Abstract: The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.
Type:
Grant
Filed:
June 13, 2011
Date of Patent:
August 19, 2014
Assignee:
Dipharma Francis S.r.l.
Inventors:
Emanuele Attolino, Mario Michieletti, Davide Rossi, Pietro Allegrini
Abstract: The invention relates to a process for the manufacture of epichlorohydrin (“ECH”) by catalytic oxidation of allyl chloride (“AC”) with an oxidant wherein the catalytic oxidation is performed in an aqueous reaction medium, wherein a water-soluble manganese complex is used as oxidation catalyst, followed by the isolation of epichlorohydrin.
Abstract: The present invention relates to a process of preparing a taxoid (X) by reacting a protected baccatin derivative (B) with a ?-lactam (C) in the presence of one or more Lewis acids and a base agent. The present invention also relates to a process of preparing the protected baccatin derivative (B) from a baccatin derivative (A) comprising a protection reaction catalyzed by one or more Lewis acids with an optional base agent.
Abstract: The invention provides novel derivatives of cyclopamine having the following formula:
Type:
Grant
Filed:
August 27, 2008
Date of Patent:
July 22, 2014
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
Abstract: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
Type:
Grant
Filed:
June 28, 2011
Date of Patent:
July 22, 2014
Assignee:
GFV, LLC
Inventors:
John K. Thottathil, Raymond P. Warrell, Jr.
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: 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: 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: 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 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: Provided is a compound having a spiro chiral carbon backbone, a stereoisomer thereof, an enantiomer thereof, an in vivo hydrolysable precursor thereof, or a pharmaceutically acceptable salt thereof. The compound having the spiro chiral carbon backbone has excellent osteoblast differentiation activity, mast cell inhibitory activity, and fatty acid synthesis inhibitory activity in the liver. Therefore, the compound can be expected to play an innovative role in treatment of osteoporosis, fatty liver, and obesity.
Type:
Grant
Filed:
October 30, 2009
Date of Patent:
April 22, 2014
Assignee:
SNU R & DB Foundation
Inventors:
Heon-Joong Kang, Jung-Rae Rho, Jeong-Ho Hong, Seung-Bum Park, Chan-Soo Shin, Jae-Hwan Lee, Jun-Young Hong, Eun-O Kim, Jeong-Ah Kim, Sang-Mi Oh
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: The present invention provides a method for the preparation of orally available pentacyclic taxane compounds, as well as intermediates useful in their preparation.
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