公开(公告)号：US09663486B2

公开(公告)日：2017-05-30

申请号：US14908164

申请日：2014-10-14

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Roch Boivin ,  Hans Hansen ,  Sally Ishizaka ,  Matthew Mackey ,  Shawn Schiller ,  Chikako Ogawa ,  Sridhar Narayan ,  Peter Bertinato ,  Gregory Berger ,  Atsushi Endo ,  Robert T. Yu ,  Lynn Hawkins

IPC: C07D401/02 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D417/14 ,  C07D401/04

CPC classification number: C07D401/02 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.

公开(公告)号：US10457698B2

公开(公告)日：2019-10-29

申请号：US15750087

申请日：2016-08-05

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07D413/00 ,  C07F9/6561 ,  C07F9/6558 ,  C07H21/00 ,  A61K31/7088

Abstract: A method of preparation of stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs) of one of the following general formulas is provided:

公开(公告)号：US20180222932A1

公开(公告)日：2018-08-09

申请号：US15750087

申请日：2016-08-05

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07F9/6561 ,  C07F9/6558

Abstract: We provide diastereomerically pure or substantially diastereomerically pure activated phosphoramidochloridate morpholino nucleosides, methods of their preparation, and methods of their use in stereospecific coupling for stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs).