公开(公告)号：US11542269B2

公开(公告)日：2023-01-03

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 ,  C07D307/28 ,  C07D493/04 ,  C07D407/06 ,  C07D407/14 ,  A61P35/00

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：US11434246B2

公开(公告)日：2022-09-06

申请号：US17141557

申请日：2021-01-05

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

Inventor： Wanjun Zheng ,  Xiaojie Zhu ,  Hong Du ,  Maarten Postema ,  Yimin Jiang ,  Jing Li ,  Robert Yu ,  Hyeong-Wook Choi ,  Jaemoon Lee ,  Francis G. Fang ,  Daniel Custar

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.

公开(公告)号：US10913749B2

公开(公告)日：2021-02-09

申请号：US16387820

申请日：2019-04-18

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

Inventor： Francis G. Fang ,  Dae-Shik Kim ,  Hyeong-Wook Choi ,  Charles E. Chase

IPC: C07D493/22 ,  C07F9/655

Abstract: The invention provides methods for the synthesis of a halichondrin macrolides 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), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

公开(公告)号：US10308661B2

公开(公告)日：2019-06-04

申请号：US15571921

申请日：2016-05-09

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

Inventor： Francis G. Fang ,  Dae-Shik Kim ,  Hyeong-Wook Choi ,  Charles E. Chase

IPC: C07D493/22 ,  C07F9/655

Abstract: The invention provides methods for the synthesis of a halichondrin macrolides 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), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.