New fused-ring di:hydro-pyridine-acetic acid derivs. - useful as cardio-protective and cerebro-protective agents, antiinflammatory agents and anticoagulants or platelet aggregation inhibitors

摘要

Fused-ring dihydropyridine acetic acid derivs. of formula (I) and their acid-addn. salts are new. A = benzo, thieno or indolo (also pyrrolo in disclosure); when A = benzo, m = 2 and R11 = OH, 1-4C alkoxy, mesyloxy or NHSO2Me, or adjacent R11+R11 = OCH2O or OCH2CH2O (M and R11 are not otherwise defined); R1 = 4-6C cycloalkyl or (4-6C)cycloalkyl(1-5C)alkyl, or when A = pyrrolo, R1 may also be H, 1-10C alkyl, phenyl(1-5C)alkyl, 1-4C alkoxy or NHCOX (X - 1-5C alkyl); R2 and R3 = H or 1-5C alkyl, or CR2R3 is a 5- or 6-membered carbocyclic ring; R5 = H or 1-4C alkyl; R4 = 1-4C alkoxy or NR9R10; R9 and R10 = H, 3-6C alkenyl, 3-6C alkynyl, or 1-12C alkyl opt. substd. by OH, 1-4C alkoxy, di(1-4C alkyl)amino, furyl, pyridyl, pyrrolidinyl, morpholino, indolyl, CN, thienyl or phenyl (opt. substd. by OH, OMe, F, NHSO2Me, mesyloxy or OCH2O); or R9 = H and R10 = phenyl, fluorophenyl, pyridyl or N-benzylpiperidyl; or NR9R10 = pyrrolidino, piperidino, morpholino or 1-piperazinyl opt. 4-substd. by Me, Ph, mono- or di(1-4C alkoxy)phenyl, pyrimidinyl or phenyl(1-4C)alkyl. A typical cpd. is 3,4-dihydro-6,7-dimethoxy-alpha- cyclohexyl-N-(2- methoxybenzyl)-isoquinoline-1-acetamide. HCl, m.pt. 116-127 deg. C. USE/ADVANTAGE - (I) are cardioprotective and cerebroprotective agents, antiinflammatory agents (e.g. for treating asthma and arthritis), and anticoagulants or platelet aggregation inhibitors.