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.
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
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
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.
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.
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.
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.
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.
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
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
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
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
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
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
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.
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
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.
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
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.