公开(公告)号：US10906919B2

公开(公告)日：2021-02-02

申请号：US16220847

申请日：2018-12-14

Applicant: UCB Biopharma SRL ,  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 ,  C07D491/08 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  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：US10766906B2

公开(公告)日：2020-09-08

申请号：US16086414

申请日：2017-03-31

Applicant: UCB Biopharma SRL ,  Sanofi

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

IPC: C07D487/22 ,  C07D487/18 ,  C07D487/04

Abstract: Disclosed are substituted fused hexacyclic benzimidazole derivatives of Formula (I) wherein the variables A, B, D, X, M, Q, n, p, q, Z, E, R5, and R12 are defined herein. These compounds are potent modulators of human TNFα activity and 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：US10669286B2

公开(公告)日：2020-06-02

申请号：US16086418

申请日：2017-03-31

Applicant: UCB Biopharma SRL ,  Sanofi

Inventor： Michael Louis Robert Deligny ,  Jag Paul Heer

IPC: C07D487/04 ,  C07D519/00 ,  C07D487/18 ,  C07D487/22 ,  A61P25/28 ,  A61P37/04 ,  A61P9/00 ,  A61P3/10 ,  A61P35/00

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：US11912721B2

公开(公告)日：2024-02-27

申请号：US17102790

申请日：2020-11-24

Applicant: UCB Biopharma SRL ,  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 MacCoss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC: C07D519/00 ,  C07D491/08 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  C07D495/18 ,  C07D513/18 ,  C07F7/18 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55

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：US20220073485A1

公开(公告)日：2022-03-10

申请号：US17299137

申请日：2019-11-27

Applicant: UCB Biopharma SRL

Inventor： Anne Marie Foley ,  Jag Paul Heer ,  Fabien Claude Lecomte ,  Nathaniel Julius Thomas Monck ,  Matthew Duncan Selby ,  Mengyang Xuan ,  Lihu Yang

IPC: C07D309/04 ,  C07D413/14

Abstract: A series of functionalised amine derivatives of formula (I) as defined herein, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

公开(公告)号：US20210155637A1

公开(公告)日：2021-05-27

申请号：US17102790

申请日：2020-11-24

Applicant: UCB Biopharma SRL ,  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 ,  C07D491/08 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  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：US10953019B2

公开(公告)日：2021-03-23

申请号：US16487988

申请日：2018-03-14

Applicant: UCB Biopharma SRL ,  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：US10669263B2

公开(公告)日：2020-06-02

申请号：US16349734

申请日：2017-12-08

Applicant: UCB Biopharma SRL

Inventor： Jag Paul Heer

IPC: A61K31/506 ,  A61K31/4184 ,  C07D403/04 ,  A61P37/00 ,  A61P25/28 ,  A61P3/00 ,  A61P9/00 ,  A61P37/08 ,  A61P29/00 ,  A61P35/00

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：US10654861B2

公开(公告)日：2020-05-19

申请号：US16086408

申请日：2017-03-31

Applicant: UCB Biopharma SRL ,  Sanofi

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

IPC: C07D487/18 ,  C07D487/04

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：US10793578B2

公开(公告)日：2020-10-06

申请号：US16086311

申请日：2017-03-31

Applicant: UCB Biopharma SRL ,  Sanofi

Inventor： Jag Paul Heer ,  Jean Keyaerts

IPC: C07D487/18 ,  C07D487/04 ,  C07D487/22 ,  A61P25/28 ,  A61P37/04 ,  A61P3/00 ,  A61P9/00

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.