Patents Examined by Floyd D. Higel
  • Patent number: 6548677
    Abstract: A novel process for preparing the compounds of the formula I where: n is 0, 1 or 2; R1, R2 are C1-C6-alkyl; R3, R4, R5 are hydrogen or C1-C6-alkyl, or R4 and R5 together form a bond; R6 is Cl, Br, which comprises a synthesis sequence starting from 1,2-dialkylbenzenes of the formula II with subsequent halogenation to give 3,6-dihalo-1,2-dialkylbenzenes, haloalkylation to give benzyl bromides, oxidation to give benzaldehydes, oximation, reaction with alkenes to give isoxazoles, conversion into thioethers and, if appropriate, oxidation to give sulfenyl or sulfonyl derivatives of the formula I.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: April 15, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Rack, Norbert Götz, Helmut Hagen, Wolfgang von Deyn, Ernst Baumann, Rene Lochtman, Joachim Gebhardt
  • Patent number: 6528653
    Abstract: The invention is directed to substituted thieno[2,3-b]pyrrolidin-5-ones. The compounds are useful as inhibitors of cellular production of tumor necrosis factor (TNF-&agr;) and as antiproliferative agents. These compounds are useful in the treatment or control of neuro-degenerative diseases, cardiovascular diseases, cancer or inflammatory diseases.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: March 4, 2003
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Adrian Liam Gill, William Harris
  • Patent number: 6518434
    Abstract: There is provided a process for the production of a compound of formula I, which process comprises reaction of a compound of formula II, with a compound of formula III, wherein R1, R2, n and R3 have meanings given in the description.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: February 11, 2003
    Assignee: AstraZeneca AB
    Inventors: Jörgen Alvhäll, Daniel Edvardsson, Panagiotis Ioannidis, Magnus Sjögren, Maria Szönyi
  • Patent number: 6515184
    Abstract: The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) to a process for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: April 6, 1998
    Date of Patent: February 4, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Michael Ruther, Alan Graff, Arno Widdig, Jacques Dumas, Christoph Erdelen, Peter Dahmen, Markus Dollinger, Ulrike Wachendorff-Neumann
  • Patent number: 6515133
    Abstract: Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are novel.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: February 4, 2003
    Assignees: Neurogen Corporation, Pfizer, Inc.
    Inventors: Andrew Thurkauf, Jun Yuan, Alan Hutchison, Charles A. Blum, Richard L. Elliott, Marlys Hammond
  • Patent number: 6504043
    Abstract: The present invention relates to a process for preparing a colour-stable, aqueous dimethylaminoacetonitrile solution from a formaldehyde source, dimethylamine and hydrocyanic acid, wherein the reaction mixture contains 2,4-diamino-6-phenyl-1,3,5-triazine(benzoguanamine) in a concentration of from 0.001 to 5% by weight, based on formaldehyde, prior to the reaction and the starting substances are used stoichiometrically or in a ratio of 0.98-1.02 mol of formaldehyde and 0.95-1.10 mol of dimethylamine per mol of hydrocyanic acid. The resulting product remains colour-stable without a further purification step even after prolonged storage.
    Type: Grant
    Filed: March 5, 2001
    Date of Patent: January 7, 2003
    Assignee: Clariant GmbH
    Inventors: Rainer Fell, Götz Wilbert, Thomas Stährfeldt
  • Patent number: 6498256
    Abstract: Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one hetero atom selected from the group O, S and NR, or ferrocenyl; R is H or C1-C4alkyl; each R4 individually or both R4 together are a hydrocarbon radical having from 1 to 20 carbon atoms; and R01 and R02 are each independently of the other a hydrogen atom or a hydrocarbon radical having from 1 to 20 carbon atoms, are chiral ligands for metal complexes with metals of sub-groups I and VII, which are catalysts for asymmetric addition reactions, for example of hydrogen, to prochiral unsaturated organic compounds.
    Type: Grant
    Filed: September 20, 2001
    Date of Patent: December 24, 2002
    Assignee: Solvias AG
    Inventors: Andreas Pfaltz, Joerg R. Blankenstein, Frederik Menges
  • Patent number: 6492528
    Abstract: This invention provides a convenient process for manufacturing 1,3-dialkyl-2-imidazolidinones in a direct one-step reaction from industrially available alkylene carbonate, N-alkylethanolamine or 1,2-diol, which can minimize forming solid materials and be readily conducted in an industrial large-scale production with a higher yield and less byproducts. The process is characterized in that alkylene carbonate, N-alkylethanolamine or 1,2-diol is reacted with monoalkylamine and carbon dioxide, alkylcarbamate alkylamine salt, and/or 1,3-dialkylurea, by heating them at 50° C. or higher in a reactor whose area in contact with at least part of the reactants and/or products is made of a metal comprising titanium or zirconium and/or an oxide thereof or inorganic glass.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: December 10, 2002
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Katsuhiko Matsuba, Shinichi Nakagawa, Takazou Katou, Yoshihiro Yamamoto
  • Patent number: 6486187
    Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
    Type: Grant
    Filed: July 25, 2000
    Date of Patent: November 26, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
  • Patent number: 6486339
    Abstract: The isomerization of an alkylated phenol composition that contains an ortho-alkyl substituted phenol component to isomerize and reduce the level of ortho-alkyl substituted phenol component therein can be accomplished by heating that composition in the presence of a catalytically effective amount of a solid acid catalyst to carry out such isomerization and reduction in the level of ortho-alkyl substituted phenol. Examples of suitable solid acid catalysts can be selected from the H-form zeolites, the supported sulfonic acids, and the heteropoly acids. The resulting isomerized product can be subsequently phosphorylated.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: November 26, 2002
    Assignee: Akzo Nobel NV
    Inventors: Anantha N. Desikan, George E. Whitwell
  • Patent number: 6482944
    Abstract: Processes for the preparation of haloalkylamines and tertiary aminoalkylorganometallic compounds are disclosed. The haloalkylamines can be prepared by direct reaction of an amine with an &agr;, &ohgr;-dihaloalkane or an &agr;, &ohgr;-dihaloalkene. Tertiary aminoalkylorganometallic compounds can be prepared by reacting selected tertiary haloalkylamines with an alkali metal at a temperature greater than 45° C. in hydrocarbon solvents.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: November 19, 2002
    Assignee: FMC Corporation
    Inventors: James Anthony Schwindeman, Randy W. Hall, Sonia S. Stryker
  • Patent number: 6479531
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—═CH—, —S— or —O—.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: November 12, 2002
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Ian Duncan Linney, Paul Trevor Wright, Iain Mair McDonald, Katherine Isobel Mary Steel, Robert Antony David Hull, Sonia Patricia Roberts, John David Gaffen, Jeremy Gilbert Vinter, Martin Keith Walker, James Whyte Black, Gillian Fairfull Watt, Elaine Anne Harper, Nigel Paul Shankley, Matthew John Tozer, David John Dunstone, Michael John Pether, Elliot James Lilley, David Andrew Sykes, Caroline Minli Rachel Low, Eric Peter Griffin, Laurence Wright
  • Patent number: 6476233
    Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral amine oxazolinyl ligands and related ligands. Specially, a direct asymmetric hydrogenation system based on Ru-Ambox catalyst was discovered.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: November 5, 2002
    Assignee: The Penn State Research Foundation
    Inventor: Xumu Zhang
  • Patent number: 6472415
    Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in indications associated with the androgen receptor, such as cell hyperplasia dependent on androgens, hirsutism, acne and androgenetic alopecia.
    Type: Grant
    Filed: February 11, 2000
    Date of Patent: October 29, 2002
    Assignee: Biophysica, Inc.
    Inventors: Milos Sovak, Allen L. Seligson, James Gordon Douglas, III, Brian Campion, Jason W. Brown
  • Patent number: 6472533
    Abstract: Novel phosphine oxazoline ligands of formula (I) wherein m is 1, 2, 3 or 4; n, p, q, r are independently zero or 1 provided that at least one of n, p, q and r is 1; X is O, S, Se, CH2, NH; Y is N, P, As, S; R is H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; ferrocenyl; a thioalkyl group; a thioaryl group; or R is part of a polymeric structure, for example polyacrylic acid; R1 to R13 are independently selected from H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; a process for the preparation thereof,
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: October 29, 2002
    Assignee: The Texas A & M University System
    Inventor: Kevin Burgess
  • Patent number: 6472550
    Abstract: A process for the preparation of a stabilizer mixture containing a low amount of chloride comprising a) 50-80% by weight of tetrakis(2,4-di-tert-butylphenyl)biphenylene diphosphonite and its isomers, b) 5-25% by weight of bis(2,4-di-tert-butylphenyl)biphenylene monophosphonite and its isomers, and c) 5-25% by weight of a tris(2,4-di-tert-butylphenyl) phosphite, and where the sum of components (a), (b) and (c) is not greater than 100% by weight, by reacting biphenyl under Friedel-Crafts condition with phosphorus trichloride and aluminium trichloride and by reacting the product mixture with 2,4-di-tert-butyl-phenol in the presence of a tertiary amine or an aromatic amine and a solvent, separating the formed two layers, which process comprises treating the solvent layer with water, a base and a desiccant, separating the precipitate from the solution containing the stabilizer mixture and evaporating the solvent.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: October 29, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Vien Van Toan, Ronald Salathé
  • Patent number: 6469167
    Abstract: An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl group using Raney Nickel or Magnesium in alcohol having 1 to 4 carbon atoms or mixtures thereof, if desired reesterifying using sufphuric acid at a temperature in the range of 0° C. to 60° C. to obtain a compound of formula (3′) wherein R is as defined above, hydrolyzing the compound of formula (3′) wherein R is as defined above, by conventional methods to obtain the acid of formula (4), condensing the acid of formula (4) with N-methyl anthranilamide directly without any preactivation of the acid to produce the compound of formula (1) and if desired, converting the compound of formula (1) to pharmaceutically acceptable salts thereof by conventional methods.
    Type: Grant
    Filed: May 2, 2001
    Date of Patent: October 22, 2002
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Prabhakar Chebiyyam, Rajender Kumar Potlapally, Chinna Bakki Reddy Gade, Balaram Mahanti Satish, Ramabhadra Sarma Mamillapalli, Om Reddy Gaddam
  • Patent number: 6455744
    Abstract: A method of preparing vicinal difluoro aromatic compounds in high yield from hydroxy aromatic compounds and a method of preparing intermediates thereof. The hydroxy aromatic compound can be a mono-, bi- or tricyclic aromatic in which the rings are separate or fused. One or more of the rings can contain heteroatoms, such as oxygen, nitrogen, or sulfur, and can contain one or more substitutions, in addition to the hydroxy substitution.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: September 24, 2002
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Gauri Sankar Lal, Kathryn Sue Hayes
  • Patent number: 6455702
    Abstract: A high purity N,N-Carbonyl diimidazole (I) is obtained by the reaction of Imidazole, general formula-II, and bis (trichloromethyl) carbonate.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: September 24, 2002
    Assignee: Aims Fine Chemicals, Inc.
    Inventors: Inder Pal Singh, Shradha Singh
  • Patent number: 6452044
    Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.
    Type: Grant
    Filed: May 30, 2001
    Date of Patent: September 17, 2002
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Takashi Tsukamoto, Barbara S. Slusher, Eric Wang