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    • 1. 发明申请
    • 1, 2, 4 -TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS
    • 1,2,4-异噻唑衍生物作为VASOPRESSIN ANTAGONISTS
    • WO2006123242A1
    • 2006-11-23
    • PCT/IB2006/001442
    • 2006-05-08
    • PFIZER LIMITEDBRYANS, Justin, StephenJOHNSON, Patrick, StephenROBERTS, Lee, RichardRYCKMANS, Thomas
    • BRYANS, Justin, StephenJOHNSON, Patrick, StephenROBERTS, Lee, RichardRYCKMANS, Thomas
    • C07D403/04C07D471/04C07D491/10C07D471/10C07D403/14C07D401/04C07D487/04C07D498/04A61K31/4196A61P15/00A61P9/00
    • C07D471/04C07D401/04C07D403/04C07D403/14C07D471/10C07D487/04C07D491/10C07D498/04
    • Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R 1 represents [CH 2 ] n -R 2 ; R 2 represents H, C 1-6 alkyloxy or Het; n represents a number selected from 0 to 6; Het represents an unsaturated heterocycle of 5 or 6 atoms containing one or more heteroatoms selected from O, N, and S; R 3 represents halo; Ring A represents a 4 to 7 membered, saturated, partially saturated, or unsaturated heterocycle containing one or more heteroatoms selected from O, N, and S; Ring B represents a saturated, partially saturated, or unsaturated heterocycle of from 3 to 8 atoms containing one or more heteroatoms selected from O, N, and S, or Ring B represents a saturated or unsaturated carbocyclic ring of from 3 to 8 atoms; Ring B is optionally fused to an aryl ring and is optionally substituted with one or more groups independently selected from R 4 ; Ring A and Ring B share at least one atom; R 4 represents oxo, [CH 2 ] m -R 5 , or CH-R 6 R 7 ; R 5 represents H, OH, C 1-6 alkyloxy, COOH, or CONR 8 R 9 ; m represents a number selected from 0 or 1 ; and R 6 , R 7 , R 8 and R 9 independently represent H or C 1-6 alkyl; are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
    • 式(I)化合物或其药学上可接受的盐,溶剂合物,酯或酰胺,其中R 1表示[CH 2 N] -R 2 ; R 2表示H,C 1-6烷氧基或Het; n表示选自0〜6的数; Het表示含有一个或多个选自O,N和S的杂原子的5或6个原子的不饱和杂环; R 3表示卤素; 环A表示含有一个或多个选自O,N和S的杂原子的4至7元饱和的,部分饱和的或不饱和的杂环; 环B表示含有一个或多个选自O,N和S的杂原子的3至8个原子的饱和,部分饱和或不饱和杂环,或环B表示3至8个原子的饱和或不饱和碳环; 环B任选地与芳环稠合并且任选地被一个或多个独立地选自R 4的基团取代; 环A和环B共享至少一个原子; R 4表示氧代,[CH 2 CH 2] m -R 5或CH-R 6 - [R 7 ; R 5表示H,OH,C 1-6烷氧基,COOH或CONR 8 R 9; m表示选自0或1的数字; 且R 6,R 7,R 8和R 9独立地表示H或C 1〜 6烷基; 可用于治疗指示V1a拮抗剂的疾病,特别是痛经。