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.

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。

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。

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

公开(公告)号：US09309243B2

公开(公告)日：2016-04-12

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： C07D491/02 ,  C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5513 ,  A61K31/554 ,  C07D491/107

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。

公开(公告)号：US20150191482A1

公开(公告)日：2015-07-09

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： C07D491/107 ,  A61K31/5377 ,  C07D451/02 ,  A61K31/506 ,  C07D487/04 ,  C07D471/08 ,  A61K31/5513 ,  A61K31/4985

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-α]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 disorder; 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咪唑并[1,2-α]吡嗪衍生物在治疗和/或预防各种人类疾病中是有益的，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。