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公开(公告)号：US10202405B2
公开(公告)日：2019-02-12
申请号：US15513357
申请日：2015-10-02
申请人： UCB Biopharma SPRL , Sanofi
发明人： 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分类号： 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
摘要： 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.
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公开(公告)号：US20170305932A1
公开(公告)日：2017-10-26
申请号：US15513357
申请日：2015-10-02
申请人： UCB Biopharma SPRL , Sanofi
发明人： 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分类号： C07D519/00 , C07D495/18 , C07D487/18 , C07D491/18 , C07F7/18 , C07D513/18
CPC分类号： 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
摘要： 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.
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公开(公告)号：US09932343B2
公开(公告)日：2018-04-03
申请号：US15102003
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： 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分类号： 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分类号： C07D487/04 , A61K31/4188 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： 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.
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4.发明申请公开(公告)号：US20160304530A1
公开(公告)日：2016-10-20
申请号：US15101798
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： 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分类号： C07D491/147 , C07D471/04 , C07D471/14
CPC分类号： C07D491/147 , C07D471/04 , C07D471/14 , C07D491/14
摘要： 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.
摘要翻译： 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。
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5.发明申请公开(公告)号：US20160304523A1
公开(公告)日：2016-10-20
申请号：US15102003
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： 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分类号： C07D487/04 , C07D519/00 , C07D513/04 , C07D471/04 , C07D498/04
CPC分类号： C07D487/04 , A61K31/4188 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US10087179B2
公开(公告)日：2018-10-02
申请号：US15101767
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： 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分类号： C07D471/04 , C07D519/00 , A61K31/437
摘要： 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.
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公开(公告)号：US09890174B2
公开(公告)日：2018-02-13
申请号：US15101798
申请日：2014-12-08
申请人： UCB BIOPHARMA SPRL
发明人： 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分类号： C07D491/14 , C07D471/04 , A61K31/437 , A61K31/4375 , C07D491/147 , C07D471/14
CPC分类号： C07D491/147 , C07D471/04 , C07D471/14 , C07D491/14
摘要： 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.
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公开(公告)号：US10906919B2
公开(公告)日：2021-02-02
申请号：US16220847
申请日：2018-12-14
申请人： UCB Biopharma SRL , Sanofi
发明人： 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分类号： 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
摘要： 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.
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公开(公告)号：US11912721B2
公开(公告)日：2024-02-27
申请号：US17102790
申请日：2020-11-24
申请人： UCB Biopharma SRL , Sanofi
发明人： 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分类号： 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分类号： 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
摘要： 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.
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公开(公告)号：US20210155637A1
公开(公告)日：2021-05-27
申请号：US17102790
申请日：2020-11-24
申请人： UCB Biopharma SRL , Sanofi
发明人： 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分类号： 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
摘要： 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.
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