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1. 发明申请

WO1993005025A1 C-LINKED PYRAZOLE DERIVATIVES 审中-公开
标题翻译： C连接的吡唑衍生物
公开(公告)号：WO1993005025A1
公开(公告)日：1993-03-18
申请号：PCT/GB1991001521
申请日：1991-09-06
申请人： GLAXO GROUP LIMITED
发明人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , MIDDLEMISS, David , ELDRED, Colin, David , MONTANA, John, Gary , SHAH, Pritom
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07C45/455 , C07C49/175 , C07C49/255 , C07C205/45 , C07D231/14 , C07D403/10
摘要： The invention provides compounds of general formula (I) or a plysiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof in which R represents a hydrogen atom or a group selected from C1-6alkyl or C2-6alkenyl; R represents a hydrogen atom or a group selected from C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, C3-6alkenyl, fluoroC1-6alkyl, fluoroC3-6alkenyl, phenyl, -(CH2)kCOR or -(CH2)kSO2R ; R represents a hydrogen atom or a group selected from C1-6alkyl optionally substituted by a hydroxy or C1-6alkoxy group, C2-6alkenyl, fluoroC1-6alkyl, -(CH2)mR , -(CH2)nCOR or -(CH2)pNR COR ; R represents a group selected from -CO2H, -NHSO2CF3 or a C-linked tetrazolyl group; R represents a group selected grom C1-6alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR R ; R represents a phenoxy or benzyloxy group; R represents a hydrogen atom or a group selected from hydroxy, C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR R ; R represents a hydrogen atom or a C1-6alkyl group; R represents a hydrogen atom or a group selected from C1-6alkyl, C1-6alkoxy, phenyl, benzyl, phenoxy or the group -NR R ; R and R which may be the same or different each independently represent a hydrogen atom or a C1-4alkyl group or -NR R forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; k represents zero or an integer from 1 to 4; m represents an integer from 1 to 4; n represents zero or an integer from 1 to 4; and p represents an integer from 1 to 4. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译：本发明提供了通式（I）的化合物或其衍生物可接受的盐，溶剂合物（例如水合物）或其代谢不稳定的酯，其中R 1表示氢原子或选自C 1-6烷基或C 2-6烯基的基团; R 2表示氢原子或选自C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，C 3-6烯基，氟C 1-6烷基，氟C 3-6烯基，苯基， - （CH 2）k COR 5或 - （CH2）kSO2R <5>; R 3表示氢原子或选自任选被羟基或C 1-6烷氧基取代的C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 6， - （CH 2）n COOR 7>或 - （CH 2）p NR R 8 COR 9; R 4表示选自-CO 2 H，-NHSO 2 CF 3或C连接的四唑基的基团; R 5表示选自C 1-6烷基，C 2-6烯基，C 1-6烷氧基或基团-NR 10 R 11的基团。 R 6表示苯氧基或苄氧基; R 7表示氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 10 R 11的基团。 R 8表示氢原子或C 1-6烷基; R 9表示氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苄基，苯氧基或基团-NR 10 R 11的基团。 R 10和R 11可以相同或不同，各自独立地表示氢原子或C 1-4烷基，或-NR 10 R 11形成饱和杂环，其具有5或6个环成员并且可以任选地在环中含有一个氧原子; k表示0或1至4的整数; m表示1〜4的整数， n表示0或1至4的整数; 并且p表示1至4的整数。该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

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