公开(公告)号：EP4048399A1

公开(公告)日：2022-08-31

申请号：EP20880270.2

申请日：2020-10-23

申请人： ONO Pharmaceutical Co., Ltd. ,  Vanderbilt University

发明人： LINDSLEY, Craig W ,  ENGERS, Darren W ,  CHILDRESS, Elizabeth S ,  BOLLINGER, Sean R ,  SCHMITT, Joza ,  CHOPKO, Trevor C ,  DENTON, Jerod S ,  TANAKA, Motoyuki ,  KURATA, Haruto

IPC分类号： A61P21/00 ,  A61P21/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  C07C237/40 ,  C07C237/42 ,  C07C271/28 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D213/75

公开(公告)号：EP4048659A1

公开(公告)日：2022-08-31

申请号：EP20878092.4

申请日：2020-10-23

申请人： ONO Pharmaceutical Co., Ltd. ,  Vanderbilt University

发明人： LINDSLEY, Craig W ,  ENGERS, Darren W ,  CHILDRESS, Elizabeth S ,  BOLLINGER, Sean R ,  SCHMITT, Joza ,  GARRISON, Aaron T ,  PERRY, Charles K ,  DENTON, Jerod S ,  TANAKA, Motoyuki

IPC分类号： C07D309/34 ,  C07D333/10 ,  C07D307/02 ,  C07D231/02 ,  C07D231/56 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55

公开(公告)号：EP3702357A1

公开(公告)日：2020-09-02

申请号：EP20170445.9

申请日：2015-12-09

申请人： ONO Pharmaceutical Co., Ltd.

发明人： TANAKA, Motoyuki ,  KONDO, Takashi ,  HIROOKA, Yasuo ,  NISHIYAMA, Taihei ,  HIRAMATSU, Atsushi ,  KODA, Tomoyuki ,  KOUYAMA, Sho

IPC分类号： C07D471/04 ,  A61K31/444 ,  A61P7/02 ,  A61P43/00

摘要： A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：EP3231803A1

公开(公告)日：2017-10-18

申请号：EP15867764.1

申请日：2015-12-09

申请人： ONO Pharmaceutical Co., Ltd.

发明人： TANAKA, Motoyuki ,  KONDO, Takashi ,  HIROOKA, Yasuo ,  NISHIYAMA, Taihei ,  HIRAMATSU, Atsushi ,  KODA, Tomoyuki ,  KOUYAMA, Sho

IPC分类号： C07D471/04 ,  A61K31/444 ,  A61P7/02 ,  A61P43/00

CPC分类号： C07D471/04 ,  A61K9/20 ,  A61K31/444 ,  A61K31/519 ,  A61P43/00 ,  C07D487/04

摘要： A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

摘要翻译： 由通式（I）表示的化合物（其中所有符号如说明书中所定义）或其盐，溶剂合物，N-氧化物形式或前药是有效的FXIa抑制剂，在血液中具有优异的口服吸收特性和动力学， 在口服给药后长时间发挥有效的抗凝血活性，并且其抗凝血活性与其CYP抑制活性之间具有差异。 因此，化合物或其盐，溶剂合物，N-氧化物形式或其前药可以用作血管闭塞性疾病的有效预防和/或治疗剂。