公开(公告)号：US20130211103A1

公开(公告)日：2013-08-15

申请号：US13733562

申请日：2013-01-03

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

Inventor： Roch Boivin ,  Silvio A. Campagna ,  Hong Du ,  Francis G. Fang ,  Thomas Horstmann ,  Charles-Andre Lemelin ,  Jing Li ,  Pamela McGuinness ,  Xiang Niu ,  Matthew J. Schnaderbeck ,  Kevin (kuo-ming) Wu ,  Xiaojie (jeff) Zhu

IPC: C07D313/00 ,  C07D317/30

CPC classification number: C07D313/00 ,  C07D317/22 ,  C07D317/24 ,  C07D317/30 ,  C07D319/08 ,  C07D493/04 ,  Y02P20/55

Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.

Abstract translation: 本文公开了可用于制备大环内酯类的方法和中间体，例如其中R 1 -R 12如本文所定义的式（IV）化合物。

公开(公告)号：US10316040B2

公开(公告)日：2019-06-11

申请号：US15768668

申请日：2016-10-14

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 ,  Frank 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：US20180193478A1

公开(公告)日：2018-07-12

申请号：US15892921

申请日：2018-02-09

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

Inventor： Earl F. Albone ,  Xin Cheng ,  Daniel W. Custar ,  Keiji Furuuchi ,  Jing Li ,  Utpal Majumder ,  Toshimitsu Uenaka

IPC: A61K47/68 ,  C07K16/28 ,  C07K16/32 ,  A61K31/357

CPC classification number: A61K47/6803 ,  A61K31/357 ,  A61K47/6849 ,  A61K47/6889 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32 ,  C07K2317/14 ,  C07K2317/40 ,  C07K2317/565 ,  C07K2317/77 ,  C07K2317/92

Abstract: Linker toxins and antibody-drug conjugates that bind to human oncology antigen targets such as folate receptor alpha and/or provide anti-tubulin drug activity are disclosed. The linker toxins and antibody-drug conjugates comprise an eribulin drug moiety and can be internalized into target antigen-expressing cells. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the antibody-drug conjugates provided herein.

公开(公告)号：US09802953B2

公开(公告)日：2017-10-31

申请号：US15092850

申请日：2016-04-07

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

Inventor： Charles E. Chase ,  Atsushi Endo ,  Francis G. Fang ,  Jing Li

IPC: C07D493/22 ,  C07D307/28 ,  C07D307/33 ,  C07D493/08 ,  C07D493/18 ,  C07D493/20 ,  C07D493/04

CPC classification number: C07D493/20 ,  C07D307/20 ,  C07D307/26 ,  C07D307/28 ,  C07D307/33 ,  C07D309/16 ,  C07D405/06 ,  C07D405/14 ,  C07D493/04 ,  C07D493/08 ,  C07D493/18 ,  C07D493/22 ,  Y02P20/55

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

公开(公告)号：US10548986B2

公开(公告)日：2020-02-04

申请号：US15448497

申请日：2017-03-02

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

Inventor： Earl F. Albone ,  Xin Cheng ,  Daniel W. Custar ,  Keiji Furuuchi ,  Jing Li ,  Utpal Majumder ,  Toshimitsu Uenaka

IPC: A61K47/68 ,  C07K16/30 ,  A61K31/357 ,  C07K16/28 ,  C07K16/32

Abstract: Linker toxins and antibody-drug conjugates that bind to human oncology antigen targets such as folate receptor alpha and/or provide anti-tubulin drug activity are disclosed. The linker toxins and antibody-drug conjugates comprise an eribulin drug moiety and can be internalized into target antigen-expressing cells. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the antibody-drug conjugates provided herein.