Processes Patents (Class 536/55.3)
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Patent number: 6987091Abstract: A novel compound, 2?/3?-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2? and 3? regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2?-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2?/3?-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2?/3?-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2?/3?-O-acetyl-ADP-ribose are also provided.Type: GrantFiled: November 21, 2002Date of Patent: January 17, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Jef D. Boeke, Anthony Sauvé, Ivana Celic
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Patent number: 6982327Abstract: The invention relates to a method for producing protoplasts of cassava or closely related species, which protoplasts are capable of regeneration into plants. The method comprises producing friable embryogenic callus from explants of cassava or closely related species and isolating protoplasts from said friable embryogenic callus. The invention also concerns protoplasts obtainable by said method. The invention further relates to a method for transforming such a protoplast of cassava or closely related species, and transformed protoplasts obtainable thereby. In addition, the invention concerns a method for regenerating plants from these protoplasts and a cassava plant or closely related species obtainable thereby. Starch isolated from tubers of such cassava plants have an increased amylopectin content. The starch and a method for isolating it from said plants also forms part of the invention.Type: GrantFiled: April 11, 2001Date of Patent: January 3, 2006Assignee: Cooperatieve Verkoop-en Productievereniging van Aardeppelmeel en Derivaten ABEBE, B.A.Inventors: Richard G. F. Visser, Christiann J. J. Raemakers, Evert Jacobson, Johanna E. M. Bergervoet van Deelan
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Patent number: 6979734Abstract: The present invention relates to rubber latex comprising an amount of starch, which rubber latex has a reduced allergen activity as compared to the same rubber latex without starch. In addition, the invention relates to the use of modified starch as donning powder for surgical gloves, wherein the used starch is a granular, low crystalline, preferably a non-crystalline starch.Type: GrantFiled: May 8, 2000Date of Patent: December 27, 2005Assignee: Budev Medical B.V.Inventors: Max Gregor Paping, Johannes Jeekel
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Patent number: 6972330Abstract: Process for chemical synthesis of methoxy nucleosides.Type: GrantFiled: May 8, 2003Date of Patent: December 6, 2005Assignee: Sirna Therapeutics, Inc.Inventors: Leonid Beigelman, Peter Haeberli, Alexander Karpeisky, David Sweedler
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Patent number: 6951932Abstract: The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.Type: GrantFiled: October 24, 2002Date of Patent: October 4, 2005Assignee: King Pharmaceuticals Research & Development, Inc.Inventor: Allan R. Moorman
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Patent number: 6949640Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.Type: GrantFiled: February 16, 2001Date of Patent: September 27, 2005Assignee: Southern Research InstituteInventors: John A. Montgomery, Anita T. Fowler, John A. Secrist, III
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Patent number: 6946551Abstract: Compositions and methods of preparing compositions containing hyaluronic acid derived from eggshell membrane are disclosed. The compositions can contain essentially pure hyaluronic acid or hyaluronic acid in combination with other naturally occurring constituents derived from eggshell membrane. In another aspect, the invention is directed to a method of treating a mammal that will benefit from the administration of hyaluronic acid, which includes administering to the mammal a composition containing hyaluronic acid derived from eggshell membrane.Type: GrantFiled: July 9, 2003Date of Patent: September 20, 2005Assignee: New Life Resources, LLCInventors: Frank Daniel Long, Randall Gene Adams, Dale Paul DeVore
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Patent number: 6933372Abstract: The present invention provides a new method to process a solution containing heparin; heparin salts or heparin complexes in a solvent or a mixture of solvents to a solid form of heparin products characterized by use of a drum dryer at atmospheric pressure or under vacuum and at a suitable drying temperature.Type: GrantFiled: February 27, 2004Date of Patent: August 23, 2005Assignee: Warner-Lambert CompanyInventors: Ranganatha Raghavan, Jay Lee Jett
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Patent number: 6933381Abstract: Process for the production of polysaccharide ethers, e.g. cellulose ethers, are disclosed wherein salts formed during the process, e.g., sodium nitrate or sodium acetate, are converted to their corresponding acids and bases by means of an electric current, preferably in combination with a bipolar membrane and suitable catiion and/or anion membranes. The acids and bases recovered from the process can be recycled, thereby avoiding the need to provide for disposal of salts.Type: GrantFiled: February 2, 2001Date of Patent: August 23, 2005Inventors: Charles B. Mallon, John S. Vames, John I. Sarlis, Benito See, David M. Trampe, Rathin Datta
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Patent number: 6921753Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.Type: GrantFiled: June 19, 2001Date of Patent: July 26, 2005Assignee: Pfizer IncInventors: Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
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Patent number: 6921819Abstract: The invention relates to a process for the crosslinking of polysaccharides. The process of the invention is a process for the crosslinking of at least one polymer selected from polysaccharides and their derivatives, under the action of at least one polyfunctional crosslinking agent, characterized in that said polyfunctional crosslinking agent is reacted with said polymer, in the solid state, during hydration. The invention is applied to the manufacture of hydrogels and gels that can be used, in particular, in plastic or cosmetic surgery.Type: GrantFiled: July 16, 2001Date of Patent: July 26, 2005Assignee: Laboratoires d'Esthetique AppliqueeInventors: Estelle Piron, Raymonde Tholin
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Patent number: 6916920Abstract: A process for producing hydrazinomonosaccharide derivatives and use of hydrazines in determining the structures of aldose and ketose monosaccharides located at the reducing ends of saccharides.Type: GrantFiled: July 30, 2001Date of Patent: July 12, 2005Assignee: Takara Bio Inc.Inventors: Tsuyoshi Miyamura, Tomoe Egashira, Mutsumi Sano, Brad K. Bendiak, Ikunoshin Kato
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Patent number: 6906042Abstract: The invention provides micelles, pharmaceutical formulations comprising micells, solutions comprising micells, methods for preparing micells, methods for delivering micells to patients, and methods for treating sepsis, endotoxemia, septic shock and systemic inflamatory response syndrome in patients by adiministering micelles. The micelles comprises compounds of Forumala (A): wherein the substituents are as defined herein.Type: GrantFiled: February 20, 2001Date of Patent: June 14, 2005Assignee: Eisai Co., Ltd.Inventors: James McShane, Tori Arens, Kazuhiro Kaneko, Tomohiro Watanabe, Kazuhide Ashizawa
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Patent number: 6894160Abstract: The invention relates to the industrial conversion of carbohydrates, alcohols, aldehydes or polyhydroxy compounds in aqueous phase. According to the invention a catalytic method is used for the conversion, using a metal catalyst consisting of polymer-stabilized nanoparticles. A catalyst of this type is not deactivated by the conversion reaction as long as the stabilizing interaction between the polymer and the nanoparticles is maintained.Type: GrantFiled: January 10, 2003Date of Patent: May 17, 2005Assignee: Sudzucker Aktiengesellschaft Mannheim/OchsenfurtInventors: Emine Capan, Marc Sascha Hahnlein, Ulf Prusse, Klaus-Dieter Vorlop, Alireza Haji Begli
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Patent number: 6884880Abstract: A process for substantially enhancing the regio and stereoselective synthesis of 9-?-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-?-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2?-deoxy, 3?-deoxy, 2?-deoxy-2?-?-fluoro and 2?,3?-dideoxy-2?-?-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.Type: GrantFiled: August 21, 2002Date of Patent: April 26, 2005Assignee: Ash Stevens, Inc.Inventors: Pranab K. Gupta, Stephen A. Munk
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Patent number: 6884788Abstract: The present invention relates to biscarbodiimides, thiourea derivatives, urea derivatives, and cross-linked hyaluronan derivatives having at least one intramolecular disulfide bond, and methods of preparation thereof. The invention also includes thiolated hyaluronan derivatives and salts thereof having at least one pendant thiol group or a modified pendant thiol group, and methods of preparation thereof. An example of a modified pendant thiol group is a sulfhydryl group linked to a small molecule such as a bioactive agent, for example a drug or pharmaceutically active moiety. A hyaluronan derivative having a sulfhydryl group linked to a pharmaceutically active moiety is useful as a sustained or controlled release drug delivery vehicle. Compositions containing the hyaluronan derivatives of the invention can reversibly viscosify in vivo or in vitro, in response to mild changes in condition, and are thus useful in ophthalmic surgery and in tissue engineering.Type: GrantFiled: August 14, 2003Date of Patent: April 26, 2005Assignee: Anika Therapeutics, Inc.Inventors: Paul C. A. Bulpitt, Charles H. Sherwood, Khalid K. Sadozai
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Patent number: 6884882Abstract: A 2?-deoxyuridine derivative of formula I is bioavailable and thermally stable and forms a gel in water at a low concentration; and, can be employed as a drug delivery vehicle:Type: GrantFiled: April 27, 2004Date of Patent: April 26, 2005Assignee: Postech FoundationInventors: Byeang Hyean Kim, Sun Min Park, Yoon Suk Lee
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Patent number: 6878819Abstract: The present invention relates to a process for the preparation of oligosaccharides or oligosaccharide containing compounds, especially N-acetyl-chitooligosaccharides having a fucosylated monosaccharide. The invention also relates to novel oligosaccharides or oligosaccharide containing compounds, especially N-acetyl-chitooligosaccharides, which are fucosylated and optionally covalently bound to a carrier molecule.Type: GrantFiled: September 21, 2000Date of Patent: April 12, 2005Inventor: Jari Natunen
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Patent number: 6872819Abstract: Biomaterials are disclosed comprised of biodegradable, biocompatible, and bioabsorbable non-woven fabric materials for use in surgery for the guided regeneration of tissues. The non-woven fabric materials are comprised of threads embedded in a matrix, wherein both the matrix and the threads can be comprised of esters of hyaluronic acid, used singly or in combination, or esters of hyaluronic acid in combination with esters of alginic acid or other polymers.Type: GrantFiled: May 27, 1998Date of Patent: March 29, 2005Assignee: Fidia Advanced Biopolymers S.r.l.Inventors: Alessandra Pavesio, Massimo Dona' , Lanfranco Callegaro
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Patent number: 6867296Abstract: This invention concerns a process for recovering and purifying dianhydro sugar alcohols from a vapor stream comprising dianhydro sugar alcohols, such as isosorbide, and water vapor.Type: GrantFiled: April 16, 2003Date of Patent: March 15, 2005Assignee: E. I. du Pont de Nemours and CompanyInventor: Kamlesh Kumar Bhatia
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Patent number: 6864244Abstract: The present invention relates to the hemisulfate salt of 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine (Ia) with improved stability and physical properties which facilitate manufacturing, handling and formulating I and polymorphic crystalline forms thereof.Type: GrantFiled: December 9, 2003Date of Patent: March 8, 2005Assignee: Roche Palo Alto LLCInventors: Terrence Joseph Connolly, Joseph Armstrong Martin, Anthony Prince, Keshab Sarma
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Patent number: 6849748Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst, and subsequent purification of the anhydrosugar alcohol. Very high purities are achieved, without the use of organic solvents in the process.Type: GrantFiled: September 19, 2001Date of Patent: February 1, 2005Assignee: Archer-Daniels-Midland CompanyInventors: Kevin M. Moore, Alexandra Jan Sanborn
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Patent number: 6846810Abstract: The present invention relates to nucleoside derivatives for the treatment of Hepatitis C viral infections including compounds of formula I, pharmaceutical compositions comprising these compounds and methods for treatment or prophylaxis of Hepatitis C Virus mediated diseases employing said compounds in monotherapy or in combination therapy.Type: GrantFiled: November 19, 2003Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Joseph Armstrong Martin, Keshab Sarma, David Bernard Smith, Mark Smith
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Patent number: 6844328Abstract: The present invention is related to polysaccharide esters of N-derivatives of glutamic acid (N-GA derivatives). These polysaccharidic esters have antiproliferative activity and are characterized by a low systemic toxicity. The esters of the invention are used in the prevention and therapy of diseases caused by cellular hyperproliferation, particularly psoriasis, tumors, rheumatoid arthritis, or intestinal inflammatory pathologies.Type: GrantFiled: March 16, 2001Date of Patent: January 18, 2005Assignee: Eurand Pharmaceuticals Ltd.Inventors: Giuliana Miglierini, Luca Stucchi, Alessandro Rastrelli
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Patent number: 6838560Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3—(CH2)nS—R3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an integer ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.Type: GrantFiled: February 21, 2000Date of Patent: January 4, 2005Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Florence Marciacq, Sylvie Sauvaigo, Jean-François Mouret, Jean-Paul Issartel, Didier Molko
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Patent number: 6835718Abstract: This invention discloses compositions and methods for preparing biocleavable or biodegradable micelle compositions for carrying and releasing drugs and other active agents for therapeutic or other medical uses. Methods are also disclosed for preparing biocleavable cyclodextrin micelle carriers that release drugs under controlled conditions. The invention also discloses biocleavable or biodegradable micelle compositions that are coupled to biorecognition molecules for targeting the delivery of drugs to their site of action.Type: GrantFiled: April 10, 2001Date of Patent: December 28, 2004Assignee: KK Biomed CorporationInventor: Kenneth M. Kosak
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Patent number: 6828436Abstract: A method for purifying oligonucleotides by displacement chromatography on anion-exchange media, using high affinity, low molecular weight (less than about 10000 Da) displacers, is disclosed. Several examples of high affinity, low molecular weight anionic displacers are provided, including polycyclic aromatic compounds having sulfonic acid moieties attached thereon. The efficacy of the technique for high resolution separation of oligonucleotides is demonstrated for an industrial mixture.Type: GrantFiled: May 15, 2002Date of Patent: December 7, 2004Assignees: ISIS Pharmaceuticals, Inc., Rensselaer Polytechnic InstituteInventors: Abhinav A. Shukla, Ranjit R. Deshmukh, Steven M. Cramer, James A. Moore
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Patent number: 6825341Abstract: The present invention relates to a process for preparing functionalized polyalkyleneimines which are useful for formulating nucleic acids intended to be transfected into cells. This process consists in treating polyalkyleneimines with a functionalized hemiacetal in the presence of titanium (IV) isopropoxide and sodium borohydride.Type: GrantFiled: February 16, 2001Date of Patent: November 30, 2004Assignee: Gencell S.A.Inventors: Françoise Leclerc, Jean Herscovici, Daniel Scherman
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Patent number: 6815441Abstract: Reaction products of taurultam and glucose are useful as antineoplastic agents. They are produced by reacting an aqueous solution of taurultam and glucose at about 100 degrees Celsius for about 30 minutes, yielding a reaction product which has a melting point of 168 to 170 degrees Celsius.Type: GrantFiled: October 28, 2002Date of Patent: November 9, 2004Assignee: Ed. Geistlich Soehne AG fuer chemische IndustrieInventors: Ruediger Stendel, Rolf W. Pfirrmann
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Publication number: 20040220397Abstract: The present invention discloses novel methods and solid supports for the synthesis of 3′-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3′-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules.Type: ApplicationFiled: April 21, 2004Publication date: November 4, 2004Applicant: PROLIGO LLCInventors: Michael Leuck, Andreas Wolter
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Patent number: 6812223Abstract: The present invention relates to novel crystalline glucosamine sulphate metal salts for use in the treatment of acute and chronic forms of rheumatic and arthritic diseases and of all the pathological conditions originating from metabolic disorders of the osteo-articular tissues. More particularly, the present invention relates to novel crystalline glucosamine sulphate metal salts having low metal content wherein the metal may be either sodium or potassium. The present invention further relates to a solution-based and a solvent-free process for the preparation of the novel crystalline glucosamine sulphate metal salts having low metal content and to pharmaceutical compositions comprising the novel crystalline glucosamine sulphate metal salts having low metal content.Type: GrantFiled: June 2, 2003Date of Patent: November 2, 2004Assignee: Nicholas Piramal India LimitedInventors: Triptikumar Mukhopadhyay, Ravi Gajanan Bhat, E. S. Sreekumar
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Patent number: 6809086Abstract: A method of increasing proliferation of cells which comprises adding to cells a cellular proliferating amount of a primary hydroxyl group of N-acetylglucosamine selectively desulfated heparin having the following characteristics for an enzyme digestion product of the heparin: (1) contents of unsaturated disaccharides of the following formulae (a) and (b): measured by high performance liquid chromatography in the enzyme digestion product of the selectively desulfated heparin are less than 40% and 30 to 67%, respectively, (2) a content of disaccharides containing an N-substituted sulfate group is 75 to 95%, and (3) the weight average molecular weight Mw is 4,000 to 30,000 dalton.Type: GrantFiled: December 6, 2002Date of Patent: October 26, 2004Assignee: Seikagaku CorporationInventors: Saburo Hara, Keiichi Yoshida, Masayuki Ishihara
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Patent number: 6806259Abstract: An orally administered soft gelatin formulation preparation of low molecular weight Hyaluronic Acid (HA) for use as a nutritional supplement to provide the primary benefit of internally causing the softening of the human skin.Type: GrantFiled: December 21, 2001Date of Patent: October 19, 2004Assignee: Soft Gel Technologies, Inc.Inventors: Ronald G. Udell, Yousry M. A. Naguib
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Publication number: 20040192904Abstract: A process for the preparation of ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid.Type: ApplicationFiled: January 30, 2004Publication date: September 30, 2004Inventors: Aldo Banfi, Bruno Dall'Oro, Marco Frigerio, Alfredo Mancini
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Publication number: 20040176588Abstract: A method for production of a sugar oxazoline derivative represented by the following general formula (2), comprising the step of:Type: ApplicationFiled: December 30, 2003Publication date: September 9, 2004Inventors: Shin-ichiro Shoda, Masaya Fujita, Masako Suenaga, Kenji Saito
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Publication number: 20040176587Abstract: A process for the preparation of L-ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid and of a solvent. Said process comprises: a) the reaction of a triazole of formula (I) with a protected L-ribofuranose of formula (II)b) the removal of the Pg groups and, optionally, the conversion into a carboxyamide group of the R2 group of the compound obtained of formula (III) to give L-ribavirin.Type: ApplicationFiled: January 30, 2004Publication date: September 9, 2004Inventors: Aldo Banfi, Bruno Dall'Oro, Marco Frigerio, Alfredo Mancini
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Patent number: 6780822Abstract: The invention provides an organic diacid anhydride-modified chitosan and a method of preparing the same under high shear conditions which eliminates the use of solvents and excessive amounts of aqueous liquids. Also provided are organic diacid anhydride-modified chitosans containing an inorganic basic material which enhances the aging stability thereof. The invention also provides fluids useful in various well drilling and servicing operations comprising an alkaline aqueous liquid containing an organic diacid anhydride-modified chitosan, as well as a method of drilling wells therewith.Type: GrantFiled: January 21, 2003Date of Patent: August 24, 2004Assignee: Venture Chemicals, Inc.Inventors: Jack C. Cowan, Roy F. House, Tammy L. Rodrigue
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Patent number: 6780988Abstract: The invention describes a process for producing P1,P4-di(uridine-5′-)tetraphosphate (U2P4) or a salt thereof from uridine 5′-monophosphate (UMP); wherein the process comprises at least one of the steps (a) and (b): (a) adding UMP diphenylphosphate (UMP-DPP) in divided portions during a step of reacting UMP-DPP with an organic alkali salt of pyrophosphate (PP1) to produce a reaction mixture; wherein at least one equivalent of a first base is present during one portion of the reaction; (b) reacting UMP-DPP with a PPi-organic alkali salt in the presence of at least one equivalent of a second base to produce a reaction mixture, wherein the first base and the second base may be the same or different; (c) subsequently adding water to the reaction mixture to produce an aqueous reaction mixture; and optionally (d) adding an alkali to the aqueous reaction mixture.Type: GrantFiled: April 12, 2002Date of Patent: August 24, 2004Assignee: Yamasa CorporationInventors: Hideaki Maeda, Toshio Yamada, Hiroshi Sato, Yutaka Noda
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Publication number: 20040162424Abstract: Disclosed is a method of producing a compound with &bgr;1-4 linkage which contains the lactosamine structure involving reacting at least one donor substance Gal&bgr;OR where R is an organic group, and at least one acceptor substance which is a glucopyranosamino derivative having the formula GlcNR″-R′″, wherein NR″ is an azido, 2-N-acetyl-, 2-N-phtalimido, or an organic group bound to the 2-N-group of glucosamine, wherein R′″ is a glycosidically bound fluoro or is an O-, C-, N- or S-glycosidically bound aliphatic or aromatic compound, with the proviso that if NR″ is NRAc then R′″ is not OH and if NR″ is not NHAc then R′″ may be OH, in the presence of Bullera singularis or an E.C. group 3.2 glycosidase of essentially the same structure as an E.C. Group 3.2 glycosidase obtained from Bullera singularis to form the lactosamine derivative; and optionally isolating the compound with &bgr;1-4 linkage which contains the lactosamine structure.Type: ApplicationFiled: October 3, 2003Publication date: August 19, 2004Inventor: Kurt Nilsson
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Publication number: 20040147479Abstract: The invention provides a method of synthesizing &bgr;-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (&bgr;-L-FD4C). The method allows for large-scale production of &bgr;-L-FD4C in an efficient, cost-effective, and environmentally sound manner.Type: ApplicationFiled: April 11, 2003Publication date: July 29, 2004Applicant: Achillion Pharmaceuticals, Inc.Inventors: Bo Kowalczyk, Zhao Li, Ralph M. Schure, Lisa Dunkle
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Patent number: 6765090Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. wherein: X is Na, NH4 or H, provided that all X groups are not H.Type: GrantFiled: March 12, 2001Date of Patent: July 20, 2004Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, William Pendergast
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Patent number: 6750335Abstract: The invention relates to nucleoside derivatives with photolabile protecting groups of general formula (I) wherein R1 is H, F, Cl, Br, I, or NO2; R2 is H or CN, provided that R1 and R2 are not simultaneously H; R3 is H, 1-4 C alkyl, or phenyl; R4 is H or a conventional functional group for the synthesis of oligonuleotides; R5 is H, OH, halogen or XR6, where X=O or S, and R6 is a conventional nucleotide protecting group; and B is adenine, cytosine, guanine, thymine, uracil, 2,6-diaminopurin-9-yl, hypoxanthin-9-yl, 5-methylcytosin-1-yl, 5-amino-4-imidazolcarboxamid-1-yl or 5-amino-4-imidazolcarboxamid-3-yl, where, if B is adenine, cytosine or guanine the primary amine functionality, optionally, carries a permanent protecting group. Furthermore, these derivatives may be used for the light-controlled synthesis of oligonucleotides on a DNA chip.Type: GrantFiled: March 29, 2002Date of Patent: June 15, 2004Assignee: Nigu Chemie GmbHInventors: Wolfgang Pfleiderer, Sigrid Bühler, Heiner Giegrich
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Patent number: 6740752Abstract: Disclosed is a process for producing particles of the modified carbohydrate polymer chitosan. Such chitosan particles are “activated” as a consequence of the specific steps used in the process. The process involves precipitation of dissolved chitosan from an acid solution thereof by the step-wise addition of neutralizing agent to the solution. A partial neutralization is carried out under shear agitation to form a continuous gel phase having a pH within the range of 5.0 to 6.9. This partially neutralized chitosan gel phase is then further subjected to shear agitation for at least 10 seconds to homogenize the gel phase. The homogenized gel phase is then further neutralized under shear agitation to a pH of above 6.9 to form a gel-like suspension of discrete chitosan particles. Chitosan particles in this form are useful in a number of contexts including, in particular, in the area of plant care.Type: GrantFiled: October 23, 2002Date of Patent: May 25, 2004Assignee: The Procter & Gamble CompanyInventors: Henryk Struszcyk, Antoni Niekraszewicz, Magdalena Kucharska, Alojzy Urbanowski, Maria Wisniewska-Wrona
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Patent number: 6734300Abstract: An improved process for the purification of crude aqueous solutions of acarbose by passing such solutions through a strong acid cation-exchange resin, saturating such resin and recovering as an eluate a substantially pure acarbose solution. Purities of more than 98%, and preferably about 99% or higher, are thus obtained.Type: GrantFiled: October 24, 2002Date of Patent: May 11, 2004Assignee: VA, Farmaceutska Industrija, DDInventors: Kreso Mihaljevic, Jasna Azaric, Blazenko Bajic, Vladimir Mrsa, Dejana Kokanj
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Patent number: 6734298Abstract: A process for the preparation of cross-linked polysaccharides containg carboxy groups. The process comprises a first step of activating the carboxy groups in an anhydrous aprotic solvent and then reacting with a polyamine. The cross-linked polysaccharide may be subjected to sulfonation of the five hydroxy groups.Type: GrantFiled: June 18, 2001Date of Patent: May 11, 2004Assignee: Farmila-Thea Faraceutici S.p.A.Inventors: Rolando Barbucci, Giancarlo Sportoletti
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Patent number: 6727232Abstract: This invention relates to antibiotic compounds AA896 of the formula wherein: R1 is H, aryl, alkyl (C1-C20), —CH2-aryl, —C(O)alkyl(C1-C20), —C(O)NHalkyl(C1-C20), or —C(O)NHaryl; R2 is H, alkyl (C1-C20), —CH2aryl, alkyl (C1-C20) or —C(O)alkyl(C1-C20); R3 is —OH; R2 and R3 may optionally be taken together to form a moiety R4 is alkyl (C1-C20), or aryl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 25, 2002Date of Patent: April 27, 2004Assignee: Wyeth Holdings CorporationInventors: Yang-I Lin, Zhong Li, Gerardo DelaCruz Francisco, Leonard Alexander McDonald
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Patent number: 6720418Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.Type: GrantFiled: December 13, 2001Date of Patent: April 13, 2004Assignee: Grain Processing CorporationInventors: Richard L. Antrim, Frank W. Barresi
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Publication number: 20040068107Abstract: The present invention relates to an improved process for the preparation of pentopyranosyl nucleosides, in which a significant improvement and simplification of the process step described in DE-A-19741715 can be achieved.Type: ApplicationFiled: August 26, 2003Publication date: April 8, 2004Inventor: Gerhard Kretschmar
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Publication number: 20040063926Abstract: A novel method has been found to produce 2,2′-anhydro-1-(&bgr;-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(&bgr;-L-arabinofuranosyl)thymine. A novel method has been further found to L-2′-deoxyribose derivatives as a useful synthetic intermediate through L-2,2′-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.Type: ApplicationFiled: May 29, 2003Publication date: April 1, 2004Inventors: Hajime Iizuka, Kazuhiko Togashi, Tsuneji Suzuki
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Patent number: RE38743Abstract: Heterogeneous intimate admixtures of sulfated heparinic polysaccharides, well suited for the prophylaxis/treatment of acute thrombotic episodes in a human patient, comprise immixture of sulfated polysaccharides having a weight average molecular weight less than that of heparin and which include from 9% to 20% of polysaccharide chains having a molecular weight less than 2,000 daltons and from 5% to 20% of polysaccharide chains having a molecular weight greater than 8,000 daltons, the ratio between the weight average molecular weight and the number average molecular weight thereof ranging from 1.3 to 1.6.Type: GrantFiled: May 7, 2003Date of Patent: June 14, 2005Assignee: Aventis Pharma S.A.Inventor: Roger Debrie