Substituted tricyclic pyrazole derivatives with protein kinase activity
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A technology of kinase activity and protein kinase, which is applied in the fields of organic active ingredients, medical preparations containing active ingredients, organic chemistry, etc., and can solve the problems of non-disclosure
Inactive Publication Date: 2001-09-05
ABBOTTGMBH & CO
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To date, no direct evidence has been published for the critical role of KDR in VEGF-mediated vascular hyperpermeability
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[0030]The compounds of the invention possess anti-angiogenic properties. These anti-angiogenic properties are due at least in part to the inhibition of protein tyrosine kinases that play a key role in the angiogenesis process. For this reason, the compounds of the present invention are useful as active agents in the treatment of conditions such as arthritis, atherosclerosis, psoriasis, hemangiomas, myocardial angiogenesis, coronary and cerebral artery bypass, ischemic extremity angiogenesis, wound Healing, H. peptic ulcer disease, bone fractures, cat scratch fever, flushing, neovascular glaucoma, and retinopathy such as diabetic retinopathy or age-related macular degeneration. In addition, certain compounds of the present invention are useful as active agents in the treatment of solid tumors, malignant ascites, hematopoietic carcinomas, and hyperproliferative disorders such as thyroid hyperplasia (especially Graves' disease) and cysts (as characterized by polycystic ovary synd...
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Abstract
Chemical compounds that are derivatives of 2H[1]-benzothiepino[5,4-c]pyrazole, 2H[1]-benzoxepino[5,4-c]pyrazole, 1-benzothiopyrano[4,3-c]pyrazole, 1-benzopyrano[4,3-c]pyrazole, 4,5-dihydro-2h-furano[2,3-g]indazole and 4,5-dihydro-2h-thieno[2,3-g]indazole derivatives 2H[1]-benzothiepino[5,4-c]pyrazole, [1]-benzothiopyrano[4,3-c]pyrazole, 4,5-dihydro-2H-furano[2,3-g]indazole and 4,5-dihydro-2H-thieno[2,3-g]indazole derivatives are inhibitors of protein kinase activity. Several of the protein kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic and / or edematous processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis, edema or endothelial cell hyperproliferation or hyperpermeability is a factor. Like cancer, artritis, atherosclerosis, psoriasis, hemangioma, myocardial angiogenesis, coronary and cerebral collaterals, ischemic limb angiogenesis, corneal disease, rubeosis, neovascular glaucoma, macular degeneration, wound healing, peptic ulcer Helicobacter related diseases, fractures, diabetic retinopathy, and cat scratch fever.
Description
Background of the invention [0001] At least 400 enzymes have been identified as protein kinases. These enzymes catalyze the phosphorylation of target protein substrates. Phosphorylation is generally a transfer reaction in which a phosphate group is transferred from ATP to a protein substrate. The specific structure of the target substrate to which the phosphate group is transferred is a tyrosine, serine or threonine residue. Since these amino acid residues are the target structures for phosphoryl transfer, these protein kinases are often referred to as tyrosine kinases or serine / threonine kinases. [0002] Phosphorylation and resistance phosphatase reactions on tyrosine, serine and threonine residues are involved in a myriad of cellular processes that become responsive to different intracellular signals (usually mediated through cellular receptors) Fundamental to responding, regulating cellular function, and activating or inactivating cellular processes. Protein kinase cas...
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