i-3heteroaryl, or -C(=0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2 , heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (1) -C(O)NH(CH2CH20-)M0 terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyI)2, -CH2CH2-l-pyrrolidinyI, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholiny), -CH2CH2-l~piperazinyl, -CH2CH2-1- (4-CH3)-piperazinyl or -C(=0)alkyl; 'OX TV * (m) -C(=0)NH2, -C(=0)NH(C,.2o)alkyl, -C(=0)NH(C3.6)cycloalkyl, or ~-- '^ " -C(=0)N(alkyl)2, wherein said -C(=O)NH(C,.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently /»0l selected from: -OH,-Oalkyl,-NH2,-NHalkyl,-N(alkyl)2, heterocycloalkyl, "^ -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -0C(=0)alkenyl, -NHC(=0)aryl/ -C(=0)OH, -C(=0)0-alkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -O-alkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2),.3aryl, -C(=0)NHaryl, -C(=0)NH(CH2),.3heteroaryl, or -C(=0)NHheteroaryl, wherein said -C(=0)NH(CH2),.3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)i-3heteroaryl, and -C(=0)NHheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=O)NHCH2CH2NH(CH2CH2NH-)0-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-l-pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl,-CH2CH2-l-piperazinyl,-CH2CH2-l-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2C:H3, -CH2CH2OC(=0)alkyl, or -C(=0)aryl; wherein the aryl portion of said -C(=())aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -O-alkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy,"* amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(O)0alkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2, thio. •£-V—B10-f?) thioalkyl, * ^-^, and— V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-. -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl>, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(--0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyk B20 is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and v_^ is selected from the group consisting of: aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. 9. The compound as claimed in claim 7 wherein: L is a linking group selected from the group consisting of: -(CH2)-, -(CH2)3-4-, -CI I(R100)-, -C(=R100)-, and -C(R100)2-. 11. The compound as claimed in claim 7 wherein: R9 and R,0are independently selected from the group consisting of: 1-piperidinyl, 2-(pyrrolidin-l-yl)-ethoxy, 2,3-dihydroxy-propoxy, 2-hydroxy-3-pyrrolidin-l-yl-propoxy, 3-(4-methyl- piperazin-1 -yl)-propoxy, 3-(N,jV-dimethj l-amino)-propoxy, 3-hydroxy-propoxy, 3-imidazol-l-yl- (k) -C(=0)Ophenyl optionally substituted with one or more chloro, fluoro groups^ (1) -C(=0)NH(CH2CH20-)i-io terminating with-H; ^* (m) -C(=0)NH(Ci-2o)alkyl optionally substituted with one or more groups independently selected from: -NH2, -NHalkyl. -N(alkyl)2, pyrrolidinyl, morpholinyl, -NHC(=0)alkyl. -OC(=0)alkenyl, -NHC(=0)phenyl or -C(=0)Oalkyl; and, wherein the phenyl portion of said -NHC(=0)phenyl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen and nitrile; (n) -C(=0)NHphenyl optionally substituted with one or more fluoro groups; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with -CH2CH2OH and -C(=0)phenyl; wherein the phenyl portion of said -C(=0)phenyl may be optionally substituted with one or more -OH groups; (p) -C(=S)NH2; (u) -S02N(alkyl)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. A^-(2-l//-pyrrolidin-l-yl-ethyl)-amino-carbonyl, yV-(2-amino-ethyl)-amino-carbonyl, Ar-(2-morpholin-4-yl-ethyl)-amino-carbonyl, iV-(3-ethoxy-3-oxo-propyl)-amino-carbon"y iV-(3-fluoro-phenyl)-amino-carbonyl, A^-(pentadecyl)-amino-carbonyl, N, N-dimethyl-amino-sulfonyl, jV-[2-(2-methenyl-1 -oxo-propoxy)-ethyl]-amino-carbonyl, N-[2-(3-methyl-1 -methoxy-1 -oxo)-/7-butyl]-amino-carbonyl, /V-[2-(4-methyl-l-methoxy-l-oxo)-pentyl]-amino-carbonyl, Ar-[2-(A^,A^-dimethyl-amino)-ethyl]-amino-carbonyl, A^-[2-(A^-benzoyl-amino)-ethyl]-amino-carbonyl, jV-[2-(A^-methyl-amino)-ethyl]-amino-carbonyl, N-[2-[2-(2-hydroxy-ethoxy)-ethoxy]-ethyl]-amino-carbonyl, N-[2-[N-( 1 -oxo-ethyl)-amino]-ethyl]-amino-carbonyl, Ar-[2-[Ar-(2-hydroxy-benzoyl)-amino]-ethyl]-amino-carbonyl, A^-[2-[A^-(2-hydroxy-ethyl)-amino]-ethyl]-amino-carbonyl, Af-[2-[jV-(2-methyl-1 -oxo-propyl)-amino]-ethyl]-amino-carbonyl, jV-methyl-amino-carbonyl, iV-methyl-amino-thiocarbonyl, and phenoxy-carbonyl, provided that when R6 is present, R7 is absent; and provided that when R7 is present, R6 is absent. methyl-phenyl; 3-methylthio-phenyl; 3-trifluoromethoxy-phenyl; 3-trifluoromethyl- phenyl; 4-(4-methyl-piperazin-l-yl)-phenyl; 4-(ethoxy-carbonyl)-phenyl; 4-(NM dimethyl-amino)-phenyl; 4-(piperidin-4-yl-sulfonyl)-phenyl; 4-benzyloxy-phenyl; 4- bromophenyl; 4-chloro-phenyl; 4-cyano-phenyl; 4-dimethylamino-phenyl; 4-fluoro-3- chloro-phenyl; 4-fluoro-3-nitro-phenyl; 4-fluoro-3-trifluoromethyl-phenyl; 4-fluoro- phenyl; 4-methyl-3-[A^-[4-(3-pyridyl)-pyrimidin-2-yl]amino]-phenyl; 4-methyl-phenyl; 4- trifluoromethoxy-phenyl; 4-trifluoromethyl-phenyl; 5-bromo-2,3-dihydro-1 //-indol-1 -yl; 5-chloro-2-methoxy-phenyl; 5-chloro-2-methyl-phenyl; 5-trifluoromethyl-2-fluoro- phenyl; and phenyl. 15. The compound as claimed in claim 14. wherein R100 is selected from the group consisting of: H, methyl, and ethyl; RBand Rc arc independently selected from the group consisting of: methoxy and ethoxy; and R5 is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, bromo, and fluoro. Rc is -0(CH2)3OH; R100 is selected from the group consisting of: H and alkyl; RB is selected from the group consisting of: alkoxy: and R5 is selected from the group consisting of: alkoxy and halogen; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. 17. The compound as claimed in claim 16, wherein R1 ° is selected from the group consisting of: H, methyl, and ethyl; RB is selected from the group consisting of: methoxy and ethoxy; and R5 is selected from the group consisting of: methoxy, ethoxy, isopropoxy, chloro, bromo, and fluoro. R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl,-N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(aIkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; L2 is a linking group selected from the group consisting of: -(CH2)M-, -CH(R100)-, -C(=R100)-, -C(R100)2-; wherein R100is selected from: alkyl, hydroxy, aryl, alkoxy, oxo, -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH; provided that when L2 is -CH2CH2-, neither R6 nor R7 is -CH2-(C=0)NHalkyl, -CH2-(C=0)N(alkyl)2 or -CH2C(=0)Oalkyl; 419 R10 is independently selected from the group consisting of ~— X1 A22 fcP) S V_y and-X'-A^-Y'-A21; wherein X1 and Y1 are each independently absent or selected from the group consisting of: -(alkyl)C(=0)N(alkyI)-, -C(=0)N(alkyl>, -C(=0)NH-, -C(O)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)NH-. -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(O)-, -NHC(=0)N(alkyl)-, -NHC(=())NH, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(-0)0-, -S-, -SO-, -S02-, -S02N(alkyl)-, and -S02NH-; A20 is absent or selected from alkyl or alkenyl; and A21 is selected from alkyl, alkenyl, or H; wherein when A20 or A21 is alkyl or alkenyl, the alkyl or alkenyl may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02a)kyl, -OC(=0)alkyl, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; © ^—y is selected from the group consisting of aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl,^r benzo-fused heterocycloalkyl, are optionally substituted with one or more substkuents independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy. alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylarnino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -0C(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; (d) -C(=O)(CH2CH2O-)i-i0 terminating with H, methyl, ethyl, or benzyl; (e) -C(=O)CH2O(CH2CH2O-)M0 terminating with H, methyl, ethyl, or benzyl; . (0 -C(=0)alkyl, or -C(=0)(C3.6)cycloalkyl, wherein said -C(=0)alkyl, and -C(=0)(C3-6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -Oalkylaryl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, or -OC(=0)alkyl; (g) -C(0)(CH2)i-3aiyl, -C(=0)aryl, -C(=0)(CH2)i-3heteroaryI, or -C(=0)heteroaryl, wherein said -C(=0)(CH2),.3aryl, -C(=0)aryl, -C(=0)(CH2),.3heteroaryl, and -C(=0)heteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -0C(=0)alkyl; (h) -C(=0)(CH2)|.6C(=0)-terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(0)0(CH2CH20-)Mo terminating witli H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyl, or -C(=0)0(C3.6)cycloalk\ 1. wherein said -C(=0)Oalkyl, and -C(=0)0(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH;, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2),.3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i.3heteroaryI, or -C(=0)Oheteroar> 1 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NMS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (1) -C(=O)NH(CH2CH2O-)M0 terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-l-pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl. -CH2CH2-l-piperazinyl, -CH2CH2-1- (4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(Ci.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, or -C(=0)N(alkyl)2, wherein said -C(=O)NH(C1.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)i.3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)i.3heteroaryl, or -C(=0)NHheteroaryl, wherein said -C(=0)NH(CH2)i.3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)i.3heteroaryl, and -C(=0)NHheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or . *;'*V * -OC(=0)alkyl; A^' * (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-l-pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl, -CH2CH2-1 -piperazinyl. -CH2CH2-1 -(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)aIkyI, or -C(=0)aryl; wherein the aryl portion of said -C(=())aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; (q) -C(=S)NHalkyl; (r) -C(=S)N(alkyl)2; (s) -S02NH2; (t) -S02NHalkyl; (u) -S02N(alkyl)2; (v) -P(=0)(OCH3)2; and (w) -P(=0)(OCH2CH3)2; provided that when R6 is present, R7 is absent; and provided that when R7 is present, R is absent; r is an integer from 0 to 4; and R is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2, thio, thioalkyl, 5 ~^, and— V—B10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-. -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-. -NHC(=0)0-, -NHS02-, -0-. -OC(=0). -OC(=0)N(alkyI)-, -OC(=0)NH-. -OC(=0)0-, -S-, -SO-. -S02-, -S02N(alkyl)- and -S02NH-; B is absent or selected from alkyl or alkenyl; B is absent or selected from alkyl, alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(-0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyI)2, -OC(=0)NHalkyl, -S02alkyL thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutical^ acceptable salt thereof. R9 is independently selected from the group consisting of: alkoxy, alkyl, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalk\i.-N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio and thioalkyl; L2 is a linking group selected from the group consisting of: -(CH2)|.4-, -CH(R100)-, -C(=R100)-, -C(R100)2-; wherein R,00is selected l'rom: alkyl, hydroxy, aryl, alkoxy, oxo. -NH2, -NH(alkyl) -N(alkyl)2, =N(OH) or -NH2OH; —^ is selected from the group consisting of aryl. cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, nine to ten membered benzo-fused cycloalkyl, and nine to ten membered benzo-fused heterocycloalkyl; wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyj t>r benzo-fused heterocycloalkyl. are optionally substituted with one or more substituehls independently selected from halogen, hydroxy, amino, thio. nitro. cyano. alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(=0)NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -OC(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oalkyl, -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(=0)OH, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated SO2-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl. -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2. -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02aIkyl, -S02NH2, thio, thioalkyl, , and—V—B,10—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(=0)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-. -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -OC(=0)N(alkyl)-, -OC(=0)NH-, -OC(=0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl; B20 is absent or selected from alkyl. alkenyl, or H; wherein, when B10 or B20 is alkyl or alkenyl. the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyI)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(==0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -0C(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyl, thio or thioalkyl; and ^—' is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl. a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membercd benzo-fused heterocycloalkyl, r y * wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, .'$*> heterocycloalkyl, benzo-fused cycloalkyl, or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2,-N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)()alkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. independently selected from halogen, hydroxy, amino, thio, nitro, cyano, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, alkylamino, -NHC(=0)alkyl, -N(alkyl)C(=0)alkyl, or dialkylamino, -NHC(= C))NH2, -NHC(=0)NHalkyl, -N(alkyl)C(=0)NHalkyl, -0C(=0)NHalkyl, -NHC(=0)Oalkyl, -N(alkyl)C(=0)Oj#$)^,,v' -NHS02alkyl, -N(alkyl)S02alkyl, thioalkyl, halogenated thioalkyl, -S02alkyl, T halogenated -S02alkyl, -NHC(=0)N(alkyl)2, -N(alkyl)C(=0)N(alkyl)2 or -OC(=0)N(alkyl)2; (f) -C(=0)alkyl, or -C(=0)(C3.6)cycloalkyl, wherein said -C(=0)alkyl, and -C(=0)(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -Oalkylaryl, -NH2, -NHalkyl, -N(alkyi heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, or -OC(=0)alkyl; (g) -C(=0)(CH2),.3aryl, -C(=0)aryl, -C(=0)(CH2),.3heteroaryl, or -C(=0)heteroaryl, wherein said -C(=0)(CH2),.3aryl, -C(=0)aryl, -C(-0)(CH2)i.3heteroaryl, and -C(=0)heteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -0C(=0)alkyl; (h) -C(=0)(CH2)i-6C(=0)- terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(=0)0(CH2CH20-)i.io terminating with H, methyl, ethyl, or benzyl; 0) -C(=0)Oalkyl, or -C(=0)0(C3.6)cycloalkyl, wherein said -C(=0)Oalkyl, and -C(=0)0(C3.6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl. -0C(=0)alkyl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2)i.3aryl, -C(=0)Oaryl, -C(=0)0(CH2),.3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)i.3heteroaryl, or -C(==0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; ^ v (1) -C(=O)NH(CH2CH2O-),.|0 terminating with -H, methyl, ethyl, benzyl, ./.,»*$*' -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1 -pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl -CH2CH2-l-piperazinyL -CH2CH2-1- (4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(C,.20)alkyl, -C(=0)NH(C3.6)cycloalkyl, or -C(=0)N(alkyl)2, wherein said -C(=O)NH(C,.20)alkyl, -C(=0)NH(C3-6)cycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(-0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2),.3aryl, -C(=0)NHar>l, -C(=0)NH(CH2),.3heteroaryl, or -C(=0)NHheteroaryl, wherein said -C(=0)NH(CH2)i-3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)i.3heteroaryl, and -C(=0)NHheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=O)NHCH2CH2NH(CH2CH2NH-)0-3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-1-pyrrolidinyl, -CH2CH2-l-piperidinyl, L3 is absent; —y is aryl; r is an integer from 0 to 4; and R5 is independently selected from the group consisting of: alkyl, alkyl amino, alkyloxy, amino, -C(=0)NH2, -C(=0)Oalkyl, -C(O)0H, -CH2OH, cyano, dialkylamino, halogen, halogenated alkyl, halogenated alkyloxy, halogenated S02-alkyl, halogenated thioalkyl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl, -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl, -S02NH2, thio, .£_v B10-TF) thioalkyl. * ^^, and— V—Bl()—W—B20; wherein, V and W are each independently absent or selected from the group consisting of: -C(=0), -C(=0)N(alkyl)-, -C(=0)NH-, -C(=0)0-, -N(alkyl)-, -N(alkyl)C(=0)-, -N(alkyl)C(=0)N(alkyl)-, -N(alkyl)C(=0)NH-, -N(alkyl)C(=0)0-, -N(alkyl)S02-, -NH-, -NHC(O)-, -NHC(=0)N(alkyl)-, -NHC(=0)NH-, -NHC(=0)0-, -NHS02-, -0-, -OC(=0), -0C(O)N(alkyl)-, -OC(=0)NH-, -OC(-0)0-, -S-, -SO-, -S02-, -S02N(alkyl)- and -S02NH-; B10 is absent or selected from alkyl or alkenyl: B20is absent or selected from alkyl, alkenyl. or H: wherein, when B10 or B20 is alkyl or alkenyl, the alkyl or alkenyl group may be optionally substituted with one or more groups independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated -S02alkyl, halogenated thioalkyl, hydroxy -N(alkyl)C(=0)alkyl. -N(alkyl)C(=0)N(alkyl)2, -N(alkyl)C(=0)NH2, -N(alkyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(=0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=0)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, -0C(=0)alkyl, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -OC(=0)Oalkyl, -S02alkyL thio or thioalkyl; and is selected from the group consisting of: an aryl, a cycloalkyl, a partially unsaturated carbocycle, a heteroaryl, a heterocycloalkyl, a nine to ten membered benzo-fused cycloalkyl, and a nine to ten membered benzo-fused heterocycloalkyl, wherein, the aryl, cycloalkyl, partially unsaturated carbocycle, heteroaryl, heterocycloalkyl, benzo-fused cycloalkyl. or benzo-fused heterocycloalkyl, is optionally substituted with one or more substituents independently selected from: alkoxy, alkylamino, amino, cyano, dialkylamino, halogen, halogenated alkoxy, halogenated alkyl, halogenated -S02alkyl, halogenated thioalkyl, heteroaryl, hydroxy, hydroxy alkyl, -N(alkyl)C(=0)alkyl,-N(alkyl)C(=0)N(alkyl)2.-N(a!kyl)C(=0)NHalkyl, -N(alkyl)C(=0)Oalkyl, -N(alkyl)S02alkyl, -NHC(0)alkyl, -NHC(=0)N(alkyl)2, -NHC(=0)NH2, -NHC(=Q)NHalkyl, -NHC(=0)Oalkyl, -NHS02alkyl, nitro, -OC(=0)N(alkyl)2, -OC(=0)NHalkyl, -S02alkyl. thio or thioalkyl; or an optical isomer, enantiomer, diastereomer, racemate, or pharmaceutically acceptable salt thereof. 24. The compound as claimed in claim 23. wherein L is a linking group selected from the group consisting of: -(CH2)-, -CH(CH3)-, -CH(CH2CH3)-. (h) -C(=0)(CH2)1-6C(=0)- terminating with methyl, ethyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (hh) -C(=0)alkylOC(=0)alkyl- terminating with -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, or heterocycloalkyl; (i) -C(=0)0(CH2CH20-)1-10 terminating with H, methyl, ethyl, or benzyl; (j) -C(=0)Oalkyl, or -C(=0)0(C3.6)cycloalkyl, wherein said -C(=0)Oalkyl, and -C(=0)0(C3-6)cycloalkyl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -0C(=0)alkyl, -C(=0)OH, -C(=0)Oalkyl, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; (k) -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)1-3heteroaryl, or -C(=0)Oheteroaryl, wherein said -C(=0)0(CH2),.3aryl, -C(=0)Oaryl, -C(=0)0(CH2)1-.3heteroaryl, or -C(=0)Oheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl. -NHS02alkyl, halogen, nitrile. or -OC(=0)alkyl: (1) -C(=0)NH(CH2CH20-)1-10 terminating with -H, methyl, ethyl, benzyl, -CH2CH2NH2, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-l-pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl. -CH2CH2-l-piperazinyl, -CH2CH2-1- (4-CH3)-piperazinyl or -C(=0)alkyl; (m) -C(=0)NH2, -C(=O)NH(C1-.20)alkyl, -C(=0)NH(C3-6)cycloalkyl, or -C(=0)N(alkyl)2, wherein said -C(=0)NH(C1-2o)alkyl, -C(=0)NH(C3-6)cycloalkyl, and -C(=0)N(alkyl)2 may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2 -NHaiky, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, -OC(=0)alkyl, -OC(=0)alkenyl, -NHC(=0)aryl, -C(=0)OH, -C(=0)Oalky, -C(=0)NH2, -C(=0)NHalkyl, or -C(=0)N(alkyl)2; and, wherein the aryl portion of said -NHC(=0)aryl may be optionally substituted with one or more groups independently selected from: alkyl, -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (n) -C(=0)NH(CH2)1-3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)1-3heteroaryl, or -C(=0)NHheteroaryl, wherein said -C(=0)NH(CH2)1-3aryl, -C(=0)NHaryl, -C(=0)NH(CH2)1-3heteroaryl, and -C(=0)NHheteroaryl may be optionally substituted with one or more groups independently selected from: -OH, -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, heterocycloalkyl, -NHC(=0)alkyl, -NHS02alkyl, halogen, nitrile, or -OC(=0)alkyl; (o) -C(=0)NHCH2CH2NH(CH2CH2NH-)o.3 terminating with H, methyl, ethyl, -CH2CH2NHalkyl, -CH2CH2N(alkyl)2, -CH2CH2-l-pyrrolidinyl, -CH2CH2-l-piperidinyl, -CH2CH2-4-morpholinyl,-CH2CH2-1-piperazinyL-CH2CH2-1-(4-CH3)-piperazinyl, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH3, -CH2CH2OC(=0)alkyl, or -C(=0)aryl; wherein the aryl portion of said -C(=0)aryl may be optionally substituted with one or move groups independently selected from: alkyl, -OH , -Oalkyl, -NH2, -NHalkyl, -N(alkyl)2, halogen or nitrile; (p) -C(=S)NH2; (q) -C(=S)NHalkyl; (r) -C(=S)N(a\ky\)2; 31. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 1. 32. The pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 7. 33. The pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 14. 34. The pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 16. 35. The pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 25. 36. The pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound as claimed in claim 26. 37. The pharmaceutical composition comprising a pharmaceutical ly acceptable carrier and a compound as claimed in claim 27. The invention is directed to : N-Substituted tricyclic 3-aminopyrazole derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical composition comprising the compounds of the presentinvention and to methods for treating conditions such as tumors and other cell proliferative disorders. |
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1925-kolnp-2004-granted-abstract.pdf
1925-kolnp-2004-granted-assignment.pdf
1925-kolnp-2004-granted-claims.pdf
1925-kolnp-2004-granted-correspondence.pdf
1925-kolnp-2004-granted-description (complete).pdf
1925-kolnp-2004-granted-examination report.pdf
1925-kolnp-2004-granted-form 1.pdf
1925-kolnp-2004-granted-form 13.pdf
1925-kolnp-2004-granted-form 18.pdf
1925-kolnp-2004-granted-form 2.pdf
1925-kolnp-2004-granted-form 26.pdf
1925-kolnp-2004-granted-form 3.pdf
1925-kolnp-2004-granted-form 5.pdf
1925-kolnp-2004-granted-reply to examination report.pdf
1925-kolnp-2004-granted-specification.pdf
| Patent Number | 229502 | |||||||||||||||||||||||||||||||||||||||
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| Indian Patent Application Number | 1925/KOLNP/2004 | |||||||||||||||||||||||||||||||||||||||
| PG Journal Number | 08/2009 | |||||||||||||||||||||||||||||||||||||||
| Publication Date | 20-Feb-2009 | |||||||||||||||||||||||||||||||||||||||
| Grant Date | 18-Feb-2009 | |||||||||||||||||||||||||||||||||||||||
| Date of Filing | 15-Dec-2004 | |||||||||||||||||||||||||||||||||||||||
| Name of Patentee | JANSSEN PHARMACEUTICA N.V. | |||||||||||||||||||||||||||||||||||||||
| Applicant Address | TURN-HOUTSEWEG 30, B-B-B 2340 BEERSE | |||||||||||||||||||||||||||||||||||||||
Inventors:
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| PCT International Classification Number | C07D 231/54, 231/56 | |||||||||||||||||||||||||||||||||||||||
| PCT International Application Number | PCT/US03/15193 | |||||||||||||||||||||||||||||||||||||||
| PCT International Filing date | 2003-05-13 | |||||||||||||||||||||||||||||||||||||||
PCT Conventions:
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