公开(公告)号：US20200046723A1

公开(公告)日：2020-02-13

申请号：US16497217

申请日：2018-04-24

Applicant: UCB Biopharma SPRL ,  SANOFI

Inventor： Daniel Christopher Brookings ,  Teresa De Haro Garcia ,  Yann Foricher ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Malcolm Maccoss ,  Mengyang Xuan ,  Zhaoning Zhu

IPC: A61K31/55 ,  C07D487/18

Abstract: A compound of formula (I) as defined herein, 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：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：US09550737B2

公开(公告)日：2017-01-24

申请号：US14406848

申请日：2013-06-11

Applicant: UCB Biopharma SPRL

Inventor： Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Ellen Olivia Gallimore ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  Martin Alexander Lowe ,  Timothy John Norman ,  John Robert Porter ,  Joanna Rachel Quincey ,  James Thomas Reuberson ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Zhaoning Zhu ,  Anne Marie Foley

IPC: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D491/107 ,  C07D235/12 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D405/06

CPC classification number: C07D235/12 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/06 ,  C07D491/107

Abstract: A series of benzimidazole 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：US09475820B2

公开(公告)日：2016-10-25

申请号：US14414299

申请日：2013-07-05

Applicant: UCB Biopharma SPRL

Inventor： Jonathan Mark Bentley ,  Daniel Christopher Brookings ,  Julien Alistair Brown ,  Thomas Paul Cain ,  Laura Jane Gleave ,  Alexander Heifetz ,  Victoria Elizabeth Jackson ,  Craig Johnstone ,  Deborah Leigh ,  James Madden ,  John Robert Porter ,  Matthew Duncan Selby ,  Zhaoning Zhu

IPC: A61K31/4985 ,  C07D241/36 ,  C07D491/107 ,  C07D487/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5513 ,  C07D451/02 ,  C07D471/08

CPC classification number: C07D491/107 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5513 ,  C07D451/02 ,  C07D471/08 ,  C07D487/04

Abstract: A series of imidazo[1,2-a]pyrazine 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. The imidazo[1,2-a]pyrazine derivatives of the disclosure are of general formula

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：US10464932B2

公开(公告)日：2019-11-05

申请号：US16076387

申请日：2017-02-22

Applicant: UCB Biopharma SPRL

Inventor： Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Richard David Taylor ,  Zhaoning Zhu

IPC: C07D417/10 ,  C07D417/14 ,  A61P33/06

Abstract: A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US20190040053A1

公开(公告)日：2019-02-07

申请号：US16076387

申请日：2017-02-22

Applicant: UCB Biopharma SPRL

Inventor： Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Richard David Taylor ,  Zhaoning Zhu

IPC: C07D417/10 ,  C07D417/14 ,  A61P33/06

CPC classification number: C07D417/10 ,  A61P33/06 ,  C07D417/14

Abstract: A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US09815797B2

公开(公告)日：2017-11-14

申请号：US15101283

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

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

IPC: 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 classification number: 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

Abstract: 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：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：US20150203486A1

公开(公告)日：2015-07-23

申请号：US14414287

申请日：2013-07-05

Applicant: UCB Biopharma SPRL

Inventor： Jonathan Mark Bentley ,  Daniel Christopher Brookings ,  Julien Alistair Brown ,  Thomas Paul Cain ,  Praful Tulshi Chovatia ,  Anne Marie Foley ,  Ellen Olivia Gallimore ,  Laura Jane Gleave ,  Alexander Heifetz ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  Victoria Elizabeth Jackson ,  James Andrew Johnson ,  Craig Johnstone ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  Deborah Leigh ,  Martin Alexander Lowe ,  James Madden ,  John Robert Porter ,  Joanna Rachel Quincey ,  Laura Claire Reed ,  James Thomas Reuberson ,  Anthony John Richardson ,  Sarah Emily Richardson ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Zhaoning Zhu

IPC: C07D471/04 ,  A61K31/496 ,  A61K31/506 ,  C07D491/107 ,  A61K31/5377 ,  A61K31/5513 ,  A61K31/554 ,  A61K31/437 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5513 ,  A61K31/554 ,  C07D491/107 ,  C07D519/00

Abstract: A series of imidazo[1,2-a]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.

Abstract translation: 因此，作为人类TNFα活性的有效调节剂的一系列式（I）的咪唑并[1,2-a]吡啶衍生物因此有益于治疗和/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。