Abstract: 6-Substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

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

Abstract: 2-Amino-pyrimidininone derivatives possessing antihistaminic and serotonin-antagonistic properties. Compositions containing these compounds as the active ingredient and a method of treating subjects from allergic diseases.

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

Abstract: The present invention provides a novel process for producing oxetanocin G by hydrolysis of alkoxylated 2-amino-oxetanocin A thereby to convert ##STR1## at the 6-position thereof into >C.dbd.O. Oxetanocin G is expectedly useful as an antiviral agent.

Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

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: Antihypertensive phosphodiesterase inhibitors having an optionally substituted purine derivative portion and a benzo- or cyclopenta-furan derivative portion are disclosed.

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: 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: Novel 1-alkyl substituted benzimidazole derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

Abstract: Compounds which are active against retroviruses have the following formulaHOH.sub.2 C--CH.dbd.C.dbd.CH--Bwherein B is a purine or pyrimidine heterocyclic ring which is preferably selected from the group consisting of cytosine, 5-halo substituted cytosine, 5-alkyl substituted cytosine, 6-aminopurine, 2,6-diaminopurine, 6-hydroxypurine, 2-amino-6-hydroxypurine, 3-deazapurines, 7-deazapurines, 8-azapurines, and 6-azapyrimidines.

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: Novel purine derivatives are described as agents for treating autoimmune diseases as well as a method of manufacture and pharmaceutical compositions as well as novel intermediates in the manufacture thereof.

Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## its pharmaceutically acceptable salts thereof wherein R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## and R.sub.1 is either a purine, pyrimidine or an analog thereof.

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: Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.

Abstract: This invention relates to purinone derivatives which have bronchodilator, vasodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)-6-purinone.

Abstract: 6-Substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

Abstract: A compound of the formula ##STR1## wherein X has the formula ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl; wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent; wherein R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R.sup.

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: Disclosed are compounds having the formula ##STR1## wherein Prot is a hydroxyl protecting group. The compounds are useful as intermediates in the preparation of compounds of the formula ##STR2## which in turn are useful as antiviral agents.

Abstract: Hypoxanthine administered intradermally at a dosage range of 2.times.10.sup.-8 to 1.times.10.sup.-5 grams to a mammalian subject for the purpose of treating rheumatoid arthritis and osteoarthritis.

Abstract: The compounds of formula I, ##STR1## in free form or in salt form have cardiotonic and antiarrhythmic activity. They may be used as medicaments. They are obtained by means of appropriate 3-amino-2-hydroxy-propylation of purines.

Abstract: The present invention relates to a novel compound having hypoxanthine base represented by the following formula: ##STR1## as well as to use of said compound and process for producing said compound.The novel compound of the present invention has an immunosuppressive and antiviral actions and is expected to be useful as a medical drug.

Abstract: Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II)wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle;R' is a lower alkyl group, a halogen atom or an aminoalkyl group; andn is 0 or an integer of from 1 to 4;and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".

Abstract: Novel purine derivatives are described as agents for treating autoimmune diseases as well as a method of manufacture and pharmaceutical compositions as well as novel intermediates in the manufacture thereof.

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 comprises novel adamantyl purine derivatives, in which the purine ring is substituted at the 6-position with a moiety incorporating an adamantane ring system. The purine may also be substituted at the 9-position with a carbohydrate, to give a nucleoside analog, or may be unsubstituted at that position.The substituent at the 6-position contains an adamantane ring system, either substituted or unsubstituted, in which a linker connects a carbon atom in the adamantane ring system with the 6-carbon of the purine ring. This linker consists of a combination of a heteroatom such as N, O or S, which is directly connected to the purine, and a short (five or less) atom chain, consisting either of carbon or other atoms such as N, O or S, with or without additional pendant moieties, which is connected either to the secondary or tertiary carbon of the adamantane ring system. The adamantane ring system itself may be unsubstituted, or substituted with a wide variety of non-ionic groups.

Abstract: This invention relates to a novel 1,4-dihydropyridine derivative of the formula ##STR1## wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.

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: 6-purinyl N-(2-chloroethyl) carbamate and thiocarbamate are disclosed of the general formula I, ##STR1## in which X stands for an oxygen or sulfur atom, and also a process for their preparation by reacting a purine derivative of the general formula II (hypoxanthine or 6-mercaptopurine, respectively) with 2-chloroethylisocyanate. The subject compounds of formula I show a remarkable antineoplastic effect in vitro and in vivo, and consequently have great potential for the treatment of malignant neoplastic diseases in mammals.

Abstract: Compounds of the general formula: ##STR1## wherein Ar is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and Het is a heterocyclic group which may optionally be substituted or fused to a phenyl, substituted phenyl or further heterocyclic ring; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.

Abstract: Griseolic acid derivatives of formula (I): ##STR1## wherein A represents: ##STR2## have enzyme-inhibitory activity, especially against cAMP PDE and cGMP PDE. When formulated as compositions with appropriate carriers or diluents, they may be used for the treatment of a variety of organic disorders and show toxicities less than griseolic acid itself.

Abstract: Novel 4-substituted-5-hydroxymethyl-1,2-cyclopentanediols or 1-cyclopentanol substituted at the 3-position by various heterocyclic groups are useful as antiviral agents.

Abstract: There are prepared compounds of the formulae ##STR1## where R is lower alkyl, chlorine, or bromine and n is an integer from 1 to 5. The compounds of formula (1) can be used to make erythro-9-(2-hydroxy-3-nonyl) hypoxanthine and its homologues and also to make the compounds of formulae (2) and (3). All three classes of compounds are useful as immunomodulators.

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: A purified isolate of an actinomycete identified as ATCC 39364 is capable of producing the antimicrobial/antitumor compound 2-amino-1,9-dihydro-6H-purine-6-one-7-oxide, commonly known as guanine-N.sup.7 -oxide.Guanine-N.sup.7 -oxide is produced by cultivating isolate ATCC 39364 under aerobic conditions in a culture medium containing assimilable sources of carbon and nitrogen until a substantial amount of the compound is produced and thereafter isolating the compound.The antibiotic/antitumor compound guanine-N.sup.7 -oxide and pharmaceutical compositions comprising this compound or one of its pharmaceutically acceptable salts together with a pharmaceutically acceptable carrier are also disclosed as is a method of treating microbial infections in a mammal or of treating tumors in a mammal.

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

Abstract: Aminodesoxy-1.4;3.6-dianhydrohexitol derivatives of the general formula I, ##STR1## wherein R.sup.1 and R.sup.2 in each case independently of one another, signifies a hydrogen atom or a lower alkyl group with 1 to 4 C-atoms or wherein R.sup.1 signifies a hydrogen atom and R.sup.2 an adamant(1)yl radical or wherein R.sup.1 , and R.sup.2, together with the nitrogen atom to which they are attached, (a) signify the residue of a cyclic, non-aromatic secondary amine possibly containing a further hetero atom or (b) the aden(9)yl radical possibly mono- or disubstituted on the 6-amino group or (c) the 6-alkylmercaptopurin(9)yl radical or (d) the theophyllin-(7)yl radical or (e) the 6-chloropurin-9-yl radical or wherein R.sup.1 signifies a hydrogen atom or a lower alkyl group with 1 to 4 C-atoms and R.sup.2 an .omega.-theophyllin(7)ylalkyl radical or an .omega.-theobromin-1-ylalkyl radical or an .omega.

Abstract: .alpha.-Mercaptobenzylacetic acid derivatives of imidazole-containing compounds and analogues thereof, and their use as immunomodulating agents are disclosed.

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: Diclycidyl substituted heterocyclic compounds of the formula: ##STR1## wherein X and Y can be the same or different and are either nitrogen or the radical C-R, where R is a hydrogen, or a hydrocarbon group, e.g., a straight or branched chain saturated or unsaturated hydrocarbon group, a substituted or unsubstituted cycloaliphatic group, an aromatic hydrocarbon-substituted alkyl group, a cycloaliphatic hydrocarbon-substituted alkyl group, an aromatic hydrocarbon group, a heterocyclic group, or a hetero-cyclic-substituted alkyl group, and where the glycidyl group in the five-membered ring is attached to a ring nitrogen atom; processes for their preparation; and compositions and methods for their use as cytostatic agents.

Abstract: There are prepared compounds of the formula ##STR1## where R.sup.1 is alkyl of 1 to 8 carbon atoms and R.sup.2 is the ester group of an unsubstituted monocarboxylic acid, aromatic carboxylic acid, aminocarboxylic acid, unsubstituted dicarboxylic acid, phosphoric acid, or nitric acid or a glycoside or an acetaldehyde acetal. The compounds are immunomodulators, have antiviral activity and antitumor activity and also are enzyme inhibitors. The compounds can also be used to introduce the corresponding alcohol into biological systems, in some cases with enhanced potency.

Abstract: The preparation of 9-[.alpha.-(2.alpha.,3.beta.-dihydroxy-4.alpha.-(hydroxymethyl) cyclopentyl)]-6-substituted purines: ##STR1## and their derivatives wherein R is amino, mercapto, methylmercapto, hydroxy, halogen, or substituted amino: ##STR2## wherein R' and R" may be the same or different and are hydrogen, methyl, ethyl, propyl or phenyl. The compounds exhibit anti-viral and antitumor activity and are resistant to adenosine deaminase. Acid salts and esters of the purine nucleosides have also been prepared.

Abstract: 9-Hydroxyethoxymethyl (and related) derivatives of certain 6-, and 2,6-substituted purines have been discovered to have potent anti-viral activities. Novel compounds and their pharmaceutically acceptable salts, pharmaceutical formulations containing the compounds of this invention, and the treatment of viral infections with these formulations are all disclosed. 9-(2-hydroxyethoxymethyl) guanine and 2-amino-9-(2-hydroxyethoxymethyl)adenine are examples of especially active compounds of this invention.

Abstract: There are prepared compounds of the formula ##STR1## where R.sup.1 is alkyl of 1 to 8 carbon atoms and R.sup.2 is the ester group of an unsubstituted monocarboxylic acid, aromatic carboxylic acid, aminocarboxylic acid, unsubstituted dicarboxylic acid, phosphoric acid, or nitric acid or a glycoside or an acetaldehyde acetal. The compounds are immunomodulators, have antiviral activity and antitumor activity and also are enzyme inhibitors. The compounds can also be used to introduce the corresponding alcohol into biological systems, in some cases with enhanced potency.

Abstract: The preparation of (.+-.)-9-[.alpha.-(2.alpha.,3.beta.-dihydroxy-4.alpha.-(hydroxymethyl)cycl opentyl)]-6-substituted purines: ##STR1## and (.+-.)-3-[.alpha.-(2.alpha.,3.beta.-dihydroxy-4.alpha.-(hydroxymethyl)cycl opentyl)]-7-substituted-v-triazolo[4,5d]pyrimidines: ##STR2## and their derivatives wherein R is amino, mercapto, methylmercapto, hydroxy, halogen, or substituted amino: ##STR3## wherein R' and R" may be the same or different and are of hydrogen, methyl, ethyl, propyl or phenyl. The preparation of the single intermediate from which either of these series of compounds may be synthesized is also disclosed. The compounds exhibit antiviral and antitumor activity. Acid salts and esters of the purine nucleosides have also been prepared.

Abstract: Compounds of the formula ##STR1## where X is OH, NH.sub.2, SH, OR or SR (where R is alkyl of 1 to 4 carbon atoms or benzyl), R.sup.1 is H or alkyl of 1 to 8 carbon atoms, R.sup.2 is H or methyl, Y is the salt of an amine of the formula ##STR2## where R.sup.3 and R.sup.4 are lower alkyl, e.g., 1 to 4 carbon atoms and n is an integer of 2 to 4 with p-acetamidobenzoic acid and where z is a number from 0 to 10 are useful as immunomodulators, as antiviral agents and in specific cases have anti-leukemic activity. The compounds and compositions where z is 1 to 10 are novel per se. When R.sup.2 is H the presence of Y enhances the immunoregulatory activity and the antiviral activity. If X is the NH.sub.2 there is immunoinhibitory activity but no immunostimulatory (immunopotentiatory) activity.

Abstract: Compounds of the formula ##STR1## where X is OH, NH.sub.2, SH, OR or SR (where R is alkyl of 1 to 4 carbon atoms or benzyl), R.sup.1 is H or alkyl of 1 to 8 carbon atoms, R.sup.2 is H or methyl, Y is the salt of an amine of the formula ##STR2## where R.sup.3 and R.sup.4 are lower alkyl, e.g., 1 to 4 carbon atoms and n is an integer of 2 to 4 with p-acetamidobenzoic acid and where z is a number from 0 to 10are useful as immunomodulators, as antiviral agents and in specific cases have anti-leukemic activity. The compounds and compositions where z is 1 to 10 are novel per se. When R.sup.2 is H the presence of Y enhances the immunoregulatory activity and the antiviral activity. If X is the NH.sub.2 there is immunoinhibitory activity but no immunostimulatory (immunopotentiatory) activity.