Patents Examined by T. A. Solola
  • Patent number: 6780859
    Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: August 24, 2004
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
  • Patent number: 6716990
    Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: April 6, 2004
    Assignee: Altana Pharma AG
    Inventors: Wolf-Rüdiger Ulrich, Christian Scheufler, Thomas Fuchss, Jörg Senn-Bilfinger
  • Patent number: 6670390
    Abstract: Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(&agr;)-OH, 3-(&bgr;)-OH, 3-(&agr;)-O-sugar, or 3-(&bgr;)-O-sugar.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: December 30, 2003
    Assignee: Mars Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck, Laurie S. Post, Giovanni G. Cipolla, Craig A. McClelland, Jeff A. Mundt, Harold H. Schmitz
  • Patent number: 6653340
    Abstract: The present invention is concerned with new compounds, and particularly those having a fused bicyclic ring substituted with an amidine moiety. These compounds are each potent inhibitors of Factor D of the alternate pathway of complement, C1s of the classical pathway of complement, Factors Xa, XIIa, VIIa and thrombin of the coagulation pathway, plasmin in the fibrinolytic pathway, and kallikrein and high molecular weight kininogen in the inflammatory pathways. These proteases, which have serine in their active site, are called serine proteases and they are pivotal to most of the processes of inflammation and coagulation. In fact, these various systems are interactive with one another and it is difficult to activate one pathway without it influencing the others.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: November 25, 2003
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, J. Claude Bennett, Shri Niwas, R. Scott Rowland
  • Patent number: 6632947
    Abstract: A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.
    Type: Grant
    Filed: November 8, 2001
    Date of Patent: October 14, 2003
    Assignee: SmithKline Beecham plc
    Inventors: Robert Gordon Giles, Norman John Lewis, Stephen Moore, Colin Ripley Pool, John Kirby Quick, Michael Urquhart
  • Patent number: 6617324
    Abstract: A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: September 9, 2003
    Assignee: G. D. Searle & Company
    Inventors: Ashok S. Naraian, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xi, Ish K. Khanna, Yi Yu
  • Patent number: 6608211
    Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and W are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: August 19, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Hagemann, Reiner Fischer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Udo Schneider, Wolfram Andersch
  • Patent number: 6573396
    Abstract: A process for the production of a dialkyl carbonate and a diol from a cyclic carbonate and an aliphatic monohydric alcohol wherein the cyclic carbonate and aliphatic monohydric alcohol are reacted in the presence of a transesterification catalyst to form a crude product stream which contains a dialkyl carbonate, a diol, a hydroxy alkyl carbonate, which is formed as an intermediate of the two step transesterification reaction, unreacted aliphatic monohydric alcohol and unreacted cyclic carbonate. The dialkyl carbonate and unreacted aliphatic monohydric alcohol are separated from the crude product stream and then the hydroxy alkyl carbonate is diminished, reduced or eliminated from the crude product stream, prior to the separation and purification steps needed to recover the diol, resulting in improved yields and product purity.
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: June 3, 2003
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: J. Scott Buchanan, Jose G. Santiesteban, Zhaozhong Jiang
  • Patent number: 6545168
    Abstract: 1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.
    Type: Grant
    Filed: May 5, 1997
    Date of Patent: April 8, 2003
    Assignee: Florida State University
    Inventors: Robert A. Holton, Suhan Tang, Feng Liang, Carmen Somoza
  • Patent number: 6545162
    Abstract: The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: April 8, 2003
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Eldon E Baird
  • Patent number: 6525088
    Abstract: Compounds represented by the following general formula (I): wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-6 alkyl group or an aryl group which may be substituted, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, and R11 represents a hydrogen atom or a C1-6 alkanoyl group, or salts thereof. The aforementioned compounds are substantially non-fluorescent and react with singlet oxygen under a physiological condition to give a fluorescent substance, and therefore they are useful as agents for measurement of singlet oxygen.
    Type: Grant
    Filed: January 3, 2001
    Date of Patent: February 25, 2003
    Inventors: Tetsuo Nagano, Naoki Umezawa
  • Patent number: 6525209
    Abstract: The present invention relates to the preparation of epoxides by the oxidation of olefins using molecular oxygen with the addition of an aldehyde additive, characterized in that the oxidation is performed in compressed carbon dioxide as the solvent, which, as compared to many conventional organic solvents, is stable towards oxidation, reduces the danger of explosion and is toxicologically and ecologically safe.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: February 25, 2003
    Assignee: Studiengesellschaft Kohle mbH
    Inventors: Walter Leitner, Frank Loeker
  • Patent number: 6525059
    Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R 2, R3 and R4 are as described in the specification.
    Type: Grant
    Filed: February 24, 2000
    Date of Patent: February 25, 2003
    Assignee: G. D. Searle & Company
    Inventors: Ashok Anantanarayan, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu, Ish K. Khanna, Yi Yu
  • Patent number: 6521797
    Abstract: The present invention is an oxime carboxylic acid derivative having the formula I: wherein n is 1 or 0, X is O, R2 and R3 being part of an oxime R2R3C═NOH are individually, substituted or unsubstituted, branched or unbranched alkyl-, alkenyl-, akinyl-, cycloalkyl-, cycloalkenyl-, or aromatic radical and contain less than 30 carbon atoms, and R1 is a substituted or unsubstituted, branched or unbranched alkyl-, alkenyl-, akinyl-, cycloalkyl-, cycloalkenyl-, alkoxyalkyl-, aryloxyaryl-, alkoxyaryl-, aryloxyalkyl-, or aromatic radical, or XnR1 is which are useful as precursors for the delivery of organoleptic compounds, especially for flavors, fragrances and masking agents, and/or antimicrobial compounds.
    Type: Grant
    Filed: August 17, 1999
    Date of Patent: February 18, 2003
    Assignee: Givaudan AG
    Inventors: Denise Anderson, Georg Frater
  • Patent number: 6521619
    Abstract: The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: February 18, 2003
    Assignees: Icos Corporation, Abbott Laboratories
    Inventors: James T. Link, Bryan K. Sorensen
  • Patent number: 6512126
    Abstract: Mint lactone can be prepared by hydrogenating hydroxymenthofurolactone to give the intermediate dihydrohydroxymenthofurolactone with the subsequent elimination of water.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: January 28, 2003
    Assignee: Haarmann & Reimer GmbH
    Inventors: Oskar Koch, Walter Kuhn
  • Patent number: 6512128
    Abstract: A titanium-containing silicon oxide catalyst satisfying all of the following conditions (1) to (4): (1): an average pore size of 10 Å or more, (2): a pore size of 90% or more of the total pore volume of 5 to 200 Å, (3): a specific pore volume of 0.2 cm3/g or more, and (4): a quarternary ammonium ion represented by the following general formula (I) is used as a template and then said template is removed by solvent extraction operation; [NR1R2R3R4]+  (I) wherein, R1 represents a linear or branched hydrocarbon chain having 2 to 36 carbon atoms, and R2 to R4 represent an alkyl group having 1 to 6 carbon atoms, a method for producing said catalyst, and a method for producing propylene oxide by reacting propylene with a hydroperoxide, except for ethylbenzene hydroperoxide, in the presence of said catalyst.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: January 28, 2003
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Jun Yamamoto, Junpei Tsuji
  • Patent number: 6511976
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: January 28, 2003
    Assignee: Jannsen Pharmaceutica, N.V.
    Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
  • Patent number: 6506787
    Abstract: A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralkyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR (R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: January 14, 2003
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Tomokazu Yoshinaga
  • Patent number: 6504039
    Abstract: The present invention relates to supported catalysts which are composed of titanium oxide hydrates coated with nanoscale gold particles. The catalysts of the present invention have increased activity over known catalysts.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: January 7, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Markus Weisbeck, Ernst-Ulrich Dorf, Gerhard Wegener, Christoph Schild, Bernhard Lücke, Herbert Dilcher, Ulrich Schülke