Patents Examined by C. Warren Ivy
  • Patent number: 5708001
    Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R.sup.1 and R.sup.2 i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, or ii) taken together are a --CH.sub.2 -- group forming a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond; R.sup.3 is preferably hydrogen, halogen or lower alkyl, R.sup.4 is preferably hydrogen or lower alkyl, X is preferably CH.sub.2, Y is preferably hydrogen and Z is preferably CONR.sup.14 R.sup.15 and R.sup.14 and R.sup.15 are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 13, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Robert Carl Andrews, Cynthia Markert Cribbs, Stephen Vernon Frye, Curt Dale Haffner, Patrick Reed Maloney
  • Patent number: 5708008
    Abstract: This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R, R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: January 13, 1998
    Assignee: Eli Lilly and Company
    Inventors: James Edmund Audia, Bruce Anthony Dressman, James Joseph Droste, James Erwin Fritz, Stephen Warren Kaldor, Daniel James Koch, Joseph Herman Krushinski, Jr., Jeffrey Scott Nissen, Vincent Patrick Rocco, John Mehnert Schaus, Dennis Charles Thompson
  • Patent number: 5708029
    Abstract: Disclosed is the method of determining the effectiveness of an agent for the relief of elevation of the blood pressure, comprising the steps ofa) administering to a susceptible subject a quantity of a trigger substance reproducibly effective in producing within a period of six hours a perceptible increase in blood pressure lasting for at least twenty-four hours in the absence of treatment,b) administering to said subject having received said quantity of trigger substance a predetermined quantity of the agent whose effectiveness is to be determined,c) measuring the duration of said elevation of blood pressure upon administering said agent, andd) comparing the duration of said elevation with and without the administration of said agent.Also disclosed are effective quantities of certain nutrient substances which can reproducibly relieve elevated blood pressure produced in a susceptible subject by the administration of a trigger substance.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: January 13, 1998
    Inventor: Arthur Vanmoor
  • Patent number: 5708174
    Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: January 13, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
  • Patent number: 5707931
    Abstract: The present invention relates to novel 4-amino-2-quinolinone derivatives of the formula (I) useful in agriculture, especially as fungicides, insecticides and herbicides ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkyithio, NO.sub.2, CN, C.sub.1 -C.sub.4 alkoxy carbonyl, phenyl, phenoxy, benzoyl, benzenesulfonyl, benzyl or morpholine; R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, cyclopropyl, phenyl, halophenyl, benzyl or phenylthiomethyl; R.sub.6 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl; and R.sub.7 is ##STR2## wherein, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, R.sub.18, R.sub.19, R.sub.20, X, Y, m, n, p and q are defined within the description.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: January 13, 1998
    Assignee: Korea Research Intsituted of Chemical Technology
    Inventors: Chwang Siek Pak, Eun Bok Choi, Gyu Hwan Yon, Heui Cheol Yang, Hyeon Kyu Lee, Ge Hyeong Lee, Jin Pyo Lee, Gyung Ja Choi
  • Patent number: 5705661
    Abstract: A catalyst for oxidizing ethylene and producing ethylene oxide, said catalyst being prepared by pretreating a porous carrier with a solution containing a lithium compound and a cesium compound, thereafter, impregnating a solution containing a silver compound and a cesium compound in the pretreated porous carrier and then heat-treating the impregnated porous carrier.The use of the catalyst of this invention provides high selectivity in the production of ethylene oxide by the vapor contact oxidation of ethylene.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: January 6, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Tomoatsu Iwakura, Takako Imamoto, Katsumi Nakashiro
  • Patent number: 5705504
    Abstract: Compounds of general formula I and their salts and solvates are PAF antagonists and as such are useful in the treatment of various diseases or disorders mediated by PAF. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
    Type: Grant
    Filed: October 22, 1996
    Date of Patent: January 6, 1998
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Elena Carceller, Pere J. Jimenez, Nuria Recasens, Jordi Salas, Carmen Almansa, Javier Bartroli
  • Patent number: 5705701
    Abstract: In a process for producing trimethylsulfoxonium bromide by reacting dimethyl sulfoxide and methyl bromide, methyl bromide is added to a mixture of dimethyl sulfoxide and a stabilizing agent under atmospheric pressure intermittently or continuously so that the final molar ratio of methyl bromide to dimethyl sulfoxide becomes 0.40:1 to 0.70:1, with the temperature of dimethyl sulfoxide being maintained at a temperature of 50.degree. to 75.degree. C. This process can realize a reduction of reaction time, an improvement of yield and establishment of safety of producing operations.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: January 6, 1998
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventor: Kazuhiko Sunagawa
  • Patent number: 5705144
    Abstract: A composition for topical application to human skin in order to promote the repair of photo-damaged skin and/or to reduce or prevent the damaging effects of ultra-violet light on skin and/or to lighten the skin comprising retinol or a derivative thereof and a dioic acid.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: January 6, 1998
    Assignee: Unilever Patent Holdings B.V.
    Inventors: Clive Roderick Harding, Caroline Marian Lee, Ian Richard Scott
  • Patent number: 5705509
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5705707
    Abstract: A process for the preparation of n-butyraldehyde and/or n-butanol, whereina) 1,3-butadiene is caused to react with an alcohol of the formula IROH I,to form a mixture of adducts of the formulas II ##STR1## and III ##STR2## b) the adduct III is isomerized to the adduct II, c) the adduct II is isomerized in the presence of a homogeneous or heterogeneous transition metal element catalyst to form the enol ether of the formula IV ##STR3## and d) n-butyraldehyde and/or n-butanol is/are produced from this ether IV by the reaction thereof with hydrogen and water or water only in the presence of a homogeneous or heterogeneous catalyst.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: January 6, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Jurgen Kanand, Michael Roper, Rolf Pinkos, Rocco Paciello, Alfred Thome
  • Patent number: 5705708
    Abstract: Discoloration of cumene hydroperoxide is reduced or inhibited by adding to the cumene hydroperoxide an effective amount on the order of 30 to 1000 ppm of a stabilizer of the formula R'C(O)OM wherein R' is alkyl, alkenyl, cycloalkyl or aryl containing 1-40 carbon atoms, or the formula R.sub.4 NOH wherein each R is independently alkyl or cycloalkyl containing 1-40 carbon atoms.
    Type: Grant
    Filed: September 23, 1996
    Date of Patent: January 6, 1998
    Assignee: Witco Corporation
    Inventor: Peter Frenkel
  • Patent number: 5705716
    Abstract: The present invention provides hydrochlorofluorocarbons having 3 to 5 carbons atoms, 1 to 2 chlorine atoms, and an OH rate constant from about 8 to about 25 cm.sup.3 /molecule/sec.times.10.sup.-14. The hydrochlorofluorocarbons are useful as solvents and blowing agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 6, 1998
    Assignee: AlliedSignal Inc.
    Inventor: Chien Chi Li
  • Patent number: 5705648
    Abstract: Mepiquat chloride is formed from the reaction between N-methylpiperidine and chloromethane in an anhydrous liquid solvent selected from the group consisting of acetone, methyl ethyl ketone, toluene, tetrahydrofuran, isopropanol, acetonitrile, N,N-dimethylformamide and methylene chloride in the absence of sodium hydroxide. Mepiquat chloride precipitates as a solid of high purity and is recovered under a substantially moisture-free atmosphere.The solid mepiquat chloride can be sealed into a water soluble pouch or into a water soluble encapsulated solid form (e.g., granule, pellet, or briquette) for convenient handling. The pouch contains powdered mepiquat chloride or the encapsulated solid is merely introduced directly into a spray tank or reservoir for application with low human exposure and no containers in contact with the mepiquat chloride that require disposal.Mepiquat chloride is used as a component of a system for growing a number of commodity plants including cotton.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: January 6, 1998
    Assignee: Micro Flo Co.
    Inventors: Richard U. Clark, James S. Lovell, James C. Thigpen, David William Bristol, John Raymond Tyndall, Albert Roger Frisbee
  • Patent number: 5705705
    Abstract: A process for the oxidation of alkylaromatic compounds is provided. The process comprises oxidizing a substrate alkylaromatic compound with a peroxygen compound in the presence of a source of cerium (III) or (IV), a source of bromide and a carboxylic acid or anhydride solvent. Preferably, the source of cerium is cerium (III) acetate, the source of bromide is sodium bromide and the solvent is acetic or propionic acid. The process is particularly suited to the selective oxidation of methylaromatic compounds to the corresponding aldehydes.
    Type: Grant
    Filed: March 26, 1996
    Date of Patent: January 6, 1998
    Assignee: Solvay Interox Limited
    Inventors: Scott William Brown, Kevin Auty
  • Patent number: 5703084
    Abstract: This invention disclosed (2S,3R)-3(6-aminopurin-9-yl) aralkan-2-ols, a novel class of adenine derivatives (also called 9-aralkyladenines, ARADS), which have been shown to inhibit the enzyme adenosine deaminase at therapeutically useful levels. The relevant inhibitory constant (K.sub.i) values are in the range of 10.sup.-7 -10.sup.-10 M. These compounds with potencies in this range can reversibly inhibit ADA in an effective manner, without permanently deactivating the enzyme. ADA inhibitors that have similar biological profiles have been shown to be of therapeutic value when used to protect heart muscle against ischemic damage.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: December 30, 1997
    Assignee: The Board of Governors for Higher Education, State of Rhode Island and Providence Plantations
    Inventors: Elie Abushanab, Palle V. P. Pragnacharyulu
  • Patent number: 5703094
    Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by an unsaturated bicyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: December 30, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Michael Ruther, Thomas Schenke, Klaus Dieter Bremm, Rainer Endermann
  • Patent number: 5703096
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or alkyl; R.sup.2 is alkylene; R.sup.3 is hydrogen, alkyl, alkoxy, alkylthio, halogen, nitro group, amino group, monoalkylamino, dialkylamino, aryl, or aralkyl; X is aryl, or aromatic heterocyclic; Y is oxygen, sulfur or a group of formula >N-R.sup.4, in which R.sup.4 is hydrogen, alkyl or acyl; and Z is a group of formula (Za), (Zb), (Zc) or (Zd): ##STR2## and salts thereof can be used to treat or prevent are included those arising from hyperlipidemia, hyperglycemia, obesity, impaired glucose tolerance (IGT), insulin resistant non-IGT (NGT), non-diagnostic glucose tolerance, insulin resistance, diabetic complications, fatty liver, polycystic ovary syndrome (PCOS) and gestational diabetes mellitus (GDM); in addition the compounds of the present invention have aldose reductase inhibitory activity.
    Type: Grant
    Filed: October 5, 1995
    Date of Patent: December 30, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroaki Yanagisawa, Takashi Fujita, Koichi Fujimoto, Takao Yoshioka, Kunio Wada, Minoru Oguchi, Toshihiko Fujiwara, Hiroyoshi Horikoshi
  • Patent number: 5703133
    Abstract: The invention provides for a method of making isoalcohols using syngas-to-alcohol catalyst and method of making it. The catalyst is a highly dispersed, alkali promoted, La stabilized, microcrystalline Cu.sub.2 O having a particle size of .ltoreq.6 nm in the presence of an alumina structural promoter, wherein on a mole % alkali free metals-only basis Cu is present in from 45 to 55%, Zn from 10 to 20%, Al from 10 to 25%, La from 5 to 15%, and wherein the alkali is from 0.01 to 0.91% K and from 3 to 6.5% Cs. The method of making it involves coprecipitation at a constant pH from a solution of soluble metal salts of copper, zinc, lanthanum and aluminum with an alkali hydroxide, washing the coprecipitate in the essential absence of CO.sub.2, drying and calcining it, then contacting it with K and Cs to form the promoted catalyst. The promoted catalyst is dried and recalcining to produce a catalyst precursor with highly dispersed CuO crystallites. The catalyst is activated in flowing hydrogen.
    Type: Grant
    Filed: December 8, 1995
    Date of Patent: December 30, 1997
    Assignee: Exxon Research and Engineering Company
    Inventors: Thomas Henry Vanderspurt, Russell John Koveal
  • Patent number: 5703125
    Abstract: The invention relates to platelet aggregation inhibitors which are substituted beta amino acid derivatives of the formula: ##STR1## wherein Z, A, Z', Z", W, q, R.sup.1 and R.sup.2 are as defined in the specification.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 30, 1997
    Assignees: G. D. Searle & Co., The Monsanto Company
    Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki