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.

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.

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：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。

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。