Abstract: Novel xanthine compounds represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof have a diuretic action, a renal-protecting action and a vasodilative action.The compounds are useful as a diuretic, a renal-protecting agent and an antihypertensive agent.

Abstract: Xanthine derivative which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectively and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: This invention relates to oxetanocin-related compounds represented by the following formula (I): ##STR1## [in formula (I), R.sub.1, Y and B have the following meanings: (a) R.sub.1 represents --CH.sub.2 OH or --CH.sub.2 OCO-(alkyl),(b) Y represents ##STR2## provided that R.sub.2 is --H, --OH or --CH.sub.2 OH and R.sub.3 is --H, --OH, halogen atom, --CH.sub.2 OH, lower alkyl group, --CH.sub.2 -N.sub.3, --CH.sub.2 -F, --N.sub.3, --COOH, --NH.sub.2, --CH.sub.2 OSO.sub.3 H or --CH.sub.2 OCO-(lower alkyl), and(c) B represents a residue of purine base,(d) provided that R.sub.1 and R.sub.3 cannot simultaneously represents --CH.sub.2 OH]and their salts which have activities such as an antiviral activity and the like and are expectedly useful as a pharmaceutical and the like.

Abstract: 1,3-Alkyl substituted-8-phenylxanthines in which the straight chain alkyl substituents are different and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds have 1-n-propyl-3-methyl and 1-methyl-3-n-propyl substituents. The compounds are potent bronchodilators.

Abstract: Cyclopentyl purine derivatives, novel intermediate thereof and processes for their preparation are disclosed.

Abstract: A 6-thioxanthine of formula I or a pharmaceutically acceptable salt thereof ##STR1## wherein R.sub.3 is a C.sub.2 to C.sub.6 alkyl group, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group and R.sub.8 is a C.sub.1 to C.sub.6 alkyl group, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group provided that when R.sub.3 is an ethyl, n-propyl or n-butyl group, R.sub.8 is a C.sub.3 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group.These 3,8-disubstituted-6-thioxanthines have enhanced bronchodilator activity.

Abstract: Novel process for preparing cyclopentyl purine derivatives is disclosed.

Abstract: An antiviral compound of the formula: ##STR1## wherein A is selected from a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group and a heterocyclic isostere of a pyrimidin-1-yl group; andG and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl and substituted derivatives thereof, --OH, --C(O)H, --CO.sub.2 R.sub.1 l wherein R.sub.1 is hydrogen or C.sub.1 to C.sub.10 alkyl and --OCH.sub.2 PO.sub.3 H.sub.2, with the proviso that one of D or G is other than hydrogen or C.sub.1 to C.sub.10 alkyl; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to certain novel 8-phenylxanthines substituted in the 3 or 4 position of the phenyl group by an alkenylene, alkenyleneoxy, alkynylene or alkynyleneoxy bearing a terminal acidic grouping, and to their use in human and veterinary therapy, particularly for conditions associated with the cell surface effects of adenosine.

Abstract: A compound of the formula: ##STR1## wherein R is a hydroxyl group which may be protected and Y is a purine base which may be protected, and the saltts thereof, which are useful as an antiviral agent.

Abstract: The present invention relates to new compounds of Formula I ##STR1## and physiologically acceptable salts thereof wherein A and B stand for oxygen or --CH.sub.2 group with the proviso that if A stands for oxygen, then B stands for --CH.sub.2 group and R stands for hydrogen and, if A represents a --CH.sub.2 group, then B stands for oxygen, R stands for a --CH.sub.2 Q group wherein Q stands for hydrogen, and pyrrolidino, piperidino or morpholino and a process for the preparation thereof and pharmaceutical compositions containing as active ingredient a compound of the Formula (I) or a physiologically acceptable salt thereof.

Abstract: Antiviral and antitumor compounds are disclosed of general formula: ##STR1## wherein Z is H, OR' or NH.sub.2, wherein R' is H, (C.sub.1 -C.sub.4)-alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH).sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R.sub.2), SR, OR' or halogen, wherein R is H, lower-(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable salts thereof.

Abstract: A hydrophilic theophylline powder formulation consisting of(a) from 5 to 15% by weight of theophylline,(b) from 15 to 30% by weight of lechithin,(c) from 45 to 80% by weight of sugar,(d) from 0 to 5% by weight of a flow agent and(e) from 0 to 30% by weight of further additives, and a process for its preparation.

Abstract: A 6-thioxanthine of general formula I or a pharmaceutically acceptable salt thereof ##STR1## wherein R.sub.3 is a C.sub.2 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group and R.sub.8 is a C.sub.1 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group provided that when R.sub.3 is an ethyl, n-propyl or n-butyl group, R.sub.8 is a C.sub.3 to C.sub.6 alkyl, a C.sub.3 to C.sub.7 cycloalkyl group or a C.sub.4 to C.sub.8 cycloalkylalkyl group.These 3,8-disubstituted-6-thioxanthines have enhanced bronchodilator activity.

Abstract: Antiviral and antitumor compounds are disclosed of general formula: ##STR1## wherein Z is H, OH or NH.sub.2, Y is CH or N, the bond indicated by C.sub.1 '--C.sub.2 ' is absent or, in combination with the C.sub.1 '--C.sub.2 ' bond is the unit CH.dbd.CH, and X is selected from the group consisting of H, N(R.sub.2), SR, OR or halogen, wherein R is H, lower (C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically acceptable salts thereof.

Abstract: A process for the preparation of 7-(2-diethylaminoethyl)-theophylline acetylsalicylate and use of the product obtained. The process comprises prior filtering of a solution of the reactants through a layer of diatomaceous earth and activated carbon, cooling and treatment with a source of high frequency ultrasounds. The product is used in the manufacture of anti-agglutination and anti-thrombotic agents.The process provides products having a high level of purity.

Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.

Abstract: The present invention relates to certain novel 8-phenylxanthines substituted in the 3 or 4 position of the phenyl group by an alkenylene, alkenyleneoxy, alkynylene or alkynyleneoxy bearing a terminal acidic grouping, and to their use in human and veterinary therapy, particularly for conditions associated with the cell surface effects of adenosine.

Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.

Abstract: New derivatives of theophylline are described, which have the general formula: ##STR1## in which R is selected from the group consisting of 2'-(1'-oxy-1', 3'-dithiolanyl), 2'-(1', 3'-dithiolanyl) and 2'-(1',3'-dithianyl), possibly substituted in position 4'. The derivatives have high antibronchospastic, antitussive and mucolytic activities.

Abstract: A novel competitive assay for theophylline wherein caffeine-like (7-substituted) labeled conjugates are used to detect the presence and/or amount of theophylline present in a test sample. The use of such conjugates in a competitive assay for theophylline results in improved sensitivity of the assay method. Where the assay method is a nephelometric or turbidimetric inhibition immunoassay procedure, the assay was found to be less temperature dependent than prior art immunoassays.

Abstract: Tertiary hydroxyalkylxanthines having the general formula (I), characterized by the fact that at least one of the residues R.sup.1 and R.sup.3 represents a tertiary hydroxyalkyl group of formula (Ia) in which R.sup.4 represents an alkyl group having up to 3 carbon atoms and n a whole number from 2 to 5; the other residue which may remain R.sup.1 or R.sup.3 is a hydrogen atom or an aliphatic hydrocarbon residue R.sup.5 having up to 6 carbon atoms, in which the carbon chain may be separated by a maximum of two oxygen atoms or be substituted by an oxo group or two hydroxy groups at the most, and R.sup.2 represents an alkyl group with 1 to 4 carbon atoms. Also described is a process for manufacturing these compounds, which are suitable for the manufacture of medicines, in particular for use in the prevention and/or treatment of peripheral and/or cerebral irrigation disorders.

Abstract: The invention relates to a process for the preparation of a new crystalline monohydrate of 1-(3', 4'-diethoxy-benzyl-6, 7-diethoxy-3,4-dihydro-isoquinolinium-theophylline-7-acetate and if desired of pure 1-(3', 4'-diethoxy-benzyl)-6,7-diethoxy-3, 4-dihydro-isoquinolinium-theophylline-7-acetate free of contaminating oxidation products which comprises reacting 1-(3',4'-diethoxy-benzyl)-6,7-diethoxy-3,4-dihydro-isoquinolinium with theophylline-7-acetate acid in the presence of water and one or more organic solvent(s) and if desired dehydrating the 1-(3',4'-diethoxy-benzyl) 6,7-diethoxy-3,4-dihydro-isoquinolinium-theophyl line-7-acetate-monohydrate thus obtained.

Abstract: Compounds of the formula ##STR1## wherein R.sup.3 is ethyl, n-propyl or n-butyl, andR.sup.8 is hydrogen, methyl or ethyl,exhibit bronchodilating activity with reduced side effects and increased half-like. A method of achieving bronchodilation with reduced undesired effects (diuresis, CNS activity), by administering the said compounds to a patient, is also provided.

Abstract: New compounds of formulas I and II ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamino, n-lower alkylamino and ##STR2## wherein Ar is optionally substituted phenyl; Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or nothing;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB;R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy;R.sub.4 is lower alkyl; andR.sub.5 is hydrogen or lower alkyl,are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold. They are also vasodilators.

Abstract: 1,3-alkylsubstituted-8-(3,4-,3- or 4-substituted phenyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. The 3-substituents are hydrogen, dimethylaminomethyl, or 2,3-dihydroxypropyloxy. The 4-substituents are selected from hydroxy, cyano, --NHCON(R.sub.5).sub.2, --C(.dbd.NH)N(R.sub.5).sub.2, --NH--C(.dbd.NH)N(R.sub.5).sub.2, with each R.sub.5 independently being hydrogen or an alkyl group of one to three carbons and provided that when the 3-substituent is hydrogen the 4-substituent is not hydroxy or hydrogen.The compounds are potent adenosine receptor antagonists having relatively low lipophilicity. The compounds are intended for use as bronchodilators and cardiotonics.

Abstract: A method for the preparation of enprofylline is disclosed, which method comprises(a) treating 6-amino-1-n-propyl-2,4-(1H,3H)-pyrimidinedione in formic acid with sodium nitrite in the presence of a catalyst to the formation of 6-amino-5-formamido-1-n-propyl-2,4-(1H,3H)-pyrimidinedione and(b) performing a ring-closure reaction on the formed 6-amino-5-formamido-1-n-propyl-2,4-(1H,3H)-pyrimidinedione to the formation of 3,7-dihydro-3-n-propyl-1H-purin-2,6-dione.

Abstract: New 8-substituted nucleoside and purine derivatives of the general formula: ##STR1## wherein R represents an amino group or an hydroxy group possibly in the corresponding keto tautomeric form, R.sub.1 is hydrogen or an amino group, R.sub.2 is hydrogen or a .beta.-D-ribofuranosyl radical wherein the primary hydroxy group and/or the two secondary hydroxy groups may be derivatized, R.sub.3 is an optionally substituted aryl or monocyclic heteroaryl radical and, X is --O-- or --S--. The new compounds have antihyperlipaemic activity.

Abstract: The present invention is various novel diallyl analogs of xanthine. Additionally, the invention is pharmaceutical compositions having as the active compound diallyl analogs of xanthines and methods of use therefor. Processes of preparation of diallyl analogs of xanthine are also the invention. The use of the analogs relates particularly to a desirable affinity at adenosine receptors, particularly the A.sub.1 receptor. The analogs are adenosine receptor antagonists. The analogs, thus, for example provide activity for use as a CNS stimultant cognition activator, antifibrillatory agent, and bronchodilator.

Abstract: Novel 8-phenylxanthines which are potent adenosine receptor antagonists.

Abstract: The present invention is a novel disubstituted derivative of xanthine, pharmaceutical composition and method of use therefor. Activity of the novel xanthine includes particularly cognition activation.

Abstract: Salts of basic caffeine-8-ethers having the following general formula are disclosed: ##STR1## where X=2 or 3 and R is an alkyl group having from 1 to 3 carbon atoms, whereby the chain may be branched, in the form of fumarates. The components have pharmaceutical properties including effectiveness as anti-psoriatics.

Abstract: Compounds of general formula (I) ##STR1## wherein: m is zero or 1;n is zero, 1, 2, 3 or 4;A is a 3,7-dimethylxanthine-1-yl or 1,3-dimethylxanthine-7-yl residue;show marked anti-platelet activity.

Abstract: There are disclosed carbocyclic analogs of 2-amino-6-substituted-purine ribofuranosides and 2-amino-6-substituted-8-azapurine ribofuranosides. These compounds are useful in the treatment of viral infections.

Abstract: The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.

Abstract: Histamine H.sub.1 -receptor antagonists of the formula: ##STR1## where R.sup.1 is hydrogen or alkyl; one of R.sub.2 and R.sup.3 is alkyl and the other is ##STR2## where R.sup.4 is pyridin-2-yl, pyridin-4-yl, thienyl, or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, nitro, trifluoromethyl, hydroxy or alkoxy of 1 to 6 carbon atoms substituent; and R.sup.5 is pyridin-2-yl, pyridin-4-yl or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, nitro or trifluoromethyl substituent.

Abstract: Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.

Abstract: N-Theophyllin-7-ylalkylene-N.sup.1 -(bis-p-fluorophenyl)methyl-piperazine derivatives as histamine H.sub.1 -antagonists.

Abstract: Compounds of the formula ##STR1## wherein R.sup.3 is ethyl, n-propyl or n-butyl, andR.sup.8 is hydrogen, methyl or ethyl,exhibit bronchodilating activity with reduced side effects and increased half-life. A method of achieving bronchodilation with reduced undesired effects (diuresis, CNS activity), by administering the said compounds to a patient, is also provided.

Abstract: New derivatives of theophylline having the formula ##STR1## wherein R is hydrogen or a hydroxy group, and n is an integer of 0.ltoreq.n.ltoreq.3 and/or the pharmaceutically acceptable, acid addition salts thereof, exhibit in addition to other properties, histamine-serotinine- bradykynine- antagonistic, anti-anaphylactic and .beta.-adrenergic stimulating effects.

Abstract: A novel theophylline-7- acetic acid ester is described. Said ester is obtained by reacting, at a temperature from 1.degree. to 20.degree. C., theophylline-7-acetic acid chloride with d,l-trans-sobrerol.There are further described pharmaceutical compositions with mucosecretolytic-fluidizing and antibronchospastic activity containing the novel ester.

Abstract: Compounds having activity against chronic obstructive airway disease or cardiac disease, characterized by the formula ##STR1## wherein R.sup.1 is n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexylmethyl, and R.sup.2 is hydrogen or methyl, provided that R.sup.2 is methyl when R.sup.1 is n-propyl, n-butyl or isobutyl, or a physiologically acceptable salt thereof.

Abstract: 1.4;3.6-Dianhydrohexitol nitrates substituted by purine bases, namely, adenyl-desoxy-1.4;3.6-dianhydrohexitol nitrates of the general formula Ia as well as theophyllinyl-desoxy-1.4;3.6-dianhydrohexitol nitrates of the general formula Ib, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and, independently of one another signify(a) a hydrogen atom,(b) a straight-chained or branched alkyl group with 1 to 7 C-atoms,(c) an .omega.-phenylalkyl group, whereby the alkyl group has 1 to 7 C-atoms and whereby the phenyl ring can be halogen-substituted in the p-position, or wherein(d) R.sup.1 signifies one of the residues given under (a) to (c) and R.sup.2 an acyl radical or an aliphatic, possibly methyl-substituted monocarboxylic acid with 2 to 7 C-atoms, or wherein(e) R.sup.1 and R.sup.

Abstract: New ester derivatives of 7-(.omega.-oxyalkyl theophylline with the general formula ##STR1## where X is an aroylpyrrole group, a pyrrylphenyl group, or an aroylpyrrol acetamide group and Y is hydrogen, methyl or a theophylline radical, show anti-platelet aggregation, antinflammatory and broncholytic activity, accompanied by low toxicity.

Abstract: Compounds of the formula ##STR1## wherein one of the radicals R.sup.1, R.sup.2 or R.sup.3 denotes a straight-chain alkyl group having 4 to 8 C atoms and two vicinal hydroxyl groups in the .omega.,.omega.-1 or .omega.-1,.omega.-2 positions and the two other radicals represent straight-chain or branched alkyl groups having up to 12 C atoms in the position of R.sup.1 and R.sup.3 and up to 4 C atoms in the position of R.sup.2, the total of C atoms in these two alkyl substituents being a maximum of 14, are prepared by oxidation of the corresponding alkenylxanthines and by alkylation with compounds which introduce the dihydroxyalkyl radical or a precursor thereof. The dihydroxyalkyldialkylxanthines are suitable for the treatment of obstructive respiratory tract diseases.

Abstract: New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

Abstract: Derivatives of theophylline substituted at the 7 position with various substituents containing a homopiperazine nucleus. The compounds can be prepared reacting theophylline or reactive intermediate containing same with a homopiperazine compound. The compounds exhibit antihistaminic activity and vasodilating activity.

Abstract: Novel 8-phenylxanthines which are potent adenosine receptor antagonists.

Abstract: The new compound 3-(1,2,3,6-tetrahydro-1,3-dimethyl-2,6-Dioxopurine-7-acetyl-8-(2-phenyleth yl)-1-oxa-3,8-diazaspiro-(4,5)decan-2-one and the process of preparation are described.

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.