Abstract: Sparsomycin derivatives of the formula ##STR1## wherein X and Y are each independently an oxo or an imino group; n is 0 or the integer 1 or 2; R.sub.1 is a hydrogen or 1 to 4 carbon alkyl group; R.sub.2 is a hydrogen, a 1 to 4 carbon alkyl, a 2 to 5 carbon acyl or a benzoyl group; and R is a 1 to 6 carbon alkyl, 3 to 8 carbon alkenyl, cyanomethyl carboxymethyl, carbalkoxymethyl wherein the alkoxy moiety is a 1 to 4 carbon alkoxy group, nitromethyl, alkylcarbonylmethyl wherein the alkyl moiety is a 1 to 4 carbon alkyl group, pyridyl, furanyl, or furfuryl group or a phenyl or benzyl group optionally substituted by a methylenedioxy or one to two halogen, 1 to 4 carbon alkyl, 1 to 4 carbon alkoxy, 1 to 4 carbon alkylthio, hydroxy, nitro or cyano groups or a pharmaceutically acceptable acid addition salt thereof. Also described are their use as antiprotozoals and antibacterials.
Abstract: Substituted 5-phenylthio-6-aminopyrimidinones of the general formula I ##STR1## in which R denotes an amino or hydroxyl group, and their tautomeric forms and acid addition salts thereof, have diuretic, saluretic and uricosuric actions. They can be used as medicaments for the treatment of hypertension, hyperuricemia and edemas.
Abstract: Novel pyrazolo[4,3-c]cinnolin-3-one derivatives of the formula ##STR1## wherein R may be in the 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --NO.sub.2 and --CF.sub.3 and R' is hydrogen or R and R' taken together form an alkylenedioxy of 1 to 4 carbon atoms at the 7- or 8-positions and R.sub.1 is selected from the group consisting of phenyl, pyridyl, thiazolyl, dihydrothiazolyl and thienyl, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, mono-, di- and tri- halomethyl and aralkoxy of 7 to 12 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties and novel intermediates therefore.
Type:
Grant
Filed:
January 16, 1985
Date of Patent:
May 27, 1986
Assignee:
Roussel Uclaf
Inventors:
Jean-Claude Gasc, Daniel Humbert, Peter F. Hunt
Abstract: Pyrazolo[3,4,5-k1]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
Abstract: Novel imidazo[1,2-a]pyrimidines of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 12 carbon atoms, aryl of 6 to 12 carbon atoms, thienyl and pyridyl, each of said group being optionally substituted with at least one member of the group consisting of halogen, alkyl of 1 to 5 carbon atoms, alkoxy and alkylthio of 1 to 5 carbon atoms, trifluoromethyl, amino, alkylamino of 1 to 5 alkyl carbon atoms and dialkylamino with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.
Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen, alkyl, trifluoromethyl, halogen, alkoxycarbonyl, alkoxy or alkanoyl, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, methyl, alkoxy or alkoxyethoxy, and R is hydrogen or a group SR.sup.6, in which R.sup.6 is the lone, unpaired electron of the 12-sulfenyl radical, hydrogen, optionally substituted alkyl, alkenyl, alkynyl, alkanoyl, optionally mono- or poly-substituted benzoyl, fuoryl, phenacyl, phenoxyacetyl, phenylacetyl or another conventional thiol-protective group, and to physiologically acceptable salts thereof, and to processes for their preparation, to their use as a gastric acid secretion inhibitor and to pharmaceutical preparations based on these compounds.
Type:
Grant
Filed:
September 13, 1984
Date of Patent:
April 29, 1986
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Volker Hitzel, Gerhard Rackur, Martin Bickel
Abstract: A solution of a di-alkyl carbonate, e.g. dimethyl carbonate, in the corresponding alcohol, e.g. methanol, is concentrated by contacting the solution with a hydrophobic zeolite e.g. silicalite. The di-alkyl carbonate is absorbed preferentially. Where the solution also contains water, e.g. as in the case of the products from certain di-alkyl carbonate synthesis reactions, the water can be removed using a hydrophilic zeolite prior to recycle of the alcohol.
Abstract: The invention concerns novel sparsomycin (S.sub.c -R.sub.s) derivatives having superior cytostatic activity compared to sparsomycin itself. Said derivatives contain a lipophilic group R.sup.2, selected from C.sub.2 -C.sub.20 -alkyl, aryl, aralkyl and alkaryl, which is preferably n-octyl or benzyl.
Type:
Grant
Filed:
December 9, 1983
Date of Patent:
April 8, 1986
Assignee:
Stichting Katholieke Universiteit
Inventors:
Henricus C. J. Ottenheijm, Robertus M. J. Liskamp
Abstract: A process for preparing a 5-perfluoroalkyl-dihydrouracil derivative of the general formula ##STR1## wherein R.sub.f represents a perfluoroalkyl group, each of R.sup.1 and R.sup.2 represents a hydrogen atom, or an alkyl, cycloalkyl, aryl, aralkyl or heterocyclic group, and Y is an oxygen or sulfur atom, which comprises (a) reacting a compound of the general formula ##STR2## wherein X represents a halogen atom or hydroxyl group, with a urea derivative of the general formula ##STR3## provided that when X is a hydroxyl group and at least one of R.sup.1 and R.sup.2 is a hydrogen atom, said reaction is carried out in the presence of a condensing agent, or (b) cyclizing a compound of the general formula ##STR4## and a novel intermediate compound of the above formula (IV).
Abstract: This invention relates to the use of 6-aryluracils as antiinflammatory and antiarthritic agents and also to both novel intermediates and novel processes for the preparation of selected 6-aryluracils.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
March 25, 1986
Assignee:
The Upjohn Company
Inventors:
Harvey I. Skulnick, Herman W. Smith, Robert J. Smith, Wendell Wierenga
Abstract: 1H-2-benzopyran-1-yl alkyl or 1-(isochroman-1-yl) alkyl 4-phenyl piperazines are prepared and exhibit antipsychotic and hypotensive activity.
Abstract: A new therapeutic agent with anti-platelet aggregant activity is described, with the chemical formula of 7-(1-methyl-5-p-methylbenzoylpyrrole-2-acetamidoethyl)-theophylline: ##STR1##
Abstract: 7-Aminoazolo[1,5-a]pyrimidine of the formula ##STR1## where R.sup.1 is unsubstituted or substituted alkyl, halogen, alkoxy, cyano, or cycloalkyl, or is aryl, aryloxy, arylthio, arylalkyl, arylalkoxy or arylalkylthio, each of which may be substituted, or is indane, tetrahydronaphthalene or benzene, each of which may be substituted and is fused to the phenyl ring, R.sup.2 and R.sup.3 are each hydrogen, alkyl or aryl, n is 1 or 2, A is nitrogen or a CR.sup.4 group, where R.sup.4 has the meanings of R.sup.2 and may furthermore be halogen, cyano or alkoxycarbonyl, or together with R.sup.3 is alkylene which may have up to 2 double bonds, and fungicides containing these compounds.
Type:
Grant
Filed:
September 18, 1984
Date of Patent:
January 28, 1986
Assignee:
BASF Aktiengesellschaft
Inventors:
Karl Eicken, Klaus Scheib, Hans Theobald, Ernst-Heinrich Pommer, Eberhard Ammermann
Abstract: Isoindolazines which, in one of their tautomeric structures, have the formula ##STR1## where the rings designated X and T can be substituted andA.sup.1 and A.sup.2 represent the divalent radical of a compound having two replaceable hydrogen atoms on a C or N atom, in particular the divalent radical of an active methylene compound, of an amine, of a hydrazine, of a hydrazide or of a hydrazone,salts and complexes of these compounds, processes for their preparation, and their use as pigments.
Type:
Grant
Filed:
August 3, 1983
Date of Patent:
January 14, 1986
Assignee:
Bayer Aktiengesellschaft
Inventors:
Meinhard Rolf, Rutger Neeff, Walter Muller, Volker Hederich
Abstract: Compounds of general formula (I): ##STR1## wherein R is a chlorine, bromine or iodine atom and physiologically acceptable salts thereof with bases of use as antiviral agents.
Type:
Grant
Filed:
September 16, 1983
Date of Patent:
January 14, 1986
Assignee:
Glaxo Group Limited
Inventors:
David I. C. Scopes, Roger F. Newton, Richard C. Cookson
Abstract: This disclosure describes novel pyrazolylpiperazines useful as hypotensive agents in mammals and as intermediates for the preparation of certain pyrazolo[1,5-a]pryrimidines.
Type:
Grant
Filed:
October 9, 1984
Date of Patent:
December 31, 1985
Assignee:
American Cyanamid Company
Inventors:
Andrew S. Tomcufcik, Walter E. Meyer, Shin S. Tseng
Abstract: A process for the transesterification of a carboxylic or carbonic acid ester comprises reacting the carboxylic or carbonic acid ester under transesterification conditions with an alcohol in the presence, as catalyst, of either (i) a Group V element-containing Lewis base and an epoxide or (ii) a cyclic amidine.The Lewis base can be an organic compound containing trivalent phosphorus or nitrogen and can be an amine, for example an amidine.The process can be operated in the liquid phase at a temperature of from 15.degree. to 150.degree. C., and the catalyst is employed in solution.Preferred catalysts are those where the cyclic amidine forms part of a fused ring system containing six and five membered rings, six and seven membered rings or two six membered rings.
Abstract: A method is disclosed whereby uracil is obtained from alkali formyl acetic acid alkyl esters by reacting such esters with thiourea and then with hydrogen peroxide without isolating the intermediates, and then separating the uracil by precipitation with acids.