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公开(公告)号：US09969729B2
公开(公告)日：2018-05-15
申请号：US15100915
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437
摘要： A series of substituted 1H imidazo[4,5-b]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.
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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：US20160355509A1
公开(公告)日：2016-12-08
申请号：US15038555
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
IPC分类号： C07D471/04 , A61K31/444 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444
摘要： A series of substituted 3H-imidazo[4,5-c]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取代的式（I）的3H-咪唑并[4,5-c]吡啶衍生物因此有益于治疗和/或预防各种人类疾病，包括自身免疫和炎症 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：US20160304513A1
公开(公告)日：2016-10-20
申请号：US15101089
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Michael Louis Robert Deligny , Jag Paul Heer , Victoria Elizabeth Jackson , Boris Kroeplien , Fabien Claude Lecomte , John Robert Porter
IPC分类号： C07D471/04 , A61K31/506 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/506
摘要： A series of substituted 3H imidazo[4,5-b]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.
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公开(公告)号：US20160297827A1
公开(公告)日：2016-10-13
申请号：US15100690
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Mezher Hussein Ali , Daniel Christopher Brookings , Julien Alistair Brown , Victoria Elizabeth Jackson , Boris Kroeplien , John Robert Porter
IPC分类号： C07D487/04 , A61K31/5377 , A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377
摘要： A series of substituted imidazo[1,2-a]pyrimidine 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.
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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：US10775385B2
公开(公告)日：2020-09-15
申请号：US15736614
申请日：2015-10-22
申请人： UCB Biopharma SPRL
发明人： James Philip O'Connell , John Robert Porter , Alastair Lawson , Boris Kroeplien , Stephen Edward Rapecki , Timothy John Norman , Graham John Warrellow , Tracy Lynn Arakaki , Alex Buntin Burgin , William Ross Pitt , Mark Daniel Calmiano , David Andreas Schubert , Daniel John Lightwood , Rebecca Jayne Wootton
IPC分类号： G01N33/68 , C07K14/525 , C07K14/705 , C07K16/24 , A61P37/00 , C07D401/14 , C07D471/00 , C07D213/72 , C07D235/04 , C07D239/26 , C07D471/04 , A61K47/64 , A61P35/00
摘要： A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.
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公开(公告)号：US09969728B2
公开(公告)日：2018-05-15
申请号：US15038239
申请日：2014-12-08
申请人： UCB Biopharma SPRL
发明人： Sabine Defays , Jag Paul Heer , Victoria Elizabeth Jackson , James Andrew Johnson , Boris Kroeplien , John Robert Porter
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4184
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/437 , A61K2300/00
摘要： A series of substituted 5,6,7,8-tetrahydroimidazo[1,2-α]pyridine 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.
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公开(公告)号：US09926313B2
公开(公告)日：2018-03-27
申请号：US15101089
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： Michael Louis Robert Deligny , Jag Paul Heer , Victoria Elizabeth Jackson , Boris Kroeplien , Fabien Claude Lecomte , John Robert Porter
IPC分类号： C07D471/04 , A61K31/437 , A61K31/506
CPC分类号： C07D471/04 , A61K31/437 , A61K31/506
摘要： A series of substituted 3H imidazo[4,5-b]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.
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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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