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36 条记录 (耗时 0.02 秒)

    1,2,4-Triazole derivatives, processes for their production and pharmaceutical compositions containing them
    7.
    发明公开
    1,2,4-Triazole derivatives, processes for their production and pharmaceutical compositions containing them 失效
    1,2,4-三唑衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0016565A1

    公开(公告)日：1980-10-01

    申请号：EP80300617.0

    申请日：1980-02-29

    申请人： GLAXO GROUP LIMITED

    发明人： Clitherow, John Watson ,  Bradshaw, John ,  Price, Barry John ,  Martin-Schmith, Michael ,  Mackinnon, John Wilson Macfarlane ,  Judd, Duncan Bruce ,  Hayes, Roger ,  Carey, Linda

    IPC分类号： C07D249/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/41

    CPC分类号： C07D295/096 ,  C07D249/14 ,  C07D307/52 ,  C07D317/22 ,  C07D333/36

    摘要： The invention relates to compounds of the general formula (I)
    and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

    R 1 and R 2 , which may be the same of different, each represent hydrogen, C 1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino dialkylamino or cycloalkyl or R, and R 2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C 1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur;
    Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,
    Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2-and 5- positions, the furan ring optionally bearing a further substituent R 6 adjacent to the group R 1 R 2 N-Alk, or Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 - and 3- or 1 - and 4. positions;
    R 4 represents halogen or C 1-4 alkyl which may be substi. tuted by hydroxy or C 1-4 alkoxy; X represents -CH 2 -, -0-, -S- or

    where R 5 represents hydrogen or methyl;
    n represents zero, 1 or 2;
    M represents 2, 3 or 4;
    R represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl with at least two carbon atoms, alkoxyalkyl, or aryl, and
    R 4 represents hydrogen, alkyl, alkenyl, aryl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy, alkoxy, alkylthio or halogen or the group NR 7 R 8 where
    R 7 represents hydrogen, alkyl, alkenyl or aralkyl or
    R 6 represents the group COR 9 where R 9 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroarylalkyl or R 4 represents the group SO 2 R 10 where R 10 represents alkyl or aryl, or R 8 represents the group
    where Y is oxygen or sulphur and R 11 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl.

    The compounds of formula (I) show pharmacological activity as selective histamine H 2 - antagonists.

    摘要翻译： 本发明涉及（I）及其生理学上可接受的盐，它们的水合物在生物前体其中R1和R2的通式的化合物和，烷基，其可以是相同或不同的，各自代表氢，C 1-10烷基，环烷基， 链烯基，炔基，芳烷基，三氟烷基，或由羟基，烷氧基，氨基，烷基二烷基氨基或环烷基或R 1和R 2可以与氮原子一起与它们所连接形成5至10元环，该环可以是饱和的或烷基substituiertem可 含有至少一个双键，可以是unsubstituiertem或可以被一个或多个C 1-3烷基基团或羟基和/或substituiertem可以含有另一杂原子的所有其为氧或硫; ALK darstellt 1的直链或支链亚烷基至6个碳原子，Q darstellt在其中掺入呋喃或噻吩环到分子的其余部分是通过结合在2-和5-位，呋喃环轴承任选地另外的 取代基R6毗邻组R1R2N-ALK或Q darstellt在其中掺入苯环成的其余部分

    Benzanilide derivatives as 5-HT1D antagonists
    8.
    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：EP0533267A1

    公开(公告)日：1993-03-24

    申请号：EP92202805.5

    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

    IPC分类号： C07D213/56 ,  A61K31/50

    CPC分类号： C07D213/56

    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, a halogen atom or a group selected from C₁₋₆alkyl and C₁₋₆alkoxy;
    R² represents a pyridinyl group optionally substituted by one or two substituents selected from halogen atoms, C₁₋₆alkyl, hydroxyC₁₋₆alkyl, C₁₋₆alkoxyC₁₋₆alkyl, C₁₋₆alkoxy, hydroxy, -CN, -NO₂, -CO₂R⁶, -COR⁶, -CONR⁶R⁷ and -(CH₂) m OC(O)C₁₋₄alkyl;
    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, R⁷ and R⁸, which may be the same or different, each independently represent a hydrogen atom or a C₁₋₆alkyl group; and
    m represents zero or an integer from 1 to 3.
    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，卤原子或选自C 1-6烷基和C 1-6烷氧基的基团; R 2代表任选被一个或两个选自卤素原子，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，羟基，-CN，-NO 2，-CO 2 R 8，-COR 6， - CONR 8 R 9和 - （CH 2）mOC（O）C 1-4烷基; 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 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; 并且m表示0或1至3的整数。所述化合物可用于治疗或预防抑郁症和其他CNS病症。

    Benzanilide derivatives as 5-HT1D antagonists
    9.
    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：EP0533266A1

    公开(公告)日：1993-03-24

    申请号：EP92202804.8

    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 ,  Baxter, Ian Campbell

    IPC分类号： C07D295/135 ,  A61K31/50 ,  C07D295/155 ,  C07D295/192

    CPC分类号： C07D295/192 ,  C07D295/135 ,  C07D295/155

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

    or a physiologically acceptable salt or solvate thereof wherein
    R¹ represents a halogen or hydrogen atom or a C₁₋₆alkyl or C₁₋₆alkoxy group;
    R² represents a phenyl group optionally substituted by one or two substituents;
    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 or C₁₋₆alkyl.
    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代表卤素或氢原子或C 1-6烷基或C 1-6烷氧基; R 2表示任选被一个或两个取代基取代的苯基; R 3代表基团R 4和R 5，它们可以相同或不同，各自独立地代表氢原子或卤原子，或选自羟基，C 1-6烷氧基或C 1-6烷基的基团。 该化合物可用于治疗或预防抑郁症和其他CNS疾病。