Abstract: Disclosed in the present invention is a type of indole substituted piperidine compounds as an estrogen receptor down-regulator. Specifically disclosed are a compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate or prodrug thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof as an estrogen receptor down-regulator in the treatment of estrogen receptor positive breast cancers.
Abstract: Provided are methods of increasing metabolic maturation of an immature hepatocyte, by contacting an immature hepatocyte which expresses alpha-fetoprotein (AFP) and albumin with an effective amount of a fatty acid or a small molecule selected from the group consisting of: an amphipathic carboxylic acid, Thiazolidinedione (TZD), WY-14643 (Pirinixic Acid), GW409544, GW6471, Leukotriene B4, GW 7647, Perfluorooctanesulfonic Acid, Perfluorooctanoic Acid, CP-775146, CP-865520, UNII-999KY5ZIGB, and Gemfibrozil. Also provided are isolated hepatocytes and uses thereof.
Type:
Grant
Filed:
March 15, 2017
Date of Patent:
September 15, 2020
Assignee:
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd
Inventors:
Yaakov Nahmias, Michal Zimerman, Gahl Levy, Yishai Avior
Abstract: The present invention provides a composition for lipolysis, for example a pharmaceutical composition for preventing or treating obesity including localized fat deposits (LFD), comprising certain phosphocholine derivatives or pharmaceutically acceptable salt thereof. The pharmaceutical composition of the present invention shows an excellent lipolytic activity as well as a uniform lipolytic activity. And also, the pharmaceutical composition of the present invention can minimize side effects such as inflammation, tissue necrosis, etc., at the administered site. In addition, the pharmaceutical composition of the present invention has excellent storage stability.
Type:
Grant
Filed:
February 27, 2018
Date of Patent:
September 8, 2020
Assignee:
PENMIX LTD.
Inventors:
Dongkyu Park, Sang Yun Lee, Young Sub Song, Surin Kim, Joo Hwan Kim, Ji Hyun Moon, Seung Jun Lee, Hana Lee, Seung Ho Ji
Abstract: A method for treating a sarcoma by administering a tyrosine kinase inhibitor and a biguanide compound. Also described is a method for treating a tumor of the Ewing Sarcoma family by obtaining a tumor sample; determining in the sample gene expression levels of ACTB, B2M, MLH1, PRKDC, XPC, APEX1, ERCC5, MMS19, or RAD23; and administering a tyrosine kinase inhibitor and a biguanide compound. Furthermore, a pharmaceutical composition for treating a Ewing family tumor is disclosed. The composition contains a tyrosine kinase inhibitor, a biguanide compound, and a pharmaceutically acceptable excipient.
Abstract: The present invention provides a food intake regulating agent which improves anorexia and overeating and is safe for ingestion for a long term. The present invention relates to a food intake regulating agent containing 3 kinds of amino acids: threonine, methionine and tryptophan, as active ingredients.
Abstract: The present invention provides compounds that modulate protein translocation in mitochondria, compositions thereof, and methods of identifying, making and using these.
Type:
Grant
Filed:
November 16, 2017
Date of Patent:
September 1, 2020
Assignee:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Carla M. Koehler, Samuel A. Hasson, Kiyoko Miyata, Michael A. Teitell, Deepa Dabir
Abstract: The invention relates to a potentiated antimicrobial agent for use in the treatment of a microbial infection, characterised in that said antimicrobial agent is used in association with a compound of formula (I), the mass ratio of compound of formula (I): antimicrobial agent varying between 8:1 and 1:10.
Abstract: The invention relates to antagonists of integrin ?4 and their use in pharmaceutical compositions, primarily topically administered ophthalmic compositions. The pharmaceutical compositions are useful for treating ocular inflammatory conditions, such as dry eye disease, non-infectious uveitis (e.g., anterior, intermediate, posterior, pan-uveitis), non-infectious conjunctivitis, iritis, or scleritis in animals, and particularly mammals, including humans.
Abstract: Provided are methods for treating pancreatic cancer in a patient by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin.
Type:
Grant
Filed:
June 19, 2018
Date of Patent:
August 18, 2020
Assignee:
Ipsen Biopharm Ltd.
Inventors:
Eliel Bayever, Navreet Dhindsa, Jonathan Basil Fitzgerald, Peter Laivins, Victor Moyo, Clet Niyikiza, Jaeyeon Kim
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a benzimidazole or imidazopyridine structure which function as inhibitors of DYRK1A protein, and their use as therapeutics for the treatment of Alzheimer's disease, Down syndrome, glioblastoma, autoimmune diseases, inflammatory disorders (e.g., airway inflammation), and other diseases.
Type:
Grant
Filed:
September 2, 2016
Date of Patent:
August 4, 2020
Assignees:
ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA, THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
Inventors:
Christopher Hulme, Travis Dunckley, Yeng-Jeng Shaw
Abstract: The present invention relates to an oxazine derivative BACE-1 inhibitor and pharmaceutical compositions comprising such oxazine derivative for use in the treatment or prevention of cerebral amyloid angiopathy and, in particular, wherein the patient carries one or two copies of the ApoE4 allele.
Abstract: The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.
Type:
Grant
Filed:
May 9, 2014
Date of Patent:
July 28, 2020
Assignee:
Morphochem Aktiengesellschaft Für Kombinatorische Chemie
Inventors:
Thomas Kapsner, Axel Dalhoff, Thomas Gramatte
Abstract: The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.
Abstract: The present invention features compositions and methods for treatment of snoring. We describe compositions comprising an antihistamine or a pharmaceutically acceptable salt thereof and one or more dietary supplements or pharmaceutically acceptable salts thereof. The compositions can be administered to a subject suffering from snoring.
Abstract: Biocompatible phase invertible proteinaceous compositions and methods for making and using the same are provided. Phase invertible compositions in accordance with the invention are prepared by combining a liquid proteinaceous substrate and a liquid crosslinking composition, where the liquid crosslinking composition includes a macromolecular crosslinking agent. Also provided are kits for use in preparing the subject compositions. The subject compositions, kits and systems find use in a variety of different applications.
Type:
Grant
Filed:
May 2, 2019
Date of Patent:
June 9, 2020
Assignee:
Baxter International Inc.
Inventors:
Ronald Dieck, Ian J. Handley, Neil Winterbottom, Joanna Wong
Abstract: Disclosed is a compound of formula (Ia) for the use thereof in the treatment or prevention of diseases relating to the instability of mitochondrial DNA.
Type:
Grant
Filed:
December 1, 2015
Date of Patent:
May 5, 2020
Assignees:
UNIVERSITE PARIS-SUD, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE D'ANGERS, CENTRE HOSPITALIER UNIVERSITAIRE D'ANGERS
Abstract: Disclosed herein are methods for treating conditions and/or disorders related to hyperglycemia. Such conditions and/or disorders related to hyperglycemia include, but are not limited to, type I, II diabetes mellitus, gestational diabetes, other forms diabetes, and disorders related thereto. In particular, the present invention relates to methods of using (R)-(+)-verapamil or a pharmaceutically acceptable salt thereof and an ?-glycosidase inhibitor in the treatment of conditions and/or disorders related to hyperglycemia.
Abstract: Pharmaceutical compositions comprising epinephrine, methods of administration, and methods of making the same. Compositions may comprise at least one of an active agent, a pH raising agent, an antioxidant, a transition metal complexing agent, a pH lowering agent, a tonicity regulating agent, optionally a preservative, and optionally a solvent.
Type:
Grant
Filed:
January 25, 2019
Date of Patent:
April 21, 2020
Assignee:
PAR PHARMACEUTICAL, INC.
Inventors:
Suketu Sanghvi, Vinayagam Kannan, Matthew Kenney
Abstract: The invention provides safe and efficacious treatments for Female Sexual Disorders, genitopelvic pain/penetration disorders; vulvovaginal atrophy, vestibulodynia, dyspareunia, sexual interest/arousal disorder, low female libido, and female orgasmic disorder.
Abstract: The present application provides a novel phenyl derivative, 5-[(2,4-dinitrophenoxy)methyl]-1-methyl-2-nitro-1H-imidazole or a pharmaceutically acceptable salt thereof, which is useful for regulating mitochondria activity, reducing adiposity, treating diseases including diabetes and diabetes-associated complications.