Patents Examined by Cecilia Shen
  • Patent number: 5112991
    Abstract: A process is provided herein for preparing an organo-substituted sodium aluminum hydride by reacting sodium, aluminum, an organic compound of specific structure containing a hydroxyl group and hydrogen.In such process, an aluminum alloy is used as the aluminum.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: May 12, 1992
    Assignee: Mitsui Toatsu Chemicals Incorporated
    Inventors: Tetsuya Iwao, Shuichi Osaka, Takao Sakaki, Tadao Nishida, Kiyoshi Yamamura, Seijiro Koga, Reiji Hirai, Haruo Nakagawa
  • Patent number: 5110929
    Abstract: The synthesis of 4-, 4-(1,1)-and 3,5-substituted N-alkyl-pyridinium salts as well as of 2-carboxamide substituted N(1,4)diazinium compounds are described. The N-surfactants obtained have a small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter. These surfactants produce micells of different size and form depending on the nature of the anions. 4-(1,1)-substituted and 3,5-substituted N-alkyl-pyridinium components are capable of forming vesicles in equeous solutions of different forms and sizes. The N-surfactants synthesized can be used as pharmaceuticals.
    Type: Grant
    Filed: June 14, 1990
    Date of Patent: May 5, 1992
    Assignee: Medice Cham.-Pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5110816
    Abstract: The present invention relates to the products of general formula (I): ##STR1## in which R.sub.1 and R.sub.2 are identical or different and are selected om a hydrogen atom, a halogen atom, a hydroxyl radical, an alkyl radical having from 1 to 5 (sic) carbon atoms, an alkoxy radical having from 1 to 5 carbon atoms or a phenoxy, benzyloxy, trifluoromethyl or acetyl radical.It further relates toa method of preparing said productsand the drugs in which said products are present.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: May 5, 1992
    Assignee: Institut de Recherches Chimiques et Biologiques Appliquees (I.R.C.E.B.A.)
    Inventors: Patrick Houziaux, Jean-Pierre Riffaud, Jean-Yves Lacolle, Bernard Danree
  • Patent number: 5110952
    Abstract: A method of producing a high melting point 3-dibutyl amino-6-methyl-7-anilinofluoran characterized by peaks at diffraction angle (2 .theta.) of 6.9.degree., 11.0.degree., 18.5.degree. and 18.9.degree. in X-ray diffractiometry using Cu-K .alpha. ray and having a melting point in the range of 179.degree.-186.degree. C., which comprises: condensing 2-(4-dibutylamino-2-hydroxy-benzoyl) benzoic acid with 4-methoxy-2-methyldiphenylamine in the presence of concentrated sulfuric acid to provide a phthalide at a temperature in the range of 0.degree.-50.degree. C., neutralizing the phthalide, and then subjecting the phthalide to ring closure reaction using an alkali in an amount of 0.5-15 mols per mol of the compound used in smaller amounts of 2-(4-dibutylamino-2-hydroxy-benzoyl) benzoic acid and 4-methoxy-2-methyldiphenylamine at a temperature of not less than 50.degree. C. in the presence or absence of an organic solvent.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: May 5, 1992
    Assignee: Yamamoto Chemicals, Inc.
    Inventors: Hiroaki Harada, Yasuhisa Iwasaki
  • Patent number: 5110928
    Abstract: N-Aryl-substituted 2-amino-alkyl-2-hydroxyalkylamines and N-aryl-substituted piperazines Ia and Ib respectively ##STR1## (Ar=aryl; R.sup.1 =hydrogen, methyl, identical or different, R.sup.2 =hydrogen, alkyl) are prepared by reacting an N,N-di(2-hydroxyalkyl)-N-arylamine II ##STR2## with ammonia or a primary amine IIIH.sub.2 N-R.sup.2 IIIat elevated temperature and under elevated pressure in the presence of hydrogen and of a catalyst which is a supported catalyst whose active mass predominantly contains copper and/or nickel and/or cobalt in the form of the metal or an oxide.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: May 5, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Schroeder, Guenther Ruider
  • Patent number: 5106854
    Abstract: Novel quinolonecarboxylic acids of the formula: ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 each is identically or differently hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.4 is cyclopropyl, phenyl, halo-phenyl, or thienyl optionally substituted by C.sub.1 -C.sub.4 alkyl or halogen, and R.sup.5 is halogen, or pharmaceutically acceptable salts thereof having a more potent and longer lasting antibacterial activities against G(+) and G(-) bacteria than known analogues, useful as antibacterial agents at an oral dose of 1-500 mg, preferably 50-100 mg per day to an adult.
    Type: Grant
    Filed: December 13, 1990
    Date of Patent: April 21, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Teruji Tsuji, Hisao Sato, Tetsuo Okada
  • Patent number: 5106850
    Abstract: 3-[4-(4-p-Methoxyphenylpiperazino)butyl]-5-methoxyindole and the salts thereof can be used as psychopharmaceuticals and antihypertensives.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: April 21, 1992
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Henning Butcher, Christopy Seyfried, Hartmut Greiner
  • Patent number: 5104895
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2, that can be the same or different, are hydrogen, alkyl, aryl, aralkyl groups or, if taken together, cycloalkyl groups;A is a carbon atom, a residue of 2,3-dioxybutandioic-2,4-dioxyphtalic acid or disubstituted malonic acid derivatives;n.sub.1 and n.sub.2 are selected in such a manner that the result of their addition is from 2 to 40;T.sub.1 and T.sub.2 that can be the same or different, are hydrogen, alkyl, benzyl, phenyl, acyl or cycloalkyl or a residue of formulae ##STR2## Compounds I are useful as anti-tumor agents in human therapy.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: April 14, 1992
    Assignee: Boehringer Mannheim Italia S.p.A.
    Inventors: Silvano Spinelli, Alessandro Pasini, Ernesto Menta, Franco Zunino, Sergio Tognella
  • Patent number: 5104874
    Abstract: A series of 2-amino-5,6-dimethyl-1,4-benzoquinone derivatives, inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergic and antiinflammatory agents.
    Type: Grant
    Filed: December 13, 1990
    Date of Patent: April 14, 1992
    Assignee: Pfizer Inc.
    Inventors: Takafumi Ikeda, Hiroaki Wakabayashi, Masami Nakane
  • Patent number: 5104876
    Abstract: Novel benzopyrido piperidiene, piperidylidene and piperazine compounds of the generalized formula ##STR1## are disclosed as useful for the treatment of asthma, allergy and inflammation. Novel pharmaceutical compositions containing such compounds and processes for producing the compounds are also disclosed.
    Type: Grant
    Filed: October 26, 1990
    Date of Patent: April 14, 1992
    Assignee: Schering Corporation
    Inventors: John J. Piwinski, Jesse K. Wong, Michael J. Green, Ashit K. Ganguly, Frank J. Villani
  • Patent number: 5104987
    Abstract: This invention relates to a process for the alkoxylation of an active hydrogen-containing compound comprising contacting the active hydrogen-containing compound with an alkylene carbonate in the presence of a mixed metal oxide catalyst under conditions effective to alkoxylate the active hydrogen-containing compound.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: April 14, 1992
    Assignee: Union Carbide Chemicals & Plastics Technology Corporation
    Inventor: Stephen W. King
  • Patent number: 5104880
    Abstract: An acetylcholinesterase inhibitor is provided of the general formula (I): ##STR1## wherein R.sub.1 is H, (C.sub.1 -C.sub.8)alkyl or halo; R.sub.2 is H or (C.sub.1 -C.sub.8)alkyl; R.sub.3 and R.sub.4 are individually H, (C.sub.1 -C.sub.8)alkyl, NO.sub.2, hydroxy or halo; R.sub.5 and R.sub.6 are individually H, (C.sub.1 -C.sub.8)akyl, aryl or aralkyl; R.sub.7 is H, halo or (C.sub.1 -C.sub.8)alkyl, R.sub.8 is halo or (C.sub.1 -C.sub.8)alkyl; R.sub.9 is absent or is H; and the bonds represented by--are individually absent or, together with the adjacent bond, form the unit C.dbd.C, with the proviso that if both of the bonds represented by--are present, R.sub.3 and R.sub.4 cannot both be H unless R.sub.7 or R.sub.8 is halo; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: April 14, 1992
    Assignee: Mayo Foundation for Medical Education and Research
    Inventor: Alan P. Kozikowski
  • Patent number: 5102901
    Abstract: The invention relates to a group of new 3-N substituted carbamoyl-indole derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.
    Type: Grant
    Filed: April 13, 1990
    Date of Patent: April 7, 1992
    Assignee: Duphar International Research B.V.
    Inventors: Ineke van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
  • Patent number: 5101023
    Abstract: The invention relates to a process for preparing a compound of formula (I) ##STR1## in which R.sub.1 is H, an alkyl radical or an alkoxy, hydroxyalkyl or halogen radical, and R.sub.3 is N.sub.3 or a CN radical, characterized in that a compound of formula (II): ##STR2## is reacted with a phosphine derivative and an azodicarboxylic acid diester and a carboxylic acid R.sub.2 --COOH in a solvent compatible with the reaction conditions, to form the compound of formula (III): ##STR3## which, after separation if required, is opened in the presence of an azide or a cyanide in a solvent compatible with the reaction conditions, and the compound of formula (I) is then isolated from the reaction medium after deprotection of the 5'-position.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: March 31, 1992
    Assignee: Universite Pierre et Marie Curie (Paris VI)
    Inventors: Stanislas Czernecki, Jean-Marc Valery, Guy Ville
  • Patent number: 5101032
    Abstract: Cycloalkylidene dyes have the formula ##STR1## where m is 0 or 1,L is a chemical bond or C.sub.1 -C.sub.2 -alkylene, which may be substituted,R.sup.1 is hydrogen, C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl,Y is oxygen or two hydrogens,X.sup.1 is oxygen andX.sup.2 is C.sub.1 -C.sub.8 -alkanoyloxy, substituted or unsubstituted benzoyloxy, C.sub.1 -C.sub.6 -trialkylsilyloxy or a radical of the formula OR.sup.1 or NR.sup.2 R.sup.3, where R.sup.1 is as defined above and R.sup.2 and R.sup.3 are identical or different and each is independently of the other C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl, or C.sub.3 -C.sub.7 -cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom joining them are saturated heterocyclyl, or else one of R.sup.2 and R.sup.3 is hydrogen, or X.sup.1 and X.sup.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: March 31, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel
  • Patent number: 5098898
    Abstract: Phospholipid derivatives resulting from coupling of ascorbic acid to a glycerol ester or ether via a phosphoric acid residue and having antioxidant activity and lipid peroxide inhibiting activity, which have the formula ##STR1## wherein R.sup.1 and R.sup.2 represent the same or different and each represents an alkyl or acyl group and neither formula represents any particular configuration nor conformation.
    Type: Grant
    Filed: December 27, 1990
    Date of Patent: March 24, 1992
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Kyozo Yamamoto, Takahiro Matsumoto
  • Patent number: 5098903
    Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes substituents comprising a hydroxy group, a hydrogen atom, an acetate group or a substituted or unsubstituted alkoxy group. The compounds are useful as antiestrogens and antitumor agents.
    Type: Grant
    Filed: November 6, 1989
    Date of Patent: March 24, 1992
    Assignee: Board of Regents of the University of Oklahoma
    Inventors: Robert A. Magarian, Joseph T. Pento, Kwasi S. Avor
  • Patent number: 5099020
    Abstract: The present invention provides methods and compositions for assaying biological samples, such as human serum, for barbiturates. In one aspect, analogs of barbiturates derivatized with fluorescein and analogs of barbiturates derivatized with immunogenic polypeptides are provided. The fluorescent analogs are employed as tracers in a competitive homogeneous immunoassay, i.e., a fluorescence polarization immunoassay, for detecting barbiturates. The immunogenic analogs are employed to make anti-barbiturate antiserum of the invention for use in the immunoassay method. Intermediates for preparing the fluorescent and immunogenic analogs are also provided. Further provided are test kits, comprising a fluorescent tracer and an antiserum according to the invention, for analyzing biological samples by fluorescence polarization immunoassay for the presence of a barbiturate.
    Type: Grant
    Filed: June 27, 1990
    Date of Patent: March 24, 1992
    Assignee: Abbott Laboratories
    Inventors: Jonathan Grote, Hsiang Hu
  • Patent number: 5097031
    Abstract: The invention relates to a novel stereoselective process for the preparation of dihdyrolysergol from lysergol by hydrogenation in the presence of solvent and palladium catalyst applied on a carrier, which comprises hydrogenating lysergol in the presence of one or more aprotic solvent(s) containing tertiary nitrogen atom(s) and a palladium catalyst applied on activated carbon, and recovering the product obtained from the reaction mixture in a known manner.
    Type: Grant
    Filed: June 22, 1990
    Date of Patent: March 17, 1992
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Istvan Polgar, Jozsef Foldesi, Janos Kiss, Piroska Major nee Forstner, Karoly Molnar, Andras Sugar, Tamas Szen, Katalin Balogh nee Nemes
  • Patent number: 5097030
    Abstract: 2-(methylthio)barbituric acid is obtained with high yields and degree of purity by reacting a solution or suspension of an alkali metal salt or alkaline earth metal salt of 2-thiobarbituric acid with methyl bromide at a pressure of 1.5 to 5 bar.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Huels Aktiengesellschaft
    Inventors: Marcel Feld, Friedrich Goerentz