首页> 外国专利> 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

机译:新的羟基,烷氧基,酰氧基和氧代取代的吡咯烷嗪衍生物可用于治疗风湿性和过敏性疾病,例如牛皮癣,荨麻疹和湿疹

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.
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。

著录项

  • 公开/公告号DE19845446A1

    专利类型

  • 公开/公告日2000-04-06

    原文格式PDF

  • 申请/专利权人 MERCKLE GMBH;

    申请/专利号DE1998145446

  • 申请日1998-10-02

  • 分类号C07D487/04;A61K31/40;

  • 国家 DE

  • 入库时间 2022-08-22 01:42:32

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