公开(公告)号：US20170240560A1

公开(公告)日：2017-08-24

申请号：US15501658

申请日：2015-08-04

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

Inventor： Francis G. FANG ,  Hyeong-Wook CHOI ,  Silvio CAMPAGNA ,  Steven MATHIEU

IPC: C07D493/22 ,  C07D313/00 ,  C07D493/08 ,  C07B57/00

CPC classification number: C07D493/22 ,  C07B57/00 ,  C07D313/00 ,  C07D493/08 ,  C07D493/18

Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

公开(公告)号：US20200331928A1

公开(公告)日：2020-10-22

申请号：US16959882

申请日：2019-01-03

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

Inventor： Hyeong-Wook CHOI ,  Francis G. FANG

IPC: C07D493/22

Abstract: The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

公开(公告)号：US20200223864A1

公开(公告)日：2020-07-16

申请号：US16833923

申请日：2020-03-30

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 ,  C07F7/18 ,  C07D407/14 ,  C07D307/28 ,  C07D407/06 ,  C07D493/14

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.

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：US20180186810A1

公开(公告)日：2018-07-05

申请号：US15906401

申请日：2018-02-27

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

Inventor： Francis G. FANG ,  Hyeong-Wook CHOI ,  Silvio CAMPAGNA ,  Steven MATHIEU

IPC: C07D493/22 ,  C07D493/18 ,  C07D493/08 ,  C07B57/00 ,  C07D313/00

CPC classification number: C07D493/22 ,  C07B57/00 ,  C07D313/00 ,  C07D493/08 ,  C07D493/18

Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.

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.