公开(公告)号：US20250163095A1

公开(公告)日：2025-05-22

申请号：US18842196

申请日：2023-03-01

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

Inventor： Praveen Kumar VEMULA ,  Hyeong Wook CHOI ,  Francis G. FANG ,  Mingde David SHAN

IPC: C07H19/173 ,  C07F9/6561

Abstract: Bis-protected, activated guanine monomers or pharmaceutically acceptable salts thereof for use in the synthesis of polymorpholino oligonucleotides and methods of making the bis-protected, activated guanine monomers are provided.

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：US20200055866A1

公开(公告)日：2020-02-20

申请号：US16521691

申请日：2019-07-25

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 ,  C07D313/00 ,  C07B57/00

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：US20190263826A1

公开(公告)日：2019-08-29

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

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

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.

公开(公告)号：US20160376294A1

公开(公告)日：2016-12-29

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: C07F7/18

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):