公开(公告)号：US20220380352A1

公开(公告)日：2022-12-01

申请号：US17661909

申请日：2022-05-03

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

Inventor： Ermira PAZOLLI ,  Silvia BUONAMICI ,  Thiwanka SAMARAKOON ,  Sudeep PRAJAPATI ,  Nathan FISHKIN ,  James PALACINO ,  Michael SEILER ,  Ping ZHU ,  Andrew COOK ,  Peter SMITH ,  Xiang LIU ,  Shelby ELLERY ,  Dominic REYNOLDS ,  Lihua YU ,  Zhenhua WU ,  Shouyong PENG ,  Nicholas CALANDRA ,  Megan SHEEHAN ,  Yonghong XIAO

IPC: C07D405/12 ,  A61P35/00 ,  A61K47/68 ,  A61K47/60 ,  A61K9/127 ,  A61K9/51 ,  A61K31/365 ,  A61K31/496 ,  A61K39/00 ,  A61K39/395 ,  A61K45/06 ,  C07D313/00 ,  C07D405/06 ,  C07K16/24 ,  C07K16/28 ,  C07K16/30 ,  C07K16/32 ,  C07K16/40 ,  C12Q1/6886 ,  G01N33/50 ,  G01N33/574

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

公开(公告)号：US20210163456A1

公开(公告)日：2021-06-03

申请号：US17045952

申请日：2019-04-08

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

Inventor： Gregg F. KEANEY ,  John WANG ,  Baudouin GERARD ,  Kenzo ARAI ,  Xiang LIU ,  Guo Zhu ZHENG ,  Kazunobu KIRA ,  Lisa A. MARCAURELLE ,  Marta NEVALAINEN ,  Ming-Hong HAO ,  Morgan Welzel O'SHEA ,  Parcharee TIVITMAHAISOON ,  Sudeep PRAJAPATI ,  Touping LUO ,  Nicholas C. GEARHART ,  Jason T. LOWE ,  Yoshihiko KOTAKE ,  Satoshi NAGAO ,  Regina Mikie KANADA SONOBE ,  Masayuki MIYANO ,  Norio MURAI ,  Andrew COOK ,  Shelby ELLERY ,  Atsushi ENDO ,  James PALACINO ,  Dominic REYNOLDS

IPC: C07D407/06 ,  C07D405/14 ,  A61P35/00 ,  C07D313/00 ,  C07D491/107 ,  C07D487/08 ,  C07D487/10 ,  A61K45/06 ,  C07D405/12 ,  C07D417/12 ,  C07D413/12

Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

公开(公告)号：US20180141913A1

公开(公告)日：2018-05-24

申请号：US15821367

申请日：2017-11-22

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

Inventor： Mark BOCK ,  Ming-Hong HAO ,  Manav KORPAL ,  Vijay Kumar NYAVANANDI ,  Xiaoling PUYANG ,  Susanta SAMAJDAR ,  Peter Gerard SMITH ,  John WANG ,  Guo Zhu ZHENG ,  Ping ZHU ,  Lorna Helen MITCHELL ,  Nicholas LARSEN ,  Nathalie RIOUX ,  Sudeep PRAJAPATI ,  Dominic REYNOLDS ,  Morgan O'SHEA ,  Thiwanka SAMARAKOON

IPC: C07D231/56 ,  C07D401/14 ,  C07D401/10 ,  C07D413/12 ,  C07D413/14 ,  A61P35/00

CPC classification number: C07D231/56 ,  A61P35/00 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.