ANTI-INFLAMMATORY OXO DERIVATIVES AND HYDROXY DERIVATIVES OF PYRROLIZINES, AND THEIR PHARMACEUTICAL USE

摘要

1-(Hydroxy, alkoxy, acyloxy or oxo)-6,7-di(hetero)aryl-pyrrolizine derivatives are new. Pyrrolizine derivatives of formula (I) and their optical isomers, salts and physiologically hydrolysable esters are new: R1, R2 = aryl or mono- or bicyclic heteroaryl containing 1-3 N, O and/or S atoms (each optionally substituted by 1-3 alkyl, halo, CF3, alkoxy, aryloxy and/or CN and optionally fused with phenyl or naphthyl); R3 = H; alkyl; COOH; COO-alkyl; COO-Alk-phenyl; COCOOH; COCOO-alkyl; CHO; or A-Y; A = 1-8C alkylene or 2-8C alkenylene optionally substituted by OH or alkoxy; Y = COOH; SO3H; OPO(OH)2; OP(OH)2; tetrazolyl; COO-alkyl; SO3-alkyl; CHO; or OH; Alk = 1-4C alkylene; R4-R7 = H or alkyl; one of R8 and R9 = H or alkyl; and the other is OH; alkoxy; or acyloxy; or R8 + R9 = oxo.