公开(公告)号：US20240060068A1

公开(公告)日：2024-02-22

申请号：US18256428

申请日：2021-12-10

Applicant: Francis G. FANG ,  Dai-Shik KIM ,  Hyeong Wook CHOI ,  Yoshinori TAKAHASHI ,  Kenji KIKUTA ,  Hikaru KAWASHIMA ,  Toshiki KUROKAWA ,  Tamaki HOSHIKAWA ,  Mingde SHAN ,  John WANG ,  Eisai R&D Management Co., Ltd.

Inventor： Francis G. Fang ,  Dae-Shik Kim ,  Hyeong Wook Choi ,  Yoshinori Takahashi ,  Kenji Kikuta ,  Hikaru Kawashima ,  Wataru Itano ,  Toshiki Kurokawa ,  Tamaki Hoshikawa ,  Mingde SHAN ,  John Wang

IPC: C12N15/113 ,  C07H21/04

CPC classification number: C12N15/113 ,  C07H21/04 ,  C12N2310/341 ,  C12N2310/3233 ,  C12N2310/315

Abstract: Gapmers or pharmaceutically acceptable salt of the gapmers and methods of making the gapmers are provided. The gapmers include a gap region that contains deoxyribonucleosides linked to each other by phosphorothioate bonds, a 5′ wing region positioned at the 5′ end of the gap region that contains morpholino monomers linked to each other by phosphorodiamidate bonds, and a 3′ wing region positioned at the 3′ end of the gap region that contains morpholino monomers linked to each other by phosphorodiamidate bonds. Antisense oligonucleotides are also provided. These antisense oligonucleotides are useful in the preparation of gapmers for inhibition of Tau mRNA transcription.

公开(公告)号：US11339188B2

公开(公告)日：2022-05-24

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：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.

公开(公告)号：US20140309429A1

公开(公告)日：2014-10-16

申请号：US14316321

申请日：2014-06-26

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

Inventor： Branko Mitasev ,  Dae-Shik Kim ,  Huiming Zhang ,  Christopher N. Farthing

IPC: C07D498/04

CPC classification number: C07D307/22 ,  C07D498/04 ,  C07D513/04

Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.

Abstract translation: 提供了可用于制备可用作β-位淀粉样蛋白前体蛋白（APP）消除酶抑制剂的化合物的化合物和方法。