公开(公告)号：US20220195437A1

公开(公告)日：2022-06-23

申请号：US17643807

申请日：2021-12-10

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

Inventor： Dae-Shik KIM ,  Hyeong-Wook CHOI ,  Francis G. FANG ,  Yoshinori TAKAHASHI ,  Kenji KIKUTA ,  Hikaru YOSHIMURA ,  Wataru ITANO ,  Toshiki KUROKAWA ,  Ryo DAIRIKI ,  Zhi ZHOU ,  Mingde SHAN

IPC: C12N15/113 ,  A61K31/712 ,  A61P25/28

Abstract: Antisense oligonucleotides are provided. These antisense oligonucleotides are useful in the preparation of gapmers for inhibition of Tau mRNA transcription. Inhibition of Tau mRNA transcription may result in decrease of amounts of Tau protein in a subject, allowing treatment of diseases and disorders related to expression of Tau, including Alzheimer's disease and primary tauopathies.

公开(公告)号：US20200299321A1

公开(公告)日：2020-09-24

申请号：US16781352

申请日：2020-02-04

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：US20190308992A1

公开(公告)日：2019-10-10

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：US20190144463A1

公开(公告)日：2019-05-16

申请号：US16246999

申请日：2019-01-14

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

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：US20210188867A1

公开(公告)日：2021-06-24

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

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：US20160264594A1

公开(公告)日：2016-09-15

申请号：US15033970

申请日：2014-11-04

Applicant: Francis G. FANG ,  Eisai R&D Management Co., Ltd.

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

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

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.

Abstract translation: 本发明提供了通过大环化策略合成干燥蛋白或其药学上可接受的盐（例如甲磺酸艾美林）的方法。 本发明的大环化策略涉及使非大环中间体进行碳 - 碳键形成反应（例如，烯化反应（例如，Homer-Wadsworth-Emmons烯化），Dieckmann反应，催化闭环烯烃复分解， 或Nozaki-Hiyama-Kishi反应），得到大环中间体。 本发明还提供了用作合成干扰素或其药学上可接受的盐的中间体的化合物及其制备方法。

公开(公告)号：US20210205348A1

公开(公告)日：2021-07-08

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：US20190161495A1

公开(公告)日：2019-05-30

申请号：US16313196

申请日：2017-06-30

Applicant: Charles E. Chase ,  Hyeong-Wook CHOI ,  Atsushi ENDO ,  Francis G. FANG ,  Dae-Shik KIM ,  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：US20180118755A1

公开(公告)日：2018-05-03

申请号：US15571921

申请日：2016-05-09

Applicant: Francis G. FANG ,  Charles E. CHASE ,  EISAI R&D MANAGEMENT CO., LTD.

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

IPC: C07D493/22 ,  C07F9/655

CPC classification number: C07D493/22 ,  C07F9/6552

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.

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.