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1. 发明申请

WO2011069951A1 IMIDAZOLIDINEDIONE DERIVATIVES 审中-公开
标题翻译：咪唑啉衍生物
公开(公告)号：WO2011069951A1
公开(公告)日：2011-06-16
申请号：PCT/EP2010/068946
申请日：2010-12-06
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DECOR, Anne , FONTANA, Stefano , HAMPRECHT, Dieter , LARGE, Charles , MARASCO, Agostino
发明人： ALVARO, Giuseppe , DECOR, Anne , FONTANA, Stefano , HAMPRECHT, Dieter , LARGE, Charles , MARASCO, Agostino
IPC分类号： C07D233/76 , C07D401/04 , C07D403/04 , A61K31/4166 , A61P25/18
CPC分类号： A61K31/506 , A61K31/4166 , A61K31/4439 , C07D213/643 , C07D233/72 , C07D233/76 , C07D239/22 , C07D239/47 , C07D401/04 , C07D403/04
摘要： The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.
摘要翻译：本发明提供式（Ia）化合物及其药学上可接受的盐。本发明还提供了化合物或盐作为Kv3.1和/或Kv3.2的调节剂的用途，以及用于治疗需要Kv3.1和/或Kv3.2调节剂的疾病或病症，例如抑郁症情绪障碍，听觉障碍，分裂症，药物滥用障碍，睡眠障碍或癫痫。

2. 发明申请

WO2012168710A1 HYDANTOIN DERIVATES AS KV3 INHIBITORS 审中-公开
标题翻译： HYDANTOIN衍生物作为KV3抑制剂
公开(公告)号：WO2012168710A1
公开(公告)日：2012-12-13
申请号：PCT/GB2012/051278
申请日：2012-06-07
申请人： AUTIFONY THERAPEUTICS LIMITED , ALVARO, Giuseppe , DECOR, Anne , HAMPRECHT, Dieter , MARASCO, Agostino
发明人： ALVARO, Giuseppe , DECOR, Anne , HAMPRECHT, Dieter , MARASCO, Agostino
IPC分类号： C07D405/14 , C07D401/04 , C07D403/04 , C07D405/12 , C07D307/87 , C07D307/94 , C07D311/76 , A61K31/506 , A61K31/4439 , A61K31/4166 , A61P25/00
CPC分类号： C07D307/93 , C07D307/87 , C07D307/94 , C07D311/76 , C07D401/04 , C07D403/04 , C07D405/12 , C07D405/14
摘要： The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
摘要翻译：本发明提供式（I）化合物：所述化合物是Kv3通道的抑制剂，并且用于预防或治疗相关病症。

3. 发明申请

WO2006133945A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006133945A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005767
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ARISTA, Luca , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio
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; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, halo C 1-4 alkyl, C 1-4 alkoxy, halo C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; 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, C 1-4 alkyl or C 1-6 cycloalkyl optionally substituted by 1or 2 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, halo C 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, halo C 1-4 alkyl, C 1-4 alkoxy, 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 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，卤素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; R 2是氢或C 1-4烷基; R 3是C 1-4烷基; R 4是氢，任选被1或2个选自以下的取代基取代的C 1-4 - 烷基或C 1-6 - 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; R 5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，并且这样的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 1-4烷氧基，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。治疗药物依赖性，或作为抗精神病药物，或治疗强迫性强迫性疾病或早泄。

4. 发明申请

WO2006108700A1 3-TRIAZOLYLTHIOALKYL-3-AZABICYCLO (3 - 1 - O) HEXANES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS 审中-公开
标题翻译： 3-三唑基三唑-3-基亚氨基（3 - 1 - O）HEXANES及其作为DOPAMINE D3受体配体使用
公开(公告)号：WO2006108700A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003553
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ANDREOTTI, Daniele , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio
IPC分类号： C07D403/12 , C07D413/12 , A61K31/4196 , A61K31/422 , A61P25/00
CPC分类号： C07D413/12 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein • R 1 is hydrogen or C 1-4 alkyl; • R 2 is C 1-4 alkyl; • R 3 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 and SF 5 ; • p is 0, 1 , 2, 3 or 4; and • R 4 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 and C 1-4 alkanoyl; • n is 0 or 1 ; wherein when R 4 is chlorine and p is 1 , such R 4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R 3 comprises at least one SF 5 group as a substituent; 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.
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R 1是氢或C 1-4烷基; R 2是C 1-4烷基; R 3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，C 1-4烷酰基和SF 5; p是0，1，2，3或4; R 4和R 4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烷氧基和C 1-4烷酰基; n为0或1; 其中当R 4为氯且p为1时，相对于与分子的其余部分的连接键，该R 4不在邻位; 并且其中，如果n是0，则R 3 3包含至少一个SF 5基团作为取代基; 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。

5. 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
标题翻译： 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
公开(公告)号：WO2006108701A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003554
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： 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
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： 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.
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。}

6. 发明申请

WO2006002928A1 COMPOUNDS HAVING AFFINITY FOR THE DOPAMINE D3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：多巴胺D3受体具有重要性的化合物及其在医药中的应用
公开(公告)号：WO2006002928A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/007069
申请日：2005-06-29
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
发明人： BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
IPC分类号： C07D498/04
CPC分类号： C07D513/04
摘要： Compounds of formula (I) or a salt thereof are disclosed, wherein A, m R 1 , R 2 , R 3 , q, W 1 , W 2 , R 4 and R 5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物或其盐，其中A，m R 1，R 2，R 3，q，W W 1，W 2，R 4和R 5如说明书中所定义。还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

7. 发明申请

WO2005087764A1 TETRAHYDROBENZAZEPINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS (ANTIPSYCHOTIC AGENTS) 审中-公开
标题翻译：作为DOPAMINE D3受体（抗生素代谢物）的调节剂的四氢苯并噻吩衍生物
公开(公告)号：WO2005087764A1
公开(公告)日：2005-09-22
申请号：PCT/EP2005/002635
申请日：2005-03-04
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
发明人： ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
IPC分类号： C07D413/14
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, 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. as agents to treat various aspects 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，例如，作为治疗各方面药物依赖的药剂或作为抗精神病药。

8. 发明申请

WO2004089897A1 COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF 审中-公开
标题翻译：在5HT2C受体上具有活性的化合物及其用途
公开(公告)号：WO2004089897A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003678
申请日：2004-04-05
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio , TERRENI, Silvia
发明人： BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio , TERRENI, Silvia
IPC分类号： C07D209/46
CPC分类号： C07D209/46
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1 6alkylthio, hydroxy, amino, mono or di C1 6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, -COOR3, -COR4 (wherein R3 and R4, are independently hydrogen or C1-6alkyl) or -COR5 (wherein R5 is amino, mono or di C1 6alkylamino or an N-linked 4 to 7 membered heterocyclic group); p is 0, 1 or 2 or 3; Q is a 6- membered aromatic group or a 6-membered heteroaromatic group; A is -(CH2-CH2)-, -(CH=CH)-, or a group -(CHR7)- wherein R7 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1 6alkylthio; R2 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1 6alkylthio, amino, mono or di C1 6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is oxygen, sulfur, -CH2- or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, -CH2-, -(CH2)2- or -CH=CH-; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is -NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, such as for depression or anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中R 1是卤素，氰基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基，C 1-6烷硫基，羟基，氨基，单或二C 1-6烷基氨基， N-连接的4至7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，-COOR 3，-COR 4（其中R 3和R 4独立地为氢或C 1-6烷基）或-COR 5（其中R 5为氨基，单或二C 1-6烷基氨基或N-连接的4至7元杂环基）; p为0,1或2或3; Q是6-元芳基或6元杂芳基; A是 - （CH 2 -CH 2） - ， - （CH = CH） - 或 - （CHR 7） - ，其中R 7是氢，卤素，羟基，氰基，硝基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基或C 1-6烷硫基; R2是氢，卤素，羟基，氰基，硝基，C1-6烷基，C1-6烷酰基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二C 1-6烷基氨基或N-连接的4至7元杂环基; X是氧，硫，-CH 2 - 或NR 8，其中R 8是氢或C 1-6烷基; Y是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; Z为任选取代的N-连接的杂环基或含有至少一个氮的C连接的4至7元杂环基，或Z为-NR 9 R 10，其中R 9和R 10独立地为氢或C 1-6烷基。还公开了其在治疗中的制备方法及其用途，例如抑郁症或焦虑症。

9. 发明申请

WO2004078718A1 COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF 审中-公开
标题翻译：在5HT2C受体上具有活性的化合物及其用途
公开(公告)号：WO2004078718A1
公开(公告)日：2004-09-16
申请号：PCT/EP2004/001843
申请日：2004-02-24
申请人： GLAXO GROUP LIMITED , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
发明人： DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein R 1 is hydrogen, fluoro, chloro, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy or haloC 1-6 alkoxy; m is 0 when ==== is a double bond and m is 1 when ==== is a single bond; R 2 is hydrogen, halogen, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is -(CH 2 -CH 2 )-, -(CH=CH)-, -(CH 2 ) 3 -, -C(CH 3 ) 2 -, -(CH=CH-CH 2 )-, -(CH 2 -CH=CH)- or a group -(CHR 5 )- wherein R 5 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy or C 1-6 alkylthio; R 3 is halogen, cyano, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy, C 1-6 alkylthio, hydroxy, amino, mono- or di-C 1-6 alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC 1-6 alkyl, haloC 1-6 alkoxy, aryl, arylC 1-6 alkyl, arylC 1-6 alkyloxy, arylC 1-6 alkylthio or COOR 6 , CONR 7 R 8 or COR 9 wherein R 6 , R 7 , R 8 and R 9 are independently hydrogen or C 1-6 alkyl; p is 0, 1 or 2 or 3; R 4 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 1-6 alkanoyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, -CH 2 - or NR 10 wherein R 10 is hydrogen or C 1-6 alkyl; D is a single bond, -CH 2 -, -(CH 2 ) 2 - or -CH=CH-; and Z is -NR 11 R 12 where R 11 and R 12 are independently hydrogen or C 1-6 alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐，其中R 1是氢，氟，氯，羟基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基或卤代C 1-6烷氧基; 当====为双键时，m为0，当==为单键时，m为1; R2是氢，卤素，氰基，硝基，C1-6烷基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二C 1-6烷基氨基或 N-连接的4至7元杂环基; X是 - （CH 2 -CH 2） - ， - （CH = CH） - ， - （CH 2）3 - ， - C（CH 3）2 - ， - （CH = CH-CH 2） - ， - （CH 2 -CH = CH ） - 或基 - （CHR 5） - ，其中R 5是氢，卤素，羟基，氰基，硝基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基或C 1-6烷硫基 ; R 3是卤素，氰基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基，C 1-6烷硫基，羟基，氨基，单 - 或二-C 1-6烷基氨基，N-连接的4-7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，芳基C 1-6烷基，芳基C 1-6烷氧基，芳基C 1-6烷硫基或COOR 6，CONR 7 R 8或COR 9，其中R 6，R 7，R 8和R 9独立地为氢或C 1-6烷基; p为0,1或2或3; R4是氢，卤素，羟基，氰基，硝基，C1-6烷基，C1-6烷酰基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二 C 1-6烷基氨基或N-连接的4至7元杂环基; Y是氧，硫，-CH 2 - 或NR 10，其中R 10是氢或C 1-6烷基; D是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; 并且Z为-NR 11 R 12，其中R 11和R 12独立地为氢或C 1-6烷基，或任选取代的N-连接或C连接的4至7元杂环基。还公开了化合物在治疗中的制备和用途的方法，例如抑郁和焦虑。

10. 发明申请

WO2003089409A1 COMPOUNDS HAVING AFFINITY AT 5HT2C RECEPTOR AND USE THEREOF IN THERAPY 审中-公开
标题翻译：在5HT2C受体中具有亲和力的化合物及其治疗用途
公开(公告)号：WO2003089409A1
公开(公告)日：2003-10-30
申请号：PCT/EP2003/004180
申请日：2003-04-17
申请人： GLAXO GROUP LIMITED , DAMIANI, Federica , HAMPRECHT, Dieter , JAXA-CHAMIEC, Albert, Andrzej , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
发明人： DAMIANI, Federica , HAMPRECHT, Dieter , JAXA-CHAMIEC, Albert, Andrzej , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38 , C07D211/76 , C07D211/88 , C07D401/12
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: wherein R 1 is hydrogen, hydroxy, fluoro, chloro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy or haloC 1-6 alkoxy; m is 0 when ======= is a double bond and m is 1 when ======= is a single bond; R 2 is hydrogen, halogen, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is -(CH 2 -CH 2 )-, -(CH=CH)-, -(CH 2 ) 3 -, -C(CH 3 ) 2 -, -(CH=CH-CH 2 )-, -(CH 2 -CH=CH)- or a group -(CHR 5 )- wherein R 5 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy or C 1-6 alkylthio; R 3 is halogen, cyano, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 1-6 alkoxy, C 1-6 alkylthio, hydroxy, amino, mono- or di-C 1-6 alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC 1-6 alkyl, haloC 1-6 alkoxy, aryl, arylC 1-6 alkyl, arylC 1-6 alkyloxy, arylC 1-6 alkylthio or COOR 6 , CONR 7 R 8 or COR 9 wherein R 6 , R 7 , R 8 and R 9 are independently hydrogen or C 1-6 alkyl; p is 0, 1 or 2 or 3; R 4 is hydrogen, halogen, hydroxy, cyano, nitro, C 1-6 alkyl, C 1-6 alkanoyl, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, amino, mono- or di-C 1-6 alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, -CH 2 - or NR 10 wherein R 10 is hydrogen or C 1-6 alkyl; D is a single bond, -CH 2 -, -(CH 2 ) 2 - or -CH=CH-; and Z is an optionally substituted C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, an optionally substituted N-linked 4 to 7 membered heterocyclic group, or Z is -NR 11 R 12 where R 11 and R 12 are independently hydrogen or C 1-6 alkyl. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐：其中R 1是氢，羟基，氟，氯，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基或卤代C 1-6烷氧基; 当<=======>是双键时，m为0，当<=======>为单键时，m为1; R2是氢，卤素，氰基，硝基，C1-6烷基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二C 1-6烷基氨基或 N-连接的4至7元杂环基; X是 - （CH 2 -CH 2） - ， - （CH = CH） - ， - （CH 2）3 - ， - C（CH 3）2 - ， - （CH = CH-CH 2） - ， - （CH 2 -CH = CH ） - 或基 - （CHR 5） - ，其中R 5是氢，卤素，羟基，氰基，硝基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基或C 1-6烷硫基 ; R 3是卤素，氰基，C 1-6烷基，C 3-7环烷基，C 3-7环烷氧基，C 1-6烷氧基，C 1-6烷硫基，羟基，氨基，单 - 或二-C 1-6烷基氨基，N-连接的4-7元杂环基，硝基，卤代C 1-6烷基，卤代C 1-6烷氧基，芳基，芳基C 1-6烷基，芳基C 1-6烷氧基，芳基C 1-6烷硫基或COOR 6，CONR 7 R 8或COR 9，其中R 6，R 7，R 8和R 9独立地为氢或C 1-6烷基; p为0,1或2或3; R4是氢，卤素，羟基，氰基，硝基，C1-6烷基，C1-6烷酰基，C3-7环烷基，C3-7环烷氧基，卤代C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，氨基，单或二 C 1-6烷基氨基或N-连接的4至7元杂环基; Y是氧，硫，-CH 2 - 或NR 10，其中R 10是氢或C 1-6烷基; D是单键，-CH 2 - ， - （CH 2）2 - 或-CH = CH-; Z为含有至少一个氮原子，任意取代的N-连接的4-7元杂环基的任意取代的C连接的4至7元杂环基，或Z为-NR 11 R 12，其中R 11和R 12独立地为氢或C 1-6烷基。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁和焦虑。

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