Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
Abstract: The invention relates to compounds, methods, uses, compositions, combinations, kits and packages for the prevention and/or treatment of parasite infection (e.g., Plasmodium parasites) and/or disease (e.g., malaria) based on uses of (a) cystamine, cysteamine, and analogs, derivatives, prodrugs, precursors thereof; an agent capable of inducing their production; and/or salts thereof, and (b) artemisinin and functional derivative, analog, conjugate, metabolite, prodrug or precursor thereof, and/or salts thereof.
Type:
Grant
Filed:
July 16, 2014
Date of Patent:
March 8, 2016
Assignee:
The Royal Institution for the Advancement of Learning/McGill University
Inventors:
Philippe Gros, Gundula Min-Oo, Anny Fortin
Abstract: This invention relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated and radiofluorinated aromatic compounds.
Abstract: Disclosed is a daidzein derivative as represented by formula (I), or pharmaceutically acceptable salt thereof. Compared to the daidzein in the prior art, the daidzein derivative hydrochloride, in particular to the 7-O—N,N-diethyl-aminoacetyl daidzein hydrochloride, prepared by the daidzein derivative of the present invention, has better solubility and effect for treating cardiovascular diseases.
Abstract: An object of the present invention is to provide a compound that is useful as an orally available anti-HCV agent. The present invention relates to a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. This compound has an anti-HCV activity and is useful as a medicine.
Abstract: The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.
Type:
Grant
Filed:
February 7, 2011
Date of Patent:
February 16, 2016
Assignee:
AMITECH THERAPEUTIC SOLUTIONS, INC.
Inventors:
Eric A. Murphy, David A. Cheresh, Lee Daniel Arnold
Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.
Type:
Grant
Filed:
March 7, 2013
Date of Patent:
February 16, 2016
Assignee:
Evolva SA
Inventors:
Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Prathama S. Mainkar, Melya Hughes Crameri
Abstract: The present invention relates to modafinil or derivatives thereof as a medicine for the treatment of vascular diseases or KCa3.1 channel (Ca activated K channel) mediated diseases and a novel use of the same. More specifically, the present invention relates to a pharmaceutical composition for the prevention or treatment of vascular diseases or KCa3.1 channel-mediated diseases comprising modafinil or a derivative of modafinil, or pharmaceutically acceptable salts thereof which relax blood vessels and inhibit KCa3.1 channel currents by increasing intracellular cAMP, a method for treating vascular diseases or KCa3.1 channel-mediated diseases using the composition and a health functional food composition for the prevention or improvement of vascular diseases or the KCa3.1 channel-mediated diseases comprising modafinil or a modafinil derivative compound, or sitologically acceptable salts thereof.
Type:
Grant
Filed:
October 24, 2012
Date of Patent:
February 16, 2016
Assignee:
EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
Inventors:
Suk Hyo Suh, Jae Chul Jung, Sei Kwan Oh
Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
August 27, 2014
Date of Patent:
February 16, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
Abstract: The invention relates to derivatives of N,N?-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH3C(?O)O or halogen; n=1-5; m=0-3; Z denotes CH2, C?O or SO2; X denotes C(?NH)NH2, C(?NH)NHC(?NH)NH2 or CH2(CHR3)pCH2SO3H, where R3 denotes H, OH, CH3C(?O)O or HOSO2O and p=0-1; and G denotes low-molecular-weight organic or mineral acid, sodium, potassium or ammonium cations, or water. Said derivatives have antiaggregant, anticoagulant and vasodilatory properties. The invention further relates to a method for producing said derivatives by reacting N-substituted piperazines either with carboxamide amidating agents or salts thereof, or with haloalkyl sulfonic acids or salts thereof in organic solvents or in water in the presence of bases. The compounds may be used for the prophylaxis and treatment of disorders of the hemostatic system.
Type:
Grant
Filed:
November 8, 2011
Date of Patent:
February 2, 2016
Assignee:
Vertex Closed Joint Stock Company
Inventors:
Olga Sergejevna Veselkina, Nikolay Borisovich Viktorov, Nikolay Nikolaevich Petrishchev, Yuliya Vyacheslavovna Poplavskaya
Abstract: The preparation method includes the following steps: dissolving aripiprazole in an acidic solution having an acidifier so as to obtain a medicament having acidic solution; then, performing a wet granulation on or preparing a suspension with the obtained medicament having acidic solution, an alkalizer, and an excipient so as to obtain the aripiprazole medicament formulation; the excipient comprising an antioxidant. The aripiprazole medicament formulation obtained through the preparation method has a significantly reduced amount of related substances, great solubility, great stability, high bioavailability, reduced individual differences, and enhanced wettability and content uniformity of insoluble medicaments.
Abstract: A method to produce 5-hydroxymethylfurfural (HMF) is described in which a reactant including cellulose, lignocellulose, or a combination thereof, in a reaction mixture of a polar, aprotic solvent and an acid is reacted for a time, at a temperature, and at a hydrogen ion concentration wherein at least a portion of the cellulose or lignocellulose present in the reactant is converted to HMF. The reaction mixture is initially substantially devoid of water. As the reaction proceeds, dehydration of intermediates causes the water concentration in the reaction mixture to rise to no more than about 0.2 wt % water.
Type:
Grant
Filed:
March 28, 2014
Date of Patent:
January 26, 2016
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
James A. Dumesic, George W. Huber, Ronen Weingarten
Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of ? ketone product and ? ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.
Type:
Grant
Filed:
May 2, 2014
Date of Patent:
January 19, 2016
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Brian C. Austad, Andre Lescarbeau, Lin-Chen Yu
Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
January 12, 2016
Assignees:
Novartis AG, University of Washington through its Center for Commercialization
Inventors:
Arnab Kumar Chatterjee, Fang Liang, Casey Jacob Nelson Mathison, Pranab Kumar Mishra, Valentina Molteni, Advait Suresh Nagle, Frantisek Supek, Liying Jocelyn Tan, Agnes Vidal, Michael Herman Gelb, Frederick Simmons Buckner, Hari Babu Tatipaka, Neil Richard Norcross, John Robert Gillespie
Abstract: A powder of cold-soluble polysaccharide and polyol, which is highly viscous in water and suitable for direct compression, and a method for preparing the powder and uses thereof are described, the powder being notably intended for preparing solid forms with controlled release of an active principle.
Type:
Grant
Filed:
November 2, 2011
Date of Patent:
January 12, 2016
Assignee:
ROQUETTE FRERES
Inventors:
Baptiste Boit, Fabrice Buquet, Gregory Le Bihan, Philippe Lefevre
Abstract: The invention relates to a process for the manufacture of epichlorohydrin (“ECH”) by catalytic oxidation of allyl chloride (“AC”) with an oxidant wherein the catalytic oxidation is performed in an aqueous reaction medium, wherein a water-soluble manganese complex is used as oxidation catalyst, followed by the isolation of epichlorohydrin.
Abstract: The present invention relates to the use of a compound of Formula I for the manufacture of a medicament for treating or preventing cancer in a subject.
Abstract: A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R1 is independently selected from the group consisting of H, or halo; each R2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R2 together form —CH?CH— and form part of a polymer backbone; each R3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R4 is aryl; and each R5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.
Type:
Grant
Filed:
September 28, 2012
Date of Patent:
January 5, 2016
Assignee:
Switch Materials, Inc.
Inventors:
Neil Robin Branda, Jeremy Graham Finden, Simon James Gauthier, Ali Hayek, Kyle Andrew Hope-Ross, James Daniel Senior, Andreea Spantulescu, Serguei Sviridov
Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.
Type:
Grant
Filed:
January 7, 2015
Date of Patent:
December 29, 2015
Assignee:
Naktar Therapeutics
Inventors:
Antoni Kozlowski, Samuel P. McManus, Jennifer Riggs-Sauthier, Xiaoming Shen, Wen Zhang