公开(公告)号：US10273247B2

公开(公告)日：2019-04-30

申请号：US15038986

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Mezher Hussein Ali ,  Julien Alistair Brown ,  Victoria Elizabeth Jackson

IPC分类号： C07D513/04 ,  A61K31/429 ,  A61K45/06

摘要： A series of substituted imidazo[2,1-b]thiazole 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：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：US09815797B2

公开(公告)日：2017-11-14

申请号：US15101283

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Gregory Foulkes ,  Martin Clive Hutchings ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  James Thomas Reuberson ,  Sarah Margaret Rook ,  Zhaoning Zhu

IPC分类号： C07D239/74 ,  A61K31/47 ,  A61K31/472 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  C07D215/14 ,  C07D237/28 ,  A61K31/502 ,  C07D215/06 ,  C07D237/32 ,  C07D241/44 ,  A61K45/06 ,  C07D217/16 ,  C07D241/42 ,  C07D403/04

CPC分类号： C07D239/74 ,  A61K31/47 ,  A61K31/472 ,  A61K31/498 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K45/06 ,  C07D215/06 ,  C07D215/14 ,  C07D217/16 ,  C07D237/28 ,  C07D237/32 ,  C07D241/42 ,  C07D241/44 ,  C07D403/04 ,  A61K2300/00

摘要： A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, 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：US09890174B2

公开(公告)日：2018-02-13

申请号：US15101798

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Julien Alistair Brown ,  Michael Deligny ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Sophie Jadot ,  Boris Kroeplien ,  Malcolm Mac Coss ,  Yogesh Anil Sabnis ,  Dominique Louis Léon Swinnen ,  Nathalie Van Houtvin ,  Zhaoning Zhu

IPC分类号： C07D491/14 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  C07D491/147 ,  C07D471/14

CPC分类号： C07D491/147 ,  C07D471/04 ,  C07D471/14 ,  C07D491/14

摘要： A series of substituted fused tricyclic imidazole derivatives, in particular dihydro-1H-pyrano[4′,3′:4,5]imidazo[1,2-a]pyridine, 1,2,3,4-tetrahydroimidazo[1,2-a:5,4-c′]dipyridine, dihydro-1H-pyrano[3′,4′:4,5]imidazo[1,2-a]pyridine and tetrahydro-6H-cyclohepta[4,5]imidazo[1,2-a]pyridine, and analogs 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：US20160376290A1

公开(公告)日：2016-12-29

申请号：US15038986

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Mezher Hussein Ali ,  Julien Alistair Brown ,  Victoria Elizabeth Jackson

IPC分类号： C07D513/04 ,  A61K31/429

CPC分类号： C07D513/04 ,  A61K31/429 ,  A61K45/06 ,  A61K2300/00

摘要： A series of substituted imidazo[2,1-b]thiazole 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： 因此，一系列取代的咪唑并[2,1-b]噻唑衍生物及其类似物是人TNFα活性的有效调节剂，因此有益于治疗和/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。

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：US10087179B2

公开(公告)日：2018-10-02

申请号：US15101767

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Gareth Neil Brace ,  Julien Alistair Brown ,  Mark Daniel Calmiano ,  Prafulkumar Tulshibhai Chovatia ,  Michael Deligny ,  Ellen Olivia Gallimore ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  Malcolm MacCoss ,  Joanna Rachel Quincey ,  Yogesh Anil Sabnis ,  Dominique Louis Léon Swinnen ,  Zhaoning Zhu ,  Uwe Heinelt ,  Volkmar Wehner

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61K31/437

摘要： A series of fused tricyclic imidazole derivatives, in particular dihydro-1H-cyclopenta[4,5]imidazo[1,2-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：US20160304470A1

公开(公告)日：2016-10-20

申请号：US15101283

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Gregory Foulkes ,  Martin Clive Hutchings ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  James Thomas Reuberson ,  Sarah Margaret Rook ,  Zhaoning Zhu

IPC分类号： C07D239/74 ,  C07D215/14 ,  A61K31/47 ,  C07D241/42 ,  A61K31/472 ,  C07D237/28 ,  A61K31/502 ,  C07D403/04 ,  A61K31/506 ,  C07D217/16 ,  A61K31/517 ,  A61K31/498

CPC分类号： C07D239/74 ,  A61K31/47 ,  A61K31/472 ,  A61K31/498 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K45/06 ,  C07D215/06 ,  C07D215/14 ,  C07D217/16 ,  C07D237/28 ,  C07D237/32 ,  C07D241/42 ,  C07D241/44 ,  C07D403/04 ,  A61K2300/00

摘要： A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, 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，含有两个融合的六元环的一系列取代的杂芳族化合物（tivity）在治疗和/或预防各种人类疾病中有益，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：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.

公开(公告)号：US20160304530A1

公开(公告)日：2016-10-20

申请号：US15101798

申请日：2014-12-08

申请人： UCB BIOPHARMA SPRL

发明人： Rikki Peter Alexander ,  Julien Alistair Brown ,  Michael Deligny ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Sophie Jadot ,  Boris Kroeplien ,  Malcolm Mac Coss ,  Yogesh Anil Sabnis ,  Dominique Louis Léon Swinnen ,  Nathalie Van Houtvin ,  Zhaoning Zhu

IPC分类号： C07D491/147 ,  C07D471/04 ,  C07D471/14

CPC分类号： C07D491/147 ,  C07D471/04 ,  C07D471/14 ,  C07D491/14

摘要： A series of substituted fused tricyclic imidazole derivatives, in particular dihydro-1H-pyrano[4′,3′:4,5]imidazo[1,2-a]pyridine, 1,2,3,4-tetrahydroimidazo[1,2-a:5,4-c′]dipyridine, dihydro-1H-pyrano[3′,4′:4,5]imidazo[1,2-a]pyridine and tetrahydro-6H-cyclohepta[4,5]imidazo[1,2-a]pyridine, and analogues thereof, being potent modulators of human TNF 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： 一系列取代的稠合三环咪唑衍生物，特别是二氢-1H-吡喃并[4'，3'：4,5]咪唑并[1,2-a]吡啶，1,2,3,4-四氢咪唑并[1,2 -a：5,4-c']二吡啶，二氢-1H-吡喃并[3'，4'：4,5]咪唑并[1,2-a]吡啶和四氢-6H-环庚并[4,5]咪唑并[ 1,2-a]吡啶及其类似物是人TNF活性的有效调节剂，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。