公开(公告)号：US10407439B2

公开(公告)日：2019-09-10

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 ,  C07D493/08 ,  C07D493/18 ,  C07B57/00 ,  C07D313/00

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：US12251394B2

公开(公告)日：2025-03-18

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：US10981929B2

公开(公告)日：2021-04-20

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：US10934307B2

公开(公告)日：2021-03-02

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：US11643418B2

公开(公告)日：2023-05-09

申请号：US17188819

申请日：2021-03-01

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

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., Homer-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：US10160768B2

公开(公告)日：2018-12-25

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

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：US09783549B2

公开(公告)日：2017-10-10

申请号：US15033970

申请日：2014-11-04

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

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., Homer-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：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：US10221189B2

公开(公告)日：2019-03-05

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

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.