Abstract: The purpose of the present invention is to provide a method for predicting the effectiveness of an angiogenesis inhibitor in a subject suffering from a tumor. Provided is a method comprising a step of testing for the presence or absence of an a mutation or loss of expression of B-Raf and PTEN in a sample of tumor tissue from the subject. By using the presence or absence of or a mutation or loss of expression of B-Raf and PTEN as an indicator, this method enables the antitumor effectiveness of the angiogenesis inhibitor to be predicted without administering the angiogenesis inhibitor to the subject.
Abstract: A formulation comprising liposomes, wherein the liposomes comprise, based on the liposome, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 0.5 to 3.0 mol % of a PEGylated phospholipid.
Abstract: Provided is a therapeutic agent for Lewy body disease comprising (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one represented by formula (I) or a pharmaceutically acceptable salt thereof.
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 and medical uses thereof.
Type:
Application
Filed:
April 3, 2018
Publication date:
May 14, 2020
Applicants:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD
Abstract: The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.
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:
December 14, 2017
Date of Patent:
May 5, 2020
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: 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: 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: A method of preparation of stereospecific synthesis of diastereomerically pure phosphorodiamidate morpholino oligomers (PMOs) of one of the following general formulas is provided.
Type:
Application
Filed:
September 17, 2019
Publication date:
April 16, 2020
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Atsushi ENDO, Robert T. YU, Francis FANG, Hyeong Wook CHOI, Mingde SHAN
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., Horner-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:
January 14, 2019
Date of Patent:
April 7, 2020
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase, Jaemoon Lee
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: Provided is a graft material capable of securing a sufficient space for regenerated tissue in the implantation site, and thereby promoting the regeneration of a blood vessel. Specifically, the present invention provides a revascularization graft material including an outer tube and an inner tube each being formed by knitting twisted yarns of biodegradable single yarns into a hollow tubular structure, wherein there is provided, in the lumen of the outer tube, at least one inner tube having an outer diameter smaller than the lumen diameter of the outer tube. The inner tube functions as a core material for the outer tube, and accordingly the revascularization graft material is excellent in kinking resistance, and the occlusion of the lumen hardly occurs.
Abstract: The present invention provides a pharmaceutical composition comprising a PDE9 inhibitor. Specifically, the PDE9 inhibitor is (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quin olin-4(5H)-one or pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
May 30, 2018
Publication date:
March 12, 2020
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Edgar Schuck, Robert Lai, Ishani Savant Landry, Bhaskar Rege, Mai Miyamoto, Sadaharu Kotani, Kanta Horie
Abstract: Provided is a container including a main body, a lid body, and a fixing mechanism that fixes the lid body to prevent the lid body from opening from the main body when the lid body is closed, the fixing being released when the lid body moves to a front side with respect to the main body. Cutouts are formed in side plates of the main body. The container is configured such that, by a rear plate tilting forward toward the cutouts of the side plates, the lid body moves to the front side with respect to the main body and the fixing of the lid body is released, and as the rear plate and a top plate of the lid body form a single plane, the top plate rises and the lid body opens.
Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.
Type:
Application
Filed:
July 25, 2019
Publication date:
February 20, 2020
Applicant:
Eisai R&D Management Co., Ltd.
Inventors:
Francis G. FANG, Hyeong-wook CHOI, Silvio CAMPAGNA, Steven MATHIEU
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.
Type:
Grant
Filed:
April 13, 2016
Date of Patent:
February 18, 2020
Assignee:
Eisai R&D Management Co., LTD.
Inventors:
George Moniz, Kristen Sanders, Arani Chanda, Kenshi Yoshida