公开(公告)号：EP3201196A1

公开(公告)日：2017-08-09

申请号：EP15771976.6

申请日：2015-10-02

申请人： UCB Biopharma SPRL ,  SANOFI

发明人： DE HARO GARCIA, Teresa ,  DELIGNY, Michael ,  HEER, Jag Paul ,  QUINCEY, Joanna Rachel ,  XUAN, Mengyang ,  ZHU, Zhaoning ,  BROOKINGS, Daniel Christopher ,  CALMIANO, Mark Daniel ,  EVRARD, Yves ,  HUTCHINGS, Martin Clive ,  JOHNSON, James Andrew ,  JADOT, Sophie ,  KEYAERTS, Jean ,  MAC COSS, Malcolm ,  SELBY, Matthew Duncan ,  SHAW, Michael Alan ,  SWINNEN, Dominique Louis Léon ,  SCHIO, Laurent ,  FORICHER, Yann ,  FILOCHE-ROMME, Bruno

IPC分类号： C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  A61K31/4188 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00

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 ,  C07F7/1852

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.

摘要翻译： 一系列稠合的五环咪唑衍生物是人TNFα活性的有效调节剂，因此在治疗和/或预防各种人类疾病中是有益的，所述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; 疼痛和伤害性疼痛; 心血管疾病; 代谢紊乱; 眼病; 和肿瘤疾病。 特别地，本发明涉及6,7-二氢-7,14-亚甲基苯并咪唑并[1,2-b] [2,5]苯并二氮杂-5（14H） - 酮衍生物及其类似物。

公开(公告)号：EP3080121B1

公开(公告)日：2019-09-04

申请号：EP14816158.1

申请日：2014-12-08

申请人： UCB Biopharma SPRL

发明人： ALEXANDER, Rikki Peter ,  CALMIANO, Mark Daniel ,  DEFAYS, Sabine ,  DURIEU, Véronique ,  DELIGNY, Michael ,  HEER, Jag Paul ,  JACKSON, Victoria Elizabeth ,  KEYAERTS, Jean ,  KROEPLIEN, Boris ,  MAC COSS, Malcolm ,  SABNIS, Yogesh Anil ,  SELBY, Matthew Duncan ,  SWINNEN, Dominique Louis Léon ,  VAN HOUTVIN, Nathalie ,  ZHU, Zhaoning ,  WEHNER, Volkmar ,  HEINELT, Uwe

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61P29/00

公开(公告)号：EP3080114B1

公开(公告)日：2019-10-02

申请号：EP14808659.8

申请日：2014-12-08

申请人： UCB Biopharma SPRL

发明人： ALEXANDER, Rikki Peter ,  BROWN, Julien Alistair ,  DELIGNY, Michael ,  HEER, Jag Paul ,  JACKSON, Victoria Elizabeth ,  JADOT, Sophie ,  KROEPLIEN, Boris ,  MAC COSS, Malcolm ,  SABNIS, Yogesh Anil ,  SWINNEN, Dominique Louis Léon ,  VAN HOUTVIN, Nathalie ,  ZHU, Zhaoning

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  C07D471/14 ,  C07D491/14

公开(公告)号：EP3080113A1

公开(公告)日：2016-10-19

申请号：EP14808658.0

申请日：2014-12-08

申请人： UCB Biopharma SPRL

发明人： ALEXANDER, Rikki Peter ,  BRACE, Gareth Neil ,  BROWN, Julien Alistair ,  CALMIANO, Mark Daniel ,  CHOVATIA, Praful Tulshi ,  DELIGNY, Michael ,  GALLIMORE, Ellen Olivia ,  HEER, Jag, Paul ,  JACKSON, Victoria Elizabeth ,  KROEPLIEN, Boris ,  MAC COSS, Malcolm ,  QUINCEY, Joanna, Rachel ,  SABNIS, Yogesh, Anil ,  SWINNEN, Dominique, Louis, Léon ,  ZHU, Zhaoning ,  WEHNER, Volkmar ,  HEINELT, Uwe

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D519/00

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.

摘要翻译： 因此，一系列稠合的三环咪唑衍生物，特别是二氢-1H-环戊[4,5]咪唑并[1,2-a]吡啶衍生物及其类似物是人TNFα活性的有效调节剂， 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; 疼痛和伤害性疼痛; 心血管疾病; 代谢紊乱; 眼病; 和肿瘤疾病。

公开(公告)号：EP3080121A1

公开(公告)日：2016-10-19

申请号：EP14816158.1

申请日：2014-12-08

申请人： UCB Biopharma SPRL

发明人： ALEXANDER, Rikki Peter ,  CALMIANO, Mark Daniel ,  DEFAYS, Sabine ,  DURIEU, Véronique ,  DELIGNY, Michael ,  HEER, Jag Paul ,  JACKSON, Victoria Elizabeth ,  KEYAERTS, Jean ,  KROEPLIEN, Boris ,  MAC COSS, Malcolm ,  SABNIS, Yogesh Anil ,  SELBY, Matthew Duncan ,  SWINNEN, Dominique Louis Léon ,  VAN HOUTVIN, Nathalie ,  ZHU, Zhaoning ,  WEHNER, Volkmar ,  HEINELT, Uwe

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61P29/00

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.

公开(公告)号：EP3080114A1

公开(公告)日：2016-10-19

申请号：EP14808659.8

申请日：2014-12-08

申请人： UCB Biopharma SPRL

发明人： ALEXANDER, Rikki Peter ,  BROWN, Julien Alistair ,  DELIGNY, Michael ,  HEER, Jag Paul ,  JACKSON, Victoria Elizabeth ,  JADOT, Sophie ,  KROEPLIEN, Boris ,  MAC COSS, Malcolm ,  SABNIS, Yogesh Anil ,  SWINNEN, Dominique Louis Léon ,  VAN HOUTVIN, Nathalie ,  ZHU, Zhaoning

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  C07D471/14 ,  C07D491/14

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.