Abstract: The present invention is directed to methods for treating ebola virus infections or Marburg virus infections comprising administering to a subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 14, 2017
Date of Patent:
November 30, 2021
Assignees:
EISAI R&D MANAGEMENT CO., LTD, THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Alexander Bukreyev, Fabian Gusovsky, Patrick Younan, Michael Everson
Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
Abstract: There is provided a therapeutic agent for Alzheimer's disease and Lewy body dementia for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (1): or a pharmaceutically acceptable salt thereof, and donepezil represented by formula (II): or a pharmaceutically acceptable salt thereof.
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
Type:
Application
Filed:
January 5, 2021
Publication date:
November 11, 2021
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Wanjun ZHENG, Xiaojie ZHU, Hong DU, Maarten POSTEMA, Yimin JIANG, Jing LI, Robert YU, Hyeong-Wook CHOI, Jaemoon LEE, Francis G. FANG, Daniel CUSTAR
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 compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
April 23, 2018
Date of Patent:
November 2, 2021
Assignee:
Eisai R&D Management Co., LTD.
Inventors:
Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
Abstract: The present invention provides a crystal of the compound represented by formula (I) having applicability as a drug substance of pharmaceuticals.
Abstract: There is provided a therapeutic agent for Alzheimer's disease for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (I): or a pharmaceutically acceptable salt thereof, and memantine represented by formula (II): or a pharmaceutically acceptable salt thereof.
Abstract: Provided is an anti-EphA4 antibody that can bind to EphA4 and enhance the cleavage of EphA4, as well as a pharmaceutical composition comprising the antibody as the active ingredient. A mouse anti-EphA4 antibody that has binding affinity towards EphA4 and can enhance the cleavage of EphA4 was obtained, and the sequence of the complementarity-determining region (CDR) of the mouse anti-EphA4 antibody was identified. Subsequently, the anti-EphA4 antibody of interest was obtained by producing a humanized antibody of the mouse anti-EphA4 antibody.
Abstract: The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
Type:
Grant
Filed:
June 30, 2017
Date of Patent:
October 5, 2021
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Charles E. Chase, Hyeong-Wook Choi, Atsushi Endo, Francis G. Fang, Dae-Shik Kim
Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine 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.
Type:
Grant
Filed:
April 10, 2020
Date of Patent:
September 28, 2021
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
Abstract: The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, and medical uses thereof.
Type:
Application
Filed:
February 4, 2021
Publication date:
August 26, 2021
Applicants:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD.
Abstract: Disclosed is: a fluorescent dye comprising a compound, a tautomer of the compound, or a salt of the compound or the tautomer; a labeled composite substance comprising the fluorescent dye and a composite substance which are bonded to each other; a composition containing the fluorescent dye or the labeled composite substance; and a method for acquiring information about a substance of interest by a super-resolution microscopy.
Abstract: Disclosed herein is a method for treating tumor, comprising administering a liposomal composition comprising eribulin or a pharmaceutically acceptable salt thereof and a PD-1 antagonist to a patient in need thereof.
Abstract: Provided herein is a combination therapy useful for the treatment breast cancer. The combination comprises an ER-alpha inhibitor and a CDK 4/6 inhibitor.
Type:
Grant
Filed:
March 16, 2018
Date of Patent:
August 10, 2021
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Craig D. Karr, Manav Korpal, Nathalie Rioux, Peter Gerard Smith
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:
July 6, 2018
Publication date:
July 29, 2021
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: A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof, and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: wherein, R1 is a hydrogen atom, a C1-6 alkyl group or a C3-8 cycloalkyl group; and R2 is a hydrogen atom or a methoxy group.