Abstract: A pharmaceutical composition containing as an essential ingredient a compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is an .omega.- or (.omega.-1)-hydroxyalkyl group having from 5 to 8 carbon atoms in which the hydroxy group is separated from the xanthine nucleus by at least 2 carbon atoms, radicals R.sub.1 and R.sub.3 which are no hydroxylalkyl group, are hydrogen or methyl and equal or different, and R.sub.2 is said hydroxyalkyl group or methyl, a compound of formula (I) and a pharmaceutical product for treatment of diseases involving insufficiency of cerebral blood flow.

Abstract: Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.

Abstract: A novel compound has the following formula: ##STR1## in which R.sub.1 and R.sub.2 are methyl or a group having the formula: ##STR2## provided that one of R.sub.1 and R.sub.2 is methyl and the other is said group, wherein R stands for a hydrogen atom or a lower alkyl group, Z stands for a group ##STR3## in which X.sub.1 and X.sub.2, which may be the same or different, stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, or a pyridyl group or a group ##STR4## in which Y.sub.1 and Y.sub.2, which may be the same or different stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, X stands for a nitrogen or carbon atom, and n is an integer of from 2 to 10, provided that when R.sub.2 is the group having the formula II, X is not carbon and Z is not pyridyl.

Abstract: New xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or alkyl from C.sub.1 to C.sub.5 inclusive;R.sub.2 is a hydrocarbon radical up to C.sub.6 having optionally a double bond, phenyl or benzyl;R.sub.3 is hydrogen, alkyl, hydroxyalkyl or dihydroxyalkyl each from C.sub.1 to C.sub.5R.sub.4 represents: ##STR2## in which: Y is hydrogen, halogen, alkyl or alkoxy from C.sub.1 to C.sub.5 or hydroxyl;Z is methylene or a straight or branched hydrocarbon radical from C.sub.2 to C.sub.5 optionally substituted by hydroxyl; andA is an amino group of the formula: ##STR3## p being 2 or 3; ##STR4## in which q is 1 or 2, and X is a single bond, oxygen or ##STR5## in which R.sub.5 is hydrogen, alkyl or alkylene up to C.sub.5, or ##STR6## in which m is an integer from 2 to 6 and R.sub.6 is alkyl from C.sub.1 to C.sub.5.

Abstract: 1H-Indol-3-yl containing 1,3-dimethyl-1H-purine-2,6-diones having psychotropic activity.

Abstract: The invention refers to compounds having activity against chronic obstructive airway disease or cardiovascular disease, characterized by the formula ##STR1## wherein R.sup.1 is ethyl, n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexylmethyl, and R.sup.2 is methyl, ethyl, n-propyl, isopropyl, cyclopropyl, n-butyl, isobutyl, tert. butyl, or cyclobutyl provided that R.sup.1 is ethyl when R.sup.2 is methyl, or a physiologically acceptable salt thereof. The invention also refers to processes for the preparation of these compounds, a pharmaceutical preparation containing one of the compounds and a method for the treatment of chronic obstructive airway disease and cardiovascular disease.

Abstract: Alkyl-substituted xanthines having a prevailingly peripheral theophylline-assimilated activity, process for their preparation, pharmaceutical compositions containing said xanthines and their therapeutic use.

Abstract: A pharmaceutical composition containing as an essential ingredient a compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is an .omega.- or (.omega.-1)-hydroxyalkyl group having from 5 to 8 carbon atoms in which the hydroxy group is separated from the xanthine nucleus by at least 2 carbon atoms, radicals R.sub.1 and R.sub.3 which are no hydroxyalkyl group, are hydrogen or methyl and equal or different, and R.sub.2 is said hydroxyalkyl group or methyl, a compound of formula (I) and a pharmaceutical product for treatment of diseases involving insufficiency of cerebral blood flow.

Abstract: A complex of 3-methoxy-N-methylmorphinan with 7-theophyllineacetic acid (1:2) is prepared by reacting the reactive materials in a polar solvent. The complex has antitussive activity.

Abstract: There are disclosed theobromine derivatives wherein theobromine is substituted at the 1 position with substituted piperazino, homopiperazino and piperidino groups, and pharmacologically acceptable acid addition salts thereof. The compounds exhibit vasodilating and psychotropic and analgesic activities.

Abstract: The invention relates to xanthines corresponding to the formula ##STR1## and physiologically acceptable salts thereof, in which R.sub.1 represents C.sub.2 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -isoalkyl, CH.sub.2 -(C.sub.2 -C.sub.3 -alkenyl) or CH.sub.2 -(C.sub.3 -isoalkenyl);R.sub.3 represents C.sub.3 -C.sub.5 -alkyl, C.sub.3 -C.sub.5 -isoalkyl, CH.sub.2 -(C.sub.2 -C.sub.4 -alkenyl) or CH.sub.2 -(C.sub.3 -C.sub.4 -isoalkenyl);R.sub.8 represents H, methyl or ethyl;with the proviso that(1) when R.sub.8 represents H, R.sub.1 is allyl and(2) R.sub.1 and R.sub.3 cannot both represent butyl or allyl at the same time.The compounds show non-specific or anxiolytic sedative activity.

Abstract: Intermediates in the preparation of 9-position derivatives of theophylline useful in synthesizing theophylline immunogens and labeled conjugates. The labeled conjugates and the antibodies produced against the immunogens are particularly useful in homogeneous nonradioisotopic immunoassay for measuring theophylline in biological fluids such as serum.

Abstract: Compounds of the formula (II): ##STR1## wherein: X is sulphur and Y is oxygen or sulphur;R.sub.1 is an alkyl group of up to 6 carbon atoms;R.sub.2 is an alkyl group of up to 6 carbon atoms; andn is 1; orX is oxygen and Y is sulphur; one of R.sub.1 and R.sub.2 is an alkyl group of up to 6 carbon atoms and the other is an alkyl group of 2 to 6 carbon atoms; andn is 1 or 2, having useful pharmacological activity, pro-drugs therefor, a process for their preparation, pharmaceutical compositions containing said compounds or pro-drugs, and intermediates in their preparation of the compounds.

Abstract: Substituted 8-phenylxanthines and their use as bronchodilators is described. Methods for their preparation and use as well as pharmaceutical compositions containing them are also described.

Abstract: Ketals of 1-(1,3-dialkylxanthin-7-yl)propan-2-ones are of use in the treatment of vascular disorders. A representative embodiment is 2-methyl-2-(1,3-dibutylxanthin-7-ylmethyl)-1,3-dioxalane.

Abstract: A novel compound has the following formula: ##STR1## in which R.sub.1 and R.sub.2 are methyl or a group having the formula: ##STR2## provided that one of R.sub.1 and R.sub.2 is methyl and the other is said group, wherein R stands for a hydrogen atom or a lower alkyl group, Z stands for a group ##STR3## in which X.sub.1 and X.sub.2, which may be the same or different, stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, or a pyridyl group or a group ##STR4## in which Y.sub.1 and Y.sub.2, which may be the same or different stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, X stands for a nitrogen or carbon atom, and n is an integer of from 2 to 10, provided that when R.sub.2 is the group having the formula II, X is not carbon and Z is not pyridyl.

Abstract: Pure hydroxypropyltheophylline is produced by the catalytic reaction of theophylline with glycidol in the presence of a hydroxide of a short chain alcoholate of an alkali metal or an alkali metal salt of a pseudohydrohalic acid which has a readily polarizable anion. The catalyst is suitably employed in an amount between 0.01 and 0.2 moles per mole of theophylline. The dihydroxypropyltheophylline is obtained directly in the reaction in a high purity.

Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.

Abstract: Compounds of the following general formula ##STR1## wherein: X and Y are different from each other and represent --CH.sub.2 -- or an oxygen atom; R represents a radical selected from hydroxy, bromo, acetoxy, pyrrolidino, morpholino, piperazino and piperazino substituted at the position 4 by a carbethoxy, benzyl, phenyl, halophenyl, methoxyphenyl or trifluoromethylphenyl group, or when X is --CH.sub.2 -- and Y is an oxygen atom, R may represent also chloro; methods for their preparation; pharmaceutical compositions containing them. The compounds possess a remarkable antitussive activity.

Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.

Abstract: A new compound 3(4-phenyl-1-piperazinio-1-yl)-1,2-propanediol 3(theophyllin-7-yl)-1-propanesulphonate, possesses antitussive action and is therefore usable in therapy. The compound is obtained by treating 3(theophyllin-7-yl)-1-propanesulphonic acid with 3(4-phenylpiperazin-1-yl)-1,2-propanediol in a suitable solvent.

Abstract: There is disclosed zinc complexes of amine salts of theophylline. The preferred compound disclosed is the zinc complex of aminophylline. These compounds are useful as bronchodilators and have antibronchospasmotic activity. They are substantially insoluble and do not impart an unpleasant taste to oral formulations. In addition, they are storage stable. The compounds are prepared by reacting a water soluble simple zinc salt with the amine salt of theophylline at temperatures of from 60.degree.-90.degree. C. for about 8 to 16 hours.

Abstract: The substituted theophyllines of the formula: ##STR1## (wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or phenylalkyl of 7 to 10 carbon atoms, each of which may be unsubstituted or substituted by one or more hydroxy groups, alkoxy or alkylthio groups of 1 to 4 carbon atoms, halogen atoms, cyano groups, nitro groups, carboxy groups, alkoxycarbonyl groups of 2 to 5 carbon atoms, amino groups, alkylamino groups of 1 to 4 carbon atoms or dialkylamino groups of 2 to 8 carbon atoms, or when the group is phenyl or phenylalkyl, by one or more alkyl groups of 1 to 4 carbon atoms;or R.sup.2 and R.sup.3 together represent a hydrocarbon chain of 3 to 6 carbon atoms optionally interrupted by a heteroatom;and n represents an integer of from 1 to 6)and the acid additional salts thereof, are novel compounds which are useful in the treatment of cardiac disorders.

Abstract: The invention relates to 1-isopropyl- and 1-isobutyl-3,7-dimethyl xanthines as medicaments. They have a sedative effect comparable with that of a standard neuroleptic.

Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## Wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.

Abstract: The present invention provides xanthine derivatives of the general formula: ##STR1## wherein one of the symbols R.sub.1 and R.sub.2 stands for a methyl radical and the other for a radical of the general formula: ##STR2## wherein R.sub.3 is a hydrogen atom or an acyl radical; and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them and is also concerned with the use thereof for the preparation of pharmaceutical compositions for the treatment of allergies.

Abstract: Compounds of the formula: ##STR1## useful in treating dermal inflammation in warm-blooded animals are provided.

Abstract: There is described a process for the production of theophylline derivatives of the formula ##STR1## where T is the theophyllinyl-(7)-residue, Alk is a straight or branched alkylene chain having 2 to 4 carbon atoms, R is hydrogen or a methyl group, n is 1 or 2 with the proviso that two hydroxy groups of the phenyl ring cannot be in the 3,4-positions by reacting an aminoalkyltheophylline of the formula ##STR2## with a bromoketone of the formula ##STR3## where R' is a lower alkyl group and the two --OCOR' groups of the phenyl ring cannot be in the 3,4 positions to an intermediate compound of the formula ##STR4## and subsequently hydrolytically splitting off the R'CO protective group wherein the bromoketone of formula III is produced free of dibromide by bromination of a ketone of the formula ##STR5## followed by treatment with a lower trialkyl phosphite.

Abstract: 7-(Oxoalkyl)-1,3-dialkyl xanthines whose substituents in the 1- and 3-positions are alkyl groups of 2 to 6 carbons, cyclohexyl, alkoxyalkyl or hydroxyalkyl, such as 7-(3-oxobutyl)-1,3-di-n-butylxanthine, are effective vasodilators, having a marked activity in promoting blood flow through skeletal muscle, while at the same time exhibiting low toxicity.

Abstract: Compounds of the formula ##STR1## or physiologically acceptable salts thereof in which formula R.sup.1 is methyl, ethyl or n-propyl, R.sup.2 is methyl or n-propyl and R.sup.3 is ##STR2## methods for the preparation thereof; intermediates useful for their preparation; pharmaceutical preparations containing at least one of these compounds; and the use thereof in the treatment of allergy and bronchial asthma.

Abstract: N-{3- and 4-[R.sub.1 -(phenyl)-C(.dbd.X)]-phenyl-lower-alkyl}amines, useful as anti-inflammatory agents, are prepared either by reduction of 3- or 4-[R.sub.1 -(phenyl)-CO]-phenyl-lower-alkanoylamines, which are also useful as anti-inflammatory agents; by benzoylating a phenyl-lower-alkylamine; by reaction of a 3- or 4-lithiophenyl-lower-alkylamine with a R.sub.1 -(phenyl)-carboxaldehyde, a R.sub.1 -(phenyl)-lower-alkyl ketone or a R.sub.1 -(phenyl)-carbonitrile or by transformations involving manipulations of a carbonyl or carbinol group.

Abstract: A pharmaceutical composition having as an essential ingredient a compound of the formula ##STR1## wherein one to three of R.sup.1, R.sup.2 and R.sup.3 represent an alkenyl group having from 4 to 8 carbon atoms, the other ones are alkyl having from 1 to 12 carbon atoms, and R.sup.1 may also be hydrogen, the compounds themselves and a process for preparing them.

Abstract: The present invention related to a new compound useful for pharmaceutical purposes, namely, theophylline magnesium salicylate.

Abstract: A method is described for preparing an .alpha.-substituted-.alpha.-acylacetamide wherein an .alpha.-acyl-.alpha.-halo-acetamide is allowed to react with an organic compound with pKa between 7 and 12 in a medium of an aprotic solvent and in the presence of a tetraalkylguanidine as basic condensing agent.

Abstract: Novel compounds of the general formula ##STR1## (m = 0 or 1; n = 2 or 3 and R = H or CH.sub.3) are produced by reacting a 2-aminoalkyl alkylene urea with an allyl ester of a carbonylic acid. Among the particular allyl esters disclosed as reactants are diallyl carbonate, allyl and methallyl chloroformate, diallyl and dimethallyl oxalate. The recovered allyl esters of the alkyleneureido amic acid compounds find particular use as functional comonomers for imparting wet adhesion properties to emulsion systems containing vinyl ester polymers used in paints and coating compositions.

Abstract: Compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is a hydroxyalkyl group containing from 4 to 8 carbon atoms, one of the other two, which may be the same or different, is an alkyl group containing from 2 to 12 carbon atoms and the third one is an alkyl group containing from 1 to 12 carbon atoms or a hydrogen atom, R.sub.2 however being an alkyl or hydroxyalkyl group, at least one of the groups R.sub.1, R.sub.2 and R.sub.3 containing at least 5 carbon atoms, a process for their preparation and a pharmaceutical composition containing said compounds.