Abstract: The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
Type:
Grant
Filed:
July 25, 2013
Date of Patent:
October 31, 2017
Assignee:
Tapestry Pharmaceuticals, Inc.
Inventors:
James D. McChesney, Gilles H. Tapolsky, David Lloyd Emerson, John Marshall, Michael Kurman, Manuel R. Modiano
Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
August 30, 2016
Assignee:
Proximagen Limited
Inventors:
Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
Abstract: Provided are compositions, methods of making the compositions, and methods of using the compositions. The compositions can be provided as pharmaceutical preparations for use in disease treatment, such as cancer therapy. The compositions include novel pharmaceutical preparations which contain effective concentrations of a chemical compound. One compound used is 10H-1,3-Dioxolo[4,5-g]pyrano[3?,4?:6,7]indolizino[1,2-b]quinoline-8,11(7H,12H)-dione, 7-ethyl-7-hydroxy-, (S)-. The invention also provides methodologies for preparing pharmaceutical preparations for use in intravenous and oral pharmaceutical preparations that contain drug compounds that are difficult to dissolve in water.
Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
Type:
Grant
Filed:
April 9, 2012
Date of Patent:
June 7, 2016
Assignee:
SPHAERA PHARMA PTE. LTD
Inventors:
Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
Abstract: Process for the synthesis of 2,5-furandicarboxylic acid through the oxidation of -hydroxymethylfurfural in a flow of oxygenor a compound containing oxygen, catalyzed by a supported catalyst containing a metal of the platinum group, carried out in aqueous solution in which the pH is maintained higher than 7 and lower than 12 through the addition of a weak base.
Abstract: The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4?-acetoxy-2?-benzoyloxy-5?,20-epoxy-1?-hydroxy-7?,10?-dimethoxy-9-oxo-11-taxen-13?-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.
Type:
Grant
Filed:
June 11, 2014
Date of Patent:
April 12, 2016
Assignee:
AVENTIS PHARMA S.A.
Inventors:
Eric Didier, Nicolas Tremaudeux, Lionel Zaske
Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.
Type:
Grant
Filed:
February 24, 2014
Date of Patent:
April 5, 2016
Assignee:
Phyton Holdings, LLC
Inventors:
James H. Johnson, T. G. Sambandam, Barry J. Hand, Christopher D. Howe, Roland R. Franke, Brian A. Bucher, John S. Juchum, Rex T. Gallagher, Marc A. Plante, Edward M. Desimone, III, Dong S. Yang
Abstract: The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
Abstract: The present invention relates to a new process for the preparation of 6-hydroxy-5-arylbicyclo[2.2.2]octan-2-one compounds of the formula (II); which may subsequently be further transformed to compounds of the formula (I): The present invention further relates to novel compounds as such, which compounds are useful intermediates in the above process.
Abstract: Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation.
Type:
Grant
Filed:
November 23, 2012
Date of Patent:
March 29, 2016
Assignee:
THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, & THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIV. TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
Inventors:
David George Lloyd, Darren Fayne, Mary Jane Meegan, Miriam Carr, Gemma Karena Kinsella, Laura Caboni, Wiliam Nicholas Jagoe, Billy Egan, Fernando Blanco, D. Clive Williams
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: 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: 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: 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: 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