Abstract: Novel 5-acyloxy-4(5H)-oxazolonium salts of the formula ##STR1## in which R.sup.1 represents an optionally substituted aliphatic group with up to 12 carbon atoms, an optionally substituted cycloalkyl group with 3 to 10 carbon atoms, an optionally substituted phenyl or naphthyl group or an optionally substituted heterocyclic group andR.sup.2 and R.sup.3 are identical or different and represent a hydrogen atom or an optionally substituted aliphatic group with up to 8 carbon atoms or an optionally substituted phenyl group andX.sup..crclbar. represents the anion of an inorganic or organic acid having a pK.sub.a value of less than 2,are obtained in solution when an acyl cyanide of the general formulaR.sup.1 --CO--N (II)is reacted with a carboxylic acid anhydride of the general formulaR.sup.2 --CO--O--CO--R.sup.3 (III)whereinR.sup.1, R.sup.2 and R.sup.3 each have the abovementioned meaning, in the presence of one or more inorganic or organic acids.
Type:
Grant
Filed:
October 25, 1989
Date of Patent:
December 25, 1990
Assignee:
Bayer Aktiengesellschaft
Inventors:
Gerhard Bonse, Gerhard Marzolph, Heinz U. Blank
Abstract: A novel (-)-optically active piperazine derivative of the formula: ##STR1## (wherein the mark of * indicates an optically active carbon) shows an increased cerebral circulation-improving effect as well as an enhanced safety.
Abstract: Quaternary ammonium phosphates produced by reacting a dicarboxylic acid with an alkoxylated tertiary amine to prepare an amino-functional polyester, mixing the polyester in the presence of water with a phosphoric acid ester, and reacting the mixture with an alkylene oxide at elevated pressure and temperature. The quaternary ammonium phosphates are useful as anti-static agents for textile fiber materials.
Type:
Grant
Filed:
March 3, 1989
Date of Patent:
December 11, 1990
Assignee:
Henkel Kommanditgesellschaft auf Aktien
Inventors:
Guenter Uphues, Uwe Ploog, Wolfgang Becker, Irmhild Goebel
Abstract: A process for the preparation of optically active 3-demethylmevalonic acid derivatives of the formula I ##STR1## (3,5-dihydroxy carboxylic acid derivatives) or of the formula II ##STR2## in which R, R.sup.1 and Y have the indicated meanings, is described. The invention furthermore relates to aldehydes of the formula XII ##STR3## in which M represents the indicated protective groups.
Type:
Grant
Filed:
November 20, 1989
Date of Patent:
December 11, 1990
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Gunther Wess, Kurt Kesseler, Ekkehard Baader, Gerhard Beck
Abstract: Amino piperazine esters, preferably of the formula: ##STR1## wherein x is 0 or 1 and each R is independently hydrogen or inert substitution, are produced by reacting an (optionally substituted) N-(2-aminoethyl) piperazine with an (optionally substituted) alkylene carbonate. The novel compounds are biocides that retard the growth of fungi and are also useful in preparing polymers.
Abstract: Substituted cyclohexenes are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
Type:
Grant
Filed:
December 6, 1989
Date of Patent:
December 4, 1990
Assignee:
Warner-Lambert Company
Inventors:
Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
Abstract: Cyclopentenyl pyrimidine compounds have potent anti-viral, anti-tumor and differentiating activity. Of these compounds, cyclopentenyl cytosine has proved to be particularly effective in a variety of tumors, as well as having good antiviral activity and potent differentiating properties.
Type:
Grant
Filed:
January 31, 1989
Date of Patent:
December 4, 1990
Assignee:
The United States of America as represented by the Secretary of the Department of Health and Human Services
Inventors:
Victor E. Marquez, John S. Driscoll, Mu-Ill Lim, Christopher K. Tseng, Alberto Haces, Robert I. Glazer
Abstract: Disclosed are pyrimidine derivatives of the formula (I) and optical isomers thereof and a herbicide containing one or more of them as an active ingredient. ##STR1## where W is O or S; X is a lower alkyl group or a lower alkoxycarbonyl group; R is H, an optionally substituted lower alkyl group, an optionally substituted lower alkenyl group, an optionally substituted lower alkynyl group, an alkyali metal, an alkaline earth metal or an optionally substituted ammonium cation; R.sup.1 and R.sup.2 each are a halogen atom, an optionally substituted lower alkyl group or an optionally substituted lower alkoxy group; n is 3 to 5; m is 0 to 2; and is a single bond or a double bond.
Abstract: A process for the production of esters or lactones, comprising reacting in the presence of a catalyst and under hydrogenation conditions hydrogen and an acyclic or cyclic carboxylic anhydride to produce the corresponding ester or lactone, wherein the catalyst is a supported catalyst comprising:(a) a group VIII metal, Re and Fe;(b) a group VIII metal on TiO.sub.2 ;(c) Ru and at least one of Re, Ag or Cu; or(d) Pd and Fe.Preferably, the anhydride has the formula ##STR1## and is reacted to form an ester of the formula ##STR2## or a lactone of the formula ##STR3## wherein R and R.sup.1 independently are lower alkyl or cycloalkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5 independently are hydrogen, lower alkyl, cycloalkyl or aryl; and wherein R.sup.3 and R.sup.4 taken together may form a saturated or unsaturated ring, or an aromatic ring. The more preferred starting material is phthalic anhydride.
Abstract: New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.
Type:
Grant
Filed:
September 13, 1988
Date of Patent:
November 27, 1990
Assignee:
Istituto de Angeli
Inventors:
Massimo Nicola, Arturo Donetti, Enzo Cereda, Marco Turconi, Giovanni B. Schiavi, Rosamaria Micheletti
Abstract: Pharmaceutical composition which is useful as a medicinal product, in particular for the treatment of disorders of the central nervous system, characterized in that it contains customary pharmaceutical excipients, and at least one of the compounds of formula ##STR1## in which the trifluoromethyl substituent is at the 4-position, at the 5-position, or at 4- and 5-positions of the pyridinyl ring, and the substituent R denotes either hydrogen or a halogen, such as chlorine, at position(s) of the pyridinyl ring not occupied by CF.sub.3, and its pharmaceutically acceptable salts.
Type:
Grant
Filed:
November 21, 1989
Date of Patent:
November 20, 1990
Assignee:
Akzo N.V.
Inventors:
Patrick Carlier, Andre Monteil, Claude Poisson
Abstract: Chromogenic di-[bis-(indolyl)ethylenyl] tetrahalophthalides are disclosed of the formula ##STR1## wherein each X.sup.1, X.sup.2, X.sup.3, and X.sup.4 is independently selected from chlorine or bromine;wherein each of R.sup.1 and R.sup.7 is independently selected from cycloalkyl, aralkyl, alkoxyalkyl, or aroxyalkyl;wherein each of R.sup.2 and R.sup.8 is independently selected from alkyl (C.sub.1 -C.sub.8) or aryl (substituted or unsubstituted);wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 is independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, aryl (substituted or unsubstituted), halogen, alkoxy (C.sub.1 -C.sub.8), aroxy, cycloalkoxy, dialkylamino including symmetrical and unsymmetrical (C.sub.1 -C.sub.
Abstract: 2-bromo-8-ergolinyl compounds of the formula ##STR1## wherein R.sup.8 is NH.sub.2, NH--CONEt.sub.2, CONH.sub.2, ##STR2## and ##STR3## wherein R.sup.1 =C.sub.1-4 -alkyl andR.sup.2 =C.sub.1-4 -alkyl and benzyl,R.sup.9 and R.sup.10 each mean hydrogen or, together, a bond, and the substituent R.sup.8 can be in the .alpha.- or .beta.- position, and their acid addition salts,can be prepared from corresponding 8-ergolinyl compounds and their acid addition salts by bromination with elemental bromine in the presence of hydrogen bromide in a halogenated hydrocarbon.
Type:
Grant
Filed:
November 5, 1984
Date of Patent:
November 13, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Helmut Borner, Gregor Haffer, Gerhard Sauer
Abstract: Novel capped polymeric quaternary ammonium compositions formed by reacting ionene type polymers with tertiary amines are useful as microbicides, corrosion inhibitors, debonding agents, flocculants, softeners, plant growth regulators, and demulsifiers.
Type:
Grant
Filed:
May 23, 1989
Date of Patent:
November 13, 1990
Assignee:
Buckman Laboratories International, Inc.
Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.
Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.
Type:
Grant
Filed:
October 10, 1989
Date of Patent:
November 6, 1990
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
Abstract: This invention relates to the use of acyclic substituted pyrrolo[2,3-d]pyrimidine nucleoside analogs in the treatment of viral infections. Such substituted compounds retain antiviral properties present in their parent compounds, yet exhibit significantly decreased levels of cytotoxicity, thereby having therapeutic potential as antiviral agents.
Type:
Grant
Filed:
June 21, 1989
Date of Patent:
November 6, 1990
Assignee:
The Regents of The University of Michigan
Inventors:
Leroy B. Townsend, John G. Drach, Charles Shipman, Jr., Jeffrey S. Pudlo
Abstract: Ergoline derivatives of general Formula I ##STR1## wherein C.sub.8 C.sub.9 and C.sub.9 C.sub.10 are both CC-single bonds or one is a C.dbd.C-double bond,R.sup.6 is C.sub.1-4 alkyl,R.sup.8 is methyl, hydroxymethyl, carbonylmethoxy, ureido or N,N-diethylureido, each in the .alpha.- or .beta.-position, andR is hydrogen or nitro,are prepared by dehydrogenation of corresponding 2,3-dihydroergoline derivatives using an electrophilic reagent in an apolar solvent and a base.
Type:
Grant
Filed:
May 25, 1989
Date of Patent:
November 6, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Gerhard Sauer, Helmut Biere, Gregor Haffer, Andreas Huth
Abstract: New 6-oxo-pyridazine derivatives corresponding to the general formula I ##STR1## which represent new, positive inotropic compounds having a higher and more selective inotropy-increasing activity are described.A process of preparation and the medical use of these substances or of a medicament containing these substances are also described.
Type:
Grant
Filed:
April 14, 1989
Date of Patent:
November 6, 1990
Assignee:
Heumann Pharma GmbH & Co.
Inventors:
Peter Morsdorf, Rolf Herter, Heidrun Engler, Volker Pfahlert, Reinhold Weidner, Kurt H. Ahrens