公开(公告)号：US20210323972A1

公开(公告)日：2021-10-21

申请号：US16605424

申请日：2018-05-07

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

Inventor： Ikuo Kushida ,  Yoko Ito ,  Masaaki Matsuda

IPC: C07D491/147

Abstract: The present invention provides a crystal of the compound represented by formula (I) having applicability as a drug substance of pharmaceuticals.

公开(公告)号：US20210177802A1

公开(公告)日：2021-06-17

申请号：US17180107

申请日：2021-02-19

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

Inventor： Taro Semba ,  Yasuhiro Funahashi

IPC: A61K31/357 ,  A61P35/04 ,  C07K16/28

Abstract: Disclosed herein is a method for treating tumor, comprising administering a liposomal composition comprising eribulin or a pharmaceutically acceptable salt thereof and a PD-1 antagonist to a patient in need thereof.

公开(公告)号：US10981929B2

公开(公告)日：2021-04-20

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：US10934307B2

公开(公告)日：2021-03-02

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.

公开(公告)号：US20210023047A1

公开(公告)日：2021-01-28

申请号：US16835719

申请日：2020-03-31

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

Inventor： Taro Semba ,  Yasuhiro Funahashi

IPC: A61K31/357 ,  C07K16/28 ,  A61P35/04

Abstract: Disclosed herein is a method for treating tumor, comprising administering a liposomal composition comprising eribulin or a pharmaceutically acceptable salt thereof and a PD-1 antagonist to a patient in need thereof

公开(公告)号：US10889866B2

公开(公告)日：2021-01-12

申请号：US15755225

申请日：2016-08-30

Applicant: 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: C12Q1/6886 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/55 ,  C12Q1/02 ,  C12Q1/6806 ,  C12Q1/6841

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：US20200347050A1

公开(公告)日：2020-11-05

申请号：US16845594

申请日：2020-04-10

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

Inventor： Roch BOIVIN ,  Eric CARLSON ,  Atsushi ENDO ,  Hans HANSEN ,  Lynn D. HAWKINS ,  Sally ISHIZAKA ,  Matthew MACKEY ,  Sridhar NARAYAN ,  Takashi SATOH ,  Shawn SCHILLER

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/55

Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.

公开(公告)号：US10822410B2

公开(公告)日：2020-11-03

申请号：US15821296

申请日：2017-11-22

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

Inventor： Daniel John O'Shannessy ,  Elizabeth B. Somers

IPC: A61K39/395 ,  C07K16/28 ,  G01N33/82 ,  A61P35/00 ,  G01N33/574

Abstract: Described herein are antibodies, and antigen-binding fragments thereof, that are specific for folate receptor alpha, related polynucleotides, expression vectors, and cells that express the described antibodies. Also provided are methods of using the described antibodies, and antigen-binding fragments thereof, and related kits to detect folate receptor alpha. Provided herein are also methods for diagnosing folate receptor alpha-expressing cancers using the described antibodies, and antigen-binding fragments thereof. The methods involve determining the amount of folate receptor alpha in a sample derived from a subject and comparing this level with the level of folate receptor alpha in a control sample or reference sample.

公开(公告)号：US10822307B2

公开(公告)日：2020-11-03

申请号：US16559293

申请日：2019-09-03

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

Inventor： Taiju Nakamura ,  Taichi Abe ,  Yusuke Miyashita ,  Hirofumi Kuroda ,  Yusuke Ayata ,  Atsushi Akao

IPC: C07D215/48 ,  A61P35/00 ,  A61K31/47

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

公开(公告)号：US20200341014A1

公开(公告)日：2020-10-29

申请号：US16078557

申请日：2017-03-16

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

Inventor： Mai Kimura ,  Sotaro Motoi ,  Takashi Obara ,  Katsuhiro Moriya ,  Hideaki Ogasawara ,  Yoshihisa Arita ,  Tetsu Kawano

IPC: G01N33/92 ,  C12Q1/6883

Abstract: The present invention provides a method for evaluating the pharmacological action of HGF that utilizes a PD marker in which fluctuation is recognized by administration of hepatocyte growth factor (HGF) in a broader range of subjects. A method for evaluating the pharmacodynamic action of HGF is provided. The aforementioned evaluation method is characterized in that it comprises a step of measuring the ApoA4 level in a biological sample collected from a test subject who was administered HGF. According to the present invention, a kit for evaluating the pharmacodynamic action of HGF comprising an anti-ApoA4 antibody is further provided.