公开(公告)号：US11524009B2

公开(公告)日：2022-12-13

申请号：US16760313

申请日：2018-10-30

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

Inventor： Daniel Aird ,  Laura Corson ,  Ping Zhu ,  Markus Warmuth ,  Silvia Buonamici ,  Peter Gerard Smith ,  Peter Fekkes

IPC: A61K31/496 ,  A61P35/00 ,  A61K31/05 ,  A61K31/11 ,  A61K31/166 ,  A61K31/343 ,  A61K31/352 ,  A61K31/395 ,  A61K31/404 ,  A61K31/426 ,  A61K31/4355 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/5355

Abstract: The present disclosure provides pharmaceutical combinations comprising at least one spliceosome modulator and at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors. Also provided are methods of treating cancer comprising administering a therapeutically effective amount of at least one spliceosome modulator and a therapeutically effective amount of at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors.

公开(公告)号：US11352348B2

公开(公告)日：2022-06-07

申请号：US17247117

申请日：2020-11-30

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：US20220081486A1

公开(公告)日：2022-03-17

申请号：US17339549

申请日：2021-06-04

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

Inventor： Ryan Henry ,  Thiwanka Samarakoon ,  Nathan Fishkin ,  Ping Zhu ,  Ermira Pazolli ,  James Palacino ,  Juan C. Almagro

IPC: C07K16/28 ,  A61K47/68 ,  A61K47/60 ,  A61K47/65 ,  A61K45/06 ,  A61K39/395 ,  A61P35/00

Abstract: Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates (ADCs) such as those comprising a splicing modulator) that bind to BCMA are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering a composition provided herein.

公开(公告)号：US20200255415A1

公开(公告)日：2020-08-13

申请号：US16349479

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: C07D413/14 ,  A61P35/00 ,  C07D231/56 ,  C07D401/10 ,  C07D401/14 ,  C07D401/12 ,  C07D413/12 ,  C07D403/10

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.

公开(公告)号：US20180318312A1

公开(公告)日：2018-11-08

申请号：US15755225

申请日：2016-08-30

Applicant: Lihua YU ,  Kian Huat LIM ,  Jacob D. FEALA ,  Silvia BUONAMICI ,  Yoshiharu MIZUI ,  Peter G. SMITH ,  Ping ZHU ,  Eunice Sun PARK ,  Michael W. SEILER ,  Marco Peter FEKKES ,  Eisai R&D Management Co., Ltd.

Inventor： Lihua Yu ,  Kian Huat Lim ,  Jacob D. Feala ,  Silvia Buonamici ,  Yoshiharu Mizui ,  Peter G. Smith ,  Ping Zhu ,  Eunice Sun Park ,  Michael W. Seiler ,  Marco Peter Fekkes

IPC: A61K31/55 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/495 ,  C12Q1/6886 ,  C12Q1/02

CPC classification number: A61K31/55 ,  A61K31/4545 ,  A61K31/495 ,  A61P35/00 ,  C12Q1/025 ,  C12Q1/6806 ,  C12Q1/6841 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158

Abstract: Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.

公开(公告)号：US09796683B2

公开(公告)日：2017-10-24

申请号：US15167373

申请日：2016-05-27

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

IPC: A01N43/40 ,  A61K31/44 ,  C07D231/56 ,  C07D403/12 ,  C07D471/14 ,  C07D403/06 ,  C07D401/06 ,  C07D401/14

CPC classification number: C07D231/56 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D471/14

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.