公开(公告)号：US20200055883A1

公开(公告)日：2020-02-20

申请号：US16486954

申请日：2018-02-16

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: C07F9/6587

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

公开(公告)号：US20180237468A1

公开(公告)日：2018-08-23

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

CPC classification number: C07H21/02 ,  A61K31/7084 ,  A61P31/04 ,  A61P35/02 ,  A61P37/04 ,  C07F9/6587 ,  C07H21/00

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

公开(公告)号：US20180002342A1

公开(公告)日：2018-01-04

申请号：US15707412

申请日：2017-09-18

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

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

IPC: C07D493/22 ,  C07D407/14 ,  C07D307/28 ,  C07D407/06 ,  C07F7/18 ,  C07D493/14

CPC classification number: C07D493/22 ,  C07D307/28 ,  C07D407/06 ,  C07D407/14 ,  C07D493/14 ,  C07F7/1804

Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.