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：US20110092539A1

公开(公告)日：2011-04-21

申请号：US12996183

申请日：2009-06-03

申请人： Jonathan Gillespie ,  Craig Jamieson ,  Zoran Rankovic

发明人： Jonathan Gillespie ,  Craig Jamieson ,  Zoran Rankovic

IPC分类号： A61K31/437 ,  C07D231/10 ,  A61K31/415 ,  C07D405/12 ,  C07D403/12 ,  C07D471/04 ,  C07D307/02 ,  A61K31/341 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P25/22 ,  A61P25/08

CPC分类号： C07D231/14 ,  C07D231/12 ,  C07D231/18 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

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化物。 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：US07687515B2

公开(公告)日：2010-03-30

申请号：US11653600

申请日：2007-01-16

申请人： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Stephen Jones ,  David Jonathan Bennett ,  Iain Cumming ,  Jonathan Gillespie

发明人： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Stephen Jones ,  David Jonathan Bennett ,  Iain Cumming ,  Jonathan Gillespie

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04

摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

摘要翻译： 本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物 包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途 ，如神经性疼痛。

公开(公告)号：US20070179138A1

公开(公告)日：2007-08-02

申请号：US11653600

申请日：2007-01-16

申请人： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Jones ,  David Bennett ,  Iain Cumming ,  Jonathan Gillespie

发明人： Jiaqiang Cai ,  Zoran Rankovic ,  Philip Jones ,  David Bennett ,  Iain Cumming ,  Jonathan Gillespie

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04

摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

摘要翻译： 本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物 包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途 ，如神经性疼痛。

公开(公告)号：US08536214B2

公开(公告)日：2013-09-17

申请号：US12996183

申请日：2009-06-03

申请人： Jonathan Gillespie ,  Craig Jamieson ,  John Kinaird Fergusen MaClean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

发明人： Jonathan Gillespie ,  Craig Jamieson ,  John Kinaird Fergusen MaClean ,  Elizabeth Margaret Moir ,  Zoran Rankovic

IPC分类号： A61K31/415 ,  C07D231/10

CPC分类号： C07D231/14 ,  C07D231/12 ,  C07D231/18 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

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化物。 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：US08633237B2

公开(公告)日：2014-01-21

申请号：US13262992

申请日：2010-04-08

申请人： Kevin J. Gillen ,  Jonathan Gillespie ,  Craig Jamieson ,  John K. F. MacLean ,  Elizabeth M. Moir ,  Zoran Rankovic

发明人： Kevin J. Gillen ,  Jonathan Gillespie ,  Craig Jamieson ,  John K. F. MacLean ,  Elizabeth M. Moir ,  Zoran Rankovic

IPC分类号： C07D231/18 ,  C07C311/07

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：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：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。