专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008074716A1 AZABICYCLIC COMPOUNDS AS SEROTONINE, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译：作为丝氨酸，多巴胺和诺贝那韦再摄入抑制剂的化学式
公开(公告)号：WO2008074716A1
公开(公告)日：2008-06-26
申请号：PCT/EP2007/063841
申请日：2007-12-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , MICHELI, Fabrizio , TERRENI, Silvia
发明人： BONANOMI, Giorgio , MICHELI, Fabrizio , TERRENI, Silvia
IPC分类号： C07D209/52 , A61K31/403 , A61P25/18
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of Formula (I)' or pharmaceutically acceptable salts or a solvates thereof: wherein A is and K is a mono or bicyclic aryl group; R 1 is selected from a group consisting of: halogen, C 1-4 alkyl and C 1-4 alkoxy, and such R 1 may assume different meanings on the basis of p value; p is an integer from 0 to 5; R 2 is a group P wherein P is and R 3 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-3 alkyl, haloC 1-2 alkyl or an optionally substituted phenyl group; X is oxygen, -NR 8 - or sulphur; n is 0 or 1; R 7 is hydrogen or methyl; R 4 is hydrogen or methyl; R 5 is hydrogen or C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; and R 8 is hydrogen or C 1-4 alkyl; 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：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂化物：其中A是且K是单或双环芳基; R 1选自由以下组成的组：卤素，C 1-4烷基和C 1-4 - 烷氧基，并且这样的R _{1 可以在p值的基础上具有不同的含义; p是0至5的整数; R 2是基团P，其中P是且R 3是氢，C 1-4烷基，C 3-6，环烷基，C 3-6环烷基C 1-3烷基，卤代C 1-12烷基或任选取代的苯基; X是氧，-NR 8 - 或硫; n为0或1; R 7是氢或甲基; R 4是氢或甲基; R 5是氢或C 1-4烷基; R 6是氢或C 1-4烷基; 并且R 8是氢或C 1-4烷基; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，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应用。}

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

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

WO2004078718A8 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：WO2004078718A8
公开(公告)日：2005-05-26
申请号：PCT/EP2004001843
申请日：2004-02-24
申请人： GLAXO GROUP LTD , 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 , C07D207/273 , C07D207/38 , A61K31/40
CPC分类号： C07D207/26 , C07D207/273 , C07D207/38
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ==== is a double bond and m is 1 when ==== is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, 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 -(CH2-CH2)-, -(CH=CH)-, -(CH2)3-, -C(CH3)2-, -(CH=CH-CH2)-, -(CH2-CH=CH)- or a group -(CHR5)- wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 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, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 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; Y is oxygen, sulfur, -CH2- or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, -CH2-, -(CH2)2- or -CH=CH-; and Z is -NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, 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。

6. 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。

7. 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。

8. 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。

9. 发明申请

WO2003008414A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008414A1
公开(公告)日：2003-01-30
申请号：PCT/US2002/022394
申请日：2002-07-15
申请人： SB PHARMCO PUERTO RICO INC. , NEUROCRINE BIOSCIENCES INC. , DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , REGAN, Collin, F. , SCHWAEBE, Michael, K. , ST-DENIS, Yves
IPC分类号： C07D471/16
CPC分类号： C07D471/16
摘要： The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof Please insert formula (I) here: 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：本发明涉及包括立体异构体，前体药物和药学上可接受的盐或溶剂化物的式（I）的三环吡啶化合物。请在此处插入式（I）：其制备方法，含有它们的药物组合物及其在治疗中的用途的促肾上腺皮质激素释放因子（CRF）介导的病症。

10. 发明申请

WO2003008412A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2003008412A2
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007865
申请日：2002-07-15
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
发明人： DI FABIO, Romano , MICHELI, Fabrizio , ST-DENIS, Yves
IPC分类号： C07D471/00
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)R 5 , nitro, -NR 6 R 7 , cyano, and a group R 8 ; R 1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR 6 R 7 or cyano; R 2 is hydrogen, C3-C7 cycloalkyl, or a group R 9 ; R 3 is C3-C7 cycloalkyl, or a group R 9 ; or R 2 and R 3 together with N form a 5-14 membered heterocycle, which may be substituted 1 to 3 R 10 groups; R 4 is hydrogen, C1-C6 alkyl, halogen or halo C1-C6 alkyl; R 5 is a C1-C4 alkyl, -OR 6 or NR 6 R 7 ; R 6 is hydrogen or C1-C6 alkyl; R 7 is hydrogen or C1-C6 alkyl; R 8 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 R 11 groups; R 9 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; R 10 is a group R 8 , 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)NR 6 R 7 , phenyl which may be substituted by 1 to 4 R 11 groups; R 11 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)NR 6 R 7 ; 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).
摘要翻译：本发明提供式（I）化合物，其包括其立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，其各自可以被1-4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，-C（O）R 5，硝基，-NR 6 R 7，氰基和基团R 8; 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 6 R 7或氰基; R2是氢，C3-C7环烷基或基团R9; R 3为C 3 -C 7环烷基或基团R 9; 或R 2和R 3与N一起形成5-14元杂环，其可以被取代1至3个R 10基团; R4是氢，C1-C6烷基，卤素或卤素C1-C6烷基; R5是C1-C4烷基，-OR6或NR6R7; R6是氢或C1-C6烷基; R7是氢或C1-C6烷基; R8是5-6元杂环，其可以是饱和的或可以含有一至三个双键，并且其可以被1个或多个R 11基团取代; R9是可以被一个或多个选自以下的基团取代的C 1 -C 6烷基：C 3 -C 7环烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基，卤代C 1 -C 6烷基; R 10是基团R 8，C 3 -C 7环烷基，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，羟基，卤素，硝基，氰基，C（O）NR 6 R 7，可被1至4个R 11基团取代的苯基; R 11是C 3 -C 7环烷基，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，羟基，卤素，硝基，氰基或C（ O）NR6R7; X是碳或氮; n为1或2; 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式