公开(公告)号：US20220088212A1

公开(公告)日：2022-03-24

申请号：US17408003

申请日：2021-08-20

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

Inventor： Jared Spidel ,  Earl Albone

IPC: A61K47/68 ,  A61K47/60 ,  C07K16/00 ,  A61K49/00 ,  A61K51/10 ,  A61K49/16 ,  A61P31/00 ,  A61P35/00

Abstract: Provided herein are conjugated immunoglobulins and methods for generating conjugated immunoglobulins using a microbial transglutaminase.

公开(公告)号：US11267821B2

公开(公告)日：2022-03-08

申请号：US16807335

申请日：2020-03-03

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

Inventor： Yoshiaki Ohashi ,  Yoshihiko Norimine ,  Tamaki Hoshikawa ,  Yu Yoshida ,  Yoshihisa Kobayashi ,  Nobuhiro Sato ,  Koji Hagiwara ,  Nobuaki Sato ,  Shinsuke Hirota ,  Takaaki Harada ,  Hikaru Yoshimura

IPC: C07D495/22 ,  A61K31/551 ,  A61P25/00 ,  C07D491/22 ,  C07D491/147

Abstract: The present invention provides compounds represented by formulas (I) to (XVII) or pharmaceutically acceptable salts thereof:

公开(公告)号：US20220023285A1

公开(公告)日：2022-01-27

申请号：US17502962

申请日：2021-10-15

Applicant: MERCK SHARP & DOHME CORP. ,  EISAI R&D MANAGEMENT CO., LTD.

Inventor： Andrew Evan DENKER ,  Yu KATO ,  Kimiyo TABATA ,  Yusaku HORI

IPC: A61K31/47 ,  A61K39/395 ,  A61P35/00

Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a multi-RTK inhibitor, and the use of the combination therapies for the treatment of cancer. The multi-RTK inhibitor may be represented by Formula (I): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom. A tumor therapeutic agent is disclosed that combines a compound or pharmaceutically acceptable salt thereof represented by Formula I and an anti-PD-1 antibody.

公开(公告)号：US20220023275A1

公开(公告)日：2022-01-27

申请号：US17312077

申请日：2019-12-16

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

Inventor： Geoffrey S. HIRD ,  Ganesh S.P. BOMMAREDDY ,  Anjali JOSHI, Ph.D. ,  James MCSHANE

IPC: A61K31/444 ,  A61K47/40 ,  A61K9/19 ,  A61K9/08

Abstract: An aqueous pharmaceutical formulation of a solubilizing agent with a pyridone compound that is useful as an inhibitor to non-NMDA receptors, particularly to the AMPA receptor is disclosed herein. In some embodiments the pyridone compound is supersaturated in aqueous solution at pH between 6 and 8. The formulations are particularly useful as intravenous injections.

公开(公告)号：US20220017517A1

公开(公告)日：2022-01-20

申请号：US17376452

申请日：2021-07-15

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

Inventor： Yu YOSHIDA ,  Yoichi KITA ,  Makoto KOTAKE ,  Keiichi SORIMACHI ,  Toshiyuki OHFUSA ,  Takafumi MOTOKI ,  Taro ASABA

IPC: C07D471/08

Abstract: Provided are compounds represented by the following formulas (I), (II), (III) and (IV) having orexin type 2 receptor-activating activity, or their pharmaceutically acceptable salts.

公开(公告)号：US20210349097A1

公开(公告)日：2021-11-11

申请号：US17282193

申请日：2019-10-02

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

Inventor： Yasuhiro Funahashi ,  Yukinori Minoshima ,  Michio Kanekiyo ,  Masahiro Matsuki ,  Yusuke Adachi ,  Kotaro Kodama

IPC: G01N33/574 ,  A61P35/04 ,  A61K31/47 ,  A61K31/436 ,  C12Q1/6886

Abstract: Biomarkers are provided that predict whether a human subject having a renal cell carcinoma is responsive to a combination therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate) and everolimus. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for and treating a subject having, suspected of having, or at risk of developing a renal cell carcinoma.

公开(公告)号：US20210346371A1

公开(公告)日：2021-11-11

申请号：US17059876

申请日：2019-05-31

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

Inventor： Ermira PAZOLLI ,  Silvia BUONAMICI ,  James PALACINO ,  Michael SEILER ,  Ping ZHU ,  Evan BARRY ,  Lihua YU

IPC: A61K31/496 ,  A61K39/395 ,  A61K39/00 ,  A61K39/39 ,  A61K38/21 ,  A61K38/20 ,  A61K35/17 ,  A61K47/68 ,  A61K38/19

Abstract: This disclosure relates to methods for the treatment of neoplastic disorders by administering Compound 1, or a pharmaceutically acceptably salt thereof, on its own and/or as part of a conjugate or composition, and inducing production of at least one neoantigen.

公开(公告)号：US11147803B2

公开(公告)日：2021-10-19

申请号：US16607459

申请日：2018-05-30

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

Inventor： Mai Miyamoto ,  Sadaharu Kotani

IPC: A61K31/4745 ,  A61K31/4375 ,  A61P25/28 ,  A61K31/13

Abstract: There is provided a therapeutic agent for Alzheimer's disease for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (I): or a pharmaceutically acceptable salt thereof, and memantine represented by formula (II): or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20210299269A1

公开(公告)日：2021-09-30

申请号：US17059635

申请日：2019-05-31

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

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：US11083705B2

公开(公告)日：2021-08-10

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 ,  A61K9/127 ,  A61P35/00 ,  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.