公开(公告)号：US20200283416A1

公开(公告)日：2020-09-10

申请号：US15774332

申请日：2016-11-24

Applicant: UCB Biopharma SPRL

Inventor： Rebecca Louise Charlton ,  Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Trevor Morgan ,  Richard David Taylor ,  Zhaoning Zhu

IPC: C07D403/10 ,  C07D471/04 ,  C07D417/10

Abstract: A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic 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：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：US20150152065A1

公开(公告)日：2015-06-04

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

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：US11136310B2

公开(公告)日：2021-10-05

申请号：US15774332

申请日：2016-11-24

Applicant: UCB Biopharma SPRL

Inventor： Rebecca Louise Charlton ,  Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Trevor Morgan ,  Richard David Taylor ,  Zhaoning Zhu

IPC: C07D403/10 ,  C07D417/10 ,  C07D471/04

Abstract: A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic 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：US10287299B2

公开(公告)日：2019-05-14

申请号：US15580059

申请日：2016-06-07

Applicant: UCB Biopharma SPRL

Inventor： Gareth Neil Brace ,  Prafulkumar Tulshibhai Chovatia ,  Gregory Foulkes ,  James Andrew Johnson ,  Severine Danielle Jones ,  Boris Kroeplien ,  Fabien Claude Lecomte ,  Pui Leng Loke ,  Martin Alexander Lowe ,  Ajay Mandal ,  Timothy John Norman ,  Christopher Francis Palmer ,  Yolanda Pérez-Fuertes ,  John Robert Porter ,  Donald Smyth ,  Giancarlo Trani ,  Muhammed Uddin ,  Zhaoning Zhu

IPC: A61K31/5365 ,  C07D265/36 ,  C07D498/04 ,  C07D401/06 ,  C07D413/06 ,  A61P27/02 ,  A61P3/00 ,  A61P9/00 ,  A61P23/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61K31/423 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/55 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

Abstract: A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, 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 neuradegenerative 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：US09309243B2

公开(公告)日：2016-04-12

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: C07D491/02 ,  C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/5513 ,  A61K31/554 ,  C07D491/107

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。

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.