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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。
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公开(公告)号:US20180273525A1
公开(公告)日:2018-09-27
申请号:US15762454
申请日:2016-09-28
Inventor: Helen Tracey Horsley , James Madden , James Thomas Reuberson , Julian Hugh Rowley
CPC classification number: C07D471/04 , A61K2121/00 , A61P29/00 , A61P31/12 , A61P33/06 , A61P35/00 , A61P37/06
Abstract: A series of substituted pyrido[3,2-d]pyrimidine and 1,5-naphthyridine derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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公开(公告)号:US09969748B2
公开(公告)日:2018-05-15
申请号:US15318422
申请日:2015-06-11
Inventor: Daniel James Ford , Qiuya Huang , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC: A61K31/519 , A01N43/90 , C07D498/04 , C07D487/04 , C07D495/04
CPC classification number: C07D498/04 , A61K31/519 , C07D487/04 , C07D495/04
Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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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。
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公开(公告)号:US20150274748A1
公开(公告)日:2015-10-01
申请号:US14432842
申请日:2013-10-02
Inventor: Claire Louise Kulisa , Daniel Christopher Brookings , Daniel James Ford , Richard Jeremy Franklin , James Thomas Reuberson , Anant Ramrao Ghawalkar
IPC: C07D495/04
CPC classification number: C07D495/04 , A61K31/424 , C07D413/14
Abstract: Compounds of formula (I) i.e. monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives substituted by an optionally substituted oxazolin-2-yl moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
Abstract translation: 式(I)化合物,即被任选取代的恶唑啉-2-基部分取代的单环或双环二胺取代的噻吩并[2,3-d]嘧啶和异噻唑并[5,4-d]嘧啶衍生物在治疗中是有益的 和/或预防各种人类疾病,包括炎症,自身免疫和肿瘤疾病; 病毒性疾病 和器官和细胞移植排斥反应。
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公开(公告)号:US10450320B2
公开(公告)日:2019-10-22
申请号:US16060486
申请日:2016-12-08
Applicant: UCB Biopharma SPRL , Katholieke Universiteit Leuven
IPC: C07D487/04 , A61K31/4985 , A61P31/12 , A61P37/06 , A61P33/06 , A61P29/00 , A61P35/00 , C07D519/00
Abstract: A series of 1,2,6,7,9,9a-hexahydropyrazino[1,2-d][1,2,4]triazin-4-one derivatives, substituted in the 8-position by an optionally substituted fused bicyclic heteroaromatic group, and in the 3-position by a range of functional groups, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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公开(公告)号:US20180201622A1
公开(公告)日:2018-07-19
申请号:US15924020
申请日:2018-03-16
Inventor: Daniel James Ford , Qiuya Huang , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC: C07D498/04 , C07D495/04 , A61K31/519 , C07D487/04
CPC classification number: C07D498/04 , A61K31/519 , C07D487/04 , C07D495/04 , Y02A50/411
Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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公开(公告)号:US10004737B2
公开(公告)日:2018-06-26
申请号:US15039092
申请日:2014-12-08
Applicant: UCB BIOPHARMA SPRL
Inventor: Julien Alistair Brown , Mark Daniel Calmiano , Elizabeth Pearl Jones , Boris Kroeplien , James Thomas Reuberson , Matthew Duncan Selby , Michael Alan Shaw , Zhaoning Zhu
IPC: A61K31/506 , A61K31/437 , A61K31/444 , A61K31/5377 , A61K31/4985 , C07D471/04 , C07D487/04 , C07D519/00 , A61K45/06
Abstract: A series of substituted benzimidazole, imidazo[1,2-α]pyridine and pyrazolo[1,5-α]pyridine derivatives, 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.
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公开(公告)号:US20170128445A1
公开(公告)日:2017-05-11
申请号:US15039092
申请日:2014-12-08
Applicant: UCB BIOPHARMA SPRL
Inventor: Julien Alistair Brown , Mark Daniel Calmiano , Elizabeth Pearl Jones , Boris Kroeplien , James Thomas Reuberson , Matthew Duncan Selby , Michael Alan Shaw , Zhaoning Zhu
IPC: A61K31/506 , A61K31/437 , A61K31/444 , C07D487/04 , A61K31/5377 , C07D471/04 , C07D519/00
CPC classification number: A61K31/506 , A61K31/437 , A61K31/444 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D487/04 , C07D519/00 , A61K2300/00
Abstract: A series of substituted benzimidazole, imidazo[1,2-α]pyridine and pyrazolo[1,5-α]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.
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公开(公告)号:US20170121337A1
公开(公告)日:2017-05-04
申请号:US15318507
申请日:2015-06-11
Inventor: Helen Tracey Horsley , Qiuya Huang , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC: C07D487/04
CPC classification number: C07D487/04 , A61K31/495 , A61K31/53 , C07D403/04
Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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