Abstract: Disclosed is the preparation of 2-deoxy-D-erythro-2,2-difluoro-ribofuranose-3,5-dibenzoate, a known intermediate for the preparation of Gemcitabine, by means of a reduction process; further disclosed is the purification of Gemcitabine by chromatography and the purification of Gemcitabine hydrochloride by crystallization techniques from ternary solvent mixtures. The main advantage of the invention is providing Gemcitabine hydrochloride with purity in conformity with the Pharmacopoeia requirements, as well as a process particularly convenient from the industrial point of view.
Type:
Grant
Filed:
October 21, 2009
Date of Patent:
October 30, 2012
Assignee:
Prime European Therapeucials S.p.A.
Inventors:
Alberto Varalli, Paolo Anesa, Maria Argese, Giuseppe Guazzi
Abstract: The invention provides a pseudoglycolipid effective for cancer treatment and the like and a novel synthesis intermediate therefor, as well as a medicament containing the pseudoglycolipid and the like. The inventive compound is represented by the formula (1), or a salt thereof, wherein each symbol is as defined in the specification.
Abstract: Methods of treating glioblastoma and pancreatic cancer are provided by the administration of a therapeutically effective amount of a iodo-hexose compound to a subject in need thereof. The subject disclosure includes methods of treating glioblastoma and pancreatic cancer comprising the administration of a therapeutically effective amount of a 2-deoxy-2-iodo-D-hexose compound including 2-deoxy-2-iodo-D-mannose, 2-deoxy-2-iodo-D-glucose, 2-deoxy-2-iodo-D-galactose, and/or 2-deoxy-2-iodo-D-talose to a subject in need thereof.
Type:
Grant
Filed:
October 19, 2009
Date of Patent:
October 30, 2012
Assignee:
Board of Regents, The University of Texas System
Abstract: The invention provides methods of purifying Rebaudioside D from the Stevia rebaudiana Bertoni plant extract along with Rebaudioside A. The methods are useful for producing high purity Rebaudioside D and Rebaudioside A. The high purity Rebaudiosides are useful as non-caloric sweeteners in edible and chewable compositions such as any beverages, confectionaries, bakeries, cookies, chewing gums, and alike.
Abstract: Improved methods and compositions for the treatment of native tissues with crosslinkers are provided. The methods and compositions will find particular use in increasing resistance to tearing, fissuring, rupturing, and/or delamination.
Abstract: Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.
Type:
Grant
Filed:
August 21, 2009
Date of Patent:
October 9, 2012
Assignee:
Theracos, Inc.
Inventors:
Jason Liou, Yuelin Wu, Shengbin Li, Ge Xu
Abstract: A process for sterilizing a solution comprising hyaluronic acid. The process comprises providing an aqueous solution of hyaluronic acid with a weight average molecular weight from 0.6 MDa to 3.6 MDa, and the concentration of the hyaluronic acid is from 0.04% to 0.8% by weight. The aqueous solution also has an ionic strength equivalent to an aqueous concentration of sodium chloride from 3% to 30% by weight. Once the aqueous, high salt, hyaluronic acid solution is prepared the solution is maintained at a temperature from 40° C. to 80° C. for at least 1 hour and not longer than six days. Following the heat treatment step, the aqueous solution is filtered through a sterilization filter medium to provide a sterilized high salt, hyaluronic acid solution.
Type:
Grant
Filed:
February 9, 2010
Date of Patent:
October 9, 2012
Assignee:
Bausch & Lomb Incorporated
Inventors:
X. Michael Liu, David J. Heiler, Thomas Menzel, Abbie Brongo, Susan E. Burke, Karl Cummins
Abstract: The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.
Type:
Grant
Filed:
April 8, 2009
Date of Patent:
October 9, 2012
Assignee:
Sloan-Kettering Institute for Cancer Research
Inventors:
David Gin, Michelle Adams, Kai Deng, Nicholas Perl, Annie Won, Philip Livingston, Govind Ragupathi
Abstract: Ionic liquids and cellulose ester compositions and processes for producing ionic liquids and cellulose esters. Cellulose esters can be produced by esterifying cellulose in a reaction medium comprising one or more halide ionic liquids and at least one binary component. Cellulose esters prepared via the methods of the present invention can have a degree of substitution (“DS”) of at least 1.5 and can comprise a plurality of ester substituents, where at least 50 percent of the ester substituents comprise alkyl esters having a carbon chain length of at least 6 carbons.
Type:
Grant
Filed:
August 25, 2011
Date of Patent:
September 25, 2012
Assignee:
Eastman Chemical Company
Inventors:
Charles Michael Buchanan, Norma Lindsey Buchanan
Abstract: Novel methods useful for treating a patient with bladder cancer such as superficial bladder cancer includes administering to the patient a therapeutically effective amount of valrubicin and trospium chloride.
Abstract: Intrauterine Fetal Growth Restriction (IUGR) is a very important clinical problem for which no satisfactory treatment is available so far. The current invention of intravenous (IV) hypertonic glucose supplementation to the mother to improve the glucose transfer to the fetus at the intervillous space by improved facilitated diffusion can be a safe and easy way of treating this problem, as the improved fetal blood glucose can lead to fetal lipogenesis that can conserve the fetal O2 (oxygen) utilization and also relieve the associated metabolic derangements of fetal hypoxia, hypercapnia, and acidosis, apart from replenishing the oxidized coenzymes needed for the carbohydrate metabolism. The use of trans-amniotic fetal feeding studied by animal experiments can be difficult in humans, because of the danger of infection, which can be overcome by the use of implantable ports with a sterile patch technique.
Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with orthoester-type protecting groups. The 2? protected monomers also include a second, aryl carbonate-type, protecting group. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
Type:
Grant
Filed:
December 3, 2007
Date of Patent:
August 14, 2012
Assignees:
Agilent Technologies, Inc., The Regents of the University of Colorado
Inventors:
Douglas J. Dellinger, Brian Stell, Marvin H. Caruthers
Abstract: The present invention is directed generally to stable formulations of a TLR agonist preferably a TLR7 or a TLR8 agonist, for use in the treatment of cancer, preferably solid tumors and lymphomas. Specifically, the present invention is directed to stable formulations of up to 50 mg/ml of a TLR agonist which comprise a cyclodextrin.
Type:
Grant
Filed:
July 31, 2009
Date of Patent:
August 14, 2012
Assignee:
VentiRx Pharmaceuticals, Inc.
Inventors:
J. Jeffry Howbert, Muralikrishna Duvvuri, Robert Hershberg, Gregory Dietsch
Abstract: The present invention provides methods and compositions for treating a disorder associated with a deficiency in a gene product of a CLN gene in a subject (e.g., neuronal ceroid lipofuscinosis (NCL)), comprising administering to the subject an effective amount of a sphingolipid (e.g., galactosylceramide, ceramide, lysophosphatidic acid, sulfatide and any combination thereof), thereby treating the disorder in the subject.
Type:
Grant
Filed:
November 12, 2009
Date of Patent:
August 14, 2012
Assignees:
Duke University, The American University of Beirut
Abstract: The instant invention involves a process for enhancing molecular mass of biomass reactants. The process comprises first forming a substituted or unsubstituted furfural from a biomass. The substituted or unsubstituted furfural is then reacted with an activated methylene compound in the presence of a catalyst and, if desired, a solvent to form a Knoevenagel product. The product may then be hydrogenated to products containing an alcohol, ether, aldehyde, or ketone functional groups or to an olefinic or aliphatic species wherein as much as all of the oxygen and/or nitrogen has been removed.
Type:
Grant
Filed:
July 29, 2008
Date of Patent:
August 7, 2012
Assignee:
Georgia Tech Research Corporation
Inventors:
Travis J. C. Hoskins, Carsten Sievers, Pradeep K. Agrawal, Christopher W. Jones
Abstract: Process for preparing a compound of the formula (I) R1-S(O)x—S(O)yR2 in which R1 represents a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen; R2, independently of R1, represents a carbon-containing group or a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen, and x and y are selected from 0 and 1 in such a way that the sum of x and y is not more than 1, characterized in that a compound of formula (II) R1-S(O)x—R3-Si(R4)(R5)(R6) in which R3 represents a hydrocarbon chain of two carbon atoms, which is optionally unsaturated and/or substituted, and R4, R5 and R6, which are identical or different, each represent, independently of one another, a
Abstract: Methods and compositions for reducing fibrosis are provided, wherein an admixture of at least a galactose-pronged polymer and a pharmaceutically acceptable carrier is obtained and administered, wherein the administration of a sufficient amount of the admixture is measured by a quantitative change in a fibrosis tissue marker.
Type:
Grant
Filed:
May 16, 2007
Date of Patent:
August 7, 2012
Assignee:
Galectin Therapeutics
Inventors:
David Platt, Eliezer Zomer, Anatole Klyosov
Abstract: Methods are provided for using doxorubicin active agents in which reduced host toxicity is observed. Aspects of the methods including administering to a subject an effective amount of a doxorubicin active agent in conjunction with a doxorubicin toxicity-reducing adjuvant, e.g., a nitrone compound, or a nitrone compound in combination with a bisdioxopiperazine compound. Also provided are compositions for use in practicing the subject methods. The methods and compositions find use in a variety of different applications, including in the treatment of a variety of different disease conditions.
Abstract: Disclosed are nucleosides which are useful in diagnosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.
Type:
Grant
Filed:
May 18, 2009
Date of Patent:
July 24, 2012
Inventors:
Rakesh Kumar, Babita Agrawal, D. Lorne J. Tyrrell
Abstract: New compounds and methods for the preparation of combinatorial libraries of potentially biologically active compounds are based on monosaccharides of formula I being a derivative of a furanose or pyranose form of a monosaccharide, .
Type:
Grant
Filed:
August 8, 2003
Date of Patent:
July 17, 2012
Assignee:
Alchemia Limited
Inventors:
Michael West, Peter Andrews, Tracie Elizabeth Ramsdale, Wim Meutermans, Giang Thanh Le, Chris Clark, Giovanni Abbenante, Ligong Liu