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21.发明授权Heteroaromatic urea derivatives as VR-1 receptor modulators for treating pain 失效异环脲衍生物作为治疗疼痛的VR-1受体调节剂公开(公告)号：US07285563B2
公开(公告)日：2007-10-23
申请号：US10505358
申请日：2003-03-21
申请人： Rebecca Elizabeth Brown , Victoria Alexandra Doughty , Gregory John Hollingworth , A. Brian Jones , Matthew John Lindon , Christopher Richard Moyes , Lauren Rogers
发明人： Rebecca Elizabeth Brown , Victoria Alexandra Doughty , Gregory John Hollingworth , A. Brian Jones , Matthew John Lindon , Christopher Richard Moyes , Lauren Rogers
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D401/12 , C07D215/38 , C07D217/02 , C07D217/08 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of formula (I); pharmaceutically acceptable salts and N-oxides thereof in which A, B, D and E are C or N with the proviso that one or more are N, R1, R2, R3, R4, R5 and R6 are simple substituents, n is 0-3 and y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; as VR-1 antagonists for treating conditions or diseases in which pain and/or inflammation predominates; the use of the same for manufacturing medicaments, pharmaceutical compositions comprising them and methods of treatment utilizing them
摘要翻译： 本发明提供式（I）化合物; 其中A，B，D和E为C或N的药学上可接受的盐和N-氧化物，条件是一个或多个为N，R 1，R 2， R 3，R 4，R 5和R 6是简单的取代基，n是0-3和 y是芳基，杂芳基，碳环基或稠合碳环基; 作为用于治疗其中疼痛和/或炎症占优势的病症或疾病的VR-1拮抗剂; 使用它们制造药物，包含它们的药物组合物和使用它们的治疗方法
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公开(公告)号：US07105507B2
公开(公告)日：2006-09-12
申请号：US10276127
申请日：2001-05-16
申请人： Jose Luis Castro Pineiro , Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw , Christopher John Swain
发明人： Jose Luis Castro Pineiro , Kevin Dinnell , Jason Matthew Elliott , Gregory John Hollingworth , Duncan Edward Shaw , Christopher John Swain
IPC分类号： A61K31/55 , A61K31/495 , A61K31/496 , C07D403/04 , C07D491/107
CPC分类号： C07D295/135 , C07C233/41 , C07C2601/02 , C07C2601/14 , C07D211/18 , C07D211/44 , C07D211/58 , C07D241/08 , C07D317/72 , C07D401/04 , C07D407/04 , C07D471/10 , C07D487/04
摘要： The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
摘要翻译： 本发明涉及式（I）化合物，其中环A为苯基或吡啶环; X表示选自式（a），（b），（c），（d）和（e）的连接体。 和R 1，R 2，R 3，R 4，R 5， R 6，R 7，R 13，R 14，R 15， R 16，R 17，R 21a和R 21b如本文所定义。 该化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，偏头痛，呕吐或带状疱疹后神经痛。
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23.发明授权
公开(公告)号：US6100256A
公开(公告)日：2000-08-08
申请号：US95782
申请日：1998-06-11
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen May Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen May Seward , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , A61K31/535 , A61K31/44 , A61K31/50 , A61K31/505
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675
摘要： The present invention provides a method for the treatment or prevention of schizophrenic disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
摘要翻译： 本发明提供使用口服活性的长效CNS渗透剂NK-1受体拮抗剂和包含这种NK-1受体拮抗剂的药物组合物治疗或预防精神分裂症的方法。
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公开(公告)号：US5977104A
公开(公告)日：1999-11-02
申请号：US096414
申请日：1998-06-11
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen May Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen May Seward , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/535
CPC分类号： A61K31/535
摘要： The present invention provides methods for the treatment or prevention of bipolar disorder without concomitant therapy with other antidepressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
摘要翻译： 本发明提供了治疗或预防双相情感障碍的方法，而不用与其他抗抑郁药或抗焦虑剂并用治疗，其包括口服给药口服活性的中枢神经系统渗透性NK-1受体拮抗剂和包含这种 NK-1受体拮抗剂。
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公开(公告)号：US5929054A
公开(公告)日：1999-07-27
申请号：US980730
申请日：1997-12-01
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： C07D211/56 , A61K31/4015 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/5377 , A61K31/675 , A61K45/00 , A61P15/10 , C07D209/54 , C07D265/32 , C07D413/06
CPC分类号： A61K31/445 , A61K31/5375 , A61K9/2018
摘要： The present invention provides a method for the treatment or prevention of sexual dysfunctions which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such an NK-1 receptor antagonist.
摘要翻译： 本发明提供一种治疗或预防性功能障碍的方法，其包括口服活性的长效CNS渗透性NK-1受体拮抗剂和包含这种NK-1受体拮抗剂的药物组合物。
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公开(公告)号：US5925627A
公开(公告)日：1999-07-20
申请号：US980931
申请日：1997-12-01
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： C07D491/107 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/5386 , A61K31/661 , A61K31/675 , A61K45/00 , A61P25/00 , A61P25/14 , A61P43/00 , C07D211/56 , C07D413/06 , C07D491/10
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides a method for the treatment or prevention of movement disorders using an orally active, long acting, CNS-penetrant NK-1 antagonist and pharmaceutical compositions comprising such an antagonist.
摘要翻译： 本发明提供使用口服活性的中枢神经系统渗透性NK-1拮抗剂和包含这种拮抗剂的药物组合物治疗或预防运动障碍的方法。
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27.发明授权
公开(公告)号：US5919781A
公开(公告)日：1999-07-06
申请号：US980927
申请日：1997-12-01
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/00 , A61K31/395 , A61K31/4015 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/675 , A61K45/00 , A61P25/30 , C07D211/56 , C07D265/30 , C07D413/06 , C07D491/10
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813
摘要： The present invention provides a method for the treatment or prevention of substance use disorders using an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
摘要翻译： 本发明提供使用口服活性的中枢神经系统渗透性NK-1受体拮抗剂和包含这种NK-1受体拮抗剂的药物组合物来治疗或预防物质使用障碍的方法。
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公开(公告)号：US09862711B2
公开(公告)日：2018-01-09
申请号：US15303890
申请日：2014-04-24
申请人： Benjamin Richard Bellenie , Ian Bruce , Andrew James Culshaw , Gregory John Hollingworth , James Neef , Matthew Spendiff , Simon James Watson
发明人： Benjamin Richard Bellenie , Ian Bruce , Andrew James Culshaw , Gregory John Hollingworth , James Neef , Matthew Spendiff , Simon James Watson
IPC分类号： C07D417/04 , C07D401/04 , C07D403/04 , C07D409/04 , C07D405/14 , C07D403/14 , A61K31/5377 , A61K31/497
CPC分类号： C07D417/04 , A61K31/497 , A61K31/5377 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04
摘要： The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
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公开(公告)号：US20170029414A1
公开(公告)日：2017-02-02
申请号：US15303890
申请日：2014-04-24
申请人： Benjamin Richard BELLENIE , Ian BRUCE , Andrew James CULSHAW , Gregory John HOLLINGWORTH , James NEEF , Matthew SPENDIFF , Simon James WATSON
发明人： Benjamin Richard BELLENIE , Ian BRUCE , Andrew James CULSHAW , Gregory John HOLLINGWORTH , James NEEF , Matthew SPENDIFF , Simon James WATSON
IPC分类号： C07D417/04 , C07D403/04 , C07D409/04 , A61K31/5377 , C07D401/04 , A61K31/497 , C07D405/14
CPC分类号： C07D417/04 , A61K31/497 , A61K31/5377 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04
摘要： The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
摘要翻译： 本发明提供抑制PI 3激酶γ同种型活性的式（I）化合物，其可用于治疗由PI3激酶γ同种型激活介导的疾病。
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公开(公告)号：US09499536B2
公开(公告)日：2016-11-22
申请号：US14151796
申请日：2014-01-09
申请人： Nigel Graham Cooke , Frédèric Zecri , Nicolas Soldermann , Romain Wolf , Christina Hebach , Klemens Hoegenauer , Gregory John Hollingworth , Anette Von Matt , Ross Sinclair Strang , Alexander Baxter Smith , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Frank Stowasser , Nicola Tufilli
发明人： Nigel Graham Cooke , Frédèric Zecri , Nicolas Soldermann , Romain Wolf , Christina Hebach , Klemens Hoegenauer , Gregory John Hollingworth , Anette Von Matt , Ross Sinclair Strang , Alexander Baxter Smith , Paulo Fernandes Gomes Dos Santos , Nadege Graveleau , Frank Stowasser , Nicola Tufilli
IPC分类号： A61K31/519 , A61P35/02 , A61P19/02 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , C07B2200/05
摘要： The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译： 本发明涉及式（I）的取代的四氢 - 吡啶并 - 嘧啶衍生物，其中Y，R 1，R 2和m如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。
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