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：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 。

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：US5670656A

公开(公告)日：1997-09-23

申请号：US651181

申请日：1996-05-24

申请人： John Michael Cox ,  Kevin James Gillen ,  Russell Martin Ellis ,  Shaheen Khatoon Vohra ,  Stephen Christopher Smith ,  Ian Richard Matthews

发明人： John Michael Cox ,  Kevin James Gillen ,  Russell Martin Ellis ,  Shaheen Khatoon Vohra ,  Stephen Christopher Smith ,  Ian Richard Matthews

IPC分类号： C07D207/26 ,  C07D207/273 ,  C07D207/28

CPC分类号： C07D207/273

摘要： A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.

摘要翻译： 制备通式II化合物的方法：其中R 1是氢，或C 1 -C 10烃基或具有3至8个环原子的杂环基，其中任一个可任选地被取代; 每个R 2，R 3，R 4和R 5独立地是氢或C 1 -C 4烷基; A是任选取代的芳族或杂芳族环系; 并且R 21是氢，卤素，OH或OCONHR 1，其中R 1如上所定义; 该方法包括使通式III的化合物：其中A，R 2，R 3，R 4，R 5和R 21如通式II中所定义，R 25是离去基团如卤素原子; 在基本条件下