Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Type:
Grant
Filed:
May 24, 2011
Date of Patent:
April 8, 2014
Assignee:
AbbVie Inc.
Inventors:
Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
Abstract: The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions.
Type:
Grant
Filed:
November 2, 2010
Date of Patent:
April 1, 2014
Assignee:
Emcure Pharmaceuticals Limited
Inventors:
Mukund K. Gurjar, Swapnil P. Sonawane, Pankaj S. Patil, Samit S. Mehta
Abstract: This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
April 1, 2014
Assignee:
Cubist Pharmaceuticals, Inc.
Inventors:
Jan-Ji Lai, Jian-Qiao Gu, Pradip M. Pathare, Valdas Jurkauskas, Joseph Terracciano, Nicole Miller Damour
Abstract: Disclosed is a practical method for efficiently producing an alcohol compound by hydrogenating an aldehyde by using a homogeneous copper catalyst which is an easily-available low-cost metal species. Specifically disclosed is a method for producing an alcohol compound, which is characterized in that a hydrogenation reaction of an aldehyde compound is performed in the presence of a homogeneous copper catalyst and a diphosphine compound.
Abstract: The present invention generally relates to methods for the synthesis of catalysts, including epoxidation catalysts, and related compounds and catalyst compositions. Embodiments described herein may provide efficient processes for providing catalysts (e.g., epoxidation catalysts) in large quantities and using simplified methods.
Abstract: To provide a novel organoboron compound which is useful as a reactant of organic synthesis. To provide a method for manufacturing the organoboron compound. A novel organoboron compound represented by General Formula (G1) below is provided. Note that in General Formula (G1), R1 to R9 separately represent any one of hydrogen, an alkyl group having 1 to 6 carbon atoms, and an aryl group having 6 to 16 carbon atoms. R10 and R11 separately represent hydrogen or an alkyl group having 1 to 6 carbon atoms, and R10 and R11 may be bonded with each other to form a ring. Further, X represents an oxygen atom or a sulfur atom.
Type:
Grant
Filed:
December 22, 2011
Date of Patent:
March 18, 2014
Assignee:
Semiconductor Energy Laboratory Co., Ltd.
Abstract: The invention relates to a method for manufacture of hydrocarbon fuels and oxygenated hydrocarbon fuels such as alkyl substituted tetrahydrofurans such as 2,5-dimethyltetrahydrofuran, 2-methyltetrahydrofuran, 5-methylfurfural and mixtures thereof. The method generally entails forming a mixture of reactants that includes carbonaceous material, water, a metal catalyst and an acid reacting that mixture in the presence of hydrogen. The reaction is performed at a temperature and for a time sufficient to produce a furan type hydrocarbon fuel. The process may be adapted to provide continuous manufacture of hydrocarbon fuels such as a furan type fuel.
Abstract: The invention provides novel derivatives of cyclopamine having the following formula:
Type:
Grant
Filed:
August 27, 2008
Date of Patent:
March 11, 2014
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Brian Austad, Mark L. Behnke, Alfredo C. Castro, André B. Charette, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
Abstract: Described is a process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. Also disclosed are intermediates of docetaxel and methods for preparation thereof.
Abstract: The present invention relates to novel crystalline, water-soluble salts of a plk inhibitor. Such crystal salts are for example L-tartrate, succinate, phosphate, mesylate, maleate, L-malate, hydrochloride, fumarate (half mole of counterion), fumarate, citrate (half mole of counterion), benzenesulfonate and L-aspartate (half mole of counterion). New crystal forms of the base as well as solvates and hydrates of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
Abstract: A co-crystal compound containing ammonium nitrate and benzo-18-crown-6-ether. Ammonium nitrate and benzo-18-crown-6-ether are used to form the co-crystal compound with hydrogen bonding in a mole ratio of 1:1. A melting point of the co-crystal compound falls within a range of 124˜130° C., and the co-crystal compound can be prepared by an evaporation method or an anti-solvent method. The co-crystal compound comes with a non-hygroscopic property, a low burning rate (7 MPa, 0.58 mm/s) and a high pressure index (n>0.6), which can be used for replacing the oxidizer of a common gas generator propellant.
Abstract: Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.
Abstract: Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.
Abstract: The invention relates to the use of cyclovinyl phosphine compounds in the form of complexes with copper, as catalysts for reactions leading to the formation of carbon-carbon and carbon-heteroatom bonds. The invention also relates to complexes of copper with at least one cyclovinyl phosphine, as well as to the method for creating a carbon-carbon or a carbon-heteroatom bond catalysed by a cyclovinyl phosphine/copper complex.
Type:
Grant
Filed:
September 26, 2008
Date of Patent:
December 10, 2013
Assignee:
Centre National de Recherche Scientifique (C.N.R.S.)
Inventors:
Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani
Abstract: A perimidine-based squarylium dye contains a compound represented by Formula (I), the compound containing an isomer A and satisfying the following formula: Pa?95(%) wherein the isomer A is an isomer of the peak shown in the longest retention time among all peaks due to isomers obtained by analysis of the compound by means of reversed-phase high-performance liquid chromatography, and Pa represents a value of the peak area of the isomer A relative to the peak area of all peaks.
Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.
Type:
Grant
Filed:
January 30, 2008
Date of Patent:
November 19, 2013
Assignee:
Life Technologies Corporation
Inventors:
Kyle Gee, Aleksey Rukavishnikov, Diane M. Witczak
Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.
Type:
Grant
Filed:
March 15, 2010
Date of Patent:
November 12, 2013
Assignee:
Nerviano Medical Services S.r.l.
Inventors:
Angela Scaburri, Maria Adele Pacciarini, Marina Ciomei, Bernard Laffranchi, Silvia Comis
Abstract: Inhibitors of the enzyme beta-lactamase are provided comprising compounds of formula (II) wherein R1 or R2 is a pyridyl group and R5 is a group of formula The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.
Type:
Grant
Filed:
September 27, 2012
Date of Patent:
November 5, 2013
Assignee:
Southern Methodist University
Inventors:
John D. Buynak, Anjaneyulu Sheri, Sundar Ram Reddy Pagadala