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

WO2009043883A1 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：WO2009043883A1
公开(公告)日：2009-04-09
申请号：PCT/EP2008/063166
申请日：2008-10-01
申请人： Glaxo Group Limited , BERTANI, Barbara , CARDULLO, Francesca , DAMBRUOSO, Paolo , MARZORATI, Paola , MICHELI, Fabrizio , PASQUARELLO, Alessandra , SERI, Catia , TEDESCO, Giovanna
发明人： BERTANI, Barbara , CARDULLO, Francesca , DAMBRUOSO, Paolo , MARZORATI, Paola , MICHELI, Fabrizio , PASQUARELLO, Alessandra , SERI, Catia , TEDESCO, Giovanna
IPC分类号： C07D403/14 , C07D413/14 , C07D417/14 , C07D491/052 , A61K31/513 , A61P25/00
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R 1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be 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 , and n is 1 or 2; 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R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被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，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5，n为1或2; 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。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

2. 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

3. 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。

4. 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。

5. 发明申请

WO2006133946A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：WO2006133946A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005768
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/435 , A61K31/41 , A61P25/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: (I), 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：（I）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在治疗中的用途，作为多巴胺D的调节剂 > 3个受体，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

WO2008031772A1 AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE 审中-公开
标题翻译：单一化合物作为单体反应的抑制剂
公开(公告)号：WO2008031772A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059381
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D221/04 , A61K31/435 , A61P25/00
CPC分类号： C07D221/04
摘要： The present invention relates to novel compounds of formula (I)´, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 18 , each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R 15 ) p , which can be the same or different; p is an integer from 0 to 5; R 3 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 4 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 5 is hydrogen or C 1-4 alkyl; R 7 is hydrogen or C 1-4 alkyl; or is a group X, X 1 , X 2 or X 3 ; wherein X is (IV) X 1 is (V) X 2 is (VI) and X 3 is (VII) R 6 is hydrogen or C 1-4 alkyl; or is a group X or X 1 ; R 9 is C 1-4 alkyl; R 10 is selected from a group consisting of: hydrogen, 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 8 ; R 8 is a 5-6 membered heterocycle group, which may be 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 11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 13 is selected from a group consisting of: hydrogen, 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 8 ; R 14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 15 is 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 8 ; R 16 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 17 is hydrogen or C 1-4 alkyl; R 18 is selected from a group consisting of: halog
摘要翻译：本发明涉及新的式（I）化合物，其药学上可接受的盐，前药或溶剂合物：其中R 1是氢或C 1-4烷基; R 2是基团A，K或W，其中A是（II）K是任选被1或2个基团R 18取代的a或β萘基，每个他们是相同或不同的; 并且W是（III），并且其中G是5,6-元单环杂芳基或8至11元杂芳基双环基团; 这样的G可以被相同或不同的（R 15） p是0至5的整数; R 3 3选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 4选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 5是氢或C 1-4烷基; R 7是氢或C 1-4烷基; 或者为X，X 1，X 2或X 3; 其中X是（Ⅳ）ⅩⅢ是（Ⅴ）ⅩⅥ是（Ⅵ），ⅩⅢ是（Ⅶ） 6是氢或C 1-4烷基; 或者是X或X 1族; R 9是C 1-4烷基; R 10选自：氢，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 8; R 8是5-6元杂环基团，其可以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烷氧基和C 1-4烷酰基; R 11选自：氢，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 8; R 12选自：氢，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 8; R 13选自：氢，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 8; R 14选自：氢，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 8; R 15选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4个碳原子的烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 16是氢，C 1-4烷基，C 3-6环烷基或C 3-6环烷基C _{1-3 烷基; R 17是氢或C 1-4烷基; R 18选自：卤素}

7. 发明申请

WO2007022936A1 TRIAZOLYL DERIVATIVES OF AZABICYCLO [3.1.0] HEXANE AS DOPAMINE D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZABICYCLO的三唑衍生物[3.1.0] HEXANE作为DOPAMINE D3受体调节剂
公开(公告)号：WO2007022936A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008203
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , CAPELLI, Anna Maria , FAZZOLARI, Elettra , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： CAPELLI, Anna Maria , FAZZOLARI, Elettra , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D413/14 , A61K31/422 , A61P25/18
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof, wherein 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 ; m 1 , m 2 , m 3 , and m 4 are 0; m 5 , m 6 and m 7 are each independently 0, 1 or 2 wherein the sum of m 5 , m 6 and m 7 is 1 or 2; R 6 is C 1-6 alkyl; R 7 is halogen, C 1-6 alkyl or haloC 1-6 alkyl; 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 1-4 alkoxy and C 1-4 alkanoyl; with the proviso that when m 5 =m 6 =1 , R 7 is not chlorine; 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：本发明涉及式（IC）的新化合物或其盐，其中p为0至4的整数; R 1独立地选自：卤素，羟基，氰基，C 1 -C 4 - 烷基，卤代C 1 - 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C 1-4烷氧基， 5 ; 或对应于基团R 5; m 1，m 2，m 3和m 4是0; m 5，m 6和m 7各自独立地为0,1或2，其中m为5〜 m 6和m 7是1或2; R 6是C 1-6烷基; R 7是卤素，C 1-6烷基或卤代C 1-6烷基; 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，1,1-二氧代-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 1-4 - 烷氧基和C 1-4烷酰基; 条件是当m 5 = m 6 = 1时，R 7不是氯; 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。

8. 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。

9. 发明申请

WO2008031771A3 3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION 审中-公开
公开(公告)号：WO2008031771A3
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059380
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： A61K31/435 , A61P25/24 , C07D221/04
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: formula (I), 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; such G may be substituted by (R 2 ) p , which can be the same or different; R 1 is hydrogen or C 1-4 alkyl; R 2 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 R 8 ; R 5 is hydrogen or C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; R 7 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to X, X 1 , X 2 or X 3 ; wherein X corresponds to: formula (a) X 1 corresponds to: formula (b) X 2 corresponds to: formula (c) X 3 corresponds to: formula (d) R 3 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 4 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 8 is a 5-6 membered heterocycle group, which may be 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 9 is C 1-4 alkyl; R 10 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 11 is haloC 1-2 alkyl; p is an integer from 0 to 5; n is 1 or 2. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

10. 发明申请

WO2005123717A1 7-PYRAZOLYLBENZAZEPINES HAVING AFFINITY FOR D3 RECEPTOR 审中-公开
标题翻译：具有D3受体亲和性的7-吡唑啉基苯甲酸酯
公开(公告)号：WO2005123717A1
公开(公告)日：2005-12-29
申请号：PCT/EP2005/006639
申请日：2005-06-17
申请人： GLAXO GROUP LIMITED , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
发明人： HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
IPC分类号： C07D401/14
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14
摘要： Compounds of formula (I) or a salt thereof are disclosed (I): wherein R 1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C 1-4 alkyl and haloC 1-4 alkyl; R 2 is hydrogen or methyl; and R 3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C 1-4 alkyl or haloC 1-4 alkyl. 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（I）：其中R 1是被两个或三个独立地选自卤素，C 1-4烷基和卤代C 1-4烷基的取代基取代的吡唑基; R2是氢或甲基; 并且R 3是喹啉基，恶唑基或苯基，其各自任选被一个或两个卤素，C 1-4烷基或卤代C 1-4烷基取代。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。

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