公开(公告)号：US08507521B2

公开(公告)日：2013-08-13

申请号：US13505349

申请日：2010-11-02

申请人： Julia Adam ,  Jonathan Gillespie ,  Steven Laats ,  John Kinnaird Ferguson MacLean ,  Duncan Robert McArthur

发明人： Julia Adam ,  Jonathan Gillespie ,  Steven Laats ,  John Kinnaird Ferguson MacLean ,  Duncan Robert McArthur

IPC分类号： A61K31/437 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4178 ,  C07D471/04 ,  A61P25/22 ,  C07D401/14 ,  C07D413/10 ,  C07D403/10 ,  C07D405/14 ,  A61P25/18 ,  A61K31/4725 ,  C07D401/10

CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D413/10

摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.

摘要翻译： 本发明涉及式（I）的杂环衍生物，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由谷氨酸盐功能障碍如精神分裂症和广泛性焦虑症介导的障碍。

公开(公告)号：US20120220622A1

公开(公告)日：2012-08-30

申请号：US13505349

申请日：2010-11-02

申请人： Julia Adam ,  Jonathan Gillespie ,  Steven Laats ,  John Kinnaird Ferguson MacLean ,  Duncan Robert McArthur

发明人： Julia Adam ,  Jonathan Gillespie ,  Steven Laats ,  John Kinnaird Ferguson MacLean ,  Duncan Robert McArthur

IPC分类号： A61K31/437 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4178 ,  C07D471/04 ,  A61P25/22 ,  C07D401/14 ,  C07D413/10 ,  C07D403/10 ,  C07D405/14 ,  A61P25/18 ,  A61K31/4725 ,  C07D401/10

CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D413/10

摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.

摘要翻译： 本发明涉及式（I）的杂环衍生物，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由谷氨酸盐功能障碍如精神分裂症和广泛性焦虑症介导的障碍。

公开(公告)号：US20120202781A1

公开(公告)日：2012-08-09

申请号：US13262992

申请日：2010-04-08

申请人： Kevin James Gillen ,  Jonathan Gillespie ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

发明人： Kevin James Gillen ,  Jonathan Gillespie ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

IPC分类号： A61K31/18 ,  A61K31/44 ,  A61K31/4245 ,  A61K31/4164 ,  A61K31/415 ,  C07D213/64 ,  C07D213/36 ,  C07D271/12 ,  C07D233/61 ,  C07D231/10 ,  C07D205/04 ,  C07C311/07 ,  C07D213/68 ,  A61P25/00 ,  A61K31/397

CPC分类号： C07C311/29 ,  C07C307/08 ,  C07C311/07 ,  C07C311/09 ,  C07C311/14 ,  C07C311/37 ,  C07C317/22 ,  C07C317/32 ,  C07C2601/02 ,  C07C2602/08 ,  C07D205/04 ,  C07D213/38 ,  C07D213/64 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D231/18 ,  C07D233/06 ,  C07D271/12 ,  C07D295/135 ,  C07D307/64 ,  C07D333/34

摘要： The present invention relates to anindane 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 a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.

摘要翻译： 本发明涉及式I的茚满衍生物，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。 本发明还涉及一种药物组合物，其包含一种或多种所述二氢吲哚衍生物并用于治疗，例如用于治疗或预防需要AMPA受体介导的突触应答增强的精神疾病，包括精神分裂症， 抑郁症和阿尔茨海默病。

公开(公告)号：US07820707B2

公开(公告)日：2010-10-26

申请号：US11771198

申请日：2007-06-29

申请人： Kevin James Gillen ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

发明人： Kevin James Gillen ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

IPC分类号： A61K31/4155 ,  A61K31/416 ,  C07D231/56 ,  C07D231/10

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04

摘要： The present invention relates to a 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 a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.

摘要翻译： 本发明涉及式I的杂环衍生物，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需要由AMPA受体介导的突触应答增强的精神疾病，包括精神分裂症，抑郁症和阿尔茨海默病 。

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。

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。

公开(公告)号：US20080255086A1

公开(公告)日：2008-10-16

申请号：US11771198

申请日：2007-06-29

申请人： Kevin James Gillen ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

发明人： Kevin James Gillen ,  Craig Jamieson ,  John Kinnaird Ferguson MacLean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

IPC分类号： A61K31/416 ,  C07D417/12 ,  C07D417/14 ,  A61K31/541 ,  C07D413/14 ,  A61K31/5377 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04

摘要： The present invention relates to a 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 a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.

摘要翻译： 本发明涉及式I的杂环衍生物，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需要由AMPA受体介导的突触应答增强的精神疾病，包括精神分裂症，抑郁症和阿尔茨海默病 。