公开(公告)号：US20180162885A1

公开(公告)日：2018-06-14

申请号：US15840109

申请日：2017-12-13

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

Inventor： Atsushi ENDO ,  Charles E. CHASE ,  Francis G. FANG

IPC: C07F7/18 ,  C07D307/38 ,  C07D407/06 ,  C07D493/04 ,  C07D405/12 ,  C07D307/12 ,  C07D405/06

CPC classification number: C07F7/1804 ,  C07D307/12 ,  C07D307/38 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D493/04 ,  Y02P20/55

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):

公开(公告)号：US09981040B2

公开(公告)日：2018-05-29

申请号：US14390854

申请日：2013-04-17

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

Inventor： Yosuke Ueki

IPC: A61K47/38 ,  A61K47/26 ,  A61K47/36 ,  A61K31/675 ,  A61K47/32 ,  A61K9/48 ,  A61K31/661 ,  A61K47/02

CPC classification number: A61K47/38 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4891 ,  A61K31/661 ,  A61K31/675 ,  A61K47/02 ,  A61K47/26 ,  A61K47/32 ,  A61K47/36

Abstract: An object of the present invention is to provide a capsule formulation comprising a phosphonooxymethyl derivative of ravuconazole which suppresses delay in dissolution due to storage regardless of an encapsulated amount of the phosphonooxymethyl derivative of ravuconazole. The present invention provides a capsule formulation comprising an encapsulated material comprising {[(1R,2R)-2-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-1-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propyl]oxy}methyl dihydrogen phosphate or a pharmacologically acceptable salt thereof, or a solvate of any of the foregoing, and a capsule shell not comprising gelatin.

公开(公告)号：US09957392B2

公开(公告)日：2018-05-01

申请号：US15010612

申请日：2016-01-29

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

Inventor： Hideki Hayashi ,  Masanori Fujinami ,  Taro Toyota ,  Yutaka Tamura ,  Akira Aoki ,  Yutaka Muraki ,  Kazuki Onoue

IPC: C09B23/08 ,  A61K49/00 ,  C07D209/60 ,  A61K9/127

CPC classification number: C09B23/083 ,  A61K9/127 ,  A61K49/0032 ,  A61K49/0034 ,  A61K49/0084 ,  C07D209/60 ,  C09B23/086

Abstract: Disclosed is a near-infrared fluorescent imaging agent comprising an indocyanine-based fluorescent dye and a liposome. The near-infrared fluorescent imaging agent of the present invention demonstrates high fluorescence intensity and a long anchoring time in sentinel lymph nodes, thereby making it useful for detecting sentinel lymph nodes in sentinel lymph node navigation surgery. Also disclosed is an indocyanine green derivative that is particularly suitable for use in the near-infrared fluorescent imaging agent of the present invention.

公开(公告)号：US20180111988A1

公开(公告)日：2018-04-26

申请号：US15791674

申请日：2017-10-24

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

Inventor： Nobuyuki Yasuda ,  Fumitoshi Tago ,  Hiroko Baba ,  Tomohisa Nakano ,  Masahiko Mori

IPC: C07K16/24 ,  A61P19/02

CPC classification number: C07K16/24 ,  A61K2039/505 ,  A61K2039/54 ,  A61K2039/545 ,  A61P19/02 ,  C07K2317/24 ,  C07K2317/52 ,  C07K2317/90 ,  C07K2317/94

Abstract: An object of the present invention is to provide a pharmaceutical composition comprising an anti-fractalkine antibody, and a method for treating rheumatoid arthritis using the pharmaceutical composition, wherein the pharmaceutical composition and the method bring about therapeutically effective amelioration in rheumatoid arthritis after administration to a human subject. The present invention provides a pharmaceutical composition for the treatment of rheumatoid arthritis. The pharmaceutical composition in a method for treating rheumatoid arthritis comprises an anti-fractalkine antibody and a pharmaceutically acceptable excipient and is used such that at least 100 mg per dose of the anti-fractalkine antibody is subcutaneously administered to a human in need thereof.

公开(公告)号：US20180105493A1

公开(公告)日：2018-04-19

申请号：US15841652

申请日：2017-12-14

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D211/62 ,  C12N15/113 ,  A61K48/00 ,  A61K47/22 ,  C07D207/16 ,  C07D205/04 ,  A61K9/51 ,  C12N15/11

CPC classification number: C07D211/62 ,  A61K9/5123 ,  A61K47/22 ,  A61K48/0033 ,  C07D205/04 ,  C07D207/16 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: wherein, L is an alkyl having 7-12 carbon atoms or an alkenyl having 7-12 carbon atoms, R is an alkyl having 1-2 carbon atoms, and n1 and n2 are independently an integer of 1-3.

公开(公告)号：US20180093972A1

公开(公告)日：2018-04-05

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：US20180071247A1

公开(公告)日：2018-03-15

申请号：US15554540

申请日：2016-03-03

Applicant: MERCK SHARP & DOHME CORP. ,  Eisai R&D Management Co., Ltd.

Inventor： Junji MATSUI ,  Gursel AKTAN ,  Vassiliki KARANTZA ,  RuiRong YUAN ,  Yasuhiro FUNAHASHI ,  Erhan BERRAK

IPC: A61K31/357 ,  A61K39/395 ,  C07K16/28 ,  A61K45/06 ,  A61K9/00

Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of cancer.

公开(公告)号：US20180028662A1

公开(公告)日：2018-02-01

申请号：US15550124

申请日：2016-02-23

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

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

IPC: A61K47/02 ,  A61K31/47

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：US09873669B2

公开(公告)日：2018-01-23

申请号：US15109512

申请日：2015-01-07

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

Inventor： Yuta Suzuki ,  Kenji Hyodo ,  Yohei Tanaka

IPC: C07D211/62 ,  A61K47/22 ,  A61K9/51 ,  C07D205/04 ,  C07D207/16 ,  C12N15/11 ,  A61K48/00 ,  C12N15/113

CPC classification number: C07D211/62 ,  A61K9/5123 ,  A61K47/22 ,  A61K48/0033 ,  C07D205/04 ,  C07D207/16 ,  C12N15/111 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2320/32

Abstract: The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: wherein, L is an alkyl having 7-12 carbon atoms or an alkenyl having 7-12 carbon atoms, R is an alkyl having 1-2 carbon atoms, and n1 and n2 are independently an integer of 1-3.

公开(公告)号：US20180015079A1

公开(公告)日：2018-01-18

申请号：US15547139

申请日：2016-03-23

Applicant: NATIONAL CANCER CENTER ,  Eisai R&D Management Co., Ltd.

Inventor： Tatsuhiro SHIBATA ,  Yasuhito ARAI ,  Kenichi NOMOTO ,  Tomio NAKAMURA ,  Akihiko TSURUOKA ,  Saori MIYANO

IPC: A61K31/4545

CPC classification number: A61K31/4545

Abstract: The present invention provides a therapeutic agent for bile duct cancer comprising 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.