Abstract: Provided is a combination agent that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide with an AMPA-type glutamate receptor antagonist such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or 2-fluoro-6-(3-fluoro-8-oxo-7-(pyridin-3-yl)-7,8-dihydro-6H-pyrano[3,2-b:5,4-b?]dipyridin-9-yl)benzonitrile, and it has potential for use as a therapeutic agent for epilepsy.
Type:
Grant
Filed:
March 18, 2019
Date of Patent:
May 30, 2023
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Hiroyuki Higashiyama, Hisashi Wakita, Yoshimasa Ito, Yoshihide Osada
Abstract: An apparatus for monitoring a user's health and/or sleep and/or the efficacy of a treatment (e.g. a sleep treatment or other type of health treatment) can include use of a wearable electronic device. The device can include an array of sensors for collecting user data. The user data can be used by the device to evaluate criteria related to the user's health to monitor efficacy of a treatment. In addition, or alternatively, the collected data can be transmitted to a central server and/or input/output device for evaluating different criteria for monitoring the user's health and/or sleep as well as the efficacy of a treatment being provided to the user.
Type:
Application
Filed:
March 25, 2021
Publication date:
May 18, 2023
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Rajeev NARAYANAN, Tushar D. PATEL, Alexander SCOTT, Mitsuo KOSAKA, David LEVIN
Abstract: Provided herein are vaccines including coronavirus antigens and E6020, as well as methods of mitigation of coronavirus infection by administering those vaccines.
Type:
Application
Filed:
April 6, 2021
Publication date:
May 18, 2023
Applicants:
Eisai R&D Management Co., Ltd., Variation Biotechnologies Inc.
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.
Type:
Grant
Filed:
March 1, 2021
Date of Patent:
May 9, 2023
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase, Jaemoon Lee
Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and their use for the treatment of cancer.
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.
Type:
Application
Filed:
November 23, 2022
Publication date:
April 27, 2023
Applicants:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD.
Inventors:
Yoshito Kishi, Yanran Ai, Ning Ye, Qiaoyi Wang, Kenzo Yahata, Kentaro Iso, Santhosh Reddy Naini, Shuji Yamashita, Jihoon Lee, Isao Ohashi, Takashi Fukuyama
Abstract: Provided herein are methods of treating cancer (e.g., melanoma or RCC), which comprise administering to a human patient in need thereof: (a) a PD-1 antagonist; (b) a CTLA4 antagonist; and (c) lenvatinib represented by Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are kits containing such agents and uses of therapeutic combinations of such agents for the treatment of cancer.
Abstract: The present invention provides a method for producing dopaminergic neuron progenitor cells from pluripotent stem cells, which method comprises the steps of: (i) performing adherent culture of pluripotent stem cells on an extracellular matrix in a medium containing a reagent(s) selected from the group consisting of BMP inhibitor, TGF? inhibitor, SHH signal-stimulating agent, FGF8, and GSK3? inhibitor; (ii) collecting Corin- and/or Lrtm1-positive cells from the cells obtained in Step (i) using a substance which binds to Corin and/or a substance which binds to Lrtm1; and (iii) performing suspension culture of the cells obtained in Step (ii) in a medium containing a neurotrophic factor.
Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having cancer (e.g., thyroid cancer, kidney cancer), suspected of having cancer, or at risk of developing cancer.
Type:
Grant
Filed:
March 23, 2018
Date of Patent:
March 7, 2023
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Yasuhiro Funahashi, Tadashi Kadowaki, Junji Matsui, Jason S. Simon, Lucy Xu
Abstract: Provided herein are methods of treating cancer (e.g., RCC), which comprise administering to a human patient in need thereof: (a) a PD-1 antagonist; (b) an ILT4 antagonist; and (c) lenvatinib represented by Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are kits containing such agents and uses of therapeutic combinations of such agents for the treatment of cancer.
Abstract: Provided herein are antibodies that specifically bind Tau and methods of using the same.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
February 14, 2023
Assignees:
Eisai R&D Management Co., Ltd., UCL Business LTD
Inventors:
Malcolm Ian Roberts, James Martin Staddon, Hettihewage Alfred Rohan De Silva, Jared Spidel, Hirofumi Aoyagi, Shigeru Akasofu, Yutaka Hashizume, Kishan Agarwala
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.
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.
Type:
Application
Filed:
June 23, 2022
Publication date:
January 19, 2023
Applicants:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD.
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.
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.
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).
Type:
Grant
Filed:
July 6, 2018
Date of Patent:
January 10, 2023
Assignees:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD.
Inventors:
Yoshito Kishi, Yanran Ai, Ning Ye, Qiaoyi Wang, Kenzo Yahata, Kentaro Iso, Santhosh Reddy Naini, Shuji Yamashita, Jihoon Lee, Isao Ohashi, Takashi Fukuyama
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.
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.