New fused di:hydro:pyridine cpds. - exhibit cardio- and cerebro-protective activity useful in treatment of Crohn's disease, asthma, arthritis, etc.

摘要

Fused dihydropyridine cpds. of formula (Ia), their tautomers of formula (Ib) and (Ic), and salts of these cpds. with acids, bases and complex-formers, are new. X is ORr, NHR2 or NR3R4; R is R, OH, N3, halo, CF3, RO, CHO, COR1, NHR2 or NR3R4; u is 1, 2 or 3; R is H or 1-10C alkyl opt. substd. by one or more Q; Q is e.g. CN, OH, RO, RS, ROCO, NH2, NHR, N(R)2, PhO (opt. substd. by 1-3 T), Ph (opt. substd. by 1-3 T), 3-10C cycloalkyl, etc. R is 1-4C alkyl; T is e.g. halo, CF3, RO, OH, SH, RS, R, N3, NH2, NHR, N(R)2, 2-3C acylamino, etc.; R2 is e.g. H, 3-6C alkenyl, 3-6C alkynyl, 3-6C cycloalkyl, 3-6C alkyl (fused to a benzo gp.), etc.; R3, R4 are as R2, esp. 1-6C alkyl (opt. substd. by Ph which is itself opt. substd. by 1-3 T); or NR3R4 is an opt. satd. 5-6 membered heterocycle which opt. contains up to 2 other N, O or S heteroatoms and which is opt. substd. by R, OH or (CH2)pR5; p is 0, 1, 2, 3 or 4; R5 is naphthoxy, or Ph or PhO (both opt. substd. by 1-3 T); A is e.g. (i)-(iv); R8 is H, R or RO; R6, R7 are H, OH, R, RO, NH2 or MeSO2MH; or R6+R7 is O(CH2)nO; R9 is H or 1-4C alkyl. USE/ADVANTAGE - (I) have cardio protective and cerebroprotective effects and may be used to treat patients suffering from stroke. They may also be used to treat chronic inflammatory disorders (e.g. arthritis or bronchial asthma), and to inhibit blood clotting and platelet aggregation. (I) may also be used to treat Crohn's disease and ulcerative colits. Admin. is oral, parenteral or topical in doses of 0.05-500 mg.