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7 条记录 (耗时 0.011 秒)

    HETERO-BICYCLIC CRF ANTAGONISTS
    1.
    发明授权
    HETERO-BICYCLIC CRF ANTAGONISTS 有权
    杂双环CRF拮抗剂

    公开(公告)号：EP1425280B1

    公开(公告)日：2006-08-30

    申请号：EP02764696.7

    申请日：2002-07-15

    申请人： GLAXO GROUP LIMITED

    发明人： DI FABIO, Romano, GlaxoSmithKline SpA ,  MICHELI, Fabrizio, GlaxoSmithKline SpA ,  ST-DENIS, Yves, GlaxoSmithKline SpA

    IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P25/22

    CPC分类号： C07D471/04

    摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, wherein R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R5, nitro, -NR6R7, cyano, and a group R8; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR6R7 or cyano; R2 is hydrogen, C3-C7 cycloalkyl, or a group R9; R3 is C3-C7 cycloalkyl, or a group R9; or R2 and R3 together with N form a 5-14 membered heterocycle, which may be substituted 1 to 3 R10 groups; R4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R5 is a C1-C4 alkyl, -OR6 or NR6R7; R6 is hydrogen or C1-C6 alkyl; R7 is hydrogen or C1-C6 alkyl; R8 is a 5-6 membered heterocycle, which may be saturated or may contain one to three double bonds, and which may be substituted by 1 or more R11 groups; R9 is a C1-C6 alkyl that may be substituted by one or more groups selected from: C3-C7 cycloalkyl, C1-C6 alkoxy, halo C1-C6 alkoxy, hydroxy, halo C1-C6 alkyl; R10 is a group R8, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, C(O)NR6R7, phenyl which may be substituted by 1 to 4 R11 groups; R11 is C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, hydroxy, halogen, nitro, cyano, or C(O)NR6R7; X is carbon or nitrogen; n is 1 or 2; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    CRF RECEPTOR ANTAGONISTS
    2.
    发明授权
    CRF RECEPTOR ANTAGONISTS 有权
    CRF受体拮抗剂

    公开(公告)号：EP1383498B1

    公开(公告)日：2006-03-15

    申请号：EP02718405.0

    申请日：2002-04-30

    申请人： GLAXO GROUP LIMITED

    发明人： DI FABIO, Romano, GlaxoSmithKline SpA ,  MICHELI, Fabrizio, GlaxoSmithKline SpA ,  PASQUARELLO, Alessandra, GlaxoSmithKline SpA ,  ST-DENIS, Yves, GlaxoSmithKline SpA

    IPC分类号： A61K31/4353 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/519 ,  C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  A61P29/00

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereofwherein R is aryl or heteroaryl, wherein each of the above groups R may be substituted by 1 to 4 substituents indendently selected from the group consisting of:halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R4; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, NH2, halogen or cyano; R2 is hydrogen or C(H)n(R5)q(CH2)pZR6; R3 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or [CH(R5)(CH2)p]mZR6; R4 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R4 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 mon a or dialkylamino, nitro, and cyano; R5 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or (CH2)pZR6; R6 is C1-C6 alkyl, which may be substituted by one or more groups selected from halogen, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 alkoxy, C1-C6 mono or dialkylamino, nitro, cyano and a group R4; Y and X are independently carbon or nitrogen; m and n are independently 0 or 1; p is 0 or an integer from 1 to 4;q is 1 or 2;Z is a bond, O, NH or S;to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).

    NOVEL COMPOUNDS
    3.
    发明公开
    NOVEL COMPOUNDS 有权
    新化合物

    公开(公告)号：EP1891056A1

    公开(公告)日：2008-02-27

    申请号：EP06743164.3

    申请日：2006-06-13

    申请人： GLAXO GROUP LIMITED

    发明人： ARISTA, Luca, GlaxoSmithKline SpA ,  BONANOMI, Giorgio, GlaxoSmithKline SpA ,  HAMPRECHT, Dieter, GlaxoSmithKline SpA ,  MICHELI, Fabrizio, GlaxoSmithKline SpA

    IPC分类号： C07D403/12 ,  A61K31/41 ,  A61P25/00

    CPC分类号： C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, halo C1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, C1-4alkyl or C1-6 cycloalkyl optionally substituted by 1or 2 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, C1-4alkanoyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, or as antipsychotic agents, or to treat obsessive compulsive spectrum disorders or premature ejaculation.

    摘要翻译： 本发明涉及式（I）的新化合物或其药学上可接受的盐，其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p是0-5的整数; R1独立地选自卤素，羟基，氰基，C1-4烷基，卤代C1-4烷基，C1-4烷氧基，卤代C1-4烷氧基，C1-4烷酰基和SF5; 或对应于组R5; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢，任选被1或2个选自卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基的取代基取代的C 1-4烷基或C 1-6环烷基; R5是选自下组的部分：异恶唑基，-CH2-N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基，并且这样的基团任选被一个或 两个选自卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基的取代基; 它们的制备方法，用于这些方法的中间体，含有它们的药物组合物以及它们在治疗中的用途，作为多巴胺D3受体的调节剂，例如多巴胺D3受体。 治疗药物依赖，或作为抗精神病药，或治疗强迫性强迫性光谱障碍或早泄。

    NOVEL COMPOUNDS
    5.
    发明授权
    NOVEL COMPOUNDS 有权

    公开(公告)号：EP1891056B1

    公开(公告)日：2010-10-13

    申请号：EP06743164.3

    申请日：2006-06-13

    申请人： GLAXO GROUP LIMITED

    发明人： ARISTA, Luca, GlaxoSmithKline SpA ,  BONANOMI, Giorgio, GlaxoSmithKline SpA ,  HAMPRECHT, Dieter, GlaxoSmithKline SpA ,  MICHELI, Fabrizio, GlaxoSmithKline SpA

    IPC分类号： C07D403/12 ,  A61K31/41 ,  A61P25/00

    CPC分类号： C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, halo C1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, C1-4alkyl or C1-6 cycloalkyl optionally substituted by 1or 2 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, halo C1-4alkyl, C1-4alkoxy, C1-4alkanoyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, or as antipsychotic agents, or to treat obsessive compulsive spectrum disorders or premature ejaculation.