公开(公告)号：US10245269B2

公开(公告)日：2019-04-02

申请号：US15837390

申请日：2017-12-11

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

Inventor： Kevin Wayne Kuntz ,  Kuan-Chun Huang ,  Hyeong Wook Choi ,  Kristen Sanders ,  Steven Mathieu ,  Arani Chanda ,  Francis Fang

IPC: A61K31/5377 ,  C07D405/12

Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.

公开(公告)号：US10238630B2

公开(公告)日：2019-03-26

申请号：US15314200

申请日：2015-05-28

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

Inventor： David Cox ,  Alton Kremer ,  Sharon McGonigle ,  Jiayi Wu

IPC: A61K31/357 ,  A61K31/555 ,  A61K31/519 ,  A61K45/06

Abstract: The invention features methods for treating cancer in a patient in need thereof by administering eribulin, in combination with one or more PARP inhibitors, and, optionally, a platinum-based antineoplastic drug, and kits therefor. The invention is based in part on the observation that combinations of eribulin mesylate, a PARP inhibitor (e.g., E7449), and, optionally, a platinum-based antineo-plastic drug (e.g., carboplatin), show improved (e.g., synergistic) antitumor effects. Therefore, the present invention features methods of preventing and treating cancer (e.g., homologous recombination (HR)-deficient cancer by the use of combinations of eribulin (e.g., eribulin mesylate) and one or more PARP inhibitors (e.g., E7449 or a pharmaceutically acceptable salt thereof (e.g., the tartrate salt), optionally in combination with a platinum-based antineoplastic drug (e.g., carboplatin).

公开(公告)号：US20190002588A1

公开(公告)日：2019-01-03

申请号：US16063515

申请日：2017-01-11

Applicant: National University Corporation Chiba University ,  Eisai R&D Management Co., Ltd.

Inventor： Toshinori Nakayama ,  Motoko Kimura ,  Koji Hayashizaki ,  Toshifumi Hirayama ,  Jungo Kakuta ,  Yoshimasa Sakamoto ,  Ryu Gejima ,  Daisuke Tokita ,  Kenzo Muramoto ,  Toshio Imai

IPC: C07K16/46 ,  A61P1/04 ,  A61P11/00 ,  A61P37/08 ,  A61P35/00 ,  C07K16/28

Abstract: The present invention provides an anti-Myl9 antibody or a Myl9 binding fragment thereof that binds to Myl9 and may inhibit the interaction between Myl9 and CD69 in humans, as well as a pharmaceutical composition comprising the same. A mouse anti-human/mouse Myl9 monoclonal antibody having binding affinity against Myl9 was obtained, and the sequence for the complementarity determining region (CDR) of said mouse anti-human/mouse Myl9 monoclonal antibody was identified. Accordingly, a humanized antibody comprising the CDR sequence of said mouse anti-human/mouse Myl9 monoclonal antibody in the variable region of heavy and light chains was produced.

公开(公告)号：US20190000829A1

公开(公告)日：2019-01-03

申请号：US15748980

申请日：2016-08-17

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

Inventor： Junji Matsui ,  Masahiro Matsuki ,  Akihiko Tsuruoka ,  Toshiyuki Tamai ,  Ryo Nakajima ,  Takuya Suzuki

IPC: A61K31/47 ,  A61P35/00 ,  A61K31/095

Abstract: A therapeutic agent for biliary tract cancer comprising 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide or a pharmacologically acceptable salt thereof is provided.

公开(公告)号：US20180354939A1

公开(公告)日：2018-12-13

申请号：US16108964

申请日：2018-08-22

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

Inventor： J. Eric Carlson ,  Hans Hansen ,  Lynn Hawkins ,  Sally Ishizaka ,  Matthew Mackey ,  Shawn Schiller ,  Chikako Ogawa ,  Heather Davis ,  Atsushi Endo

IPC: C07D417/14 ,  C07D403/14 ,  C07D413/04 ,  C07D401/10 ,  C07D401/14 ,  C07D471/10 ,  C07D487/10 ,  C07D471/04 ,  C07D215/48 ,  C12Q1/6897 ,  G01N33/50 ,  C07D451/04 ,  C07D487/04 ,  C07D493/10 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07B2200/07 ,  C07D215/48 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D493/10 ,  C12Q1/6897 ,  G01N33/5023 ,  G01N33/5047

Abstract: Embodiments of the disclosure relate to selectively substituted quinolone 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：US20180318422A1

公开(公告)日：2018-11-08

申请号：US16038710

申请日：2018-07-18

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

Inventor： Kentaro Nagane ,  Yosuke Ueki ,  Shusuke Sano ,  Takahisa Sakaguchi

IPC: A61K47/02 ,  A61K9/10 ,  A61K31/47 ,  A61K9/00

CPC classification number: A61K47/02 ,  A61K9/0095 ,  A61K9/10 ,  A61K31/47

Abstract: The present invention provides a method for suppressing bitterness of a quinoline derivative.

公开(公告)号：US20180303933A1

公开(公告)日：2018-10-25

申请号：US15951321

申请日：2018-04-12

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

Inventor： Nobuyuki Yasuda ,  Kiyoshi Oketani ,  Hiroko Baba ,  Tomohisa Nakano ,  Masahiko Mori

IPC: A61K39/395 ,  A61K9/00 ,  A61P1/00

CPC classification number: A61K39/3955 ,  A61K9/0019 ,  A61K2039/54 ,  A61K2039/545 ,  A61P1/00

Abstract: It is an object of the present invention to provide a pharmaceutical composition comprising an anti-fractalkine antibody that provides therapeutically effective improvement to Crohn's disease, after the administration thereof to a human subject, and a method for treating Crohn's disease. Provided is a pharmaceutical composition for treating Crohn's disease. The present pharmaceutical composition comprises an anti-fractalkine antibody and a pharmaceutically acceptable excipient, and is used, such that the anti-fractalkine antibody is intravenously administered to a human at a dose of at least 10 mg/kg of human body weight in a method for treating Crohn's disease.

公开(公告)号：US20180263998A1

公开(公告)日：2018-09-20

申请号：US15516567

申请日：2015-10-08

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

Inventor： Yasuhiro Zaima ,  Kazuo Kazama ,  Shuntaro Arase ,  Kentaro Nagane ,  Kanta Horie ,  Yosuke Ueki

IPC: A61K31/542

CPC classification number: A61K31/542 ,  A61K9/2018 ,  A61K9/2054 ,  A61P25/28

Abstract: The present invention provides a pharmaceutical composition comprising a compound represented by formula (1): or 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, or a pharmaceutically acceptable salt of the foregoing, and a salt of a compound having a C12-22 saturated aliphatic hydrocarbon group.

公开(公告)号：US10065930B2

公开(公告)日：2018-09-04

申请号：US15328166

申请日：2015-08-03

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

Inventor： Yuzo Watanabe

IPC: C07D239/34

CPC classification number: C07D239/34 ,  C07D239/36

Abstract: There are provided a method for producing 2,4-disubstituted pyrimidine-5-ol, and particularly, 2,4-dimethylpyrimidine-5-ol and an intermediate thereof used in industrial production. The production method according to the present invention includes a step of producing 2,4-disubstituted pyrimidine-5-ol according to a hydrolysis reaction of a 2,4-disubstituted-5-(4-(nitrophenyl)oxy)pyrimidine compound and is suitable for industrial production since an inexpensive and easily available starting material can be used, regioselectivity of a substituent group is easily controlled, impurities are easily controlled, and 2,4-disubstituted pyrimidine-5-ol can be produced without using reagents and intermediates causing health problems, risks and the like.

公开(公告)号：US10030032B2

公开(公告)日：2018-07-24

申请号：US15638493

申请日：2017-06-30

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).