公开(公告)号：US20200022988A1

公开(公告)日：2020-01-23

申请号：US16487988

申请日：2018-03-14

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： Julien Alistair Brown ,  Daniel Christopher Brookings ,  Jag Paul Heer ,  James Andrew Johnson ,  Zhaoning Zhu

IPC: A61K31/55 ,  C07D471/22

Abstract: A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine 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：US20170305932A1

公开(公告)日：2017-10-26

申请号：US15513357

申请日：2015-10-02

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： 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: C07D519/00 ,  C07D495/18 ,  C07D487/18 ,  C07D491/18 ,  C07F7/18 ,  C07D513/18

CPC classification number: 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

Abstract: 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：US20160304513A1

公开(公告)日：2016-10-20

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 ,  A61K31/506 ,  A61K31/437

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：US10472362B2

公开(公告)日：2019-11-12

申请号：US15580137

申请日：2016-06-07

Applicant: UCB Biopharma SPRL

Inventor： Victoria Elizabeth Jackson ,  Jag Paul Heer ,  Uwe Heinelt

IPC: C07D487/04 ,  C07D491/147 ,  C07D491/04

Abstract: A series of substituted fused tricyclic imidazo pyrazine derivatives and analoges thereof, represented by 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：US10087179B2

公开(公告)日：2018-10-02

申请号：US15101767

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： 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: C07D471/04 ,  C07D519/00 ,  A61K31/437

Abstract: 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：US20160289228A1

公开(公告)日：2016-10-06

申请号：US15038239

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： Sabine Defays ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  James Andrew Johnson ,  Boris Kroeplien ,  John Robert Porter

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K2300/00

Abstract: 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.

Abstract translation: 因此，作为人TNFα活性的有效调节剂的一系列取代的5,6,7,8-四氢咪唑并[1,2-α]吡啶衍生物在治疗和/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：US20190119302A1

公开(公告)日：2019-04-25

申请号：US16086418

申请日：2017-03-31

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： Michael Louis Robert Deligny ,  Jag Paul Heer

IPC: C07D519/00 ,  C07D487/22

Abstract: A series of substituted fused pentacyclic 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：US20190100525A1

公开(公告)日：2019-04-04

申请号：US16086408

申请日：2017-03-31

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： Michael Louis Robert Deligny ,  Jag Paul Heer ,  Jean Keyaerts ,  Luce Elsa Lepissier ,  Martin Alexander Lowe

IPC: C07D487/18

Abstract: A series of substituted fused pentacyclic 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：US10202405B2

公开(公告)日：2019-02-12

申请号：US15513357

申请日：2015-10-02

Applicant: UCB Biopharma SPRL ,  Sanofi

Inventor： 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: 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

Abstract: 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：US09969728B2

公开(公告)日：2018-05-15

申请号：US15038239

申请日：2014-12-08

Applicant: UCB Biopharma SPRL

Inventor： Sabine Defays ,  Jag Paul Heer ,  Victoria Elizabeth Jackson ,  James Andrew Johnson ,  Boris Kroeplien ,  John Robert Porter

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4184

CPC classification number: C07D471/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K2300/00

Abstract: 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.