Abstract: Bringing membrane proteins into aqueous solution generally requires the use of detergents or other amphiphilic agents. The invention provides a new class of amphiphiles, each of which includes a multi-fused ring system as a lipophilic group. These new amphiphiles confer enhanced stability to a range of membrane proteins in solution relative to conventional detergents, leading to improved structural and functional stability of membrane proteins, including integral membrane proteins. Accordingly, the invention provides new amphiphiles for biochemical manipulations and characterization of membrane proteins. These amphiphiles display favorable behavior with membrane proteins and can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
December 8, 2015
Assignees:
Wisconsin Alumni Research Foundation, The Board of Trustees of the Leland Stanford Junior University
Inventors:
Samuel Helmer Gellman, Pil Seok Chae, Brian Kobilka, Soren Rasmussen
Abstract: A process for producing triterpene alcohol, comprising sequentially conducting the following steps (A) to (C): (A) subjecting ?-oryzanol to alkaline hydrolysis; (B) mixing the alkaline hydrolysate with a low polarity organic solvent, and extracting triterpene alcohol to obtain a triterpene alcohol-containing low polarity organic solvent; and (C) adding water to the triterpene alcohol-containing low polarity organic solvent thus obtained, removing the low polarity organic solvent, and then melting triterpene alcohol in hot water, followed by cooling.
Type:
Grant
Filed:
August 19, 2011
Date of Patent:
December 1, 2015
Assignees:
Kao Corporation, Tsuno Food Industrial Co., Ltd.
Inventors:
Kohjiro Hashizume, Takuo Tsuno, Koji Kato, Hisahiro Morita
Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
December 13, 2010
Date of Patent:
December 1, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
Abstract: The invention describes a crystallized hybrid solid with an organic-inorganic matrix, of a three-dimensional structure, containing an inorganic network of indium-based metal centers that are connected to one another by organic ligands that consist of the entity —O2C—C6H3—N3—CO2—. Said solid is called IHM-2-N3 and has an X-ray diffraction diagram as given below.
Type:
Grant
Filed:
October 6, 2010
Date of Patent:
December 1, 2015
Assignees:
IFP ENERGIES NOUVELLES, CNRS
Inventors:
Marie Savonnet, David Farrusseng, Catherine Pinel, Delphine Bazer-Bachi, Nicolas Bats, Vincent Lecocq
Abstract: The present invention provides a process for isolating tigecycline which process comprises the step of spray drying a solution of tigecycline in a solvent. Preferably the solvent is water or an organic solvent. In another aspect, there is provided tigecycline obtainable by spray drying, particularly in amorphous form. In particular, the invention provides tigecycline obtainable by spray drying according to the process of the invention.
Abstract: The present invention provides compositions and methods for use in the treatment of hyperproliferative dermal diseases. Specifically, the present invention teaches pharmaceutical compositions for topical administration where the compositions contain nicotinamide and a vitamin D metabolite, calcipotriol, which are particularly effective in treating and in the maintenance treatment of psoriasis and other related dermal disorders and diseases.
Type:
Grant
Filed:
May 10, 2006
Date of Patent:
November 3, 2015
Assignee:
Dermipsor Ltd.
Inventors:
Avikam Harel, Zeev Even-Chen, Olga Bloch
Abstract: The invention describes a crystallized hybrid solid with an organic-inorganic matrix, of a three-dimensional structure, containing an inorganic network of aluminum-based metal centers that are connected to one another by organic ligands that consist of the entity —O2C—C6H3—N3—CO2—. Said solid is called MIL-53-Al—N3 and has an X-ray diffraction diagram as given below.
Type:
Grant
Filed:
October 6, 2010
Date of Patent:
October 20, 2015
Assignees:
CNRS, IFP ENERGIES NOUVELLES
Inventors:
Marie Savonnet, David Farrusseng, Catherine Pinel, Delphine Bazer-Bachi, Nicolas Bats, Vincent Lecocq
Abstract: The present invention is directed to a process for conferring cytoprotection on a population of cells which comprises administering to that population of cells a compound comprising a hydroxy-substituted aromatic ring structure and a non-fused polycyclic, hydrophobic substituent attached thereto. In particular, the present invention is directed to such a process wherein the administered compound is phenolic, such as a steriod (e.g., estrogen), and has a non-fused polycyclic, hydrophobic substituent attached to the hydroxy-substituted A-ring thereof.
Abstract: New crystalline forms of 17?-(3-Furyl)-5-?androstane-3?,14?,17?-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.
Type:
Grant
Filed:
November 23, 2006
Date of Patent:
September 8, 2015
Assignee:
ROSTAQUO S.P.A.
Inventors:
Alberto Cerri, Silvia Armaroli, Marco Torri
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 tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
Type:
Grant
Filed:
July 12, 2012
Date of Patent:
July 28, 2015
Assignee:
Paratek Pharmaceuticals, Inc.
Inventors:
Peter Viski, Beena Bhatia, Tadeusz Warchol, David Messersmith
Abstract: This invention provides a compositions and methods of using biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure, to protect genetically modified plants and their environment. An effective amount of at least one additional biological agent can be combined with the compound of Formula 1.
Type:
Grant
Filed:
July 22, 2013
Date of Patent:
July 21, 2015
Assignee:
E I DU PONT DE NEMOURS AND COMPANY
Inventors:
George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17?-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems.
Abstract: To provide a novel vitamin D3 derivative useful as a therapeutic agent for osteoporosis. Provided is a vitamin D3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.
Abstract: This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from pyrethroids, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.
Type:
Grant
Filed:
March 8, 2013
Date of Patent:
July 14, 2015
Assignee:
E I DU PONT DE NEMOURS AND COMPANY
Inventors:
George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: A compound represented by the following Formula (1) that is effective for the treatment of Paget's disease of bone or hypercalcemia or a medically acceptable solvate thereof; [wherein R1 refers to hydrogen atom, C1-C6 alkyl group optionally substituted with hydrogen group or C1-C6 alkoxy group optionally substituted with hydroxyl group, R2a and R2b refer to hydrogen atom, C1-C10 alkyl group optionally substituted with hydroxyl group, C6-C10 aryl group optionally substituted with hydroxyl group or C7-C12 aralkyl group optionally substituted with a hydroxyl group, or are combined to represent ethylene group. However, a compound in which R1 is a hydrogen atom or a methyl group and R2a and R2b are hydrogen atoms is excluded].
Abstract: This invention provides a composition comprising a a compound selected from Formula 1, an N-oxide and an agriculturally suitable salt thereof; and pymetrozine, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.
Type:
Grant
Filed:
March 8, 2013
Date of Patent:
June 9, 2015
Assignee:
E I DU PONT DE NEMOURS AND COMPANY
Inventors:
George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: The present invention provides novel dithiolopyrrolone compounds and their salts, which are useful as treatments for cancer and other proliferative diseases. The present invention also provides therapeutic compositions comprising particularly useful types of dithiolopyrrolones, the salts thereof, and methods of using the compounds within such types, particularly in treating proliferative diseases such as cancer.
Type:
Grant
Filed:
March 18, 2003
Date of Patent:
June 9, 2015
Assignee:
Welichem Biotech Inc.
Inventors:
Genhui Chen, Jianxiong Li, John Webster, Bin Li
Abstract: This invention provides a composition comprising a first compound selected from Formula 1, an N-oxide or an agriculturally suitable salt thereof; and a second compound selected from insecticidal macrocyclic lactones, wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure.
Type:
Grant
Filed:
March 8, 2013
Date of Patent:
June 9, 2015
Assignee:
E I DU PONT DE NEMOURS AND COMPANY
Inventors:
George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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 concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.