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1. 发明申请

WO2009130231A1 PYRROLO [1, 2-A] PYRAZINE DERIVATIVES AS VASOPRESSIN VIB RECEPTOR ANTAGONISTS 审中-公开
标题翻译： PYRROLO [1,2-A]吡嗪衍生物作为VASOPRESSIN VIB受体拮抗剂
公开(公告)号：WO2009130231A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054777
申请日：2009-04-22
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
发明人： DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
IPC分类号： C07D519/00 , C07D487/04 , A61K31/4985 , A61P25/22 , A61P25/24
CPC分类号： C07D519/00 , C07D487/04
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2007125061A1 SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂的螺旋体有用
公开(公告)号：WO2007125061A1
公开(公告)日：2007-11-08
申请号：PCT/EP2007/054003
申请日：2007-04-24
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TARSI, Luca , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/506 , A61P25/18
CPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： The present invention relates to compounds of formula (I) or salts thereof wherein A, X and R 4 are defined herein, 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 to enhance cognition.
摘要翻译：本发明涉及式（I）化合物或其盐，其中A，X和R 4在本文中定义，其制备方法，用于这些方法的中间体，含有它们的药物组合物及其用途在治疗中，作为多巴胺D 3受体的调节剂，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或增强认知。

3. 发明申请

WO2007113232A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113232A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053074
申请日：2007-03-30
申请人： 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
发明人： BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： 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.
摘要翻译：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

4. 发明申请

WO2007113260A1 AZABICYCLO [3. 1. O] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2007113260A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053117
申请日：2007-03-30
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TERRENI, Silvia
发明人： BERTANI, Barbara , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D405/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D405/14
摘要： The present invention relates to novel compounds or pharmaceutically acceptable saltsthereof: 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 P wherein P is p is an integer ranging from 0 to 5; Rl, R2, R3, R4,R5 and R7 are as defined in the claims, 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, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新化合物或其药学上可接受的盐衍生物：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; A为基团P，其中P为p为0至5的整数; R 1，R 2，R 3，R 4，R 5和R 7如权利要求书中所定义，其制备方法，在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。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

5. 发明申请

WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： 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
公开(公告)号：WO2005080382A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001940
申请日：2005-02-21
申请人： 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
发明人： ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
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; 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.
摘要翻译：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。

6. 发明申请

WO2007022933A1 TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂的三唑衍生物
公开(公告)号：WO2007022933A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008200
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D413/14 , C07D403/14 , A61K31/4196 , A61P25/18
CPC分类号： C07D403/14 , C07D413/14
摘要： 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.
摘要翻译：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。

7. 发明申请

WO2005118549A2 COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF 审中-公开
标题翻译：具有DOPAMINE D3受体的亲和性的化合物及其用途
公开(公告)号：WO2005118549A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/005965
申请日：2005-05-31
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D223/16
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) and salts thereof are disclosed: wherein A, R 1 , m, R 2 , n, R 3 , R 4 , q, W 1 , W 2 , R 5 and R 6 are as defined in the description. Methods of preparing the compounds and uses thereof in medicine, for example in the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物及其盐：其中A，R1，m，R2，n，R3，R4，q，W1，W2，R5和R6如说明书中所定义。还公开了制备化合物的方法及其在医药中的用途，例如治疗精神分裂症或药物依赖性。

8. 发明申请

WO2002100863A1 CORTICOTROPIN RELEASING FACTOR ANTAGONISTS 审中-公开
标题翻译： CORTICOTROPIN释放因子拮抗剂
公开(公告)号：WO2002100863A1
公开(公告)日：2002-12-19
申请号：PCT/GB2002/002656
申请日：2002-06-11
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
发明人： DI FABIO, Romano , MARCHIONNI, Chiara , MICHELI, Fabrizio , PASQUARELLO, Alessandra , PERINI, Benedetta , ST-DENIS, Yves
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , 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 and each of the above groups R 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, -COR 4 , nitro, -NR 3 R 4 cyano, or a group R 5 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 3 R 4 or cyano; R 2 corresponds to a group CHR 6 R 7 ; R 3 is hydrogen, C1-C6 alkyl; R 4 independently from R 3 , has the same meanings; R 5 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 R 5 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 dialkylamino, nitro or cyano; R 6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R 6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R 7 independently from R 6 , has the same meanings; X is carbon or nitrogen; 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).
摘要翻译：本发明提供式（I）化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素， C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自：C 1 -C 6烷氧基和羟基的基团取代; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

9. 发明申请

WO2002087573A1 CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CRF受体拮抗剂
公开(公告)号：WO2002087573A1
公开(公告)日：2002-11-07
申请号：PCT/GB2002/001981
申请日：2002-04-30
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , ST-DENIS, Yves
IPC分类号： A61K31/4353
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 R 4 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, NH 2 , halogen or cyano; R 2 is hydrogen or C(H) n (R 5 ) q (CH 2 ) p ZR 6 ; R 3 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or [CH(R 5 )(CH 2 ) p ] m ZR 6 ; R 4 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 R 4 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; R 5 is hydrogen, C2-C6 alkenyl, C2-C6 alkynyl or (CH 2 ) p ZR 6 ; R 6 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 R 4 ; 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).
摘要翻译：本发明涉及式（I）的三环嘧啶化合物，包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其中R是芳基或杂芳基，其中上述基团R中的每一个可以被1至4个取代基所取代，由以下组成：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，C 1 -C 6单或二烷基氨基，硝基，氰基和 R4; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，NH 2，卤素或氰基; R2是氢或C（H）n（R5）q（CH2）pZR6; R3是氢，C2-C6烯基，C2-C6炔基或[CH（R5）（CH2）p] mZR6; R4是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 4可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C 1 -C 6单烷基或二烷基氨基，硝基和氰基; R5是氢，C2-C6烯基，C2-C6炔基或（CH2）pZR6; R6是C1-C6烷基，其可以被一个或多个选自卤素，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基，C 1 -C 6 单或二烷基氨基，硝基，氰基和基团R 4; Y和X独立地为碳或氮; m和n独立地为0或1; p为0或1至4的整数; q为1或2; Z为O，NH或S键;其制备方法为含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）。

10. 发明申请

WO2009109608A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2009109608A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052567
申请日：2009-03-05
申请人： GLAXO GROUP LIMITED , BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04 , A61K31/435 , A61P25/00
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04
摘要： The invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及式（I）化合物，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5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE）再吸收抑制剂。

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