| abstract |
6,7-dihydro-5h-pyrido[2,3-c]pyridazine derivatives and related compounds as inhibitors of bcl-xl protein and proapoptotic agents for cancer treatment. the present invention relates to derivatives of 6,7-dihydro-5h-pyrido[2,3-c]pyridazine, 1,2,3,4-tetrahydroquinoline, 1h-indole, 3,4-di -hydro-2h-1,4-benzoxazine, 1h-pyrrolo[2,3-b]pyridin-1-yl, 7h-pyrrolo[2,3-c]pyridazine, 5h,6h,7h,8h,9h-pyridazine [3,4-b]azepine and related compounds of formula (i) as inhibitors of bcl-xl protein for use in pro-apoptotic agents for the treatment of cancer, autoimmune diseases or diseases of the immune system. formula (i). the invention describes the preparation of exemplary compounds (e.g. pages 113 to 354, examples 1 to 221) as well as pharmacological studies with relevant data (e.g. pages 355 to 367; examples a to e; tables 1 to 5). Exemplary compounds are, for example, 2-{6-[(1,3-benzothiazol-2-yl)amino]-1,2,3,4-tetrahydroquinolin-1-yl}-1,3-thiazole acid -4-carboxylic acid (example 1) or, for example, 3-{1-[(adamantane-1-yl)methyl]-5-methyl-1h-pyrazol-4-yl}-6-{3-[( 1,3-benzothiazol-2-yl)amino]-4-methyl-5h,6h,7h,8h-pyrido[2,3-c]pyridazine-8-yl]pyridine-2-carboxylic acid (Example 24). |