Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
June 19, 2013
Date of Patent:
May 12, 2015
Assignee:
Vanderbilt University
Inventors:
P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
Abstract: Methods and small molecule compounds for stem cell differentiation and treatment of animals with diseases are provided. One example of a class of compounds that may be used is represented by the compound of Formula I and II: or a pharmaceutically acceptable salt or solvate thereof, wherein A, X, Q, R1, R2, R3, R4 are as described herein.
Type:
Grant
Filed:
July 2, 2012
Date of Patent:
May 5, 2015
Assignee:
ChemRegen, Inc.
Inventors:
John Cashman, Marion Lanier, Mark Mercola, Dennis Schade, Erik Willems
Abstract: Novel compounds of the general formula (I): in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR via two nucleophilic moieties.
Type:
Grant
Filed:
March 4, 2010
Date of Patent:
April 14, 2015
Assignee:
Polytherics Limited
Inventors:
Antony Robert Godwin, Stephen James Brocchini
Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.
Type:
Grant
Filed:
January 31, 2011
Date of Patent:
April 7, 2015
Assignees:
Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation Foundation
Inventors:
Jung Beom Son, Seung Hyun Jung, Wha II Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The invention generally relates to the compositions and methods related to the use of adrenergic receptor agonists solutions for the treatment of skin and mucosal superficial wounds. Some of the preferred adrenergic receptor agonists include epinephrine, phenylephrine, norepinephrine, methoxamine, and mixtures thereof. The invention also relates to devices suitable for applying these solutions to the skin or the mucosal area. Methods according to the invention are especially effective to control superficial skin and mucosal bleeding and accelerate healing time.
Abstract: Embodiments of this invention provide methods, systems, and apparatus for determining whether a fetal chromosomal aneuploidy exists from a biological sample obtained from a pregnant female. Nucleic acid molecules of the biological sample are sequenced, such that a fraction of the genome is sequenced. Respective amounts of a clinically-relevant chromosome and of background chromosomes are determined from results of the sequencing. A parameter derived from these amounts (e.g. a ratio) is compared to one or more cutoff values, thereby determining a classification of whether a fetal chromosomal aneuploidy exists.
Abstract: Disclosed is a stable and safe antioxidant composition which can be used routinely. Specifically disclosed is an antioxidant composition which contains one or more compounds selected from the group consisting of D-aspartic acid, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving skin conditions. The skin conditions may include, but is not limited to, fine wrinkles, a rough skin, a dry skin, a skin cancer, a skin allergy, an inflammation of the skin and a photosensitive dermatosis. The composition may be used for an external preparation for the skin, a food, and a pharmaceutical product for cataract.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
February 24, 2015
Assignee:
Shiseido Company, Ltd.
Inventors:
Yosuke Tojo, Chieko Mizumoto, Yutaka Ashida, Masashi Mita
Abstract: A composition and a method of treatment utilizing a combination of statins (or HMG-CoA reductase inhibitors), a class of drug used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.
Type:
Grant
Filed:
August 13, 2012
Date of Patent:
February 10, 2015
Assignee:
Pivotal Therapeutics Inc.
Inventors:
George Jackowski, Rachelle MacSweeney, Nisar Shaikh, Jason Yantha, Valerie Schini-Kerth
Abstract: The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in dematerialised water, characterized in that the medium has a content of an aqueous phase of at least 60% by weight and a content of up to 40% by weight of solids comprising the amino(meth)acrylate polymer or copolymer, whereby the aqueous phase is charged by a sufficient amount of carbon dioxide that effects the amino(meth)acrylate polymer or copolymer to be present in solute form in the medium. The aqueous medium may be used beneficially as a coating or binding solution for the spray coating or binding of pharmaceutical compositions or nutraceutical compositions or cosmetical compositions.
Type:
Grant
Filed:
July 30, 2009
Date of Patent:
February 10, 2015
Assignee:
Evonik Röhm GmbH
Inventors:
Rosario Lizio, Michael Damm, Hans-Ulrich Petereit
Abstract: Formulations of sparingly water-soluble active ingredients, consisting of carrier particles provided with active ingredient-containing coatings, the sparingly soluble active ingredients being embedded in coatings composed of amphiphilic copolymers.
Type:
Grant
Filed:
September 13, 2010
Date of Patent:
February 10, 2015
Assignee:
BASF SE
Inventors:
Karl Kolter, Dejan Djuric, Stefan Fischer, Matthias Karl
Abstract: Gene expression profiling is a powerful tool that has varied utility. It enables classification of multiple myeloma into subtypes and identifying genes directly involved in disease pathogenesis and clinical manifestation. The present invention used gene expression profiling in large uniformly treated population of patients with myeloma to identify genes associated with poor prognosis. It also demonstrated that over-expression of CKS1B gene, mainly due to gene amplification that was determined by Fluorescent in-situ hybridization to impart a poor prognosis in multiple myleoma. It is further contemplated that therapeutic strategies that directly target CKS1B or related pathways may represent novel, and more specific means of treating high risk myeloma and may prevent its secondary evolution.
Type:
Grant
Filed:
October 6, 2009
Date of Patent:
February 10, 2015
Inventors:
John D. Shaughnessy, Jr., Bart Barlogie, Fenghuang Zhan
Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
Abstract: The invention provides a computer readable medium or media, having: (a) a first data structure relating a plurality of reactants to a plurality of reactions from a first cell, each of said reactions comprising a reactant identified as a substrate of the reaction, a reactant identified as a product of the reaction and a stoichiometric coefficient relating said substrate and said product; (b) a second data structure relating a plurality of reactants to a plurality of reactions from a second cell, each of said reactions comprising a reactant identified as a substrate of the reaction, a reactant identified as a product of the reaction and a stoichiometric coefficient relating said substrate and said product; (c) a third data structure relating a plurality of intra-system reactants to a plurality of intra-system reactions between said first and second cells, each of said intra-system reactions comprising a reactant identified as a substrate of the reaction, a reactant identified as a product of the reaction and a
Type:
Grant
Filed:
July 21, 2005
Date of Patent:
February 3, 2015
Assignee:
Genomatica, Inc.
Inventors:
Imandokht Famili, Christophe H. Schilling
Abstract: The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.
Abstract: This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.
Abstract: The invention provides a crystalline form of (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1H-[1,2,3]triazole-4-carbonyl)amino]pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
Abstract: The invention relates to methods of treating diseases, particularly cancers, that respond favorably to the inhibition of Nicotinamide phosphoribosyltransferase (Nampt); it also relates to therapeutic methods that utilize Nampt inhibitors in combination with NAD biosynthesis precursors to intentionally kill cancer cells while limiting or minimizing toxicity to normal host cells; and it relates to methods of identifying cancers that will be most responsive to treatment with Nampt inhibitors, particularly when administered in combination with nicotinic acid.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
December 16, 2014
Assignee:
Alzheimer's Institute of America, Inc.
Inventors:
Tracey C. Fleischer, Daniel M. Cimbora, Jeffrey S. Flick, Andrew D. Gassman, Vijay R. Baichwal, Damon I. Papac
Abstract: A tablet which comprises solid particles, especially magnesium oxide particles as the main component and has excellent shape retentivity with extremely low susceptibility to wearing and chipping. The tablet has a domed shape on each of the upper and lower horizontal surfaces of a cylindrical plate shape, wherein the domed shape on each of the upper and lower horizontal surfaces satisfies the following requirements (a), (b) and (c) in the cross-sectional shape including the center line of the cylindrical plate shape: (a) each corner has an angle of 25 to 45°, (b) each corner has a horizontal length of 0.30 to 1.0 mm, and (c) the cup has a depth of 0.6 to 1.2 mm.