Abstract: The subject invention provides a method of treating acne in a subject which comprises topically and periodically applying to the subject's acne a composition comprising 3-phenyl-1-benzo[f]chromen-1-one and a pharmaceutically acceptable carrier, wherein the 3-phenyl-1-benzo[f]chromen-1-one is present in an amount effective to treat the subject's acne. The subject invention also provides a method of treating a skin condition associated with abnormal sebum secretion or abnormal sebaceous gland function in a subject, compositions in such methods and a sorting method for identifying agonists of AhR pathway, useful in such methods and compositions.
Abstract: Provided are a process for preparation of darunavir or solvates or a pharmaceutically acceptable salt thereof substantially free of bisfuranyl impurities and a process for preparation of amorphous darunavir using the darunavir propionate solvate.
Type:
Grant
Filed:
July 23, 2013
Date of Patent:
October 25, 2016
Assignee:
Laurus Labs Private Limited
Inventors:
Kameswar R. Chivukula, Venkata R. Murthy, Venkata S. Indukuri, Seeta R. Gorantla
Abstract: A method for selective hydrogenation of furan-2,5-dialdehyde (DFF) into 2,5-di(hydroxymethyl)furan (DHMF) and into 2,5-di(hydroxymethyl)tetrahydrofuran (DHMTHF). In relation to the prior art, which uses C6 sugars or 5-hydroxymethyl furaldehyde (5-HMF) as raw materials, the method can be performed at low temperatures (lower than 120° C., preferably 80° C.), while consuming low amounts of catalyst relative to the initial reagent (in particular less than 5%, preferably less than 2% relative to the weight of the reagent). The heterogeneous catalyst used can also be recycled from one reaction to another. Finally, the choice of experimental conditions enables the selective formation of DHMF or DHMTHF.
Abstract: Provided is a two-step method of producing a compound of chemical formula 1 in the presence of an alcohol solvent and a Group 3B metal catalyst or a salt thereof, comprising a first step comprising alkylation or isomerization of an aldohexose-containing substrate to obtain an intermediate, and a second step comprising dehydration of the intermediate to produce a compound of chemical formula 1. Preferably, additional solvent and/or catalyst are not added in the second step.
Type:
Grant
Filed:
October 29, 2013
Date of Patent:
October 18, 2016
Assignee:
SAMSUNG ELECTRONICS CO., LTD.
Inventors:
Jong Min Lee, Hyeon Su Heo, Moo Ho Lee, Kyung Hae Lee
Abstract: A method for producing a multisubstituted biphenyl compound is represented by the following formula (2), including a step of coupling a substituted benzene compound represented by the following formula (1) in the presence of a solid catalyst with gold immobilized onto a support.
Type:
Grant
Filed:
October 9, 2013
Date of Patent:
October 18, 2016
Assignees:
KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, UBE INDUSTRIES, LTD.
Abstract: Disclosed herein is a monomer for binding nano-metal, which is useful for the preparation of a conductor having increased conductivity with ensuring flexibility and transparency. Polymerization of the monomer for binding nano-metal provides a conductive polymer composite including a nano-metal rod. A method of preparing the conductive polymer composite is also provided.
Type:
Grant
Filed:
June 26, 2015
Date of Patent:
October 4, 2016
Assignee:
SAMSUNG ELECTRONICS CO., LTD.
Inventors:
Byung Hee Sohn, Young Kwan Lee, Yi Yoiung Yun, Won Jae Joo
Abstract: The present invention relates to compounds that are useful as metal ligands and which can be bound to a biological entity such as a molecular recognition moiety and methods of making these compounds. Once the compounds that are bound to a biological entity are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilizing the radiolabelled compounds of the invention.
Abstract: The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.
Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
Type:
Grant
Filed:
September 18, 2014
Date of Patent:
September 20, 2016
Assignee:
Array BioPharma, Inc.
Inventors:
Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
Abstract: The compound “2-((4-nitrophenyl)amino)-7,8,9,10-tetrahydro cyclohepta[4,5]thieno[2,3-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-11(6H)-one” and method of synthesizing it, wherein the compound is effective to inhibit the growth and proliferation of human liver cancer cells HepG2. The compound has a higher efficiency to inhibit the growth and proliferation of these cells as it has an inhibitory concentration value (IC50) of 0.7 ?g, compared to reference medication Doxorubicin that has an (IC50) value of 1.2 ?g. It further surpasses that reference medication at all tested concentrations.
Abstract: Disclosed is a process for selectively producing (D+1)-member heterocyclic compounds from corresponding unactivated dienes or derivatives thereof in the presence of a transition metal or lanthanide catalyst or a precursor thereof, relative to D-member heterocyclic rings.
Abstract: The invention relates to macrocyclic picolinamides of Formula I and their use as fungicides.
Type:
Grant
Filed:
September 29, 2014
Date of Patent:
September 13, 2016
Assignee:
Dow AgroSciences LLC
Inventors:
Timothy P. Martin, Kevin G. Meyer, Benjamin Nugent, Chenglin Yao, W. John Owen, Anne M. Wilson, Ian O'Callaghan, Jeremy Wilmot, Johnathan E. DeLorbe, William Dent, III
Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
Abstract: The present invention describes branched and functionalized siloxanes and methods for making such compounds. The compounds have a variety of uses. One preferred application is as novel planarizing material for lithography, in which case functionalized branched siloxane, such as an epoxy-modified branched siloxane is particularly useful.
Type:
Grant
Filed:
April 8, 2015
Date of Patent:
September 6, 2016
Assignee:
Board of Regents, The University of Texas System
Inventors:
C. Grant Willson, Tsuyoshi Ogawa, Michael B. Jacobsson
Abstract: The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.
Type:
Grant
Filed:
February 12, 2014
Date of Patent:
September 6, 2016
Assignee:
AXOLABS GMBH
Inventors:
Rainer Constien, Anke Geick, Philipp Hadwiger, Torsten Haneke, Ludger Markus Ickenstein, Carla Alexandra Hernandez Prata, Andrea Schuster, Timo Weide
Abstract: Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides conjugated side-strapped phthalocyanines and methods for producing and using the same. In one particular embodiment, the conjugated side-strapped phthalocyanine is of the formula: where each of the substituents are defined herein.
Type:
Grant
Filed:
March 28, 2015
Date of Patent:
August 23, 2016
Assignee:
The Arizona Board of Regents on Behalf of the University of Arizona