公开(公告)号：US20230062861A1

公开(公告)日：2023-03-02

申请号：US17521666

申请日：2021-11-08

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

Inventor： Sudeep PRAJAPATI ,  Hyelee LEE ,  Stephanos IOANNIDIS ,  Kiyoyuki OMOTO ,  Alan ROLFE ,  Xiang LIU ,  Megan SHEEHAN ,  Paul DRANSFIELD ,  Andrew COOK

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08 ,  C07D417/14 ,  C07D491/04 ,  C07D409/14 ,  C07D498/08 ,  C07D498/04 ,  C07D487/04 ,  C07D491/10 ,  C07F5/02

Abstract: Disclosed herein are novel compounds of Formula (1) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, and methods of using the same.

公开(公告)号：US11548926B2

公开(公告)日：2023-01-10

申请号：US16078568

申请日：2017-03-15

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

Inventor： Masashi Shimizu ,  Toshitaka Sato ,  Yoshihisa Arita

IPC: C07K14/475 ,  C12P21/02 ,  C12N9/64 ,  C12N15/09 ,  C12N5/10

Abstract: The present invention provides a method for producing active hepatocyte growth factor activator (HGFA) and active hepatocyte growth factor (HGF) without using animal serum. The present invention relates to a method for producing active HGFA without using animal serum. The method is characterized in that it comprises a step of obtaining a culture supernatant comprising pro-HGFA by culturing mammalian cells expressing inactive hepatocyte growth factor activator (pro-HGFA) in a medium without serum, and a step of adjusting the culture supernatant comprising pro-HGFA obtained in the above step to weakly acidic to convert pro-HGFA into active HGFA. The present invention also relates to a method for producing active HGF with HGFA produced by said method.

公开(公告)号：US11547705B2

公开(公告)日：2023-01-10

申请号：US15554577

申请日：2016-03-03

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

Inventor： Andrew Evan Denker ,  Yu Kato ,  Kimiyo Tabata ,  Yusaku Hori

IPC: A61K39/00 ,  A61K31/47 ,  A61K39/395 ,  A61K45/06 ,  C07K16/28

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：US20220409724A1

公开(公告)日：2022-12-29

申请号：US17772468

申请日：2020-10-28

Applicant: Eisai R&D Management Co., Ltd. ,  Merck Sharp & Dohme Corp. ,  MSD International GmbH

Inventor： Yoichi OZAWA ,  Yasuhiro FUNAHASHI ,  Yu KATO

IPC: A61K39/395 ,  A61P35/00 ,  A61K31/47 ,  A61K31/53

Abstract: The present disclosure describes a combination therapy comprising an antagonist of Programmed Death 1 receptor (PD-1), a lenvatinib or a pharmaceutically acceptable salt thereof, and (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide (E7386) or a pharmaceutically acceptable salt thereof,—and the use of the combination therapies for the treatment of a cancer.

公开(公告)号：US11498916B2

公开(公告)日：2022-11-15

申请号：US16722838

申请日：2019-12-20

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

Inventor： George Moniz ,  Kristen Sanders ,  Arani Chanda ,  Kenshi Yoshida ,  Ming-Hong Hao ,  Dominic Reynolds ,  Sudeep Prajapati ,  Anand Selvaraj ,  Takashi Satoh ,  John Wang

IPC: C07D403/12 ,  C07D239/48 ,  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-y1)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：US11420980B2

公开(公告)日：2022-08-23

申请号：US17021544

申请日：2020-09-15

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

Inventor： Kenshi Yoshida ,  Yoshiaki Ohashi ,  Tamaki Hoshikawa ,  Nobuaki Sato ,  Ikuo Kushida

IPC: C07D495/22 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16

Abstract: Salts of the compound represented by formula (I) or crystals thereof have a potential use as drug substances for pharmaceuticals.

公开(公告)号：US20220251171A1

公开(公告)日：2022-08-11

申请号：US17617504

申请日：2020-06-25

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

Inventor： Hiroaki Hagiwara ,  Kanta Horie ,  Kunihiko Kanatsu ,  Yasuharu Ishihara ,  Yasuaki Goto ,  Toru Oki ,  Masafumi Tsuboi ,  Charlotte Sahlin ,  Maria Eriksson ,  Christer Möller

IPC: C07K14/775 ,  G01N33/50 ,  G01N33/92 ,  A61P25/28

Abstract: The present invention relates to novel fragments of apolipoprotein E (ApoE). These ApoE fragments have a variety of uses including as components of vaccine compositions, particularly vaccines for the prevention or treatment of neurological disorders such as Alzheimer's disease. The ApoE fragments may also be used in screening methods and methods of detection.

公开(公告)号：US11327078B2

公开(公告)日：2022-05-10

申请号：US16965161

申请日：2019-02-25

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

Inventor： Yoko Ida ,  Takashi Obara ,  Emiko Yumoto

IPC: G01N33/577 ,  C07K16/18

Abstract: The present invention provides an anti-APOA4 monoclonal antibody or an antibody fragment thereof capable of accurately measuring apolipoprotein A-IV (APOA4) in a specimen, a measurement method for immunologically measuring APOA4 using the antibody or the antibody fragment thereof, and a kit for measuring APOA4 containing the antibody or the antibody fragment thereof.

公开(公告)号：US11325960B2

公开(公告)日：2022-05-10

申请号：US16078568

申请日：2017-03-15

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

Inventor： Masashi Shimizu ,  Toshitaka Sato ,  Yoshihisa Arita

IPC: C07K14/475 ,  C12P21/02 ,  C12N9/64 ,  C12N15/09 ,  C12N5/10

Abstract: The present invention provides a method for producing active hepatocyte growth factor activator (HGFA) and active hepatocyte growth factor (HGF) without using animal serum. The present invention relates to a method for producing active HGFA without using animal serum. The method is characterized in that it comprises a step of obtaining a culture supernatant comprising pro-HGFA by culturing mammalian cells expressing inactive hepatocyte growth factor activator (pro-HGFA) in a medium without serum, and a step of adjusting the culture supernatant comprising pro-HGFA obtained in the above step to weakly acidic to convert pro-HGFA into active HGFA. The present invention also relates to a method for producing active HGF with HGFA produced by said method.

公开(公告)号：US20220112207A1

公开(公告)日：2022-04-14

申请号：US17421922

申请日：2020-01-09

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

Inventor： Francis G. FANG ,  Branko MITASEV ,  Jiong YANG

IPC: C07D491/147 ,  C07D403/06 ,  C07D487/04 ,  C07D405/14 ,  C07C311/18 ,  C07D307/33

Abstract: A method for the synthesis of diazabicyclo[6.2.0]decane compounds is provided. The synthesis proceeds by stereoselective synthesis of a chiral lactone followed by azetidine formation via a series of chemoselective reactions. Bicyclization results with the formation of diazobicyclo[6.2.0]decane related compounds.