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公开(公告)号：US09868749B2
公开(公告)日：2018-01-16
申请号：US15100825
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Rikki Peter Alexander , Jonathan Mark Bentley , Gareth Neil Brace , Daniel Christopher Brookings , Prafulkumar Tulshibhai Chovatia , Hervé Jean Claude Deboves , Craig Johnstone , Elizabeth Pearl Jones , Boris Kroeplien , Fabien Claude Lecomte , James Madden , Craig Miller , John Robert Porter , Matthew Duncan Selby , Michael Alan Shaw , Darshan Gunvant Vaidya , Ian Andrew Yule
IPC分类号： C07D519/00 , C07D471/04 , A61K31/4355 , A61K31/4709 , A61K31/538 , A61K31/5383
CPC分类号： C07D519/00 , A61K31/4355 , A61K31/4709 , A61K31/538 , A61K31/5383 , C07D471/04
摘要： A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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公开(公告)号：US20170305932A1
公开(公告)日：2017-10-26
申请号：US15513357
申请日：2015-10-02
申请人： UCB Biopharma SPRL , Sanofi
发明人： Teresa De Haro Garcia , Michael Deligny , Jag Paul Heer , Joanna Rachel Quincey , Mengyang Xuan , Zhaoning Zhu , Daniel Christopher Brookings , Mark Daniel Calmiano , Yves Evrard , Martin Clive Hutchings , James Andrew Johnson , Sophie Jadot , Jean Keyaerts , Malcolm Mac Coss , Matthew Duncan Selby , Michael Alan Shaw , Dominique Louis Leon Swinnen , Laurent Schio , Yann Foricher , Bruno Filoche-Romme
IPC分类号： C07D519/00 , C07D495/18 , C07D487/18 , C07D491/18 , C07F7/18 , C07D513/18
CPC分类号： C07D519/00 , A61K31/4184 , A61K31/506 , A61K31/55 , C07D471/18 , C07D487/08 , C07D487/18 , C07D491/08 , C07D491/18 , C07D493/18 , C07D495/08 , C07D495/18 , C07D513/18 , C07F7/1804
摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.
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公开(公告)号：US20150203486A1
公开(公告)日：2015-07-23
申请号：US14414287
申请日：2013-07-05
申请人： UCB Biopharma SPRL
发明人： Jonathan Mark Bentley , Daniel Christopher Brookings , Julien Alistair Brown , Thomas Paul Cain , Praful Tulshi Chovatia , Anne Marie Foley , Ellen Olivia Gallimore , Laura Jane Gleave , Alexander Heifetz , Helen Tracey Horsley , Martin Clive Hutchings , Victoria Elizabeth Jackson , James Andrew Johnson , Craig Johnstone , Boris Kroeplien , Fabien Claude Lecomte , Deborah Leigh , Martin Alexander Lowe , James Madden , John Robert Porter , Joanna Rachel Quincey , Laura Claire Reed , James Thomas Reuberson , Anthony John Richardson , Sarah Emily Richardson , Matthew Duncan Selby , Michael Alan Shaw , Zhaoning Zhu
IPC分类号： C07D471/04 , A61K31/496 , A61K31/506 , C07D491/107 , A61K31/5377 , A61K31/5513 , A61K31/554 , A61K31/437 , A61K31/541
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/5513 , A61K31/554 , C07D491/107 , C07D519/00
摘要： A series of imidazo[1,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
摘要翻译： 因此，作为人类TNFα活性的有效调节剂的一系列式（I）的咪唑并[1,2-a]吡啶衍生物因此有益于治疗和/或预防各种人类疾病，包括自身免疫和炎性疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。
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公开(公告)号：US10202405B2
公开(公告)日：2019-02-12
申请号：US15513357
申请日：2015-10-02
申请人： UCB Biopharma SPRL , Sanofi
发明人： Teresa De Haro Garcia , Michael Deligny , Jag Paul Heer , Joanna Rachel Quincey , Mengyang Xuan , Zhaoning Zhu , Daniel Christopher Brookings , Mark Daniel Calmiano , Yves Evrard , Martin Clive Hutchings , James Andrew Johnson , Sophie Jadot , Jean Keyaerts , Malcolm Mac Coss , Matthew Duncan Selby , Michael Alan Shaw , Dominique Louis Leon Swinnen , Laurent Schio , Yann Foricher , Bruno Filoche-Romme
IPC分类号： C07D519/00 , C07F7/18 , C07D471/18 , C07D487/18 , C07D493/18 , C07D491/08 , A61K31/4184 , A61K31/506 , A61K31/55 , C07D487/08 , C07D491/18 , C07D495/08 , C07D495/18 , C07D513/18
摘要： A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.
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公开(公告)号：US09550737B2
公开(公告)日：2017-01-24
申请号：US14406848
申请日：2013-06-11
申请人： UCB Biopharma SPRL
发明人： Daniel Christopher Brookings , Mark Daniel Calmiano , Ellen Olivia Gallimore , Helen Tracey Horsley , Martin Clive Hutchings , James Andrew Johnson , Boris Kroeplien , Fabien Claude Lecomte , Martin Alexander Lowe , Timothy John Norman , John Robert Porter , Joanna Rachel Quincey , James Thomas Reuberson , Matthew Duncan Selby , Michael Alan Shaw , Zhaoning Zhu , Anne Marie Foley
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D491/107 , C07D235/12 , A61K31/4184 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D405/06
CPC分类号： C07D235/12 , A61K31/4184 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/06 , C07D491/107
摘要： A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
摘要翻译： 因此，作为人TNFα活性的有效调节剂的一系列苯并咪唑衍生物有益于治疗和/或预防各种人类疾病，包括自身免疫和炎性疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。
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![Substituted imidazo[1,2-a]pyrazines as TNF activity modulators](/abs-image/US/2016/10/25/US09475820B2/abs.jpg.150x150.jpg)
公开(公告)号：US09475820B2
公开(公告)日：2016-10-25
申请号：US14414299
申请日：2013-07-05
申请人： UCB Biopharma SPRL
发明人： Jonathan Mark Bentley , Daniel Christopher Brookings , Julien Alistair Brown , Thomas Paul Cain , Laura Jane Gleave , Alexander Heifetz , Victoria Elizabeth Jackson , Craig Johnstone , Deborah Leigh , James Madden , John Robert Porter , Matthew Duncan Selby , Zhaoning Zhu
IPC分类号： A61K31/4985 , C07D241/36 , C07D491/107 , C07D487/04 , A61K31/506 , A61K31/5377 , A61K31/5513 , C07D451/02 , C07D471/08
CPC分类号： C07D491/107 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/5513 , C07D451/02 , C07D471/08 , C07D487/04
摘要： A series of imidazo[1,2-a]pyrazine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. The imidazo[1,2-a]pyrazine derivatives of the disclosure are of general formula
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7.发明申请公开(公告)号：US20160297837A1
公开(公告)日：2016-10-13
申请号：US15100825
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Rikki Peter Alexander , Jonathan Mark Bentley , Gareth Neil Brace , Daniel Christopher Brookings , Praful Tulshi Chovatia , Hervé Jean Claude Deboves , Craig Johnstone , Elizabeth Pearl Jones , Boris Kroeplien , Fabien Claude Lecomte , James Madden , Craig Miller , John Robert Porter , Matthew Duncan Selby , Michael Alan Shaw , Darshan Gunvant Vaidya , Ian Andrew Yule
IPC分类号： C07D519/00 , A61K31/4709 , A61K31/4355 , A61K31/538 , A61K31/5383 , C07D471/04
CPC分类号： C07D519/00 , A61K31/4355 , A61K31/4709 , A61K31/538 , A61K31/5383 , C07D471/04
摘要： A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
摘要翻译： 一系列取代的苯并咪唑，咪唑并[1,2-a]吡啶和吡唑并[1,5-a]吡啶衍生物及其类似物是人类TNFα活性的有效调节剂，因此在治疗和/或预防中有益 各种人类疾病，包括自身免疫性和炎症性疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。
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公开(公告)号：US20150152065A1
公开(公告)日：2015-06-04
申请号：US14406848
申请日：2013-06-11
申请人： UCB Biopharma SPRL
发明人： Daniel Christopher Brookings , Mark Daniel Calmiano , Ellen Olivia Gallimore , Helen Tracey Horsley , Martin Clive Hutchings , James Andrew Johnson , Boris Kroeplien , Fabien Claude Lecomte , Martin Alexander Lowe , Timothy John Norman , John Robert Porter , Joanna Rachel Quincey , James Thomas Reuberson , Matthew Duncan Selby , Michael Alan Shaw , Zhaoning Zhu , Anne Marie Foley
IPC分类号： C07D235/12 , C07D401/04 , A61K31/4439 , A61K31/454 , C07D405/06 , A61K31/4192 , C07D403/04 , A61K31/4709 , A61K31/4725 , A61K31/444 , C07D401/14 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D491/107 , A61K31/506 , A61K31/4184
CPC分类号： C07D235/12 , A61K31/4184 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/06 , C07D491/107
摘要： A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
摘要翻译： 因此，作为人TNFα活性的有效调节剂的一系列苯并咪唑衍生物有益于治疗和/或预防各种人类疾病，包括自身免疫和炎性疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。
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公开(公告)号：US09932343B2
公开(公告)日：2018-04-03
申请号：US15102003
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Rikki Peter Alexander , Mark Daniel Calmiano , Sabine Defays , Veronique Durieu , Michael Deligny , Jag Paul Heer , Victoria Elizabeth Jackson , Jean Keyaerts , Boris Kroeplien , Malcolm Mac Coss , Yogesh Anil Sabnis , Matthew Duncan Selby , Dominique Louis Leon Swinnen , Nathalie Van Houtvin , Zhaoning Zhu , Uwe Heinelt , Volkmar Wehner
IPC分类号： A61K31/415 , A61K31/495 , A61K31/44 , A61K31/425 , C07D403/02 , C07D487/00 , C07D513/00 , C07D491/00 , C07D498/02 , C07D487/04 , A61K31/4188 , C07D471/04 , C07D498/04 , C07D519/00 , C07D513/04
CPC分类号： C07D487/04 , A61K31/4188 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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10.发明申请公开(公告)号：US20160304523A1
公开(公告)日：2016-10-20
申请号：US15102003
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Rikki Peter Alexander , Mark Daniel Calmiano , Sabine Defays , Veronique Durieu , Michael Deligny , Jag Paul Heer , Victoria Elizabeth Jackson , Jean Keyaerts , Boris Kroeplien , Malcolm Mac Coss , Yogesh Anil Sabnis , Matthew Duncan Selby , Dominique Louis Leon Swinnen , Nathalie Van Houtvin , Zhaoning Zhu , Uwe Heinelt , Volkmar Wehner
IPC分类号： C07D487/04 , C07D519/00 , C07D513/04 , C07D471/04 , C07D498/04
CPC分类号： C07D487/04 , A61K31/4188 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
摘要翻译： 一系列三环苯并咪唑衍生物，特别是二氢-1H-咪唑并[1,2-a]苯并咪唑，二氢-1H-吡咯并[1,2-a]苯并咪唑，二氢-1H-吡嗪并[1,2-a]苯并咪唑 ，二氢-1H- [1,4]恶嗪并[4,3-a]苯并咪唑和二氢噻唑并[3,4-a]苯并咪唑及其类似物是人TNFα活性的有效调节剂，因此在治疗和 /或预防各种人类疾病，包括自身免疫性和炎症性疾病; 神经和神经退行性疾病; 疼痛和伤害性疾病; 心血管疾病; 代谢紊乱 眼部疾病; 和肿瘤疾病。
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