Abstract: In one aspect, the invention provides a method for inhibiting the growth and/or proliferation of a myc-driven tumor cell comprising the step of contacting the tumor cells with a CSNK1? inhibitor. In another aspect, the invention provides a method of treating a subject suffering from a tumor comprising myc-driven tumor cells, comprising administering to the subject an amount of a composition comprising a CSNK1? inhibitor effective to inhibit the growth and/or proliferation of the tumor cells.
Abstract: The invention provides a fulvestrant composition comprising not more than 2% total impurities that comprises a nonionic surfactant and/or a ricinoleate vehicle and which, optionally, is free of a non-aqueous ester solvent. The composition may be used to treat hormone receptor positive metastatic breast cancer in a subject.
Abstract: The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.
Type:
Grant
Filed:
March 27, 2017
Date of Patent:
January 15, 2019
Assignees:
President and Fellows of Harvard College, The General Hospital Corporation
Abstract: A synergistic composition comprising a THP salt and a biopenetrant, in which the biopenetrant comprises a polymer of an unsaturated carboxylic acid or a copolymer of an unsaturated carboxylic acid with a sulphonic acid, said polymer or copolymer being terminated by a mono- or diphosphonated unsaturated carboxylic acid group or having such monomers incorporated into the polymer backbone. This composition acts synergistically to enhance the biocidal efficacy of the THP salt against both planktonic (free-swimming) and sessile (attached) bacteria, and also acts synergistically to enhance the efficacy of the THP salt in the dissolution of iron sulphide scale.
Type:
Grant
Filed:
November 8, 2017
Date of Patent:
January 15, 2019
Assignee:
Solvay Solutions UK Limited
Inventors:
Robert Eric Talbot, Christopher Raymond Jones
Abstract: Roflumilast crystals have been shown to increase in size during storage. The size of the roflumilast crystals can affect the bioavailability and efficacy of a pharmaceutical composition. The growth of roflumilast crystals can be inhibited during storage by including hexylene glycol in the composition. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in a patient in need of such treatment.
Abstract: The invention relates to a method for the treatment of vasomotor symptoms comprising the administration of a therapeutically effective amount of flibanserin.
Abstract: The present disclosure relates generally to the field of nicotine delivery. The disclosure teaches a nicotine meta-salicylate. More specifically, the disclosure teaches a condensation nicotine aerosol where nicotine meta-salicylate is vaporized. This disclosure relates to aerosol nicotine delivery devices. The delivery devices can be activated by actuation mechanisms to vaporize thin films comprising a nicotine meta-salicylate. More particularly, this disclosure relates to thin films of nicotine salt with meta salicylic acid for the treatment of nicotine craving and for effecting smoking cessation.
Abstract: The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.
Type:
Grant
Filed:
October 24, 2014
Date of Patent:
January 1, 2019
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael McNevin, Yong Liu, Ian Mangion, Alfred Lee, Joyce Stellabott, Benjamin D. Sherry, Gary Martin, Kung-I Feng, Scott Schultz, Ryan Cohen, Yanfeng Zhang
Abstract: Provided are inhibitors of sphingosine kinase Type I that are useful in a number of applications, indications and diseases, as well as for monitoring pharmacokinetics and patient management. These compounds are applicable to treating tumors of the central nervous system, such as glioblastoma multiforme (GBM).
Type:
Grant
Filed:
April 16, 2018
Date of Patent:
January 1, 2019
Assignee:
Enzo Therapeutics, Inc.
Inventors:
Sarah Spiegel, Robert Elliot Zipkin, Jeffrey Kroll Adams
Abstract: The invention relates to compositions and formulations comprising isolated acidic fraction of mastic gum and uses thereof for treating impaired neurological functions as well as wound and tissue repair.
Abstract: Provided herein are methods of treating, preventing and/or managing cancer, including lymphoma, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof in a cyclic therapy regimen.
Type:
Grant
Filed:
December 1, 2016
Date of Patent:
December 25, 2018
Assignee:
Celgene Corporation
Inventors:
Patrick Hagner, Anita Gandhi, Michael Pourdehnad
Abstract: The inventive subject matter is directed to compositions and methods for ready-to-inject norepinephrine compositions with improved stability. Most preferably, compositions presented herein are substantially antioxidant free and exhibit less than 10% isomerization of R-nor epinephrine and exhibit less than 5% degradation of total norepinephrine.
Abstract: The subject disclosure provides compositions for reducing serum cholesterol and/or triglyceride levels in subjects. These compositions can comprise racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, esters of D-?-hydroxybutyrate, oligomers of D-?-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol or R-1,3 butandiol alone and can be, optionally, administered in conjunction with a low fat diet to a subject.
Type:
Grant
Filed:
November 3, 2015
Date of Patent:
December 18, 2018
Assignees:
OXFORD UNIVERSITY INNOVATION LIMITED, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Abstract: Compositions and methods for treating hyperemia and symptoms in pinguecula and pseudopteryigium are disclosed. The methods include administration of a multikinase inhibitor, an antimetabolite or a combination thereof to patients in need thereof.
Abstract: Compositions and methods for treating hyperemia and symptoms in pterygium patients are disclosed. The methods include administration of a multikinase inhibitor, an antimetabolite or a combination thereof to patients in need thereof.
Abstract: The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
Type:
Grant
Filed:
November 7, 2017
Date of Patent:
December 4, 2018
Assignee:
PELOTON THERAPEUTICS, INC.
Inventors:
Darryl David Dixon, Jonas Grina, John A. Josey, James P. Rizzi, Stephen T. Schlachter, Eli M. Wallace, Bin Wang, Paul Wehn, Rui Xu, Hanbiao Yang
Abstract: The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O?); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and di
Type:
Grant
Filed:
February 15, 2016
Date of Patent:
December 4, 2018
Assignee:
SENTINEL ONCOLOGY LIMITED
Inventors:
Robert George Boyle, David Winter Walker
Abstract: The present invention relates to the use of benzimidazole sulfide derivatives and prodrugs thereof in the treatment and/or prevention of tuberculosis.
Type:
Grant
Filed:
January 26, 2016
Date of Patent:
November 27, 2018
Assignee:
École Polytechnique Fédérale de Lausanne (EPFL)
Abstract: This application is directed to a homogeneous solution of an aqueous, topical composition useful for the treatment of infection and/or for the treatment of inflammation due to trauma to tissue. Specifically, this application relates to a homogeneous, aqueous composition of a quinolone antibiotic and an anti-inflammatory agent.