首页> 外国专利> N-SUBSTITUTED (ALPHA-IMIDAZOLYL-TOLUYL) PYRROLE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF CIRCULATORY DISORDERS

N-SUBSTITUTED (ALPHA-IMIDAZOLYL-TOLUYL) PYRROLE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF CIRCULATORY DISORDERS

机译:N-取代的(α-咪唑基-甲苯基)吡咯血管紧张素II拮抗剂治疗循环系统疾病

摘要

A class of N-substituted ( alpha -imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula IMAGE wherein m is one; wherein each of R0 and R1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R5 and R8 must be selected from COOH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, IMAGE wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
机译:一类N-取代的(α-咪唑基-甲苯基)吡咯化合物,描述用于治疗循环系统疾病。特别感兴趣的化合物是式的血管紧张素II拮抗剂,其中m是1; m是1。其中R0和R1各自独立地选自氢,烷基,羟烷基,甲酰基,卤素,卤代烷基,环烷基羰基,烷氧基,芳酰基,芳氧基,芳烷氧基,烷基羰基,烷氧基羰基,氰基,硝基,羧基,烷基羰基氧基,烷基羰基氧基烷基,烷氧基羰基烷基,烷基磺酰基,芳烷基磺酰基,芳基磺酰基;其中R2选自甲基,乙基,正丙基,异丙基,正丁基,仲丁基,异丁基,叔丁基,正戊基,异戊基,新戊基,苯基,苄基,苯乙基,环己基,环己基甲基,丙硫基,丁硫基和羟烷基;其中R3,R4,R5,R6,R7,R8,R9和R10各自独立地选自氢,卤素,硝基,三氟甲基,羟基,烷氧基,氰基,羧基和甲氧羰基;条件是R5和R8中的至少一个必须选自COOH,PO3H2,SO3H,CONHNH2,CONHNHSO2CF3,,其中R42和R43各自独立地选自氯,氰基,硝基,三氟甲基,甲氧基羰基和三氟甲基磺酰基;或其互变异构体或其药学上可接受的盐。这些化合物在治疗或控制高血压和充血性心力衰竭中特别有用。

著录项

  • 公开/公告号AU1463792A

    专利类型

  • 公开/公告日1992-10-06

    原文格式PDF

  • 申请/专利权人 G.D. SEARLE & CO.;

    申请/专利号AU19920014637

  • 申请日1992-02-19

  • 分类号C07D403/10;C07D403/14;

  • 国家 AU

  • 入库时间 2022-08-22 05:31:45

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