公开(公告)号：US09926313B2

公开(公告)日：2018-03-27

申请号：US15101089

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： Michael Louis Robert Deligny ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  John Robert Porter

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506

Abstract: 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.

公开(公告)号：US20190284170A1

公开(公告)日：2019-09-19

申请号：US16349734

申请日：2017-12-08

Applicant: UCB Biopharma SPRL

Inventor： Jag Paul Heer

IPC: C07D403/04

Abstract: 2-(5-{1-[2-(Difluoromethoxy)-6-fluorobenzyl]-2-methyl-1H-benzimidazol-6-yl}pyrimidin-2-yl)propan-2-ol, or a pharmaceutically acceptable salt 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：US10093652B2

公开(公告)日：2018-10-09

申请号：US15038287

申请日：2014-12-08

Applicant: UCB Biopharma SPRL

Inventor： Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  John Robert Porter

IPC: A61K35/28 ,  A01N1/02 ,  G01N33/569 ,  C12N5/0789 ,  C07D401/10 ,  C07D235/12 ,  A61K31/4439

Abstract: A series of substituted 4,5,6,7-tetrahydrobenzimidazole 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.

公开(公告)号：US09890174B2

公开(公告)日：2018-02-13

申请号：US15101798

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： 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: C07D491/14 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  C07D491/147 ,  C07D471/14

CPC classification number: C07D491/147 ,  C07D471/04 ,  C07D471/14 ,  C07D491/14

Abstract: 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：US20190112314A1

公开(公告)日：2019-04-18

申请号：US16086311

申请日：2017-03-31

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： Jag Paul Heer ,  Jean Keyaerts

IPC: C07D487/18 ,  C07D487/22

Abstract: A series of fused pentacyclic imidazole derivatives, being potent modulators of f 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 5,7,8,15-tetrahydro-6H-8,15- methanobenzimidazo[1,2-b][2,5]benzodiazocin-6-one derivatives and analogs thereof.

公开(公告)号：US20190100526A1

公开(公告)日：2019-04-04

申请号：US16086414

申请日：2017-03-31

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： Teresa De Haro Garcia ,  Michael Louis Robert Deligny ,  Jag Paul Heer ,  Helen Tracey Horsley ,  Sophie Jadot ,  Jean Keyaerts

IPC: C07D487/22

Abstract: A series of substituted fused hexacyclic benzimidazole 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：US09932343B2

公开(公告)日：2018-04-03

申请号：US15102003

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： 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: 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 classification number: C07D487/04 ,  A61K31/4188 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: 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

Applicant: UCB BIOPHARMA SPRL

Inventor： 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: C07D491/147 ,  C07D471/04 ,  C07D471/14

CPC classification number: C07D491/147 ,  C07D471/04 ,  C07D471/14 ,  C07D491/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160304523A1

公开(公告)日：2016-10-20

申请号：US15102003

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： 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: C07D487/04 ,  C07D519/00 ,  C07D513/04 ,  C07D471/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/4188 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160297795A1

公开(公告)日：2016-10-13

申请号：US15038287

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： Jag Paul Heer ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  John Robert Porter

IPC: C07D401/10 ,  A61K31/4439

CPC classification number: C07D401/10 ,  A61K31/4439 ,  C07D235/12

Abstract: A series of substituted 4,5,6,7-tetrahydrobenzimidazole 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.

Abstract translation: 因此，作为人类TNFα活性的有效调节剂的一系列取代的4,5,6,7-四氢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。