Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.
Type:
Grant
Filed:
September 13, 2013
Date of Patent:
November 10, 2015
Assignee:
THE GENERAL HOSPITAL CORPORATION
Inventors:
Douglas E. Raines, Stuart A. Forman, Keith W. Miller, Syed Shaukat Husain, Joseph F. Cotten
Abstract: Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
Type:
Grant
Filed:
March 5, 2013
Date of Patent:
November 3, 2015
Assignee:
MEDIVATION PROSTATE THERAPEUTICS, INC.
Inventors:
Rajendra Parasmal Jain, Remy Angelaud, Andrew Thompson, Carol Lamberson, Scott Greenfield
Abstract: The invention relates to a process for the preparation of salts having perfluoroalkyltricyano- or perfluoroalkylcyanofluoroborate anions, ((per)fluoro)phenyltricyano- or ((per)fluoro)phenylcyanofluoroborate anions, phenyltricyanoborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms or phenylcyanofluoroborate anions which are mono- or disubstituted by perfluoroalkyl groups having 1 to 4 C atoms, by reaction of alkali metal trifluoroperfluoroalkylborate with trialkylsilyl cyanide and a subsequent salt-exchange reaction or by direct reaction of an organic trifluoroperfluoroalkyl borate with trialkylsilyl cyanide.
Type:
Grant
Filed:
November 18, 2014
Date of Patent:
November 3, 2015
Assignee:
MERCK PATENT GMBH
Inventors:
Nikolai (Mykola) Ignatyev, Michael Schulte, Jan Sprenger, Maik Finze, Walter Frank
Abstract: The present invention provides: a mononuclear metal complex that has high catalytic activity and can be used as a hydrogenation reduction catalyst that allows efficient hydrogenation reduction of a substance to be reduced; a tautomer or stereoisomer thereof; or a salt thereof. Provided is the mononuclear metal complex represented by the following formula (1), a tautomer or stereoisomer thereof; or a salt thereof. In the formula (1), Ar1 is an aromatic anionic ligand or an aromatic ligand, or is not present, Ar2 is a ligand having aromaticity and may or may not be substituted, and when Ar2 is substituted, the number of substituents may be one or more, M is an atom or ion of a transition metal, A1 and A2 are both carbon atoms, or one of A1 and A2 is a carbon atom and the other is a nitrogen atom, Y is an anionic group or a cationic group, or is not present, L is any ligand or is not present, and m is a positive integer, 0, or a negative integer.
Type:
Grant
Filed:
March 4, 2011
Date of Patent:
October 27, 2015
Assignee:
OSAKA UNIVERSITY
Inventors:
Shunichi Fukuzumi, Tomoyoshi Suenobu, Yuta Maenaka
Abstract: An improved multi-reaction zone process provides improved nitrile product quality and yield. In a first reaction zone, 1,3-butadiene is reacted with hydrogen cyanide in the presence of a catalyst to produce pentenenitriles comprising 3-pentenenitrile and 2-methyl-3-butenenitrile. In a second reaction zone, 2-methyl-3-butenenitrile, recovered from the first reaction zone, is isomerized to 3-pentenenitrile. In a third reaction zone, 3-pentenenitrile recovered from the first and second reaction zones is reacted with hydrogen cyanide in the presence of a catalyst and a Lewis acid to produce adiponitrile. Unwanted production and build-up of dinitriles, including methylglutaronitrile, in the first reaction zone for the hydrocyanation of 1,3-butadiene is prevented by limiting the flow of Lewis acid into the first reaction zone.
Abstract: A method for preparing plasmalogens and derivatives thereof represented by Formula B, wherein R1 and R2 are similar or different, derived from fatty acids; R3 is selected from hydrogen and small alkyl groups. The synthetic route involves production of novel cyclic plasmalogen precursors of Formula A and their conversion to plasmalogens and plasmalogen derivatives of Formula B. Also disclosed is the therapeutic use of plasmalogens and derivatives thereof as produced by the synthetic route of the present invention.
Type:
Grant
Filed:
November 16, 2012
Date of Patent:
October 27, 2015
Assignee:
PHENOMENOME DISCOVERIES INC.
Inventors:
M. Amin Khan, Paul L. Wood, Dayan Goodenowe
Abstract: The invention relates to novel fluorescent dyes with phosphorylated hydroxymethyl groups, a method for preparing the same as well as to their use in imaging techniques. The fluorescent dyes are coumarin, rhodamine or BODIPY dyes having of one of the following general formulae I-III: wherein W=OP(O)Y1Y2 or P(O)Y1Y2, where Y1 and Y2 independently denote any of the following residues: OH, O(?), ORa and ORb, NHRa and NHRb, NRaRb and NRcRd, ORa and NHRb, ORa and NRbRc, NHRa and NRbRc; and any salt thereof.
Type:
Grant
Filed:
October 18, 2011
Date of Patent:
October 20, 2015
Assignee:
Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
Inventors:
Stefan W. Hell, Shamil Nizamov, Gerald Donnert, Kirill Kolmakov, Heiko Schill, Lars Kastrup, Christian A. Wurm, Vladimir N. Belov, Johanna Wildanger, Katrin Willig
Abstract: The present invention relates to a pyrazole amide derivative, pharmaceutical compositions containing this compound and to its use in therapy.
Type:
Grant
Filed:
October 19, 2011
Date of Patent:
October 13, 2015
Assignee:
Glaxo Group Limited
Inventors:
Anthony William James Cooper, Paul Martin Gore, David House
Abstract: This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds.
Type:
Grant
Filed:
October 6, 2014
Date of Patent:
October 13, 2015
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, Terry William Balko, Jean Marie Defauw, Jacob J. Plattner, William Hunter White, Joseph Raymond Winkle, Yong-Kang Zhang, Yasheen Zhou
Abstract: An efficient method to induce the enantioselectivity in procarbonyl compounds using chiral organometallic complexes. The present invention is also described a method for producing organo metallic complexes using a base and a metal halide.
Abstract: Organic electroluminescent material containing iridium of the following general formula, in which R is C1-C8 alkyl, is provided. The preparation method of the above organic electroluminescent material containing iridium and the organic electroluminescent element using the above organic electroluminescent material containing iridium are also provided.
Type:
Grant
Filed:
November 25, 2010
Date of Patent:
October 13, 2015
Assignee:
Ocean's King Lighting Science & Technology Co., Ltd.
Abstract: The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quinolinium, unsubstituted quinolinium, substituted benzazolium, unsubstituted benzazolium, substituted indolinium, or substituted indolinium. The invention further provides luminescent donor molecule-quencher pairs and luminescent donor molecule-quencher-luminescent acceptor molecule conjugates wherein the quencher is a cyanine compound of the present invention. The energy transfer pairs are used to detect an analyte of interest in a sample.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
October 6, 2015
Assignee:
Life Technologies Corporation
Inventors:
Rosaria Haugland, Ching-Ying Cheung, Stephen Yue
Abstract: Transesterification processes for producing a compound of formula (I) wherein R1 is H or a methyl group, A and B are each, independently, a linear or branched C2-C5 alkylene group, comprising reacting: an acrylate or methacrylate of formula (II) wherein R1 is H or a methyl group and R2 is a C1-C4 alkyl group, with a compound of formula (III) wherein the reaction is performed: (i) in the presence of calcium oxide and calcium hydroxide, and (ii) wherein the molar ratio of the compounds of formula (II) to formula (III) is less than 4:1 or 3:1 respectively.
Type:
Grant
Filed:
June 11, 2014
Date of Patent:
September 29, 2015
Assignee:
RHODA OPERATIONS
Inventors:
Laurianne Timbart, Nemesio Martinez-Castro, James Woods, Howard Prokop, Rastko Vukov
Abstract: An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
Type:
Grant
Filed:
October 26, 2012
Date of Patent:
September 29, 2015
Assignee:
Merck Sharpe & Dohme Corp.
Inventors:
Cheol K. Chung, Guy R. Humphrey, Peter E. Maligres, Timothy J. Wright
Abstract: This invention relates generally to olefin metathesis, and more particularly relates to the synthesis of terminal alkenes from internal alkenes using a cross-metathesis reaction catalyzed by a selected olefin metathesis catalyst. In one embodiment of the invention, for example, a method is provided for synthesizing a terminal olefin, the method comprising contacting an olefinic substrate comprised of at least one internal olefin with ethylene, in the presence of a metathesis catalyst, wherein the catalyst is present in an amount that is less than about 1000 ppm relative to the olefinic substrate, and wherein the metathesis catalyst has the structure of formula (II) wherein the various substituents are as defined herein. The invention has utility, for example, in the fields of catalysis, organic synthesis, and industrial chemistry.
Abstract: The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect.
Abstract: The present invention provides a pharmaceutical composition for ameliorating and/or preventing leptin resistance. The pharmaceutical composition of the present invention contains flurbiprofen.
Abstract: A method for the production of 2-hydroxy-4-methylthiobutyric acid by hydrolysis of 2-hydroxy-4-(methylthio)butyronitrile is provided. 3-Methylmercaptopropionaldehyde is reacted with hydrogen cyanide in the presence of a base as catalyst in a main reaction zone of the multizone reactor to form a reaction mixture comprising the 2-hydroxy-4-(methylthio)butyronitrile, unreacted 3-methylmercaptopropionaldehyde, the catalyst and residual amounts of gaseous hydrogen cyanide. The residual gaseous hydrogen cyanide is removed from the main reaction zone to an absorption and post-reaction zone of the reactor which comprises a mixture of 3-methylmercaptopropionaldehyde and the catalyst; and the gaseous hydrogen cyanide is further reacted with the 3-methylmercaptopropionaldehyde in the absorption and post reaction zone. A molar ratio of hydrogen cyanide to 3-(methylthio)propanal in the main reaction zone is from 0.98 to 1.03.
Type:
Grant
Filed:
March 27, 2014
Date of Patent:
September 15, 2015
Assignee:
EVONIK DEGUSSA GmbH
Inventors:
Dieter Buss, Martin Steurenthaler, Michael R. Rinner, Stephan Kretz, Hans Joachim Hasselbach, Caspar-Heinrich Finkeldei, Martin Koerfer, Pablo Zacchi
Abstract: Novel compounds of the general formula are introduced, containing 5-arylidene-3,5-dihydro-4h-imidazol-4-one core. These compounds can be used for fluorescent staining of cell membranes, biomolecules' labeling in vivo and in vitro, a number of compounds also have photoacidic properties. This allows to use them, for example, as instruments to drastically change pH of a medium, and also as dynamic fluorescent probes for investigation of complex objects like proteins and micellae, as well as in studies of hydration dynamics and in photolithography.
Type:
Grant
Filed:
August 20, 2012
Date of Patent:
September 15, 2015
Assignee:
Evrogen Joint Stock Company
Inventors:
Ilia Victorovich Yampolsky, Konstantin Anatolyevich Lukyanov, Mikhail Sergeyevich Baranov