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  Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their useUSPTO Application #: 20060160858Title: Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use Abstract: Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds. (end of abstract) Agent: Agouron Pharmaceuticals, Inc. - San Diego, CA, US Inventors: Allen J. Borchardt, Robert Steven Kania, Cynthia L. Palmer USPTO Applicaton #: 20060160858 - Class: 514333000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms, Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms, Additional Hetero Ring Other Than The Six-membered Hetero Rings The Patent Description & Claims data below is from USPTO Patent Application 20060160858. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Patent Application No. 60/434,902, filed Dec. 19, 2002, herein incorporated by reference in its entirety for all purposes. FIELD OF THE INVENTION [0002] This invention is directed to indazole compounds that mediate and/or inhibit hyperproliferative disorders, such as cancer and ophthalmic diseases, and the activity of certain protein kinases, and to pharmaceutical compositions containing such compounds. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating hyperproliferative disorders, such as ophthalmic diseases and cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds. BACKGROUND OF THE INVENTION [0003] Hyperproliferative disorders and several diseases and conditions of the posterior segment of the eye threaten vision. Age related macular degeneration (ARMD or AMD), choroidal neovascularization (CNV), retinopathies (e.g., diabetic retinopathy, vitreoretinopathy, retinopathy of prematurity), retinitis (e.g., cytomegalovirus (CMV) retinitis), uveitis, macular edema, and glaucoma are several examples. [0004] Age related macular degeneration (ARMD or AMD) is the leading cause of blindness in the elderly. ARMD attacks the center of vision and blurs it, making reading, driving, and other detailed tasks difficult or impossible. About 200,000 new cases of ARMD occur each year in the United States alone. Current estimates reveal that approximately forty percent of the population over age 75, and approximately twenty percent of the population over age 60, suffer from some degree of macular degeneration. "Wet" ARMD is the type of ARMD that most often causes blindness. In wet ARMD, newly formed choroidal blood vessels (choroidal neovascularization (CNV)) leak fluid and cause progressive damage to the retina. In the particular case of CNV in ARMD, two main methods of treatment are currently being developed, (a) photocoagulation and (b) the use of angiogenesis inhibitors. [0005] However, photocoagulation can be harmful to the retina and is impractical when the CNV is in proximity of the fovea. Furthermore, photocoagulation often results in recurrent CNV over time. [0006] Angiogenesis is the mechanism by which new capillaries are formed from existing vessels. When required, the vascular system has the potential to generate new capillary networks in order to maintain the proper functioning of tissues and organs. In the adult, however, angiogenesis is fairly limited, occurring only in the process of wound healing and neovascularization of the endometrium during menstruation. See Merenmies et al., Cell Growth & Differentiation, 8, 3-10 (1997). On the other hand, unwanted angiogenesis is a hallmark of several diseases, such as retinopathies, psoriasis, rheumatoid arthritis, age-related related macular degeneration (AMD), and cancer (solid tumors). Folkman, Nature Med., 1, 27-31 (1995). Protein kinases which have been shown to be involved in the angiogenic process include three members of the growth factor receptor tyrosine kinase family: VEGF-R2 (vascular endothelial growth factor receptor 2, also known as KDR (kinase insert domain receptor) and as FLK-1); FGF-R (fibroblast growth factor receptor); and TEK (also known as Tie-2). [0007] Oral administration of anti-angiogenic compounds is also being tested as a systemic treatment for ARMD. However, due to drug-specific metabolic restrictions, systemic administration usually provides sub-therapeutic drug levels to the eye. Therefore, to achieve effective intraocular drug concentrations, either an unacceptably high dose or repetitive conventional doses are required. Various implants have also been developed for delivery of anti-angiogenic compounds locally to the eye. Examples of such implants are disclosed in U.S. Pat. No. 5,824,072 to Wong, U.S. Pat. No. 5,476,511 to Gwon et al., and U.S. Pat. No. 5,773,019 to Ashton et al., each of which is herein incorporated by reference in their entireties for all purposes. [0008] The compounds of the present invention are improved anti-angiogenic agents that can be used alone or in combination. SUMMARY OF INVENTION [0009] The present invention provides compounds having the following structures: or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof. [0010] In another embodiment, the present invention relates to a compound represented by the formula or a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof. [0011] In another embodiment, the present invention relates to 6-(2-Prop-2-ynylcarbamoyl-phenylamino)-1H-indazole-3-carboxylic acid methylamide. [0012] In another embodiment, the present invention relates to 2-{3-[2-(5-Ethyl-pyridin-2-yl)-vinyl]-1H-indazol-6-ylamino}-N-prop-2-ynyl- -benzamide. [0013] In another embodiment, the present invention relates to N-Cyclopropyl-2-{3-[(E)-2-(4-methyl-pyridin-2-yl)-vinyl]-1H-indazol-6-yla- mino}-benzamide. [0014] In another embodiment, the present invention relates to N-Methoxy-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-benzamide- . [0015] In another embodiment, the present invention relates to N-Allyloxy-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-benzamid- e. [0016] In another embodiment, the present invention relates to N-Isopropoxy-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-benzam- ide. [0017] In another embodiment, the present invention relates to N-Cyclopropyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-benza- mide. [0018] In another embodiment, the present invention relates to 1-Methyl-1H-pyrrole-2-carboxylic acid. [0019] In another embodiment, the present invention relates to N'-(1-{2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-phenyl}-meth- anoyl)-hydrazide. [0020] In another embodiment, the present invention relates to N-Benzyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-benzamide. Continue reading... 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