公开(公告)号：US10775385B2

公开(公告)日：2020-09-15

申请号：US15736614

申请日：2015-10-22

Applicant: UCB Biopharma SPRL

Inventor： James Philip O'Connell ,  John Robert Porter ,  Alastair Lawson ,  Boris Kroeplien ,  Stephen Edward Rapecki ,  Timothy John Norman ,  Graham John Warrellow ,  Tracy Lynn Arakaki ,  Alex Buntin Burgin ,  William Ross Pitt ,  Mark Daniel Calmiano ,  David Andreas Schubert ,  Daniel John Lightwood ,  Rebecca Jayne Wootton

IPC: G01N33/68 ,  C07K14/525 ,  C07K14/705 ,  C07K16/24 ,  A61P37/00 ,  C07D401/14 ,  C07D471/00 ,  C07D213/72 ,  C07D235/04 ,  C07D239/26 ,  C07D471/04 ,  A61K47/64 ,  A61P35/00

Abstract: A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.

公开(公告)号：US20190298859A1

公开(公告)日：2019-10-03

申请号：US16337243

申请日：2017-09-27

Applicant: UCB Biopharma SPRL

Inventor： Terence Seward Baker ,  Michael Anthony William Eaton ,  Timothy John Norman ,  James Petrie Turner

IPC: A61K48/00 ,  C07F9/10 ,  C07F9/117 ,  C07F9/12 ,  C07J51/00

Abstract: Compounds of formula (I), wherein Ar is an aryl group optionally further substituted with one or more groups R3; A is a lipophilic, hydrophobic moiety; R1 is a phosphodiester, phosphotriester, thioether or amide group; X is an unsubstituted or substituted C6 to C24 alkylene or alkenylene group, which is optionally interrupted by one or more —NR9—, —O— or —S— linkages, R2 is —YC(R4)(R5)CO2R6; and pharmaceutically acceptable salts or solvates thereof are useful as endosomolytic agents particularly for the delivery of nucleic acids useful in gene therapy.

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：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：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：US20180134728A1

公开(公告)日：2018-05-17

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

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

Abstract: A series of substituted 3,4-di-hydro-2H-.1,4-benzoxazin-3-one 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.