Abstract: The present invention provides fused derivatives of Formula I: that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Type:
Grant
Filed:
December 17, 2010
Date of Patent:
June 24, 2014
Assignee:
Incyte Corporation
Inventors:
Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
Abstract: Aromatic N-halosulfonamide organic compounds have been known for over one hundred years. The ability of these compounds to release active halogen ions has been utilized in a range of biocidal and fungicidal applications. This disclosure deals with the use of halo active aromatic sulfonamide organic compounds as odor control and/or biocidal agents in a cleaning solution for use with bovines and other dairy animals.
Type:
Grant
Filed:
August 17, 2011
Date of Patent:
June 24, 2014
Inventors:
David J. Schneider, Charles A. Schneider
Abstract: This invention relates to a novel compound extracted from antrodia Cinnamomea and related compounds of formula (1), and pharmaceutical compositions comprising the compound of formula (1) and a pharmaceutically acceptable carrier or excipient. The invention further comprises the method of inhibit cancer cells by administering an effective amount of the compound of formula (1).
Abstract: This invention relates to an improved process for the preparation of compounds of Formula I, salts of the free base cis-adamantane-2-spiro-3?-8?-[[[(2?-amino-2?-methylpropyl)amino]carbonyl]methyl]-1?,2?,4?-trioxaspiro[4.5]decane, Formula (I) wherein X is an anion. The compounds of Formula (I) have antimalarial activity.
Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.
Type:
Grant
Filed:
January 16, 2013
Date of Patent:
June 10, 2014
Assignee:
Sanofi
Inventors:
Frederic Bailly, Xavier Bon, Philippe Vayron
Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
Type:
Grant
Filed:
September 27, 2012
Date of Patent:
June 3, 2014
Assignee:
AstraZeneca AB
Inventors:
Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
Abstract: The invention provides a process for making hydroxymethylfurfural comprising exposing a saccharide, e.g. glucose or fructose, to a metal complex of an N-heterocyclic carbene.
Type:
Grant
Filed:
June 18, 2008
Date of Patent:
May 20, 2014
Assignee:
Agency for Science, Technology and Research
Abstract: [Object] The main object of the present invention is to provide a fibrosis inhibitor. [Solving Means] The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
Abstract: The present invention relates to an efficient process of synthesizing some known Ertapenem compounds and to provide new intermediate compounds of Meropenem and Doripenem. The process and the intermediate can substantially increase the effective yield and reduce the impurity generation. The present invention further provides a novel and effective process for recovering and purifying ertapenem compounds by utilizing a low cost, materials with chemical stability as a carrier for isolating ertapenem compounds from extracts.
Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
Type:
Grant
Filed:
September 10, 2012
Date of Patent:
May 6, 2014
Assignees:
Children's Hospital Medical Center, Ausio Pharmaceuticals, Inc.
Inventors:
Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of ? ketone product and ? ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.
Type:
Grant
Filed:
December 24, 2008
Date of Patent:
May 6, 2014
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Brian C. Austad, Andre Lescarbeau, Lin-Chen Yu
Abstract: A means for the extraction and crystallization of quassinoids such as quassin and neoquassin from natural sources containing these compounds, using compounds that are Generally Recognized As Safe by the U.S. Food and Drug Administration is provided. In particular, a means for extraction that does not require use of lead acetate, chloroform, methanol, or diethyl ether is provided. The process includes a means of removing non-polar and very polar substances from an extracted residue to enhance crystallization of quassinoids from the residue.
Type:
Grant
Filed:
July 10, 2012
Date of Patent:
April 29, 2014
Assignee:
The University of the West Indies
Inventors:
Trevor Herbert Yee, Helen Marjorie Jacobs
Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
Type:
Grant
Filed:
February 28, 2012
Date of Patent:
April 29, 2014
Assignee:
AbbVie Inc.
Inventors:
Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.
Type:
Grant
Filed:
March 27, 2009
Date of Patent:
April 29, 2014
Assignee:
University of Kentucky Research Foundation
Inventors:
Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.
Type:
Grant
Filed:
March 27, 2009
Date of Patent:
April 29, 2014
Assignee:
University of Kentucky Research Foundation
Inventors:
Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.
Type:
Grant
Filed:
February 12, 2010
Date of Patent:
April 22, 2014
Assignee:
Phyton Holdings LLC
Inventors:
Brian A. Bucher, Edward M. Desimone, III, Roland R. Franke, Rex T. Gallagher, Barry J. Hand, Christopher D. Howe, James A. Johnson, John S. Juchum, Marc A. Plante, T. G. Sambandam, Dong S. Yang
Abstract: A process for the preparation of Darunavir comprises the reacting of 4-amino-N-(2R, 3S) (3-amino-2-hydroxy-4-phenylbutyl)-N-isobutyl-benzenesulfonamide with (3R, 3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivative in N-methyl-2-pyrrolidinone and isolating the resulting Darunavir. The process yields Darunavir with a very low level of the difuranyl impurity.
Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.
Type:
Grant
Filed:
May 22, 2013
Date of Patent:
April 15, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
Abstract: The present invention relates to novel piperazine compounds; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial and to treat diseases for which blocking the Cav2.2 and Cav3.2 calcium channels is beneficial, e.g. to treat pain.
Type:
Grant
Filed:
January 14, 2011
Date of Patent:
April 15, 2014
Assignee:
Convergence Pharmaceuticals Limited
Inventors:
Jag Paul Heer, Andrew Peter Cridland, David Norton
Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.