公开(公告)号：US20210230177A1

公开(公告)日：2021-07-29

申请号：US16628504

申请日：2018-07-06

Applicant: President and Fellows of Harvard College ,  Eisai R&D Management Co., LTD.

Inventor： Yoshito Kishi ,  Yanran Ai ,  Ning Ye ,  Qiaoyi Wang ,  Kenzo Yahata ,  Kentaro Iso ,  Santhosh Reddy Naini ,  Shuji Yamashita ,  Jihoon Lee ,  Isao Ohashi ,  Takashi Fukuyama

IPC: C07D493/22

Abstract: The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A)

公开(公告)号：US20210198282A1

公开(公告)日：2021-07-01

申请号：US17058406

申请日：2019-08-14

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

Inventor： Jun NIIJIMA ,  Hirofumi KURODA ,  So YASUI ,  Yoko ITO ,  Ikuo KUSHIDA

IPC: C07D519/00

Abstract: The present invention provides crystals of (1R,3R,15E,28R,29R,30R,31R,34R,36R,39S,41R)-29,41-Difluoro-34,39-bis(sulfanyl)-2,33,35,38, 40,42-hexaoxa-4,6,9,11,13,18,20,22,25,27-decaaza-34λ5,39λ5-diphosphaoctacyclo[28.6.4.13,36.128,31.04,8.07,12.019,24.023,27]dotetraconta-5,7,9,11,15,19,21,23,25-nonaene-34,39-dione (Compound (I)) ammonium salts, Compound (I) sodium salts, or Compound (I), possessing a potential to be used as drug substance in pharmaceuticals.

公开(公告)号：US20210188867A1

公开(公告)日：2021-06-24

申请号：US17188819

申请日：2021-03-01

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., Homer-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：US20210177837A1

公开(公告)日：2021-06-17

申请号：US17046528

申请日：2019-04-11

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

Inventor： Andrew COOK ,  Dominic REYNOLDS ,  Cheng ZHONG ,  Ryan BRAWN ,  Shelby ELLERY ,  Thiwanka SAMARAKOON ,  Xiang LIU ,  Sudeep PRAJAPATI ,  Megan SHEEHAN ,  Jason T. LOWE ,  James PALACINO

IPC: A61K31/496 ,  A61K9/00 ,  A61K39/395 ,  A61K38/21 ,  A61K38/20 ,  A61K38/19 ,  C07D313/00 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D413/14 ,  C07D498/08 ,  C07D491/107 ,  C07D407/12 ,  C07D417/10 ,  C07D413/10 ,  C07D487/04 ,  C07D453/02 ,  C07D405/14 ,  C07D413/12 ,  C07D409/12 ,  C07D471/10 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/541 ,  A61K31/506 ,  A61K31/551 ,  A61K31/5386 ,  A61P35/00

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

公开(公告)号：US11034769B1

公开(公告)日：2021-06-15

申请号：US17145001

申请日：2021-01-08

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

Inventor： Eiji Inoue ,  Akio Yamada ,  Tomomi Kawakatsu ,  Toshio Imai ,  Maki Deguchi ,  Aki Nakatani

IPC: C07K16/28 ,  A61K39/395 ,  A61P25/28 ,  C12N15/00 ,  C12N15/63 ,  A61K39/00 ,  C12N15/62

Abstract: Provided is an anti-EphA4 antibody that can bind to EphA4 and enhance the cleavage of EphA4, as well as a pharmaceutical composition comprising the antibody as the active ingredient.
A mouse anti-EphA4 antibody that has binding affinity towards EphA4 and can enhance the cleavage of EphA4 was obtained, and the sequence of the complementarity-determining region (CDR) of the mouse anti-EphA4 antibody was identified. Subsequently, the anti-EphA4 antibody of interest was obtained by producing a humanized antibody of the mouse anti-EphA4 antibody.

公开(公告)号：US20210171998A1

公开(公告)日：2021-06-10

申请号：US17159655

申请日：2021-01-27

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

Inventor： Jared Spidel ,  Earl Albone

IPC: C12P21/02 ,  C07K16/00 ,  A61K47/68

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

公开(公告)号：US10786511B2

公开(公告)日：2020-09-29

申请号：US15527375

申请日：2015-11-17

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

Inventor： Heike Keilhack ,  Brett Truitt ,  Yuta Suzuki ,  Tsukasa Murase ,  Futoshi Shikata

IPC: A61K31/5377 ,  A61K9/00 ,  A61K9/20 ,  A61K33/06 ,  A61K9/28

Abstract: The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

公开(公告)号：US20200299411A9

公开(公告)日：2020-09-24

申请号：US16345012

申请日：2017-10-26

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

Inventor： Andrew SATLIN ,  Tatsuto FUKUSHIMA

IPC: C07K16/44 ,  A61K31/542 ,  A61P25/28

Abstract: Methods and combination therapies for treating, preventing, and/or delaying the onset and/or development of Alzheimer's disease using an anti-Aβ protofibril antibody (such as, for example, BAN2401) and N-[3-((4aS,5R,7aS)-2-amino-5-methyl-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl]-5-difluoromethylpyrazine-2-carboxamide and/or a pharmaceutically acceptable salt thereof (Compound X) are provided.

公开(公告)号：US10765633B2

公开(公告)日：2020-09-08

申请号：US16713027

申请日：2019-12-13

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

Inventor： Hiroshi Ishihara ,  Katsura Hata ,  Hiroki Muto ,  Geoff Hird

IPC: A61K9/127 ,  A61K47/10 ,  A61K31/7024

Abstract: A formulation comprising liposomes, wherein the liposomes comprise, based on the liposome, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 0.5 to 3.0 mol % of a PEGylated phospholipid.

公开(公告)号：US20200268754A1

公开(公告)日：2020-08-27

申请号：US16819341

申请日：2020-03-16

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

Inventor： Margaret MOLINE ,  Gina PASTINO ,  Yurie AKIMOTO ,  Yasuhiro ZAIMA ,  Nobuya SUZUKI ,  Nobuo YOSHIDA

IPC: A61K31/506 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48

Abstract: In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.