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    • 2. 发明申请
      WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
    • AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    • AZ Y Y O O O O S S S S S S S S S S S S S S S S S S S S S S S S S S
    • WO2005080382A1
    • 2005-09-01
    • PCT/EP2005/001940
    • 2005-02-21
    • GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
    • ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
    • C07D403/12
    • C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
    • 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; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 5 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -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, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency or as antipsychotic agents.
    • 本发明涉及新的式（I）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为0〜5的整数; R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代 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; R5是选自以下的部分：异恶唑基，-CH 2 -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，任选地被一个或多个 选自以下的两个取代基：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; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。 治疗药物依赖或作为抗精神病药。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明申请
      WO2007113232A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
    • AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
    • AZABICYCLO [3。 作为DOPAMINE D3受体的调节剂的HEXYL衍生物
    • WO2007113232A1
    • 2007-10-11
    • PCT/EP2007/053074
    • 2007-03-30
    • Glaxo Group Limited , BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
    • BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
    • C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
    • C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
    • The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11 -membered heteroaryl bicyclic group; A is a group P1 or a group P2 Wherein p is an integer ranging from 0 to 5; R 1 is halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1- 4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 6 ; and when p is an integer ranging from 2 to 5, each R 1 may be the same or different; R 2 is hydrogen or C 1-4 alkyl; n is 3, 4, 5 or 6; R 6 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1 -dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R 6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1- 4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1- 4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4- alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl, haloC 1-4 alkoxy and SF 5 ; R 5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; R 7 is hydrogen or C 1-2 alkyl; R' is H, C 1-4 alkyl or C 1-4 alkanoyl; R" is defined as R'; R' and R" taken together with the interconnecting nitrogen atom may form a 5-, 6- membered saturated or unsaturated heterocyclic ring; wherein at least one of R 4 and R 5 is hydrogen; and wherein only one R 2 group may be different from hydrogen; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
    • 本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5-或6-元单环杂芳基或8-至11元杂芳基 双环基团 A是基团P1或基团P2，其中p是0至5的整数; R 1是卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷基， 烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R 6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R 2是氢或C 1-4烷基; n为3,4,5或6; R 6是选自以下的部分：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧代-2-异噻唑烷基，噻吩基，噻唑基， 吡啶基，2-吡咯烷酮基和这样的R 6 C 6基团任选地被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4 - >一
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明申请
      WO2006108701A1 3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
    • 3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
    • 3-（1,2,4-TRIAZOL-3YLALKYL）AZABRICLO（3.1.0）作为DOPAMINE D3受体的调节剂的HEXANE衍生物
    • WO2006108701A1
    • 2006-10-19
    • PCT/EP2006/003554
    • 2006-04-12
    • GLAXO GROUP LIMITED , BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
    • BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
    • C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/497 , A61P25/00 , C07D409/14
    • C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
    • The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5, or corresponds to a group R 5; " each R 2 is independently hydrogen, fluorine or C 1-4 alkyl; " n is 2, 3, 4, or 5; " R 3 is C 1-4 alkyl; " R 4 is hydrogen, or a C 1-4 alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ;or R 4 is a -SR 6 group; " R 5 is selected from a group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; " R 6 is C 1-4 alkyl or -CH 2 C 3-4 cycloalkyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
    • 本发明涉及新的式（I）化合物或其药学上可接受的盐：其中“G选自：苯基，吡啶基，苯并噻唑基和吲唑基”; p是0-5的整数; “R 1”独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基 ，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5， 或对应于基团R 5;每个R 2独立地是氢，氟或C 1-4烷基; “n为2,3,4或5;”R 3为C 1-4烷基; “R”4是氢或C 1-4烷基，苄基，苯基，杂环基，5或6元杂芳基 或8至11元双环基团，其中任何基团任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基， 烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷基， 烷酰基和SF 5;或R 4是-SR 6 C 6;选择“R 5” 由以下组成的组：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基和2-吡咯烷基，并且这种基团任选被取代 通过一个或两个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4 - 烷氧基和C 1-4烷酰基; “R 6”是C 1-4烷基或-CH 2 -SO 3 -S-环烷基;当R 相对于与分子的其余部分的连接键，R 1不在氯原子的邻位存在这样的R 1，并且当R 1 对应于R 5，p为1.它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D的调节剂 > 3受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      WO2007022933A1 TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
    • TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS
    • 作为DOPAMINE D3受体的调节剂的三唑衍生物
    • WO2007022933A1
    • 2007-03-01
    • PCT/EP2006/008200
    • 2006-08-18
    • GLAXO GROUP LIMITED , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
    • BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
    • C07D413/14 , C07D403/14 , A61K31/4196 , A61P25/18
    • C07D403/14 , C07D413/14
    • The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl or SF 5 ; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is S or -CH 2 -; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; R 5 is isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1- 4alkoxy and C 1-4 alkanoyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
    • 本发明涉及新的式（I）化合物或其盐：其中：G是5-或6-元杂芳族基团，或是含有一个或两个独立选择的杂原子的9或10元双环杂芳族基团 氮和氧，其中G不是吡啶基，吲唑基或苯并噻唑基; p为0〜4的整数。 R 1独立地选自：卤素，羟基，氰基，C 1-4 - 烷基，卤代C 1-4烷基， C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基或SF 5 N; 或对应于基团R 5; R 2是氢或C 1-4烷基; n为2或3; X是S或-CH 2 - ; R 3是C 1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被 1,2,3或4个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1 -4个烷氧基和C 1-4烷酰基; R 5是异恶唑基，-CH 2 N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中各基团 任选地被一个或两个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4 - 烷基，C 1 - 烷氧基和C 1-4烷酰基; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D 3受体的调节剂，例如。 治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO2009130231A1 PYRROLO [1, 2-A] PYRAZINE DERIVATIVES AS VASOPRESSIN VIB RECEPTOR ANTAGONISTS 审中-公开
    • PYRROLO [1, 2-A] PYRAZINE DERIVATIVES AS VASOPRESSIN VIB RECEPTOR ANTAGONISTS
    • PYRROLO [1,2-A]吡嗪衍生物作为VASOPRESSIN VIB受体拮抗剂
    • WO2009130231A1
    • 2009-10-29
    • PCT/EP2009/054777
    • 2009-04-22
    • GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
    • DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
    • C07D519/00 , C07D487/04 , A61K31/4985 , A61P25/22 , A61P25/24
    • C07D519/00 , C07D487/04
    • The present invention relates to novel compounds of formula (I) or salts thereof; wherein R is -X-[CH 2 ] n CR 4 R 5 -Y; or a group G; R 1 is H or C1 -C4 alkyl; R 2 is aryl, heteroaryl or C3-C7 cycloalkyl, which may be substituted with one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, - CN; R 3 is -CH 2 -C(=O)-NH-R 6 ; X is -CR 7 R 8 -, -O-, -NR 9 -, -S-; Y is-NR 10 R 11 R 4 is H or C1 -C4 alkyl; R 5 is H or C1 -C4 alkyl; R 6 is C1-C6 alkyl, C3-C6 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 7 is H or C1 -C4 alkyl; R 8 is H or C1 -C4 alkyl; R 9 is H or C1 -C4 alkyl; R 10 is H or C1-C4 alkyl, or together with R 11 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 12 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 11 is H or C1 -C4 alkyl; R 12 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; G is one of the groups selected from the list consisting of G1, G2, G3, G4, G5, G6, G7, G8, G9, G10, G11 and G12; R 13 is H or C1-C4 alkyl, or together with R 14 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 24 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 14 R 16 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 15 , R 17 correspond to H or C1-C4 alkyl and may assume different meanings; R 18 is H or C1-C4 alkyl, or together with R 17 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 25 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 19 , R 20 , R 21 , R 22 , R 23 , R 24 , R 25 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 26 , R 27 , R 28 , R 29 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; I, I' correspond to 1 or 2 and may assume different meanings; m, m', m", m"', m ιv , m v correspond to 0, 1 or 2 and may assume different meanings; n is 1, 2 or 3; q is 1, 2 or 3; p, p', p", p'" correspond to 0, 1, 2 or 3 and may assume different meanings; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as antagonists of V1b receptors, e.g. to treat depression and anxiety.
    • 本发明涉及新的式（I）化合物或其盐; 其中R是-X- [CH2] nCR4R5-Y; 或G组; R1是H或C1-C4烷基; R 2是可以被一个或多个取代基取代的芳基，杂芳基或C 3 -C 7环烷基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，-CN; R3是-CH2-C（= O）-NH-R6; X为-CR 7 R 8 - ， - O - ， - NR 9 - ， - S- Y是-NR 10 R 11 R 4是H或C 1 -C 4烷基; R5是H或C1-C4烷基; R6是C1-C6烷基，C3-C6环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R7是H或C1-C4烷基; R8是H或C1-C4烷基; R 9为H或C 1 -C 4烷基; R 10是H或C 1 -C 4烷基，或与R 11一起形成4-8个饱和或不饱和杂环，其可包含选自O，S和-NR 12的另外的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R 11是H或C 1 -C 4烷基; R 12是H，C 1 -C 6烷基，C 3 -C 7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; G是从由G1，G2，G3，G4，G5，G6，G7，G8，G9，G10，G11和G12组成的列表中选择的组之一; R 13是H或C 1 -C 4烷基，或与R 14一起形成4-8个饱和或不饱和的杂环，其可以包含另外的选自O，S和-NR 24的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R14R16是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R 15，R 17对应于H或C 1 -C 4烷基，并且可以具有不同的含义; R 18是H或C 1 -C 4烷基，或与R 17一起形成4-8个饱和或不饱和杂环，其可包含选自O，S和-NR 25的另外的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R19，R20，R21，R22，R23，R24，R25是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R26，R27，R28，R29是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; 我，我对应1或2，可能会有不同的含义; m，m'，m“，m”'，m？v，mv对应于0,1或2，可以具有不同的含义; n为1,2或3; q为1,2或3; p，p'，p“，p'”对应于0,1,2或3，可以具有不同的含义; 其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为V1b受体的拮抗剂，例如。 治疗抑郁症和焦虑症。
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