Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
Abstract: Antimicrobial compositions based on the synergistic combination of 2-methyl-3-isothiazolone and selected commercial microbicides where the compositions are substantially free of halogenated 3-isothiazolone, are disclosed. Particularly preferred are combinations of 2-methyl-3-isothiazolone together with benzoic acid, citric acid, sorbic acid, 1,2-dibromo-2,4-dicyanobutane, 1,3-dimethylol-5,5-dimethylhydantoin, phenoxyethanol, benzyl alcohol, zinc pyrithione or climbazole, that provide enhanced microbicidal efficacy at a combined active ingredient level lower than that of the combined individual 3-isothiazolone and commercial microbicide effective use levels.
Abstract: The invention provides new lipopolyamines of spermine type of the general formula I, wherein X is C—N bond or aminopolyethyleneglycolcarboxamide linker or o-hydroxy-alkylcarboxamide linker or ?-hydroxyalkylcarboxamidopolyethyleneglycol-carboxamide linker, and wherein a hydrophobic domain Y is an acyl symmetrically branched in the position C(2) or cholesteryl. The invention further provides a method of preparation of said lipopolyamines and their use for construction of polycationic liposomal drug carriers.
Type:
Grant
Filed:
January 14, 2013
Date of Patent:
July 19, 2016
Assignees:
USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., VYZKUMNY USTAV VETERINARNIHO LEKARSTVI, V.V.I.
Inventors:
Lukas Drasar, Miroslav Ledvina, Zina Korvasova, Jaroslav Turanek
Abstract: This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
Type:
Grant
Filed:
September 8, 2008
Date of Patent:
June 14, 2016
Assignee:
Ohr Pharmaceutical, Inc.
Inventors:
Michael McLane, Inez Ruiz-White, Henry Wolfe
Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and minocycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
Type:
Grant
Filed:
June 27, 2014
Date of Patent:
June 14, 2016
Assignee:
PARATEK PHARMACEUTICALS, INC.
Inventors:
Mark L. Nelson, Roger Frechette, Mohamed Y. Ismail, Laura Honeyman, Todd Bowser, Beena Bhatia
Abstract: Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols A, L1, G, X, Y, T and R1 have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).
Type:
Grant
Filed:
March 13, 2013
Date of Patent:
June 7, 2016
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
Abstract: Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer.
Type:
Grant
Filed:
September 23, 2013
Date of Patent:
May 17, 2016
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Margaret Clagett-Dame, Hector F. DeLuca, Nircaq J. Nieves, Lori A Plum, Mary E. Kaiser
Abstract: A medicine composition contains vitamin D and metformin, wherein vitamin D comprises vitamin D2, vitamin D3, alphacalcidol, calcifediol, calcitriol, and dihydrotachysterol. The composition can be used in the preparation of a medicine for treating and/or preventing a polyp and cancer in large intestine.
Type:
Grant
Filed:
August 17, 2011
Date of Patent:
May 10, 2016
Assignee:
GUANGDONG TAIHE MEDICINE SCIENCE & TECHNOLOGY CO., LTD
Abstract: The present invention concerns a process of isomerizing trans fused bicyclic derivatives into cis fused bicyclic derivatives and the preparation of vitamin D or analogs thereof comprising said isomerization step.
Type:
Grant
Filed:
January 24, 2011
Date of Patent:
April 19, 2016
Assignee:
HYBRIGENICS SA
Inventors:
Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean Lafay
Abstract: Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
Abstract: The present invention provides a VDR ligand which does not induce hypercalcemia that is an adverse reaction of a vitamin D3 preparation; and a composition which comprises lithocholic acid propionate, a salt thereof, a solvate thereof, or a prodrug thereof.
Abstract: Described are new insecticide compounds that are derived from 2,2-dimethyl-3-(2-methylpropenyl)cyclopropanecarboxylic acid, also known as chrysanthemic acid, insecticidal compositions that contain the compounds, methods of synthesizing the compounds and methods of eliminating harmful insects from a substrate including bringing the substrate into contact with an effective amount of one or more such compounds.
Type:
Grant
Filed:
September 15, 2008
Date of Patent:
February 2, 2016
Assignee:
Endura S.P.A.
Inventors:
Valerio Borzatta, Greta Varchi, Elisa Capparella, Alberto Guerrini, Arturo Battaglia, Federico Trefiletti
Abstract: This invention is directed to a new process for making an alkylaromatic compound. In an embodiment of this invention, the process is directed to selective synthesizing an alkylaromatic compound comprising a high amount of dialkylate product. In general, this process involves contacting at least one alkylatable aromatic compound with an alkylating agent and a catalyst under suitable reaction conditions such that the resulting reactor effluent prior to any stripping step may be characterized by a dialkylate product content of at least 44 wt % and a trialkylate and higher polyalkylate product content of no more than 20 wt %. The alkylaromatic compounds produced have excellent thermal and oxidative stabilities, good additive solvency, and improved seal compatibility while maintaining good VI and low temperature properties. They are useful as lubricant basestocks and lubricant additives.
Abstract: Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols A, L1, G, X, Y, T and R1 have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).
Type:
Grant
Filed:
April 28, 2011
Date of Patent:
December 29, 2015
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
Abstract: There is disclosed a method for isolation and purification of phytosterols from tall oil pitch comprising the steps of: a) contacting the tall oil pitch with a solvent to form a tall oil solvent mixture; b) separating the tall oil pitch solvent mixture in at least two separate streams wherein one process stream is enriched in acidic pitch components and a second stream enriched in free- and bound sterols in the form of steryl esters; c) subjecting the stream enriched in free- and steryl esters to treatment with an alcohol under transesterification conditions wherein a reaction mixture is formed and sterols comprising the steryl esters are liberated as free sterols; and d) separating the free sterols from the reaction mixture of step c) by crystallization and extraction with one or more solvents. There are disclosed free fatty acids and resin acids separated from the tall oil pitch. Moreover, there is disclosed a manufacture and separation of fatty acid alkyl esters by the method.
Abstract: The present invention relates to novel crystalline Form II of 17?-acetoxy-21-methoxy-11?-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical compositions comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.
Type:
Grant
Filed:
August 5, 2010
Date of Patent:
December 29, 2015
Assignee:
Richter Gedeon Nyrt.
Inventors:
Attila Balázs, János Csörgei, Ádám Demeter, Csaba Sánta
Abstract: An object of the present invention is to provide a process for synthesizing a vitamin D compound by simple procedures at lower costs. The present invention provides a process for preparing a vitamin D compound and an intermediate thereof, comprising the step of: (a) mixing a ketone or aldehyde, a Wittig reagent, and a base; or (b) mixing a ketone or aldehyde and a Wittig reagent, and then adding a base to the resulting mixture.
Abstract: The present invention is directed to novel processes for the preparation of paricalcitol to novel intermediates used in these processes, and to processes for preparation of the novel intermediates.
Type:
Grant
Filed:
July 22, 2009
Date of Patent:
December 15, 2015
Assignees:
AZAD PHARMACEUTICALS INGREDIENTS AG, UNIVERSITAT ZURICH
Inventors:
Thomas Bader, Alfred Stutz, Hans-Ulrich Bichsel, Changchun Fu
Abstract: Disclosed are methods of purifying the compound (20R,22R)-2-methylene-19-nor-22-methyl-1?,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Certain diol precursors formed during the synthesis of the compound and its diasteromers also may be obtained in crystalline form using ethyl acetate as a solvent.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
December 15, 2015
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Pawel Grzywacz, Lori A. Plum, Agnieszka Flores, James B. Thoden, Hazel M. Holden