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1. 发明授权

US08188123B2 (Pyrrolidin-2-yl)phenyl derivatives 有权
标题翻译：（吡咯烷-2-基）苯基衍生物
公开(公告)号：US08188123B2
公开(公告)日：2012-05-29
申请号：US12611468
申请日：2009-11-03
申请人： Simon James Anthony Grove , Ronald Palin , Ashvinkumar Dhirubhai Mistry , John Kinnaird Ferguson MacLean
发明人： Simon James Anthony Grove , Ronald Palin , Ashvinkumar Dhirubhai Mistry , John Kinnaird Ferguson MacLean
IPC分类号： A61K31/4439 , C07D401/10
CPC分类号： C07D401/10
摘要： The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
摘要翻译：本发明涉及具有通式I的（吡咯烷-2-基）苯基衍生物，其中R 1是（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基 R 2是H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; R3是H，（C1-4）烷基或卤代（C1-4）烷基; R4是H，（C1-4）烷基或卤代（C1-4）烷基; R5是H，（C1-4）烷基或卤代（C1-4） - 烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺（C 3-6）环烷基; R 6为H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; 或其药学上可接受的盐，包含其的药物组合物，以及这些（吡咯烷-2-基）苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

2. 发明申请

US20100113493A1 (PYRROLIDIN-2-YL)PHENYL DERIVATIVES 有权
标题翻译：（吡咯烷-2-基）苯基衍生物
公开(公告)号：US20100113493A1
公开(公告)日：2010-05-06
申请号：US12611468
申请日：2009-11-03
申请人： Simon James Anthony Grove , Ronald Palin , Ashvinkumar Dhirubhai Mistry , John Kinnaird Ferguson MacLean
发明人： Simon James Anthony Grove , Ronald Palin , Ashvinkumar Dhirubhai Mistry , John Kinnaird Ferguson MacLean
IPC分类号： A61K31/4439 , C07D401/10 , A61P29/00 , A61P25/00
CPC分类号： C07D401/10
摘要： The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
摘要翻译：本发明涉及具有通式I的（吡咯烷-2-基）苯基衍生物，其中R 1是（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基 R 2是H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; R3是H，（C1-4）烷基或卤代（C1-4）烷基; R4是H，（C1-4）烷基或卤代（C1-4）烷基; R5是H，（C1-4）烷基或卤代（C1-4） - 烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺（C 3-6）环烷基; R 6为H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; 或其药学上可接受的盐，包含其的药物组合物，以及这些（吡咯烷-2-基）苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

3. 发明申请

US20100210680A1 TRICYCLIC HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：三元杂环衍生物
公开(公告)号：US20100210680A1
公开(公告)日：2010-08-19
申请号：US12678184
申请日：2008-09-15
申请人： Simon James Anthony Grove , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Grant Wishart
发明人： Simon James Anthony Grove , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Grant Wishart
IPC分类号： A61K31/436 , C07D491/052 , A61K31/407 , A61K31/422 , A61P3/04 , A61P25/18
CPC分类号： C07D491/052
摘要： The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义。本发明还涉及包含这些化合物的药物组合物及其在治疗中的用途，特别是用于治疗5-羟色胺介导的疾病如肥胖，精神分裂症和认知功能障碍。

4. 发明授权

US08729274B2 Tricyclic heterocyclic derivatives 有权
标题翻译：三环杂环衍生物
公开(公告)号：US08729274B2
公开(公告)日：2014-05-20
申请号：US13255630
申请日：2010-03-09
申请人： Keneth Davies , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Mark Reid , Grant Wishart
发明人： Keneth Davies , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Mark Reid , Grant Wishart
IPC分类号： C07D209/62 , A61K31/403
CPC分类号： C07D209/62
摘要： The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述三环杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防5-羟色胺介导的障碍，例如肥胖症。

5. 发明申请

US20120232122A1 TRICYCLIC HETEROCYCLIC DERIVATIVES 有权
标题翻译：三元杂环衍生物
公开(公告)号：US20120232122A1
公开(公告)日：2012-09-13
申请号：US13255630
申请日：2010-03-09
申请人： Keneth Davies , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Mark Reid , Grant Wishart
发明人： Keneth Davies , Takao Kiyoi , Ashvinkumar Dhirubhai Mistry , Peter Christopher Ray , Mark Reid , Grant Wishart
IPC分类号： A61K31/403 , A61P3/04 , A61P3/10 , A61P9/10 , A61P3/08 , A61P3/06 , A61P25/22 , A61P25/24 , A61P25/00 , A61P25/18 , A61P25/20 , A61P15/00 , A61P29/00 , A61P1/00 , A61P25/06 , C07D209/62
CPC分类号： C07D209/62
摘要： The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.
摘要翻译：本发明涉及式（I）的三环杂环衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含所述三环杂环衍生物的药物组合物及其在治疗中的用途，例如用于治疗或预防5-羟色胺介导的障碍，例如肥胖症。

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