公开(公告)号：US10449198B2

公开(公告)日：2019-10-22

申请号：US15641751

申请日：2017-07-05

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： A61K31/5375 ,  A61K31/397 ,  A61K31/495 ,  A61K31/4453 ,  A61K31/40

摘要： The present invention relates to a method of treating pain in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate: wherein Q is as defined herein.

公开(公告)号：US09676786B2

公开(公告)日：2017-06-13

申请号：US15107653

申请日：2014-12-23

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D205/04 ,  C07D265/30 ,  C07D493/10 ,  C07D295/192 ,  C07D211/06

CPC分类号： C07D491/107 ,  C07D205/04 ,  C07D211/06 ,  C07D265/30 ,  C07D295/192 ,  C07D493/10

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US10442814B2

公开(公告)日：2019-10-15

申请号：US15953109

申请日：2018-04-13

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul M. O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D205/04 ,  C07D265/30 ,  C07D493/10 ,  C07D295/192 ,  C07D211/06 ,  A61P25/00 ,  A61P23/00

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US20180140608A1

公开(公告)日：2018-05-24

申请号：US15641751

申请日：2017-07-05

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： A61K31/5375 ,  A61K31/397 ,  A61K31/495 ,  A61K31/4453 ,  A61K31/40

CPC分类号： A61K31/5375 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/495

摘要： The present invention relates to a method of treating pain in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate: wherein Q is as defined herein.

公开(公告)号：US20190084993A1

公开(公告)日：2019-03-21

申请号：US15953109

申请日：2018-04-13

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul M. O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  A61P25/00 ,  A61P23/00 ,  C07D205/04 ,  C07D211/06 ,  C07D493/10 ,  C07D295/192 ,  C07D265/30

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US09944653B2

公开(公告)日：2018-04-17

申请号：US15587068

申请日：2017-05-04

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D205/04 ,  C07D265/30 ,  C07D295/192 ,  C07D211/06 ,  C07D493/10

CPC分类号： C07D491/107 ,  C07D205/04 ,  C07D211/06 ,  C07D265/30 ,  C07D295/192 ,  C07D493/10

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US20170298076A1

公开(公告)日：2017-10-19

申请号：US15587068

申请日：2017-05-04

申请人： The University of Liverpool

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D265/30 ,  C07D205/04 ,  C07D211/06 ,  C07D493/10 ,  C07D295/192

CPC分类号： C07D491/107 ,  C07D205/04 ,  C07D211/06 ,  C07D265/30 ,  C07D295/192 ,  C07D493/10

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

公开(公告)号：US20160318947A1

公开(公告)日：2016-11-03

申请号：US15107653

申请日：2014-12-23

申请人： THE UNIVERSITY OF LIVERPOOL

发明人： Martin Leuwer ,  Paul O'Neill ,  Neil Berry ,  Chandrakala Pidathala

IPC分类号： C07D491/107 ,  C07D211/06 ,  C07D205/04 ,  C07D295/192 ,  C07D265/30

CPC分类号： C07D491/107 ,  C07D205/04 ,  C07D211/06 ,  C07D265/30 ,  C07D295/192 ,  C07D493/10

摘要： The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.

摘要翻译： 其中Q如本文所定义。 式I的化合物作为士的宁敏感的α1-甘氨酸受体的选择性正变构调节剂。 本发明还涉及这些化合物作为治疗和/或预防涉及士的宁敏感性α1-甘氨酸受体活性的疾病或病症（例如慢性疼痛）的治疗剂的用途。本发明 本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。