Patents Examined by Mukund J. Shah
  • Morpholinones as light stabilizers
    Patent number: 6562815
    Abstract: The invention relates to new compounds containing 1-8 active groups of the type 3,3,6,6-polysubstituted 2-morpholinone and having the formula F (A′—Z)m—X  (F), wherein m is a number from 1 to 8; X is an organic anchor group of valency m and in case that m is not 1, X may also be a direct bond, SO2, P or PO; A′ is a monovalent group of the formula E  containing one linking group; Z is a direct bond, —O—, —S—, —SO—, —SO2— or —NR′14—; provided that Z is —O—, —S—, —SO—, —SO2— or —NR′14— if m is 1 and the linking group in formula E is G3 or G5; G1 is hydrogen; C1-C18alkyl; C2-C18alkyl substituted by OH and/or phenyl; oxyl; OH; C2-C12cyanoalkyl; C2-C12cyanoalkoxy; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C3-C8alkenyloxy; C7-C12phenylalkyl; C7-C12phenylalkyl substituted by hydroxy, C1-C4alkyl and/or C1-C4
    Type: Grant
    Filed: August 16, 2000
    Date of Patent: May 13, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Dario Lazzari, Thomas Bolle, Mirko Rossi, Hugh Stephen Laver
  • Dry granulation of pharmaceutical formulation comprising mexiletine
    Patent number: 6562871
    Abstract: Compaction of mexiletine hydrochloride crystals is described, which provides a powder suitable for use in capsules without use of organic solvents.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: May 13, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Michael L. Cappola
  • Substituted imidazole compounds
    Patent number: 6562832
    Abstract: Novel 1,4,5-subsituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: May 13, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Jeffrey C. Boehm, Timothy Francis Gallagher
  • Kinetic resolutions of chiral 2- and 3-substituted carboxylic acids
    Patent number: 6562966
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: May 13, 2003
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as &bgr;-secretase inhibitors
    Patent number: 6562783
    Abstract: The invention provides a compound of formula (I): or salts or hydrates thereof, useful as beta-secretase inhibitors. The invention further relates to a method of reducing plaque formation, particularly useful in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: May 30, 2001
    Date of Patent: May 13, 2003
    Assignee: Neurologic, Inc.
    Inventors: Lixin Qiao, René Etcheberrigaray
  • Process for the preparation of triethylenediamine (TEDA)
    Patent number: 6562971
    Abstract: A process for the preparation of triethylenediamine (TEDA) by reaction of ethylenediamine (EDA) in the presence of a zeolite catalyst, wherein the zeolite catalyst comprises one or more metals M in oxidation states II, III or IV as oxides, and for M=Al, has an SiO2/M2O3 molar ratio of greater than 1400:1, for M=metal in oxidation state II or M=two or more metals in oxidation state II, has an SiO2/MO molar ratio of greater than 100:1, for M=metal in oxidation state III or M=two or more metals in oxidation state III, has an SiO2/M2O3 molar ratio of greater than 100:1 and for M=metal in oxidation state IV or M=two or more metals in oxidation state IV, has an SiO2/MO2 molar ratio of greater than 10:1, and the reaction temperature is from 250 to 500° C.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: May 13, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Frauenkron, Bernd Stein
  • Recovery of dicarboxylic aromatic acids from polyester-resin contained in articles for recycling
    Patent number: 6562877
    Abstract: A method for the recovery of dicarboxylic aromatic acids, in particular terephthalic acid, from manufactured aromatic polyester-resin articles for recycling, wherein the article, fragmented into chip form, is reacted in solution in a carboxylic acid with 2-6 carbon atoms and with a pKa from 4 to 6, preferably glacial acetic acid, in the presence of catalytic quantities of a strong acid with a pKa of less than 1, preferably aqueous hydrochloric acid or sulfuric acid, operating at temperatures from 160° to 250° C.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: May 13, 2003
    Assignee: Sinco Ricerche S.p.A.
    Inventor: Hussain Al Ghatta
  • Reactive crystallization method to improve particle size
    Patent number: 6558435
    Abstract: This invention provides a method of conducting a simultaneous chemical reaction and controlled crystallization of the product employing impinging fluid jet streams containing reactants capable of producing the product with desired particle size characteristics.
    Type: Grant
    Filed: May 23, 2001
    Date of Patent: May 6, 2003
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: David J. Am Ende, Thomas C. Crawford, Neil P. Weston
  • 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
    Patent number: 6559152
    Abstract: The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: May 6, 2003
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Jay A. Markwalder, Steven P. Seitz, Susan R. Sherk
  • Kappa opioid receptor ligands
    Patent number: 6559159
    Abstract: Structurally novel kappa opioid receptor antagonists are provided and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: May 6, 2003
    Assignee: Research Triangle Institute
    Inventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
  • Compounds and methods for modulating cxcr3 function
    Patent number: 6559160
    Abstract: The invention provides compounds and compositions of the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl; R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl; each R3 is independently a substituent selected from -halogen, —OR′, —OC(O)R′, —NR′R″, —SR′, —R′, —CN, —NO2, —CO2R′, —CONR′R″, —C(O)R′, —OC(O)NR′R″, —NR″C(O)R′, —NR″C(O)2R′, , —NR′—C(O)NR″R′″, —NH—C(NH2)═NH, —NR′C(NH2)═NH, —NH—C(NH2)═NR—, —S(O)R′, —S(O)2R′, —
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: May 6, 2003
    Assignee: Chemocentryx, Inc.
    Inventors: Thomas J. Schall, Daniel J. Dairaghi, Brian E. McMaster
  • Benzylated PDE4 inhibitors
    Patent number: 6555572
    Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: April 29, 2003
    Assignee: Inflazyme Pharmaceuticals Ltd.
    Inventors: Ronald W. Lauener, David L. Burgoyne, Patrick J. Rebstein, Lloyd F. Mackenzie, Yuanlin Zhou, Yaping Shen
  • Asymmetric synthesis of quinazolin-2-ones useful as HIV reverse transcriptase inhibitors
    Patent number: 6555686
    Abstract: This invention relates generally to the asymmetric synthesis of quinazolin-2-ones that are useful as inhibitors of HIV reverse transcriptase. The synthesis is accomplished through the chiral ligand mediated addition of cyclopropylacetylide.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: April 29, 2003
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Rodney L. Parsons, Roberta L. Dorow, Akin H. Davulcu, Joseph M. Fortunak, Gregory D. Harris, Goss S. Kauffman, William A. Nugent, Lilian A. Radesca
  • Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions
    Patent number: 6555541
    Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: July 10, 2000
    Date of Patent: April 29, 2003
    Assignee: Astrazeneca UK Limited
    Inventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
  • Gemcitabine as an immunosuppressive pharmaceutical agent
    Patent number: 6555518
    Abstract: The present invention provides the use of a compound of the formula I wherein: R1 is a base defined by one of the formulae R2 is hydrogen, C1-C4 alkyl, bromo, fluoro, chloro or iodo; or a pharmaceutically-acceptable salt thereof for the manufacture of a medicament for immunosuppressive therapy of the human or animal body.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: April 29, 2003
    Assignee: Eli Lilly and Company
    Inventors: Raimund Margreiter, Günther Konwalinka
  • Method for the production of triethylene diamine making use of ethylene diamine
    Patent number: 6555688
    Abstract: The invention in question is concerned with a method for the production of triethylene diamine using ethylene diamine as an educt and zeolite catalysts of the Pentasil type.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: April 29, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Werner Klockemann, Erich Frauendorfer, Matthias Frauenkron, Bernd Stein
  • Quinazolines for treating brain tumor
    Patent number: 6552027
    Abstract: Novel substituted quinozaline compounds and conjugates useful to inhibit the growth of brain tumor cells and to inhibit adhesion and migration of brain tumor cells. The compounds of the invention include 4-(3′-bromo-4′-hydroxy phenyl)-amino-6,7-dimethoxyquinazoline and this compound covalently bound to EGF.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: April 22, 2003
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
  • Pyrrolo[2,1-c][1,2,4] thiadiazoles and Pyrollo[2,1-c][1,12,4]oxadiazoles useful as nitric oxide synthase inhibitors
    Patent number: 6552052
    Abstract: Pyrrolo[2,1-c][1,2,4]thiadiazole or pyrollo[2,1-c][1,2,4]oxadiazoles having the formula: or pharmaceutically acceptable salts thereof, useful as nitric oxide synthase inhibitors wherein each substituent is defined herein.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: April 22, 2003
    Assignee: Monsanto/G.D. Searle
    Inventors: Donald W. Hansen, Jr., R. Keith Webber, E. Ann Hallinan, Mihaly V. Toth, Barnett S. Pitzele, Alok K. Awasthi, Alan E. Moormann, Suzanne Metz, Jeffery S. Snyder, William M. Moore, Jeffrey A. Scholten
  • 2-pyrimidineamine derivatives and processes for their preparation
    Patent number: 6552029
    Abstract: Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group —X1—R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: April 22, 2003
    Assignee: Celltech R&D Limited
    Inventors: Peter David Davis, David Festus Charles Moffat, Mark James Batchelor, Martin Clive Hutchings, David Mark Parry
  • Oxidation process for the production of alkenes and carboxylic acids
    Patent number: 6548697
    Abstract: A process for the oxidation of a C2 to C4 alkane to produce the corresponding alkene and carboxylic acid which process comprises contacting in an oxidation reaction zone, said alkane, molecular oxygen-containing gas, and optionally, at least one of the corresponding alkene and water, in the presence of at least two catalysts each active, with different selectivities, for the oxidation of the alkane to the corresponding alkene and carboxylic acid, to produce a product stream comprising said alkene, carboxylic acid and water, and in which process the molar ratio of alkene to carboxylic acid produced in said oxidation reaction zone is adjusted or maintained at a pre-determined value by controlling the relative proportions of the at least two catalysts in said oxidation reaction zone. Such an oxidation process may be used in an integrated process, such as for the manufacture of ethyl acetate or vinyl acetate.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: April 15, 2003
    Assignee: BP Chemicals Limited
    Inventors: Brian Ellis, Mark Stephen Roberts