| 摘要 |
Disclosed are 3-methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-3H-imidazo[4,5-b]pyridine-6-carboxylic acid amides, 1-methyl-2-(6-trifluoromethyl-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid amides, 2-(6-chloro-benzothiazol-2-ylamino)-1-methyl-1H-benzoimidazole-5-carboxylic acids and their derivatives as represented by the general formula (I), wherein v is 1, R2 is selected from trifluoromethyl, trifluoromethoxy or chloro; R3 is hydrogen; R4 is selected from methyl, ethyl or 2-methoxy-ethyl; X1 is selected from CH or N; X2 is selected from CH or CF; X3 is carbon substituted with a carboxamide group as defined herein; and X4 is CH. Representative compounds include 3-methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-3H-imidazo[4,5-b]pyridine-6-carboxylic acid (2-methoxy-5 ethyl)-amide, 3-methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-3H-imidazo[4,5-b]pyridine-6-carboxylic acid (2-morpholin-4-yl-ethyl)-amide, 1-methyl-2-(6-trifluoromethyl-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide, 2-(6-chloro-benzothiazol-2-ylamino)-1-methyl-1H-benzoimidazole-5-carboxylic acid (2-methoxy-ethyl)-amide, 6-fluoro-1-methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid ethylamide, 1-ethyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid (2-ethoxy-ethyl)-amide, 1-(2-methoxy-ethyl)-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid (2-ethoxy-ethyl)-amide, 1-methyl-2-(6-trifluoromethyl-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid [2-((S)-3-methoxy-pyrrolidin-1-yl)-2-oxo-ethyl]-amide, and 1-methyl-2-(6-trifluoromethyl-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid ((S)-1-dimethylcarbamoyl-ethyl)-amide. Also disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier or diluent, for use in treating a disease, disorder, or condition selected from the group consisting of: (i) a cardiovascular disease (such as arteriosclerosis or hypertension); (ii) diabetes and diabetic-related complications, including glomerular nephropathy; (iii) a cerebral nerve degenerative disease (such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, or multiple sclerosis); (iv) asthma; (v) chronic obstructive pulmonary disease; (vi) a skin disease; (vii) an eye disease including macular degeneration, cataracts, light retinopathy, and retinopathy of prematurity; and (viii) cancer. |
