Patents Examined by Laura R. Cross
  • Patent number: 5900426
    Abstract: Benzothiazole derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component possess a lipid lowering activity and are useful pharmaceuticals for the treatment of hyperlipemia. The lipid lowering agents are of the formula: ##STR1## wherein R.sub.1 is halogen, trifluoromethyl, acetamido or --OX.sub.1 ; X.sub.1 is hydrogen, alkyl or acyl; R.sub.2 is hydrogen, halogen, alkyl, hydroxyalkyl, trifluoromethyl, nitro, amino which may be substituted with alkyl or acyl, carboxy which may be esterified with alkyl, or --OX.sub.2 ; X.sub.2 is hydrogen, alkyl, acyl, carboxyalkyl which may be esterified with alkyl; n is an integer from 1 to 3 denoting the number of substituents R.sub.2 ; and plural R.sub.2 may be the same or different when n is 2 or 3; with the proviso that R.sub.1 is a group other than halogen when R.sub.2 is hydrogen.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: May 4, 1999
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Hiroki Muramoto, Kiyoshi Fukuda, Taisuke Hasegawa, Kaoru Okamoto, Takayuki Kotani
  • Patent number: 5874382
    Abstract: Compounds of Formula I and II, and their agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X is a direct bond; O; S; NH; N(C.sub.1 -C.sub.3 alkyl); N(C.sub.1 -C.sub.3 haloalkyl); or N(allyl);R.sup.1 is H; F; Cl; or Br;R.sup.2 is H; F; Cl; Br; CF.sub.3 ; nitro; or cyano;R.sup.4 is H; C.sub.1 -C.sub.3 alkyl; or halogen;R.sup.5 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; halogen; S(O).sub.2 (C.sub.1 -C.sub.6 alkyl); or C(.dbd.O)R.sup.8 ; orR.sup.4 and R.sup.5 are taken together along with the carbon to which they are attached to form a spiro-cyclopropane ring;and R.sup.3, R.sup.8, and J are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formulae I and II and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I or II.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: February 23, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Balreddy Kamireddy, William Mark Murray
  • Patent number: 5869688
    Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5-?1-(C.sub.1-5 alkyl)-4-halo-5-(C.sub.1-3 haloalkyl)-1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyl-diketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: February 9, 1999
    Assignee: Monsanto Company
    Inventors: Bruce C. Hamper, Michael K. Mao
  • Patent number: 5846753
    Abstract: A method of detecting the presence of a substance being monitored in a medium, selected from the group of substances including organophosphorus compounds and the metal ions Zn, Be and Bi, including the steps of: providing a 1,2-dioxetane phenyl phosphate compound; providing a phosphatase that catalytically degrades the 1,2-dioxetane phenyl phosphate compound to produce light, the catalytic activity of the phosphatase toward 1,2-dioxetane phenyl phosphate compound being altered by the substance being monitored; exposing the 1,2-dioxetane phenyl phosphate compound and the phosphatase together to a medium which may contain the substance being monitored; detecting light produced after the exposing step; and determining, from the detected light, the presence and concentration in the medium of the substance being monitored.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: December 8, 1998
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Joseph A. Akkara, David L. Kaplan, Madhu S. R. Ayyagari, Kenneth A. Marx, Sanjay Kamtekar, Rajiv Pande, Sukant K. Tripathy, Jayant Kumar
  • Patent number: 5792784
    Abstract: The invention relates to a pseudo-dipeptide product obtained by coupling between histamine or methyl-substituted histamine and an amino-acid having formula ##STR1## wherein A is a radical selected in the group comprising amine radicals, amides, lactames, urethans; R.sub.1, R'.sub.1, R.sub.2, R'.sub.2. . . R.sub.n, R'.sub.n represent each a hydrogen atom, a hydrocarbon radical or a functional group; Y and Z represent each a hydrogen or a fluorine atom, or a hydrocarbon radical which may be substituted by one or a plurality of functional groups; and n is an integer higher than or equal to 1; the covalent bond with the histamine or the methyl-substituted histamine being a peptide bond between the carboxylic radical of the amino acid and the amine radical of the histamine. The pseudo-dipeptide products of the invention may be used in therapeutical, cosmetological and agro-alimentary applications and particularly for the treatment of cataracts.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: August 11, 1998
    Assignees: Marc Babizhayev, Exsymol Societe Anonyme Monegasque
    Inventors: Marie-Christine Seguin, Marc Babizhayev
  • Patent number: 5789429
    Abstract: A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: August 4, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Toshihiko Naito, Katsura Hata, Yumiko Kaku, Akihiko Tsuruoka, Itaru Tsukada, Manabu Yanagisawa, Toshio Toyosawa, Kazumasa Nara
  • Patent number: 5773456
    Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L--R.sup.1 is a leaving group, H--L--R.sup.1 is the conjugate acid thereof and, when L is N, H--L--R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H--L--R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H--L--R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: June 30, 1998
    Assignee: Sanofi
    Inventors: Richard Paul Dunlap, Albert Joseph Mura, Dennis John Hlasta, Ranjit Chimanlal Desai, Lee Hamilton Latimer
  • Patent number: 5756005
    Abstract: The present invention provides a method of stabilizing non-halogenated 3-isothiazolones in aggressive systems with pH above 8.5. The invention also discloses compositions with pH above 8.5, containing non-halogenated 3-isothiazolones and an effective stabilizing amount of a iodine-containing stabilizer.
    Type: Grant
    Filed: October 11, 1996
    Date of Patent: May 26, 1998
    Assignee: Rohm and Haas Company
    Inventors: Tirthankar Ghosh, John Robert Mattox
  • Patent number: 5712400
    Abstract: A process for the preparation of 5-hydroxymethylthiazole comprises reacting a compound of the formula, ##STR1## with a carboxylic acid salt (optimally in the presence of a quaternary ammonium salt) and hydrolyzing the resulting ester. Subsequent dechlorination gives 5-hydroxymethylthiazole.
    Type: Grant
    Filed: May 22, 1996
    Date of Patent: January 27, 1998
    Assignee: Abbott Laboratories
    Inventors: M. Robert Leanna, Howard E. Morton, Michael S. Allen
  • Patent number: 5705500
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
  • Patent number: 5700825
    Abstract: A compound comprising a diamine containing from 2-4 electron-affinic radiosensitizing functional groups or a salt thereof is provided. In a preferred embodiment the compound has the formula ##STR1## wherein A comprises a carbon chain having from about 2-10 carbons in the chain, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are H, or T, T is ##STR2## wherein A' comprises a carbon chain having from about 1-8 carbons in the chain, R.sup.5 is H, lower alkyl, or halo, and R.sup.6 is H, lower alkyl, halo or nitro, provided that at least one of R.sup.1 and R.sup.2, and at least one of R.sup.3 and R.sup.4 is T. Intermediates for, pharmaceutical compositions containing, methods for making and methods for using such compounds to radiosensitize and kill hypoxic tumor cells are also provided.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: December 23, 1997
    Assignee: Florida State University
    Inventors: Kurt G. Hofer, Li-xi Yang
  • Patent number: 5693804
    Abstract: Disclosed are compounds of formula I: ##STR1## wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl;Z is nitrogen or CH;Ar.sub.1 and Ar.sub.2 independently represent aryl groups; andY is hydrogen; orY and R.sub.1 or R.sub.2 together represent CH.sub.2 ;CH.sub.2 CH.sub.2 ; CH.sub.2 O; CH.sub.2 S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or the pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and in preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: December 2, 1997
    Assignee: Molecular Geriatrics Corporation
    Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
  • Patent number: 5693663
    Abstract: The invention relates to substituted bicyclic 3-aryl-pyrrilidine-2,4-dione derivatives of the formula ##STR1## wherein Q and A form a substituted 4- to 6-membered ring. These compounds have utility as pesticides.
    Type: Grant
    Filed: August 20, 1996
    Date of Patent: December 2, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Joachim Santel, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Christoph Erdelen, Thomas Bretschneider, Reiner Fischer, Hermann Hagemann, Bernd-Wieland Kruger, Klaus Lurssen
  • Patent number: 5693822
    Abstract: A method for the preparation of diaminobisimide compounds of the formula (I) which are substantially free of oligomers and are useful as curing agents in epoxy resin formulations: ##STR1## wherein Ar.sup.1 is an optionally substituted aromatic residue which provides for good conjugation between the nitrogen containing groups; and Ar is an optionally substituted aromatic residue, comprising heating an aromatic diamine of the formula H.sub.2 N--Ar.sup.1 --NH.sub.2, with an aromatic tetracarboxylic acid of the formula (HOOC).sub.2 (COOH).sub.2 or the corresponding dianhydride.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: December 2, 1997
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Jonathan Howard Hodgkin, Mervyn Benjamin Jackson, John West Loder
  • Patent number: 5693842
    Abstract: The invention relates to a process for preparing phosphorus-containing compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 are an alkyl radical having 1 to 8 carbon atoms, a cyclohexyl radical, a cyclopentyl radical, an aryl radical or a halogen-, alkyl- or alkoxy-substituted aryl radical, where R.sup.1 and R.sup.2 together with the phosphorus atom can also form a ring, n and m=0 or 1 and R.sup.3 and R.sup.4 are alkyl radicals having 1 to 4 carbon atoms or n=0, m=0 or 1 and R.sup.3 and R.sup.4 are H, by adding compounds of the formula II ##STR2## into dialkyl esters of fumaric acid or of maleic acid of the formula (III) or dialkyl esters of itaconic acid of the formula (IV) ##STR3## in which R.sup.3 and R.sup.4 have the meaning given above, and, optionally reacting an alkyl ester of a phosphorus-containing dicarboxylic acid of the formula (I), where n=0, with water in the presence of catalytic amounts of an acid to give the phosphorus-containing dicarboxylic acid.
    Type: Grant
    Filed: September 5, 1996
    Date of Patent: December 2, 1997
    Assignee: Hoechst AG
    Inventors: Hans-Jerg Kleiner, Volker Freudenberger, Peter Klein
  • Patent number: 5688986
    Abstract: Processes for hydrocyanation of nonconjugated acyclic aliphatic monoolefins, monoolefins conjugated to an ester group, or monoolefins conjugated to a nitrile group which utilize a catalyst precursor composition comprising a bidentate phosphite ligand and zero-valent nickel preferably in the presence of a Lewis acid prompter. Catalyst precursor compositions are also disclosed.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: November 18, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Wilson Tam, Kristina Ann Kreutzer, Ronald James McKinney
  • Patent number: 5686627
    Abstract: A process for making pure sodium enalapril is provided which includes the step of decomplexing essentially pure sodium enalapril-sodium iodide complex to yield essentially pure sodium enalapril.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: November 11, 1997
    Assignee: Brantford Chemicals Inc.
    Inventors: K. S. Keshava Murthy, Andrew Burchat, Gamini Weeratunga
  • Patent number: 5684025
    Abstract: Liquid formulations of 1,2-benzisothiazolin-3-one, and methods for making such formulations, are disclosed. Formulations according to the invention contain about 1 to 25 percent by weight 1,2-benzisothiazolin-3-one, about 3 to 7 percent by weight of sodium hydroxide, about 3 to 63 percent by weight of water and about 20 to 65 percent by weight of one or more polyglycol triols having the formula: ##STR1## wherein nx, ny and nz are individually selected from the group consisting of 2 and 3, and, when nx, ny and nz are each equal to 2, X+Y+Z has a value equal to or less than about 13.2, and, when nx, ny and nz are each equal to 3, X+Y+Z has a value equal to or less than about 4.45. Formulations exhibiting improved low temperature stability are also prepared by blending of specified co-solvents.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: November 4, 1997
    Assignee: Huls America Inc.
    Inventors: Techen Tsao, Jeffery S. Hinkle
  • Patent number: 5684010
    Abstract: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 4, 1997
    Assignee: Emory University
    Inventor: Raymond F. Schinazi
  • Patent number: 5684174
    Abstract: A method for purifying O,S-dimethyl N-acetyphosphoramidothioate, which is characterized by subjecting a crude crystal of O,S-dimethyl N-acetylphosphoramidothioate to recrystallization by using a two-phase solvent system comprising water and an organic which is an aromatic hydrocarbon, an aliphatic carboxylic acid ester or aliphatic ketone, wherein the amount of water is 0.1 to 2 parts by weight and the amount of the organic solvent is 1 to 20 parts by weight to 1 part by weight of the crude O,S-dimethyl N-acetylphosphoramidothioate.
    Type: Grant
    Filed: September 26, 1996
    Date of Patent: November 4, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoji Sakito, Mamoru Shirahata, Yujiro Kiyoshima, Kazuya Minamisaka, Atukazu Iwata