Abstract: The present invention relates to crystalline forms of valomaciclovir, processes for preparing crystalline forms of valomaciclovir, pharmaceutical compositions thereof and methods of using thereof.
Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
November 15, 2016
Assignee:
Array BioPharma, Inc.
Inventors:
Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
Abstract: The invention provides compounds that inhibit the degradation of Wee1. The compounds of the present invention are generally N-((1H-benzo[d]imidazol-2-yl)methyl)-9H-purin-6-amines. Compounds of the invention can be used for treatment of malconditions in patients for which inhibition of Wee1 is medically indicated, for example cancer, Alzheimer's, neurological disorders, psychiatric disorders, or inflammation-related disorders.
Type:
Grant
Filed:
February 26, 2013
Date of Patent:
November 15, 2016
Assignee:
The Scripps Research Institute
Inventors:
William R. Roush, Ronald Rahaim, Mathieu Bibian
Abstract: The present invention concerns a process to obtain primary, secondary or tertiary amines, via a direct amination reaction of alcohols in presence of bis(perfluoroalkylsulfonimide) acid or salts thereof catalysts, and derivatives.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
October 18, 2016
Assignees:
RHODIA OPERATIONS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Inventors:
Floryan Decampo, Damien Cartigny, Mohamad Ousmane, Marc Pera Titus
Abstract: Method for preparing certain oximes and oxime O-methyl ethers by reacting poorly water-soluble carbonyl compounds with salts of hydroxylamine or hydroxylamine O-methyl ether or the free base of hydroxylamine in the presence of certain phosphoric esters or salts thereof of the formula (I) wherein R1, R2 and X are defined as specified in the description.
Type:
Grant
Filed:
May 20, 2014
Date of Patent:
October 11, 2016
Assignee:
BAYER CROPSCIENCE AKTIENGESELLSCHAFT
Inventors:
Albert Schnatterer, Dieter Heinz, Martin Littmann, Ulrich Philipp, Juergen Ludwig, Constantin Frerick, Michael Barz
Abstract: Disclosed herein are compounds of Formula (I), wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
Abstract: A reagent for carrying out a difluoromethylation reaction of unsaturated compounds and ring-nitrogen-containing aromatic compounds, a zinc difluoro-methanesulfinate, as well as a method for making the reagent and a method for its use are disclosed.
Type:
Grant
Filed:
November 27, 2012
Date of Patent:
October 11, 2016
Inventors:
Phil S. Baran, Janice Akemi Dixon, Ryan Baxter, Yuta Fujiwara
Abstract: The presently disclosed subject matter demonstrates that ThnG and ThnQ enzymes encoded by the thienamycin gene cluster in Streptomyces cattleya oxidize the C-2 and C-6 moieties of carbapenems, respectively. ThnQ stereospecifically hydroxylates PS-5 giving N-acetyl thienamycin. ThnG catalyzes sequential desaturation and sulfoxidation of PS-5, giving PS-7 and its sulfoxide. The ThnG and ThnQ enzymes are relatively substrate selective, but give rise to the oxidative diversity of carbapenems produced by S. cattleya, and orthologues likely function similarly in allied streptomyces.
Type:
Grant
Filed:
September 21, 2015
Date of Patent:
October 4, 2016
Assignee:
THE JOHNS HOPKINS UNIVERSITY
Inventors:
Craig Arthur Townsend, Micah Jeffrey Bodner, Ryan Martin Phelan, Michael Francis Freeman
Abstract: A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream is produced that is fed to a crystallization zone followed by a solid-liquid displacement zone to form a low impurity slurry stream. The solids in the low impurity slurry stream are dissolved in a dissolution zone to produce a hydrogenation feed that is hydrogenated in a hydrogenation reactor to generate a hydrogenated FDCA composition. The hydrogenated FDCA composition is routed to a crystallization zone to form a crystallized produce stream that is separated from liquid in a solid-liquid separation zone to generate a purified wet cake stream containing FDCA that can be dried in a drying zone to generate a dry purified FDCA product stream.
Abstract: A cleaning or personal care composition containing at least one of 1,4-pentanediol and a ketal alcohol of formula (1) wherein R2 is hydrogen or C1-3 alkyl, each R3, R4, and R5 is independently hydrogen or C1-6 alkyl, R6 and R7 are each independently hydrogen or C1-6 alkyl, a=0-3, and b=0-1. R2 is hydrogen or C1-3 alkyl, each R3, R4, and R5 is independently hydrogen or C1-6 alkyl, each R6 and R7 is independently hydrogen, C1-6 alkyl optionally substituted with at least one hydroxyl groups, a=1-6, and b=0-2.
Type:
Grant
Filed:
September 20, 2013
Date of Patent:
October 4, 2016
Assignee:
GFBIOCHEMICALS LIMITED
Inventors:
Lee R. Rieth, Satyanarayana Majeti, Erich J. Molitor
Abstract: A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.
Type:
Grant
Filed:
May 15, 2015
Date of Patent:
September 20, 2016
Assignee:
Amphastar Pahmaceuticals, Inc.
Inventors:
Yinhua Qiu, Zhengyuan Wu, Song Chen, Haoning Zhang
Abstract: The present invention relates to novel nitric oxide donor compounds for the use in the treatment and/or prophylaxis of hypertensive glaucoma, normotensive glaucoma and ocular hypertension.
Type:
Grant
Filed:
October 10, 2013
Date of Patent:
September 20, 2016
Assignee:
NICOX SCIENCE IRELAND
Inventors:
Ennio Ongini, Nicoletta Almirante, Laura Storoni
Abstract: What are described are compositions comprising one or more compounds of the formula (I) and one or more compounds of the formula (II) in which R, Ra and Rb each independently of one another are straight-chain or branched saturated alkyl groups having 5 to 11 carbon atoms or straight-chain or branched mono- or polyunsaturated alkenyl groups having 5 to 11 carbon atoms, wherein the total amount of the compounds of the formulae (I) and (II), based on the total weight of the compositions, is at least 60% by weight. In an advantageous manner, the compositions are suitable for producing cosmetic, dermatological or pharmaceutical compositions, crop protection formulations, washing or cleaning compositions or paints or coatings.
Type:
Grant
Filed:
July 31, 2012
Date of Patent:
September 20, 2016
Assignee:
Clariant International Ltd.
Inventors:
Maurice Frederic Pilz, Peter Klug, Franz-Xaver Scherl, Joerg Grohmann
Abstract: Methods of treating an astrocytoma with agents effective to inhibit microglia function are provided, as well as methods of enhancing the efficacy of brain tumor radiation therapy on an astrocytoma in a subject. Also provided are methods of treating other solid tumor types, and tumor cell invasion, with guanylhydrazone compounds.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
September 13, 2016
Assignee:
The Feinstein Institute for Medical Research
Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
Type:
Grant
Filed:
August 14, 2014
Date of Patent:
September 13, 2016
Assignee:
Eolas Therapeutics, Inc.
Inventors:
Theodore M. Kamenecka, Yuanjun He, Rong Jiang, William Nguyen, Xinyi Song, Robert Jason Herr, Qin Jiang