New fused di:hydro-pyridine cpds. - useful in treatment of stroke, asthma, arthritis, etc.

摘要

Fused dihydropyridine cpds. of formula (Ia), their tautomers of formulae (Ib) and (Ic), and salts of these cpds. with acids, bases and complex formers, are new. X = OR1, NHR2 or NR3R4; R' = R, OH, N3, F, Cl, Br, I, CF3, RO, COH, COR, NHR2 or NR3R4; u = 1, 2 or 3; R1 = H or 1-10C alkyl (opt. subtd. by one or more Q); Q = CN, OH, RO, RS, ROCO, NH2, NHR, N(R)2, PhO (opt. substd. by 1-3 T), Ph (opt. substd. by 1-3 T) or Het or indole (both themselves opt. substd. by one or more R); 3-10C cycloalkyl, 5-6C cycloalkenyl, 3-6C alkynyl, 3-6C cycloalkyl, 3-6C alkyl (fused to a benzene ring), 1-10C alkyl (opt. substd. by one or more Q or naphthoxy), 3-6C cycloalkenyl or phenyl (opt. substd. by 1-3 T); R3, R4 = as R2, esp. 1-6C alkyl (opt. subtd. by phenyl (itself opt. substd. by 1-3 T); or NR3R4 = 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 = 0, 1, 2, 3 or 4; R5 = phenyl or phenoxy (both opt. substd. by 1-3 T), or napthhoxy; T = halo, CF3, RO, OH, SH, RS, R, N3, NH2, NHR, N(R)2, 2-3C acylamino, 2-3C acyloxy or the vicinally-linked gp. O(CH2)nO; n = 1 or 2; A = a gp. of formula (i)-(vii); R8 = H, R or RO; R6, R7 = H, OH, R, RO, NH2 or MeSO2NH; or R6+R7 = O(CH2)nO; R9 = H or R; R10 = H or 2-phenyl- 2-ethoxycarbonylacetyl; R = 1-4C alkyl. USE/ADVANTAGE - (I) have cardioprotective and cerebroprotective effects and can be used to treat patients suffering from stroke. They can also be used to treact chronic inflammatory disorders (e.g. arthritis and bronchial asthma) and to inhibit blood clotting and platelet aggregation. Admin. is oral, parenteral or topical, in doses of 0.05-500 mg.