公开(公告)号：US20230151022A1

公开(公告)日：2023-05-18

申请号：US18089971

申请日：2022-12-28

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

Inventor： Hyeong-Wook CHOI ,  Francis G. FANG

IPC: C07D493/22 ,  C07D307/28 ,  C07D493/04 ,  C07D407/06 ,  C07D407/14

CPC classification number: C07D493/22 ,  C07D307/28 ,  C07D493/04 ,  C07D407/06 ,  C07D407/14

Abstract: The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

公开(公告)号：US20230149381A1

公开(公告)日：2023-05-18

申请号：US17918829

申请日：2021-04-15

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

Inventor： Kyoko NISHIBATA ,  Sayo FUKUSHIMA ,  Satoshi KAWANO ,  Saori MIYANO

IPC: A61K31/4545 ,  A61K31/519 ,  A61K31/565 ,  A61P35/04

CPC classification number: A61K31/4545 ,  A61K31/519 ,  A61K31/565 ,  A61P35/04

Abstract: Provided is a therapeutic agent for treating breast cancer that has developed resistance to administration of CDK4/6 inhibitors and estrogen antagonists, the agent containing 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethox y)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.

公开(公告)号：US11642347B2

公开(公告)日：2023-05-09

申请号：US16808513

申请日：2020-03-04

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

Inventor： Heike Keilhack ,  Sarah K. Knutson ,  Danielle Johnston Blackwell ,  Larisa Reyderman ,  Lone Ottesen

IPC: A61P35/02 ,  A61K31/4412 ,  A61K31/5377 ,  C07D213/65 ,  C07D405/12 ,  A61K31/4545

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  C07D213/65 ,  C07D405/12

Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.

公开(公告)号：US20230051268A1

公开(公告)日：2023-02-16

申请号：US17757672

申请日：2020-12-18

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

Inventor： Andrew SATLIN ,  Margaret MOLINE ,  Ishani LANDRY

IPC: A61K31/506 ,  A61K9/00

Abstract: Disclosed are methods for treating insomnia, comprising administering orally a dosage form comprising Lemborexant or a pharmaceutically acceptable salt thereof to a patient in need thereof at a single daily dose ranging from 5 mg to 10 mg of lemborexant or an equivalent dose of a pharmaceutically acceptable salt thereof, provided that the maximum dose is 5 mg once per day of lemborexant or an equivalent dose of a pharmaceutically acceptable salt thereof when the patient has moderate hepatic impairment classified in Child-Pugh class B under Child-Pugh Classification.

公开(公告)号：US11572414B2

公开(公告)日：2023-02-07

申请号：US17091819

申请日：2020-11-06

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

Inventor： Earl F. Albone ,  Jared Spidel

IPC: A61P35/00 ,  C07K16/30 ,  A61K47/68 ,  A61K47/60 ,  A61K31/357 ,  G01N33/574 ,  A61K39/00

Abstract: Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates such as those comprising eribulin) thereof that bind to mesothelin are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the compositions provided herein.

公开(公告)号：US11547743B2

公开(公告)日：2023-01-10

申请号：US15305049

申请日：2015-04-24

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

Inventor： Ryo Ohori ,  Kanta Horie

IPC: A61K38/18 ,  A61K47/18 ,  A61K47/26 ,  A61K9/19 ,  A61K38/00 ,  A61K47/02

Abstract: An object of the present invention is to provide a lyophilized formulation having improved storage stability of hepatic growth factor compared to conventional lyophilized formulations. The present invention provides a lyophilized formulation comprising (1) a hepatic growth factor, (2) trehalose and (3) one or more compounds selected from the group consisting of arginine, histidine, lysine, meglumine, glutamic acid, aspartic acid, proline, creatine, creatinine, tris(hydroxymethyl)aminomethane, and pharmaceutically acceptable salts thereof.

公开(公告)号：US11407762B2

公开(公告)日：2022-08-09

申请号：US16764245

申请日：2018-11-15

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

Inventor： Yoshito Kishi ,  Kazunobu Kira ,  Ken Ito

IPC: C07D493/22 ,  A61P35/04

Abstract: The present invention provides novel compounds (e.g., compounds of Formulae (I), (II), (III), (IV)) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or pharmaceutically acceptable salts thereof, optionally in a pharmaceutically acceptable carrier, and a medical uses thereof.

公开(公告)号：US20220195437A1

公开(公告)日：2022-06-23

申请号：US17643807

申请日：2021-12-10

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

Inventor： Dae-Shik KIM ,  Hyeong-Wook CHOI ,  Francis G. FANG ,  Yoshinori TAKAHASHI ,  Kenji KIKUTA ,  Hikaru YOSHIMURA ,  Wataru ITANO ,  Toshiki KUROKAWA ,  Ryo DAIRIKI ,  Zhi ZHOU ,  Mingde SHAN

IPC: C12N15/113 ,  A61K31/712 ,  A61P25/28

Abstract: Antisense oligonucleotides are provided. These antisense oligonucleotides are useful in the preparation of gapmers for inhibition of Tau mRNA transcription. Inhibition of Tau mRNA transcription may result in decrease of amounts of Tau protein in a subject, allowing treatment of diseases and disorders related to expression of Tau, including Alzheimer's disease and primary tauopathies.

公开(公告)号：US11357769B2

公开(公告)日：2022-06-14

申请号：US16300313

申请日：2017-05-09

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

Inventor： Anand Selvaraj ,  Peter Smith

IPC: A61K31/497 ,  A61K31/535 ,  A61K31/4706 ,  A61K31/506 ,  A61K31/517 ,  A61P35/00 ,  A61K39/395

Abstract: Provided herein is a combination of agents for reducing cell viability and/or cell proliferation. The combination comprises an FGFR4 inhibitor and an EGFR inhibitor.

公开(公告)号：US11168123B2

公开(公告)日：2021-11-09

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.