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132 条记录 (耗时 0.019 秒)

    Benzanilide derivatives as 5-HT1D antagonists
    93.
    发明公开
    Benzanilide derivatives as 5-HT1D antagonists 失效
    苯甲酰苯胺衍生物作为5-HT1D拮抗剂

    公开(公告)号：EP0533268A1

    公开(公告)日：1993-03-24

    申请号：EP92202806.3

    申请日：1992-09-14

    申请人： GLAXO GROUP LIMITED

    发明人： Oxford, Alexander William ,  Mitchell, William Leonard ,  Bradshaw, John ,  Clitherow, John Watson ,  Carter, Malcolm

    IPC分类号： C07D271/06 ,  A61K31/41 ,  C07D271/10 ,  C07D249/06 ,  C07D285/16 ,  C07D249/08 ,  C07D285/18 ,  C07D285/12

    CPC分类号： C07D249/08 ,  C07D249/06 ,  C07D271/06 ,  C07D271/07 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/12

    摘要： The invention provides compounds of the general formula (I) :-

    or a physiologically acceptable salt or solvate thereof
    wherein
    R¹ represents a hydrogen atom or a halogen atom or a group selected from C₁₋₆alkyl and C₁₋₆alkoxy;
    R² represents a phenyl group substituted by a group selected from

    and optionally further substituted by one or two substituents selected from halogen atoms, C₁₋₆alkoxy, hydroxy, and C₁₋₆alkyl;
    R³ represents the group

    R⁴ and R⁵, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C₁₋₆alkoxy and C₁₋₆alkyl;
    R⁶ represents a hydrogen atom or a group selected from -NR⁹R¹⁰ and a C₁₋₆alkyl group optionally substituted by one or two substituents selected from C₁₋₆alkoxy, hydroxy, C₁₋₆acyloxy and -SO₂R¹¹;
    R⁷, R⁸ and R⁹, which may be the same or different, each independently represent a hydrogen atom or a C₁₋₆alkyl group;
    R¹⁰ represents a hydrogen atom or a group selected from C₁₋₆alkyl, C₁₋₆acyl, benzoyl and -SO₂R¹¹;
    R¹¹ represents a C₁₋₆alkyl group or a phenyl group;
    Z represents an oxygen atom or a group selected from NR⁸ and S(O) k ; and
    k represents zero, 1 or 2.
    The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

    摘要翻译： 本发明提供了通式（I）的化合物： - 或其生理学上可接受的盐或溶剂合物，其中R 1代表氢原子或卤素原子或选自C 1-6烷基和C 1-6烷氧基的基团; R 2代表被选自以下基团的基团取代的苯基，并且任选进一步被一个或两个选自卤素原子，C 1-6烷氧基，羟基和C 1-6烷基的取代基取代; R 3代表基团R 4和R 5可以相同或不同，各自独立地代表氢原子或卤原子或选自羟基，C 1-6烷氧基和C 1-6烷基的基团; R 6代表氢原子或选自-NR 9 R 10和任选被一个或两个选自C 1-6烷氧基，羟基，C 1-6酰氧基和-SO 2 R 11的取代基取代的C 1-6烷基; R 7，R 7和R 7可以相同或不同，各自独立地代表氢原子或C 1-6烷基; R 10代表氢原子或选自C 1-6烷基，C 1-6酰基，苯甲酰基和-SO 2 R 11的基团; R 11代表C 1-6烷基或苯基; Z表示氧原子或选自NR 8和S（O）k的基团; k表示0,1或2.化合物可用于治疗或预防抑郁症和其他CNS病症。

    Thiadiazinone compounds, process for their preparation, and pharmaceutical compositions containing them
    96.
    发明公开
    Thiadiazinone compounds, process for their preparation, and pharmaceutical compositions containing them 失效
    噻二嗪酮化合物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0145236A2

    公开(公告)日：1985-06-19

    申请号：EP84307553.2

    申请日：1984-11-01

    申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED

    发明人： Coates, William John

    IPC分类号： C07D285/16 ,  A61K31/54

    CPC分类号： C07D285/16 ,  C07C45/63 ,  C07C49/697 ,  C07C65/36 ,  C07C205/45 ,  C07C255/00

    摘要： Compounds of the formula (I):-
    and salts thereof, wherein R' is hydrogen, C 1-6 alkyl, halo, cyano, nitro, amino, a group -NHCOR 4 , a group -COR 5 , or a group -NHC(NCN)NHR 6 ; wherein R 4 is hydrogen, C 1-6 alkoxy, C 1-6 alkyl optionally substituted by phenyl, or R 4 is a group NR 7 R 8 wherein R 7 and R 8 are independently hydrogen, C 1-6 salkyl or benzyl; R 5 is hydroxy, hydrogen, C 1-6 alkyl, C 1-6 alkoxy, or a group -NR 7 R 8 ; and R 6 is hydrogen or C 1-6 alkyl; R 2 is hydrogen or C 1-4 alkyl; R 3 is hydrogen or C 1-4 alkyl; and n is one, and when R 3 is hydrogen n can also be two.
    Processes and intermediates for their preparation are described. Pharmaceutical compositions containing them are described, as is their use as inotropic agents.

    摘要翻译： 式（I）的化合物： - ... ...及其盐，worin - [R <1>是氢，C 1-6烷基，卤素，氰基，硝基，氨基，一组-NHCOR <4>，基团 - COR <5>，或基团-NHC（NCN）NHR <6>; worinř<4>为氢C 1-6烷氧基，C 1-6烷基，其任选由substituiertem苯基，或R <4>是基团NR <7> - [R <8> worin - [R <7>和R <8>独立地是氢， C 1-6烷基或苄基; [R <5>是羟基，氢，C 1-6烷基，C 1-6烷氧基，或基团-NR <7> - [R <8>; 且R <6>是氢或C 1-6烷基; [R <2>是氢或C 1-4烷基; [R <3>是氢或C 1-4烷基; 和n是1，和当R <3>是氢，n可以因此是两个。 ... 的方法和中间体及其制备描述。 含有它们的药物组合物描述，因为是他们的正性肌力药物使用。