Patents Issued in April 1, 2003
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Patent number: 6541598Abstract: A composition that can be used as catalyst is disclosed. The composition comprises, or is produced by combining, (A) a titanium compound; (B) either (i) a complexing agent, (ii) a combination of a complexing agent, hypophosphorous acid or a salt thereof, and optionally a solvent, a zirconium compound, or both, (iii) combinations thereof; (C) a phosphorus compound; and optionally a solvent. Also disclosed is a process that can be used for producing a polyester. The process comprises contacting, in the presence of an esterification or transesterification or polycondensation catalyst composition and a phosphorus compound, a carbonyl compound and an alcohol under a condition suitable for esterification, transesterification, or polymerization. Further disclosed is a process to make polyester with reduced insoluble particles or solids using a phosphorus compound other than the commonly used phosphoric acid.Type: GrantFiled: July 16, 2002Date of Patent: April 1, 2003Assignee: E. I. du Pont de Nemours and CompanyInventors: Jiwen F. Duan, Donald E. Putzig, Frederick K. Mallon, Timothy M. Davis
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Patent number: 6541599Abstract: A process for the manufacture of soluble hyperbranched polyamides is disclosed comprising the steps of combining multifunctional monomer reactants comprising amine and carboxylic acid functional groups in a reactor with water, and reacting amine and carboxylic acid functional groups of the multi-functional monomers at elevated temperature and pressure for a period of time sufficient to form a highly branched polyamide. The present invention advantageously provides a simple, practical, and environmentally friendly process for the manufacture of soluble hyperbranched polyamides comprising multifunctional in-chain and/or end groups. The present invention also provides a process for the manufacture of soluble hyperbranched polyamides from monomers with a broad range of the ratio of functional amine groups to acid groups.Type: GrantFiled: July 31, 2001Date of Patent: April 1, 2003Assignee: Eastman Kodak CompanyInventor: Jin-Shan Wang
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Patent number: 6541600Abstract: Highly branched polyamides prepared in a single step procedure of condensation polymerization of multifunctional monomer reactants comprising amine and carboxylic acid functional groups. Polymerization proceeds by reaction of an amine group of a first monomer unit with an acid group of a second monomer unit to form a reaction product having an amide linkage between the first and second monomer units and repetition of such amidation reaction between additional amine groups and acid groups of the multi-functional monomers and reaction products of the multi-functional monomers. In the present invention, in order to obtain a water soluble or dispersible hyperbranched polyamide, at least one of the multifunctional monomer unit reactants contains an amine, phosphine, arsenine or sulfide group, such that the highly branched polyamide contains in the backbone thereof an N, P, As or S atom capable of forming an onium ion.Type: GrantFiled: July 31, 2001Date of Patent: April 1, 2003Assignee: Eastman Kodak CompanyInventors: Jin-Shan Wang, Huijuan D. Chen
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Patent number: 6541601Abstract: Polyamide polymers with side chains from a polyamide backbone, preferably containing carbon to carbon unsaturation which provides unique conductive and color change properties, are described. In particular, unsaturation is in the form of side chains from the polyamide backbone, with aligned diacetylene groups in each side chain which are aligned and in the same plane.Type: GrantFiled: November 27, 2001Date of Patent: April 1, 2003Assignee: Board of Trustees of Michigan State UniversityInventors: Rawle I. Hollingsworth, Guijun Wang
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Patent number: 6541602Abstract: The present invention describes novel polymers, their use as organic semiconductors and/or electroluminescent materials, and electro-luminescent devices containing polymers of this type.Type: GrantFiled: May 2, 2001Date of Patent: April 1, 2003Assignee: Celanese Ventures GmbHInventors: Hubert Spreitzer, Heinrich Becker, Willi Kreuder
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Patent number: 6541603Abstract: The invention provides genetic suppressor elements that confer upon a cell resistance to platinum-based drugs, including cisplatin, methods for identifying and obtaining such elements, and methods of using such elements. The invention also provides cloned genes associated with sensitivity to cisplatin.Type: GrantFiled: August 3, 1999Date of Patent: April 1, 2003Assignee: The Board of Trustees of the University of IllinoisInventors: Deborah J. Kirschling, Andrei Gudkov, Igor B. Roninson
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Patent number: 6541604Abstract: The WSX receptor, WSX receptor extracellular domain (ECD), WSX receptor variants, chimeric WSX receptor (e.g., WSX receptor immunoadhesin), and antibodies which bind thereto (including agonist and neutralizing antibodies) are disclosed. Various uses for these molecules are described.Type: GrantFiled: January 8, 1997Date of Patent: April 1, 2003Assignee: Genentech, Inc.Inventors: Brian Bennett, William Matthews
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Patent number: 6541605Abstract: Disclosed are human mitogen-activated (MAP) kinase kinase isoforms (MKKs). MKKs mediate unique signal transduction pathways that activate human MAP kinases p38 and JNK, which result in activation of other factors, including activating transcription factor-2 (ATF2) and c-Jun. The pathways are activated by a number of factors, including cytokines and environmental stress. Methods are provided for identifying reagents that modulate MKK function or activity and for the use of such reagents in the treatment of MKK-mediated disorders.Type: GrantFiled: April 7, 1998Date of Patent: April 1, 2003Assignee: University of MassachusettsInventors: Roger J. Davis, Joel Raingeaud, Benoit Derijard
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Patent number: 6541606Abstract: This invention relates to methods for the stabilization, storage and delivery of biologically active macromolecules, such as proteins, peptides and nucleic acids. In particular, this invention relates to protein or nucleic acid crystals, formulations and compositions comprising them. Methods are provided for the crystallization of proteins and nucleic acids and for the preparation of stabilized protein or nucleic acid crystals for use in dry or slurry formulations. The present invention is further directed to encapsulating proteins, glycoproteins, enzymes, antibodies, hormones and peptide crystals or crystal formulations into compositions for biological delivery to humans and animals. According to this invention, protein crystals or crystal formulations are encapsulated within a matrix comprising a polymeric carrier to form a composition.Type: GrantFiled: August 10, 1999Date of Patent: April 1, 2003Assignee: Altus Biologics Inc.Inventors: Alexey L. Margolin, Nazar K. Khalaf, Nancy L. St. Clair, Scott L. Rakestraw, Bhami C. Shenoy
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Patent number: 6541607Abstract: An antimicrobial peptide produced by Bacillus subtilis 168 was isolated and characterized and named sublancin 168. The invention includes DNA encoding for the sublancin 168 peptides and peptides which are at least 80% identical to the sublancin 168 peptide. The peptides may be administered as anti-bacterials, or may be used in food preservation. The peptides may also be co-administered with other lantibiotics (such as nisin and subtilin), or with known antibiotics.Type: GrantFiled: April 17, 2000Date of Patent: April 1, 2003Assignee: University of MarylandInventor: J. Norman Hansen
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Patent number: 6541608Abstract: In one embodiment, the present invention is directed to a first oligonucleotide comprising the sequence of or derived from 5′-CTAGGGCGGGCGGGACTCACCTAC-3′ or the nucleic acid sequence complementary thereto. The first oligonucleotide can be used with a nucleic acid of between 15 and 30 nucleotides that does not comprise the sequence of the first oligonucleotide and is found in the region from V&bgr; to J&bgr; of the V&bgr;13.1 gene in V&bgr;13.1 T cells, wherein the sequences of the oligonucleotide and the nucleic acid are not found on the same strand of the V&bgr;13.1 gene pair, to amplify a portion of the V&bgr;13.1 gene. Alternatively, the first oligonucleotide can be used with a labeling moiety in methods of detecting a LGRAGLTY motif found in T cell receptors of V&bgr;13.1 T cells. This motif is associated with autoimmune diseases, such as multiple sclerosis (MS). Once the motif is detected, the autoimmune disease can be treated or its progress monitored.Type: GrantFiled: August 18, 2000Date of Patent: April 1, 2003Assignee: Baylor College of MedicineInventor: Jingwu Z. Zhang
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Patent number: 6541609Abstract: A substantially pure polypeptide having at least one antigenic determinant that is substantially identical to an antigenic determinant of a protein from a cell line infected with simian T-lymphotrophic virus-III or human T-lymphotrophic virus-IV (HTLV-IV), also known as HIV-2, the protein being selected from: a) a glycoprotein having a molecular weight (m.w.) of about, 160,000 daltons; a glycoprotein having a m.w. of about 120,000 daltons; a gag protein having a m.w. of about 55,000 daltons; a gag protein having a m.w. of about 24,000 daltons; and a glycoprotein having a m.w. of about 32,000 daltons. Also disclosed are various methods of immunoassay using that peptide or antibodies raised to it. Finally, immunoassays for simian specimens are disclosed using peptides that are immunologically cross-reactive with the above-described peptide, or antibodies thereto.Type: GrantFiled: February 6, 2001Date of Patent: April 1, 2003Assignee: President and Fellows of Harvard CollegeInventors: Myron E Essex, Phyllis J Kanki
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Patent number: 6541610Abstract: Fusion proteins having a tumor necrosis factor receptor (TNF-R) polypeptide and at least one additional polypeptide covalently fused thereto and selected from an interleukin-1 receptor (IL-1R) and a second TNF-R polypeptide. The receptor polypeptides are preferably fused together by a peptidyl linker. Suitable fusions include, for example, TNF-R-linker-TNF-R; TNF-R-linker-IL-1R; and TNF-R-linker-TNF-R-linker-L-1R molecules.Type: GrantFiled: March 20, 1995Date of Patent: April 1, 2003Assignee: Immunex CorporationInventor: Craig A. Smith
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Patent number: 6541611Abstract: A monoclonal antibody which binds to baboon and human CD2, and in particular LO-CD2b antibody. The antibody may be employed to prevent and inhibit an immune response in human patients, such as when the immune response is mediated by the activation and proliferation of T-cells or natural killer cells.Type: GrantFiled: June 14, 2000Date of Patent: April 1, 2003Assignee: Universite Catholique de LouvainInventors: Hervé Bazin, Dominique Latinne, Pierre Gianello
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Patent number: 6541612Abstract: Provided are rapamycin conjugates which are useful as immunogenic molecules for the generation of antibodies specific for rapamycin or a derivative thereof, for measuring levels of rapamycin or derivatives thereof; for isolating rapamycin binding proteins; and detecting antibodies specific for rapamycin or derivatives thereof. This invention also provides monoclonal antibodies specific for rapamycin or a ring opened derivative of rapamycin.Type: GrantFiled: February 2, 2001Date of Patent: April 1, 2003Assignee: WyethInventors: Katherine L. Molnar-Kimber, Craig E. Caufield, Timothy D. Ocain, Amadeo A. Failli
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Patent number: 6541613Abstract: Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hyrolyzable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs.Type: GrantFiled: December 15, 2000Date of Patent: April 1, 2003Assignee: Uyrex CorporationInventors: Sheldon S. Hendler, Jan Zielinski
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Patent number: 6541614Abstract: Polysaccharide derivatives derived from a polysaccharide or a derivative thereof by substituting a part or all of the hydrogen atoms of the hydroxyl groups of the polysaccharide or the derivative thereof with the groups represented by the following formula (1): —E1—(OA)n—E2—R (1) wherein E1 represents a divalent saturated C1-6 hydrocarbon group which may be substituted with one or more hydroxyl groups or oxo groups, n stands for a number of from 8 to 300, n numbers of As may be the same or different and each independently represent a divalent saturated C1-6 hydrocarbon group, E2 represents an ether bond or an oxycarbonyl group, and R represents a C4-30 alkyl group which may be substituted with one or more hydroxyl groups, in which the H(s) of one or more hydroxy groups in each of said groups (1) may be further substituted with the groups (1); thickeners and emulsifiers comprising these polysaccharide derivatives; as well as aqueous compositions containing said polysacchariType: GrantFiled: December 3, 2001Date of Patent: April 1, 2003Assignee: Kao CorporationInventors: Atsushi Nagasawa, Tomohito Kitsuki, Takeshi Ihara
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Patent number: 6541615Abstract: The present invention features isolated, purified, or enriched nucleic acid encoding a SIRP polypeptide and isolated, purified, or enriched SIRP polypeptide and uses thereof.Type: GrantFiled: November 14, 1997Date of Patent: April 1, 2003Assignee: Max-Planck-Gellschaft zur Foderung der Wissenschaften E.V.Inventors: Axel Ullrich, Alexei Kharitonenkov, Zhengiun Chen
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Patent number: 6541616Abstract: The invention discloses the Moraxella catarrhalis outer membrane protein polypeptide and polypeptides derived therefrom (collectively “OMP21”), nucleotide sequences encoding said OMP21, and antibodies that specifically bind OMP21. Also disclosed are pharmaceutical compositions including prophylactic or therapeutic compositions, which may be immunogenic compositions including vaccines, comprising OMP21, antibodies thereto or nucleotides encoding same. The invention additionally discloses methods of inducing an immune response to M. catarrhalis and OMP21 in an animal, preferably a human, methods of treating and methods of diagnosing Moraxella infections in an animal, preferably a human, and kits therefor.Type: GrantFiled: October 1, 1998Date of Patent: April 1, 2003Assignee: Antex Biologics Inc.Inventors: Kenneth Tucker, Ulrich F. Tillmann
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Patent number: 6541617Abstract: The invention relates to the use of particles comprising binding ligands and electron transfer moieties (ETMs). Upon binding of a target analyte, a particle and a reporter composition are associated and transported to an electrode surface. The ETMs are then detected, allowing the presence or absence of the target analyte to be determined.Type: GrantFiled: October 27, 1999Date of Patent: April 1, 2003Assignee: Clinical Micro Sensors, Inc.Inventors: Cynthia C. Bamdad, Robert C. Mucic
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Patent number: 6541618Abstract: The invention provides an asymmetric cyanine dye compound having the structure including substituted forms thereof, wherein, at least one of R1 and R2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labelled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labelled polynucleotides.Type: GrantFiled: June 21, 2000Date of Patent: April 1, 2003Assignee: Applera CorporationInventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
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Patent number: 6541619Abstract: The present invention provides a genetically engineered fusion protein consisting of hEGF that is internalized inside of the cells after tracing down the cancer cells expressing hEGF receptors and human angiogenin that is cytotoxic by degrading ribonucleotide upon internalization, a process for preparing a fusion protein in a large quantity by transforming E. coli with the expression vectors containing the gene encoding the fusion protein, and pharmaceutical application of the fusion protein as an anticancer agent. All components of the fusion protein form no antibodies and exhibit no immunotoxicity since they are derived from human. Each component alone is inactive to the cancer cells, however, once they are fused together, they kill the cancer cells selectively with a difference of 1000 fold in IC50 in spite of its low molecular weight. Therefore, the fusion protein of the present invention is capable of treating the cancer expressing hEGF receptors at high level without showing toxicity.Type: GrantFiled: July 13, 2000Date of Patent: April 1, 2003Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Myung-Hwan Park, Seung-Kook Park, Jong-Myung Yoon, Seung-Hee Han, Byung-Kwon Oh, Seung-Ho Kim, Young-Man Kim, Tai-Young Koo, Byoung-Kwang Lee
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Patent number: 6541620Abstract: The present invention provides nucleic acid molecules encoding a 30kDa TNF inhibitor or a fragment thereof having at least one non-native cysteine residue at the N-terminus, C-terminus, residue 14, or residue 15.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 2003Assignee: Angen Inc.Inventors: Michael T. Brewer, Robert C. Thompson, Tadahiko Kohno
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Patent number: 6541621Abstract: The present invention is directed to nucleic acid sequences encoding a novel regulatory element that induces a high level of expression to operably linked genes, upon exposure to hypoxic conditions. Furthermore, the regulatory element can be used to prepare an expression vector for transforming plant cells, wherein the DNA construct comprises a hypoxia inducible promoter operably linked to a gene sequence.Type: GrantFiled: March 8, 2000Date of Patent: April 1, 2003Assignee: Purdue University Research FoundationInventors: Thomas K. Hodges, Enamul Huq, Anwar Hossain
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Patent number: 6541622Abstract: The present invention provides the promoter clone discovery of an alpha-amylase gene of a starch utilizing yeast strain Schwanniomyces castellii. The isolated alpha-amylase promoter is an inducible promoter, which can regulate strong gene expression in starch culture medium.Type: GrantFiled: August 4, 2000Date of Patent: April 1, 2003Assignee: Battelle Memorial InstituteInventors: Johnway Gao, Rodney S. Skeen, Brian S. Hooker, Daniel B. Anderson
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Patent number: 6541623Abstract: The present invention provides novel nucleic acids, the novel polypeptide sequences encoded by these nucleic acids and uses thereof. These novel polynucleotide and polypeptide sequences were determined to be a novel Interleukin-1 Receptor Antagonist.Type: GrantFiled: May 22, 2000Date of Patent: April 1, 2003Assignee: Hyseq, Inc.Inventors: John Ford, Alice Suk-Yue Ho, Ann Pace
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Patent number: 6541624Abstract: This invention relates to Anacardium sp. specific genomic DNA sequence and the methods for utilization of these sequences in detection of Cashew husk in tea samples. Particularly this invention relates to a very sensitive, accurate and efficient method of identification of Anacardium occidentale (cashew) species. The method is designed to detect presence of any part of cashew plant including the dried and ground apple in market samples of made tea. The main application of this invention is to detect the adulteration of loose as well as branded tea by any part of cashew plant and thus is a part of quality control measures, in addition to the taxonomical authentication of cashew plants.Type: GrantFiled: October 30, 2000Date of Patent: April 1, 2003Assignee: Council of Scientific and Industrial ResearchInventors: Mahipal Singh, Bandana Dhiman
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Patent number: 6541625Abstract: The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of &bgr; and &agr; anomers represented by the following formula A or formula B: wherein R is selected from the group consisting of C1-6 alkyl and C6-15 aryl and Bz is benzoyl. The process comprises hydrolyzing said mixture with an enzyme selected from the group consisting of Protease N, Alcalase, Savinase, ChiroCLEC-BL, PS-30, and ChiroCLEC-PC to stereoselectively hydrolyze predominantly one anomer to form a product wherein R1 is replaced with H. The process also includes the step of separating the product from unhydrolyzed starting material. Additionally, the functional group at the C4 position is stereoselectively replaced with a purinyl or pyrimidinyl or derivative thereof.Type: GrantFiled: February 9, 2001Date of Patent: April 1, 2003Assignee: BioChem Pharma, Inc.Inventors: Alex Cimpoia, Yi Fong Wang
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Patent number: 6541626Abstract: Methods for selectively protecting the exocyclic amino function of a purine nucleoside are provided using activating agents to effect acylation at the exocyclic amino site. Methods are also provided for recycling polymer bound coupling supports from the reaction mixtures produced upon N-acylation.Type: GrantFiled: April 17, 2001Date of Patent: April 1, 2003Assignees: ISIS Pharmaceuticals, Inc., University of AllahabadInventors: Yogesh S. Sanghvi, Krishna Misra, Snehlata Tripathi
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Patent number: 6541627Abstract: A cellulose dispersion which is a dispersion comprising a dispersing medium and a cellulose having a fraction of cellulose I type crystal component of not more than 0.1 and a fraction of cellulose II type crystal component of not more than 0.4 and in which the average particle diameter of the constitutive cellulose is not more than 5 &mgr;m. A cellulose particulate and a cellulose composite particulate which have an average particle diameter of 0.2 to 20 &mgr;m, a ratio of long diameter (L) to short diameter (D) observed through a scanning electron microscope (L/D) of not more than 1.2 and a coefficient of aggregation of 1.0 to 3.0. The present invention provides a cellulose dispersion which has an excellent effect such as dispersion stability or the like and is high in transparency. Moreover, it provides a cellulose particulate and a cellulose composite particulate which have such performances as no rough feel, excellent rolling properties, high dispersibility and the like.Type: GrantFiled: June 1, 2000Date of Patent: April 1, 2003Assignee: Asahi Kasei Kabushiki KaishaInventors: Hirofumi Ono, Toshihiko Matsui, Ikuya Miyamoto
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Patent number: 6541628Abstract: A new process for the preparation of corroles, having the structure of formula I below relies on a solvent-free condensation of an aldehyde with a pyrrole. Further disclosed are several new corroles, salts, optically active isomers and complexes thereof synthesized using the process.Type: GrantFiled: June 19, 2001Date of Patent: April 1, 2003Assignees: Technion Research and Development Foundation Ltd.Inventors: Zeev Gross, Liliya Simkhovich, Nitsa Galili-Nachshon, Irina Saltsman
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Patent number: 6541629Abstract: The present invention relates to polymer conjugates having the formula: wherein T is a heterocyclic unit which is capable of inhibiting one or more proteolytic enzymes; L is a linking group; [Poly] is a polymeric unit, i indicates the number of said heterocyclic units which comprise said conjugate and has the value of from 1 to 100; z is 0 or 1, said polymer conjugates suitable for use in preventing skin irritation resulting from exposure of the skin to body fluids, inter alia, feces, menstrual fluid. The conjugates of the present invention are useful in diapers, dressings, sanitary napkins, and the like.Type: GrantFiled: September 8, 2000Date of Patent: April 1, 2003Assignee: The Procter & Gamble CompanyInventors: Scott Edward Osborne, Todd Laurence Underiner
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Patent number: 6541630Abstract: The invention provides the use in combating fungi of compounds of general formula I wherein R1 is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, Ra, Ra3Si, RaS or RaO, where Ra is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; Z is oxygen or sulfur; M is a thiophene ring; and R3 and R4, which may be the same or different, have the same meaning as Ra or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group ORc or S(O)mRc, where Rc has the same meaning as Ra or is hydrogen or acyl and m is 0, 1 or 2; or R3 and R4 together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R1 is hydrogen.Type: GrantFiled: June 13, 2002Date of Patent: April 1, 2003Assignee: Agrevo UK LimitedInventors: John Frederick Atherall, Thomas Lawley Hough, Stephen David Lindell, Mary Josephine O'Mahony, John Henry Parsons, Elizabeth Anne Saville-Stones
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Patent number: 6541631Abstract: The present invention relates to a method of preparing enantiomers and diastereomers of a 2′,3′-dideoxy-5-fluoro-3′thiocytadine (FTC) or a derivative thereof as represented by the following structural formula: In Structural Formula I, R is H, a substituted or unsubstituted organic acid radical, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted heteroaralkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted heterocycloalkyl group, a substituted or unsubstituted cycloalkylalkyl, a substituted or unsubstituted heterocycloalkylalkyl, a sugar or a protecting group.Type: GrantFiled: May 26, 2000Date of Patent: April 1, 2003Assignee: Pharma-Eco Laboratories, Inc.Inventors: Salah Zahr, David A. Swanson, Adel M. Moussa, Luning Han
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Patent number: 6541632Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.Type: GrantFiled: June 19, 2002Date of Patent: April 1, 2003Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
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Patent number: 6541633Abstract: An AB2 monomer of the formula: wherein Z is selected from the group consisting of —OH, —SH and —NH2HCl, is useful for the preparation of hyperbranched polybenzoxazoles.Type: GrantFiled: July 10, 2002Date of Patent: April 1, 2003Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Jong-Beom Baek
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Patent number: 6541634Abstract: This invention relates to improved processes for preparing compounds of Formula II, and compounds of Formula III, wherein R1, R2, R3 and Prt are defined as set forth in the specification.Type: GrantFiled: February 1, 2000Date of Patent: April 1, 2003Assignee: Pfizer Inc.Inventors: Frank R. Busch, Charles K. Chiu, Clifford N. Meltz, Ronald J. Post, Peter R. Rose
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Patent number: 6541635Abstract: The present invention discloses a method for producing angiotensin converting enzyme inhibitor of the following formula (I) and pharmaceutically acceptable salts thereof, in which a compound of the following formula (II), wherein R and R1 are defined as in the specification, is subjected to a de-protective reaction of silyl group in non-aqueous medium. This reaction is easily carried out only in the non-aqueous medium, so that by-product is minimized and the yield is high.Type: GrantFiled: June 25, 2002Date of Patent: April 1, 2003Assignee: Everlight USA, Inc.Inventors: Mong-Jong Tien, Yu-Liang Liu
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Patent number: 6541636Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrile is directly formed.Type: GrantFiled: July 24, 2002Date of Patent: April 1, 2003Assignees: Ube Industries, Ltd., Nissan Chemical Industries, Ltd.Inventors: Katsumasa Harada, Shigeyoshi Nishino, Naoko Okada, Hidetaka Shima, Takashi Harada
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Patent number: 6541637Abstract: A process for drying paroxetine hydrochloride anhydrate comprising (A) reacting a paroxetine compound with hydrogen chloride in the presence of isopropyl alcohol and crystallizing the resulting product, to obtain paroxetine hydrochloride anhydrate, and drying the resulting paroxetine hydrochloride anhydrate at a temperature of not more than 60° C. and under normal pressure or lower in an atmosphere which does not substantially contain moisture until the content of isopropyl alcohol attains to not more than 15% by weight; and (B) further drying the paroxetine hydrochloride anhydrate at a temperature of 80° to 110°C. in an atmosphere reduced to not more than 20 mm Hg until the content of isopropyl alcohol attains to not more than 5% by weight.Type: GrantFiled: December 13, 1999Date of Patent: April 1, 2003Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Mitsuru Okatake, Taro Ishibashi, Yoshihiro Kawata
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Patent number: 6541638Abstract: The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.Type: GrantFiled: July 17, 2001Date of Patent: April 1, 2003Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Denise Blum, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Bernd Michael Loeffler, Ulrike Obst, Sabine Wallbaum
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Patent number: 6541639Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.Type: GrantFiled: July 25, 2001Date of Patent: April 1, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
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Patent number: 6541640Abstract: 4-Haloalkylnicotinonitriles having the formula (I) which are suitable as intermediates in the preparation of pesticides, are obtained by: (a) reacting a 3-amino-1-haloalkyl-2-propen-1-one RF—C(O)—CH═CH—NH2 (II) in a condensation reaction with a compound of the formula (III) to (VII), (R1Z)CH═CH—CN (III) (R1Z)2CH—CH2—CN (IV) Hal-CH═CH—CN (V) Hal2CH—CH2CN (VI) HC≡C—CN (VII), to give a compound of the formula (VIII), (IX) and/or (X), RF—C(O)—CH═CH—NH—CH═CH—CN (VIII) RF—C(O)—CH═CH—NH—CH(ZR1)—CH2—CN (IX) RF—C(O)—CH═CH—NH—CH(Hal)—CH2—CN (X) wherein RF is (C1-C4)-haloalkyl, R1 is alkyl, Hal is Cl or Br and each Z, independently, is O, S, NR or OCO; and (b) subjecting the reactType: GrantFiled: December 13, 2001Date of Patent: April 1, 2003Assignee: Aventis Cropscience GmbHInventors: Sergiy Pazenok, Henricus Maria Martinus Bastiaans
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Patent number: 6541641Abstract: A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein R1 is an optionally substituted lower alkyl, and the like; R2 is a lower alkyl or an optionally substituted aralkyl, and the like: R3 is a lower alkyl, characterized in that a compound represented by the general formula (II-A) or the general formula (II-B) is treated with thionyl chloride.Type: GrantFiled: June 19, 2002Date of Patent: April 1, 2003Assignee: Shionogi & Co., Ltd.Inventors: Makoto Kobayashi, Haruo Koike, Masahiko Nagai
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Patent number: 6541642Abstract: A process for the preparation of (E)-3-(1-propenyl)-2-isoxazoline, characterized by reacting crotonaldehyde with hydroxylamine to form an oxime, and then converting the oxime into a nitrile oxide while reacting the nitrile oxide with ethylene.Type: GrantFiled: September 26, 2001Date of Patent: April 1, 2003Assignee: Nippon Soda Co., Ltd.Inventors: Tomio Yagihara, Michinori Takebayashi, Hiroyuki Yamanaka
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Patent number: 6541643Abstract: The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.Type: GrantFiled: April 17, 2002Date of Patent: April 1, 2003Assignee: Sanofi-SynthelaboInventors: Gergely Héja, Éva Csikós, Csaba Gönczi, Judit Halász, Félix Hajdú, István Hermecz, László Kis, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
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Patent number: 6541644Abstract: Processes for isolating substantially pure natural L-&bgr;-3-indolylalanine (L-&bgr;-3) from a mixture of amino acids, such as a protein hydrolysate. A protein hydrolysate, for example of casein or soy protein, is passed over a polymeric resin attractive to aromatic amino acids but not attractive to aliphatic amino acids. The aromatic amino acids are retained on the resin while the aliphatic amino acids pass over the resin and are collected. The resin is then washed to displace any residual aliphatic acids which may be physically associated with but not bound to the resin. Thereafter, the resin is eluted with a dilute acid to displace L-phenylalanine and L-tyrosine and provide a solution thereof while allowing L-&bgr;-3 to be retained on the resin. The resin is then further eluted with a dilute base to displace L-&bgr;-3 from the resin and provide a solution of L-&bgr;-3. Substantially pure natural L-&bgr;-3 is recoverable from this solution.Type: GrantFiled: August 7, 2001Date of Patent: April 1, 2003Assignee: AminoPath Labs, LLCInventors: Robert L. Pollack, John C. Godfrey
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Patent number: 6541645Abstract: Complexes of organic ligands with a metal ion exhibit unique conformation and spectroscopic properties upon changes in oxidation state of the metal ion. The metal is a redox-active metal ion and may possess additional ligands bonded to it. The organic ligand has three “arms” that are linked together at a central atom; each arm contains atoms that may also coordinate to the metal ion. At least two of the arms possess chromophoric properties. At least one arm contains two different groups that may coordinate to the metal ion. In one oxidation state, a first atom binds to the metal. In a second oxidation state, a second atom binds to the metal. This change in coordination of the metal ion results in a rotation of one of the arms, which changes the orientation of another group, which inverses the orientation of the two chromophoric species with respect to one another.Type: GrantFiled: July 26, 2000Date of Patent: April 1, 2003Assignee: New York UniversityInventors: James W. Canary, Steffen Zahn
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Patent number: 6541646Abstract: The invention relates to a method for producing compounds of general formula (I) wherein R1 is selected from the following groups: (a) OR5 and (b) mono-, di-, or tri-substituted phenyl; and R2 represents a group (C1-C6) alkyl. The method is characterized in that it comprises the following steps: a) reacting a compound of general formula (III) with an acid of general formula R1CH2 COOH (III) in a water-free medium; b) reacting the resulting compound with a strong base in an aprotic solvent in order to obtain an intermediate cyclic compound which forms a compound of general formula (I) after dehydration; and c) isolating said resulting compound of general formula (I).Type: GrantFiled: April 8, 2002Date of Patent: April 1, 2003Assignee: MerialInventors: Laetitia Canali, Paul Cruciani, Gilles Oddon
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Patent number: 6541647Abstract: The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.Type: GrantFiled: October 2, 2001Date of Patent: April 1, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Andappan Murugaiah Subbaiah Murugaiah, Sunil Vyankatesh Mhaskar, Gangavaram Vasantha Madhava Sharma, Tangallapally Rajendra Prasad, Punna Sreenivas, Vavilala Goverdhan Reddy, Aminul Islam, Chittineni Hari Prasad, Alla Venkata Rama Rao