公开(公告)号：US20200299321A1

公开(公告)日：2020-09-24

申请号：US16781352

申请日：2020-02-04

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

Inventor： Dae-Shik KIM ,  Frank FANG ,  Atsushi ENDO ,  Hyeong-wook CHOI ,  Ming-Hong HAO ,  Xingfeng BAO ,  Kuan-Chun HUANG

IPC: C07H21/02 ,  A61P35/02 ,  A61K31/7084 ,  C07F9/6587 ,  C07H21/00 ,  A61P31/04 ,  A61P37/04

Abstract: Provided herein are compounds useful for the treatment of cancer.

公开(公告)号：US20200297860A1

公开(公告)日：2020-09-24

申请号：US16702720

申请日：2019-12-04

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.

公开(公告)号：US20200216488A1

公开(公告)日：2020-07-09

申请号：US16616693

申请日：2018-06-14

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

Inventor： Yoshinori Takahashi ,  Yuta Suzuki

IPC: C07H21/02 ,  C07H21/04

Abstract: The present invention provides a modified nucleic acid monomer compound having a specific backbone such as 2-ethylglycerol or methoxymethyl-1,3-propanediol backbone instead of a ribose or deoxyribose backbone of a nucleoside, and an oligonucleic acid analogue containing the monomer compound as at least one of building blocks. The oligonucleic acid analogue containing the nucleic acid monomer compound of the present invention allows provision of an oligonucleic acid analogue having excellent biological stability and/or target gene silencing activity.

公开(公告)号：US20200206222A1

公开(公告)日：2020-07-02

申请号：US16717080

申请日：2019-12-17

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

Inventor： Dominic REYNOLDS ,  Ming-Hong HAO ,  John WANG ,  Sudeep PRAJAPATI ,  Takashi SATOH ,  Anand SELVARAJ

IPC: A61K31/505 ,  A61K31/5377 ,  A61K31/506

Abstract: Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.

公开(公告)号：US20200179382A1

公开(公告)日：2020-06-11

申请号：US16300335

申请日：2017-05-11

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

Inventor： Carsten T. Beuckmann ,  Margaret Moline ,  Andrew Satlin

IPC: A61K31/506 ,  A61P25/28 ,  A61P25/20

Abstract: Methods of treating irregular sleep-wake rhythm disorder in subjects and compositions for use in the same are disclosed.

公开(公告)号：US10562888B2

公开(公告)日：2020-02-18

申请号：US15566527

申请日：2016-04-13

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

Inventor： George Moniz ,  Kristen Sanders ,  Arani Chanda ,  Kenshi Yoshida

IPC: C07D403/12 ,  A61K31/505

Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.

公开(公告)号：US10526603B1

公开(公告)日：2020-01-07

申请号：US16354916

申请日：2019-03-15

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

Inventor： Yuta Suzuki ,  Sotaro Motoi ,  Yoshinori Takahashi ,  Kazuhiro Tahara

IPC: C12N15/113 ,  A61P7/00

Abstract: Provided is a novel double-stranded ribonucleic acid for suppressing expression of complement C5. A double-stranded ribonucleic acid comprising a combination of sense strand and antisense strand, wherein the combination of the sense strand and antisense strand are selected from the group consisting of combinations: SEQ ID NO: 13/14, SEQ ID NO: 159/160, SEQ ID NO: 115/116, SEQ ID NO: 117/118, SEQ ID NO: 119/120, SEQ ID NO: 121/122, SEQ ID NO: 123/124, SEQ ID NO: 125/126, SEQ ID NO: 127/128, SEQ ID NO: 129/130, SEQ ID NO: 131/132, SEQ ID NO: 133/134, SEQ ID NO: 137/138, SEQ ID NO: 139/140, SEQ ID NO: 141/142, SEQ ID NO: 143/144, SEQ ID NO: 145/146, SEQ ID NO: 147/148, SEQ ID NO: 149/150, SEQ ID NO: 151/152, and SEQ ID NO: 153/154.

公开(公告)号：US10517861B2

公开(公告)日：2019-12-31

申请号：US14890207

申请日：2014-05-12

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

Inventor： Yasuhiro Funahashi ,  Tadashi Kadowaki ,  Pallavi Sachdev

IPC: A61K31/47 ,  G01N33/574

Abstract: Biomarkers are provided that predict whether a subject having endometrial cancer will or will not respond to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). 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 an endometrial cancer.

公开(公告)号：US10457698B2

公开(公告)日：2019-10-29

申请号：US15750087

申请日：2016-08-05

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

Inventor： Atsushi Endo ,  Robert T. Yu ,  Francis Fang ,  Hyeong Wook Choi ,  Mingde Shan

IPC: C07D413/00 ,  C07F9/6561 ,  C07F9/6558 ,  C07H21/00 ,  A61K31/7088

Abstract: A method of preparation of stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs) of one of the following general formulas is provided:

公开(公告)号：US10450324B2

公开(公告)日：2019-10-22

申请号：US16031629

申请日：2018-07-10

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

Inventor： Yongbo Hu ,  Huiming Zhang ,  Hiroyuki Chiba ,  Yuki Komatsu ,  Bryan M. Lewis

IPC: C07D493/22

Abstract: In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).