公开(公告)号：US20210205348A1

公开(公告)日：2021-07-08

申请号：US17058817

申请日：2019-05-31

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

Inventor： Dae-Shik KIM ,  Frank FANG ,  Atsushi ENDO ,  Hyeong-Wook CHOI ,  Ming-Hong HAO ,  Xingfeng BAO ,  Kuan-Chun HUANG

IPC: A61K31/7084 ,  A61P35/04

Abstract: Provided herein are methods for the treatment of bladder cancer.

公开(公告)号：US20210171555A1

公开(公告)日：2021-06-10

申请号：US17082070

申请日：2020-10-28

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

Inventor： Atsushi ENDO ,  Robert T. YU ,  Francis FANG ,  Hyeong Wook CHOI ,  Mingde SHAN

IPC: C07F9/6561 ,  C07H21/00 ,  A61K31/7088 ,  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).

公开(公告)号：US20190161495A1

公开(公告)日：2019-05-30

申请号：US16313196

申请日：2017-06-30

Applicant: Charles E. Chase ,  Hyeong-Wook CHOI ,  Atsushi ENDO ,  Francis G. FANG ,  Dae-Shik KIM ,  EISAI R&D MANAGEMENT CO., LTD.

Inventor： Charles E. CHASE ,  Hyeong-Wook CHOI ,  Atsushi ENDO ,  Francis G. FANG ,  Dae-Shik KIM

IPC: C07D493/22

Abstract: The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.

公开(公告)号：US20160326161A1

公开(公告)日：2016-11-10

申请号：US15220949

申请日：2016-07-27

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

Inventor： Eric CARLSON ,  Hans HANSEN ,  Lynn HAWKINS ,  Sally ISHIZAKA ,  Matthew MACKEY ,  Shawn SCHILLER ,  Chikako OGAWA ,  Heather DAVIS ,  Atsushi ENDO

IPC: C07D417/14 ,  C07D413/04 ,  C07D471/10 ,  C12Q1/68 ,  C07D493/10 ,  C07D487/04 ,  C07D451/04 ,  G01N33/50 ,  C07D413/14 ,  C07D487/10

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：US20180162885A1

公开(公告)日：2018-06-14

申请号：US15840109

申请日：2017-12-13

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

Inventor： Atsushi ENDO ,  Charles E. CHASE ,  Francis G. FANG

IPC: C07F7/18 ,  C07D307/38 ,  C07D407/06 ,  C07D493/04 ,  C07D405/12 ,  C07D307/12 ,  C07D405/06

CPC classification number: C07F7/1804 ,  C07D307/12 ,  C07D307/38 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D493/04 ,  Y02P20/55

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):

公开(公告)号：US20160176841A1

公开(公告)日：2016-06-23

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

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：US20150225415A1

公开(公告)日：2015-08-13

申请号：US14624033

申请日：2015-02-17

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

Inventor： Charles E. CHASE ,  Atsushi ENDO ,  Francis G. FANG ,  Jing LI

IPC: C07D493/20 ,  C07D493/18 ,  C07D493/08 ,  C07D307/28 ,  C07D307/33

CPC classification number: C07D493/20 ,  C07D307/20 ,  C07D307/26 ,  C07D307/28 ,  C07D307/33 ,  C07D309/16 ,  C07D405/06 ,  C07D405/14 ,  C07D493/04 ,  C07D493/08 ,  C07D493/18 ,  C07D493/22 ,  Y02P20/55

Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.

公开(公告)号：US20200347050A1

公开(公告)日：2020-11-05

申请号：US16845594

申请日：2020-04-10

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

Inventor： Roch BOIVIN ,  Eric CARLSON ,  Atsushi ENDO ,  Hans HANSEN ,  Lynn D. HAWKINS ,  Sally ISHIZAKA ,  Matthew MACKEY ,  Sridhar NARAYAN ,  Takashi SATOH ,  Shawn SCHILLER

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/55

Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine 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：US20200299321A1

公开(公告)日：2020-09-24

申请号：US16781352

申请日：2020-02-04

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

Inventor： Dae-Shik KIM ,  Frank FANG ,  Atsushi ENDO ,  Hyeong-wook CHOI ,  Ming-Hong HAO ,  Xingfeng BAO ,  Kuan-Chun HUANG

IPC: C07H21/02 ,  A61P35/02 ,  A61K31/7084 ,  C07F9/6587 ,  C07H21/00 ,  A61P31/04 ,  A61P37/04

Abstract: Provided herein are compounds useful for the treatment of cancer.

公开(公告)号：US20150175620A1

公开(公告)日：2015-06-25

申请号：US14577417

申请日：2014-12-19

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

Inventor： Atsushi ENDO ,  Charles E. CHASE ,  Francis G. FANG

IPC: C07D493/04 ,  C07D307/38

CPC classification number: C07F7/1804 ,  C07D307/12 ,  C07D307/38 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D493/04 ,  Y02P20/55

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):

Abstract translation: 通常，本发明的特征在于可用于合成软骨素B的类似物的化合物，例如胡椒素或其药学上可接受的盐，例如甲磺酸埃布林。 示例性化合物具有式（I），（II）或（III）：