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New hydroxy, alkoxy, acyloxy and oxo substituted pyrrolizine derivatives useful for treatment of rheumatic and allergic disorders, e.g. psoriasis, urticaria and eczema
New hydroxy, alkoxy, acyloxy and oxo substituted pyrrolizine derivatives useful for treatment of rheumatic and allergic disorders, e.g. psoriasis, urticaria and eczema
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.
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机译:1-(羟基,烷氧基,酰氧基或氧代)-6,7-二(杂)芳基-吡咯嗪衍生物是新的。式(I)的吡咯嗪衍生物及其光学异构体,盐和生理上可水解的酯是新的:R 1,R 2 =芳基或含有1-3个N,O和/或S原子的单环或双环杂芳基(各自任选地被1-3个烷基,卤素,CF 3,烷氧基,芳氧基和/或CN取代,并且任选地与苯基或萘基稠合); R 3 = H;烷基; COOH; COO-烷基; COO-烷基-苯基;可可COCOO-烷基; CHO;或A-Y; A = 1-8C亚烷基或2-8C亚烯基,任选地被OH或烷氧基取代; Y = COOH; SO3H; OPO(OH)2; OP(OH)2;四唑基COO-烷基; SO 3-烷基; CHO;或OH; Alk = 1-4C亚烷基; R 4 -R 7 = H或烷基; R 8和R 9之一为H或烷基。另一个是OH烷氧基或酰氧基;或R 8 + R 9 =氧代。
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