公开(公告)号：US10717743B2

公开(公告)日：2020-07-21

申请号：US16284405

申请日：2019-02-25

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

Inventor： Charles E. Chase ,  Atsushi Endo ,  Francis G. Fang ,  Jing Li

IPC: C07D493/20 ,  C07D307/28 ,  C07D307/33 ,  C07D493/08 ,  C07D493/18 ,  C07D493/04 ,  C07D493/22 ,  C07D307/20 ,  C07D307/26 ,  C07D309/16 ,  C07D405/06 ,  C07D405/14

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

公开(公告)号：US20190100513A1

公开(公告)日：2019-04-04

申请号：US15529798

申请日：2016-11-17

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

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Nicholas C. Gearhart ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Silvia Buonamici ,  Lihua Yu ,  Eunice Sun Park ,  Betty Chan ,  Peter G. Smith ,  Michael P. Thomas ,  Ermira Pazolli ,  Kian Huat Lim ,  Atsushi Endo ,  Arani Chanda

IPC: C07D405/14 ,  A61P35/02

Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.

公开(公告)号：US20180273532A1

公开(公告)日：2018-09-27

申请号：US15841767

申请日：2017-12-14

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 ,  A61K31/55 ,  C07D487/04 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K31/55 ,  C07D487/04 ,  Y02P20/582

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：US09856276B2

公开(公告)日：2018-01-02

申请号：US15196600

申请日：2016-06-29

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

Inventor： Atsushi Endo ,  Charles E. Chase ,  Francis G. Fang

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

公开(公告)号：US11339188B2

公开(公告)日：2022-05-24

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：US11136335B2

公开(公告)日：2021-10-05

申请号：US16313196

申请日：2017-06-30

Applicant: 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：US10246480B2

公开(公告)日：2019-04-02

申请号：US15898533

申请日：2018-02-17

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：US10087174B2

公开(公告)日：2018-10-02

申请号：US15670904

申请日：2017-08-07

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

Inventor： J. Eric Carlson ,  Lynn Hawkins ,  Sally Ishizaka ,  Shawn Schiller ,  Chikako Ogawa ,  Atsushi Endo

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/04 ,  C07D215/48 ,  C07D471/04 ,  C07D487/10 ,  C07D471/10 ,  C07D401/14 ,  C07D401/10 ,  C07D403/14 ,  C07D451/04 ,  C07D487/04 ,  C07D493/10 ,  C12Q1/6897 ,  G01N33/50

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：US11926619B2

公开(公告)日：2024-03-12

申请号：US17045952

申请日：2019-04-08

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

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Lisa A. Marcaurelle ,  Marta Nevalainen ,  Ming-Hong Hao ,  Morgan Welzel O'Shea ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Tuoping Luo ,  Nicholas C. Gearhart ,  Jason T. Lowe ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Andrew Cook ,  Shelby Ellery ,  Atsushi Endo ,  James Palacino ,  Dominic Reynolds

IPC: C07D407/12 ,  A61K31/365 ,  A61K31/4427 ,  A61K31/497 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

CPC classification number: C07D407/06 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

公开(公告)号：US20180354939A1

公开(公告)日：2018-12-13

申请号：US16108964

申请日：2018-08-22

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

Inventor： J. Eric Carlson ,  Hans Hansen ,  Lynn Hawkins ,  Sally Ishizaka ,  Matthew Mackey ,  Shawn Schiller ,  Chikako Ogawa ,  Heather Davis ,  Atsushi Endo

IPC: C07D417/14 ,  C07D403/14 ,  C07D413/04 ,  C07D401/10 ,  C07D401/14 ,  C07D471/10 ,  C07D487/10 ,  C07D471/04 ,  C07D215/48 ,  C12Q1/6897 ,  G01N33/50 ,  C07D451/04 ,  C07D487/04 ,  C07D493/10 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07B2200/07 ,  C07D215/48 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D493/10 ,  C12Q1/6897 ,  G01N33/5023 ,  G01N33/5047

Abstract: Embodiments of the disclosure relate to selectively substituted quinolone 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.