Patents Examined by Robert Gerstl
  • Patent number: 7002020
    Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: February 21, 2006
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
  • Patent number: 6863647
    Abstract: Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptab
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: March 8, 2005
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
  • Patent number: 6825355
    Abstract: Novel benzothiazoles and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: November 30, 2004
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Jagabandhu Das, Joel C. Barrish, John Wityak
  • Patent number: 6818634
    Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: November 16, 2004
    Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts College
    Inventors: Mark L. Nelson, Stuart B. Levy, Roger Frechette, Todd E. Bowser, Mohamed Y. Ismail
  • Patent number: 6797824
    Abstract: Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: March 18, 2002
    Date of Patent: September 28, 2004
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Raymond F. Horvath, Jun Yuan, John M. Peterson
  • Patent number: 6777557
    Abstract: In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated coupling of proteins, lipids, nucleic acids, and other biomaterials, and any combination thereof. In another embodiment, the compositions and associated methods have utility in vivo to reduce the deleterious effects of sugar-mediated coupling processes in an organism, when the organism is exposed to the compound or composition internally, by ingestion, transdermal application, or other means. In yet another embodiment, the compositions and associated methods are useful for the ex-vivo treatment of organs, cells and tissues and external treatment of hair, nails and skin to rejuvenate them by changing deformability and increase the tissue diffusion coefficient. In a further embodiment, the present invention relates to novel compounds and pharmaceutical compositions.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: August 17, 2004
    Inventors: Peter C Ulrich, Sheng Ding Fang, Michael L Brines, Qiao-Wen Xie, Anthony Cerami
  • Patent number: 6759423
    Abstract: The present invention relates to the use of 4-hydroxyisothiazole compounds as antimicrobially active substances, certain new 4-hydroxyisothiazole compounds and a process for their preparation.
    Type: Grant
    Filed: October 3, 2001
    Date of Patent: July 6, 2004
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Werner Hölzl, Wolfgang Haap, Dietmar Ochs, Karin Puchtler, Marcel Schnyder, Dinesh Narendra Rele, Sitaram Pal, Asawari Bhikaji Mahtre, Surendra Umesh Kulkarni, Arakali Srinivasarao Radhakrishna
  • Patent number: 6753340
    Abstract: A compound selected from those of formula (I): wherein R1a, R1b, R2, R3, are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: June 22, 2004
    Assignee: Warner-Lambert Company LLC
    Inventors: Fabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
  • Patent number: 6750362
    Abstract: Process for making 5FVN, comprising contacting in a reactor 3PN with CO and hydrogen in the presence of a catalyst, the catalyst comprising recycled catalyst that is reactivated using hydrogen.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: June 15, 2004
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Emilio E. Bunel, Marisa Bonilla, Ronnie Ozer
  • Patent number: 6743923
    Abstract: A novel antirheumatic agent comprising as an active ingredient a compound of formula I: or a pharmaceutically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: June 1, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Hirokuni Jyoyama, Shinji Kakudo, Kohji Hanasaki, Kenzo Koizumi, Tsuneaki Sakata, Ryuji Suzuki
  • Patent number: 6737383
    Abstract: Compounds of Formula (1) and processes for their preparation, their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein Q, X1, X2, X3, R1, R2, R6 and R7 are as defined in the disclosure. Also disclosed are novel intermediates of Formula (5), Formula (8) and Formula (20) wherein R27 is —(CR6R7)q—Q; R6, R7, q, Q, X1 and X2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (1).
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: May 18, 2004
    Assignee: The Regents of the University of California
    Inventors: Gary David Annis, George Chih-Shu Chiang, David Raymond Forney, Kanu Maganbhai Patel, Morris Padgett Rorer, William Francis Smith, III, Thomas Martin Stevenson, King-Mo Sun, Chi-Ping Tseng
  • Patent number: 6734200
    Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolyzable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: May 11, 2004
    Assignee: AstraZeneca AB
    Inventor: Michael Barry Gravestock
  • Patent number: 6730793
    Abstract: Provided are chromophores of the formula Q—(—L—Z)x, wherein x is 2 or 3, wherein Q is selected from the group consisting of wherein L is wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: May 4, 2004
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Ramamurthi Kannan, Loon-Seng Tan, Bruce A. Reinhardt, Richard A. Vaia
  • Patent number: 6727282
    Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 9, 2002
    Date of Patent: April 27, 2004
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6727281
    Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
    Type: Grant
    Filed: July 23, 2002
    Date of Patent: April 27, 2004
    Assignee: Novartis AG
    Inventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer
  • Patent number: 6727267
    Abstract: Compounds, compositions and methods are provided that are useful in the treatment and prevention of certain viral infections and associated diseases. In particular, the compounds of the invention inhibit the activity of a viral RNA polymerase. The subject methods are particularly useful in the treatment of diseases causes by hepatitis C virus infection.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: April 27, 2004
    Assignee: Tularik Inc.
    Inventors: Juan C. Jaen, Jay P. Powers
  • Patent number: 6723855
    Abstract: A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided in which the carboxylic acid group of 5-methylisoxazole-4-carboxylic acid is chlorinated, forming 5-methylisoxazole-4-carboxylic acid chloride. The acid chloride is then reacted without intermediate distillation with 4-trifluoromethylaniline in the presence of an alkali metal or alkaline-earth metal bicarbonate acid scavenger.
    Type: Grant
    Filed: February 8, 2001
    Date of Patent: April 20, 2004
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Ilya Avrutov, Neomi Gershon, Anita Liberman
  • Patent number: 6719540
    Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: wherein: Q is selected from the group consisting of M is O, NR9, or CR10R11; X is O or NH; and the R groups are as defined, and therapeutic compositions containing them alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: April 13, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alicia Regueiro-Ren, Soong-Hoon Kim
  • Patent number: 6720342
    Abstract: The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical or veterinary compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: April 13, 2004
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Per Sauerberg
  • Patent number: 6716865
    Abstract: Benzoxa- and benzthiazoles substituted at the 2 position and carrying a sulfamic acid ester group bound via oxygen to the phenyl part of the ring structure, such as the compounds of formula (I) wherein the symbols have various significances, possess interesting pharmacological activity. They can be prepared by sulfamoylation of a corresponding compound carrying a hydroxy group on the phenyl part of the ring structure, or by N-substitution. They are indicated for use as steroid sulfatase inhibitors in the prevention and treatment of illnesses responsive to steroid sulfatase inhibition, such as acne.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: April 6, 2004
    Assignee: Novartis AG
    Inventors: Andreas Billich, Erwin Paul Schreiner, Barbara Wolff-Winiski