PYRIDINE DERIVATIVES AS VEGFR-2 RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS

摘要

591820 Disclosed are amides and thioamides of formula I. Specific examples of compounds of formula I include: (4-{ [2-(3,3-Dimethyl-butylcarbamoyl)-phenylamino]-methyl} -pyridin-2-yl)carbamic acid methyl ester, 2-[(2-Acetylamino-pyridin-4-ylmethyl)-amino]-N-(3-ethyI-pentyl)-benzamide, Furan-2-carboxylic acid (4-{ [2-(4-methyl-pentylcarbamoyl)-phenylamino]-methyl} -pyridin-2-yl)-amide, and Furan-2-carboxylic acid (4-{ [2-(3-ethyl-pentylcarbamoyl)-phenylamino]-methyl} -pyridin-2-yl)-amide. Compounds of formula I exhibit a high receptor tyrosine kinase inhibitory activity on the receptor VEGFR-2, also referred to as the KDR receptor. The compounds inhibit angiogenesis, which is beneficial for treating diseases such as atherosclerosis, inflammatory conditions such as dermatitis, psoriasis, rosacea and rheumatoid arthritis, eye diseases such as diabetic retinopathy and macular degeneration, and cancer.