Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.
Type:
Grant
Filed:
April 25, 2005
Date of Patent:
August 1, 2006
Assignee:
The United States of America as represented by the Secretary of the Army
Inventors:
Mark G. Hartell, Apurba K. Bhattacharjee, Rickey P. Hicks, John E. VanHamont, Wilbur K. Milhous
Abstract: A process for enriching the relative concentration of genistin from a mixture of isoflavones is described. In accordance with one aspect of the invention, the process comprises providing a material containing a mixture of isoflavones, extracting the material with an aqueous organic solvent solution, adding calcium oxide or calcium hydroxide to the extract to form calcium-isoflavone complexes and separating precipitated calcium-isoflavone complexes from the extract. The precipitated calcium-isoflavone complexes contain a higher concentration of genistin complexes than daidzin and glycitin complexes.
Abstract: The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure also includes pharmaceutical compositions comprising said forms.
Type:
Grant
Filed:
February 7, 2005
Date of Patent:
July 18, 2006
Assignee:
Pharmion Corporation
Inventors:
Dumitru Ionescu, Peter Blumbergs, Gary L Silvey
Abstract: Nucleotides comprising a reporter moiety and a polymerase enzyme blocking moiety in which the reporter moiety does not also act as a polymerase enzyme blocking moiety are described. Also described are compounds of Formula (I): wherein W is a phosphate group, B is a base, Y is a linker comprising an enzyme-cleavable group, R2 is a reporter moiety, R3 is selected from H or OH, Z and Z? are selected from H, OH, or a group X—R1, wherein X is a linker comprising an enzyme-cleavable group and R1 is a polymerase enzyme blocking group, provided that at least one of Z and Z? is X—R1.
Type:
Grant
Filed:
May 31, 2001
Date of Patent:
July 18, 2006
Assignee:
GE Healthcare UK Limited
Inventors:
Raj Odedra, Adrian Simmonds, Lee Pickering
Abstract: Methods for forming structurally defined organosilicon carbohydrates are provided. Additionally, structurally defined organosilicon carbohydrates are provided. The structurally defined organosilicon carbohydrates may be formed by contacting a hydrolase enzyme with an organosilicon reactant and a carbohydrate reactant. The enzyme may catalyze the formation of an ester bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and alcohol functional groups of the carbohydrate or organosilicon reactant. The enzyme may catalyze the formation of an amide bond between carboxylic acid, ester, or amide functional groups of the organosilicon or carbohydrate reactant and amine functional groups of the carbohydrate or organosilicon reactant.
Type:
Grant
Filed:
August 15, 2003
Date of Patent:
July 18, 2006
Assignees:
Dow Corning Corporation, Polytechnic University
Inventors:
Kurt Friedrich Brandstadt, Thomas Howard Lane, Richard A. Gross
Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphates.
Abstract: A superabsorbent polysaccharide can be obtained by crosslinking a polysaccharide or derivative thereof with at least 1% by weight of a flexible spacer having a chain length of at least 9 chain atoms and having terminal activated coupling groups. The flexible spacer may comprise a polyalkyleneglycol with a molecular weight from about 400 to 10,000. The coupling groups may be provided by divinyl sulphone units.
Type:
Grant
Filed:
March 9, 2001
Date of Patent:
July 4, 2006
Assignee:
SCA Hygiene Products AB
Inventors:
Guiseppe Mensitieri, Fabrizio Porro, Luigi Nicolais, Alessandro Sannino
Abstract: A resin composition, which comprises a biodegradable polymer and a biodegradable liquid crystalline polymer. The resin composition is useful for producing molded resin articles having good recyclability.
Abstract: The invention relates to the use of the disaccharide derivatives 3?-aminosucrose, sucrose-C6-acid and palatinose-C6?-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.
Abstract: Novel microgels, microparticles and related polymeric materials capable of delivering bioactive materials to cells for use as vaccines or therapeutic agents. The materials are made using a crosslinker molecule that contains a linkage cleavable under mild acidic conditions. The crosslinker molecule is exemplified by a bisacryloyl acetal crosslinker. The new materials have the common characteristic of being able to degrade by acid hydrolysis under conditions commonly found within the endosomal or lysosomal compartments of cells thereby releasing their payload within the cell. The materials can also be used for the delivery of therapeutics to the acidic regions of tumors and sites of inflammation.
Type:
Grant
Filed:
March 28, 2003
Date of Patent:
June 6, 2006
Assignee:
The Regents of the University of California
Abstract: The invention relates to the use of the disaccharide derivatives 3?-aminosucrose, sucrose-C6-acid and palatinose-C6?-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.
Abstract: Alcohol based hydraulic fracturing fluids useful for treating oil and gas wells are disclosed. The fluids are compatible with carbon dioxide, and comprise an alcohol, a polymer, a crosslinking agent, and a breaker. Hydroxypropyl guar with a molar substitution of about 1.2 to about 2.2 is identified as a presently preferred polymer.
Type:
Grant
Filed:
October 9, 2002
Date of Patent:
May 23, 2006
Assignee:
BJ Services Company
Inventors:
D. V. Satyanarayana Gupta, Greg Niechwiadowicz, Anita C Jerat
Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).
Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.
Type:
Grant
Filed:
July 1, 2003
Date of Patent:
May 2, 2006
Inventors:
Sudershan K Arora, Nawal Kishore, Jang Bahadur Gupta, Vishwas D Joshi
Abstract: Compositions and kits comprising combinations of ?-glucans and specific immunoglobulins are disclosed. The compositions and kits are useful in methods of preventing or treating infection by a pathogenic microorganism, in which ?-glucan is administered to a subject, and specific antibodies to a pathogenic microorganism are introduced into the subject.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
April 18, 2006
Assignee:
Nabi Biopharmaceuticals
Inventors:
Viliam Pavliak, Ali Ibrahim Fattom, Robert B. Naso
Abstract: In a reaction system having at least two liquid-liquid interfaces between an organic phase of raw material containing a compound(s) to be separated and an aqueous phase of an aqueous solution of inclusion-complexing agent and between that aqueous phase and an organic phase(s) of extraction solvent(s), the compound(s) to be separated is entrapped into the aqueous phase through formation of an inclusion complex(es) of the inclusion-complexing agent with the compound(s), while the compound(s) is entrapped into the organic phase(s) of extraction solvent(s) through dissociation of said inclusion complex(es). The foregoing operation is performed using, for example, a squarish U-shaped tube or an H-shaped tube with bottom plates. Preferred examples of inclusion-complexing agent include highly water-soluble branched cyclodextrins.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
April 18, 2006
Assignees:
National Institute of Advanced Industrial Science and Technology, Ensuiko Sugar Refining Co. Ltd., Bio Research Corporation of Yokohama
Abstract: Engineered protein kinases which can utilize modified nucleotide triphosphate substrates that are not as readily utilized by the wild-type forms of those enzymes, and methods of making and using them. Modified nucleotide triphosphate substrates and methods of making and using them. Methods for using such engineered kinases and such modified substrates to identify which protein substrates the kinases act upon, to measure the extent of such action, and to determine if test compounds can modulate such action. Also Engineered forms of multi-substrate enzymes which covalently attach part or all of at least one (donor) substrate to at least one other (recipient) substrate, which engineered forms will accept modified substrates that are not as readily utilized by the wild-type forms of those enzymes. Methods for making and using such engineered enzymes. Modified substrates and methods of making and using them.
Abstract: The present invention relates to the treatment of inflammatory skin conditions, including psoriasis, with a prodrug of 5-fluorouracil. The invention relates to methods for treatment of psoriasis with capecitabine, an oral prodrug of 5-fluorouracil.