Abstract: The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.

Abstract: A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or allergic disorders, proliferative skin disorders, and bronchodilation which method comprises the administration of an effective, non-toxic amount of a compound of formula (I): ##STR1## or if appropriate a pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 each independently represent alkyl or a moiety of formula (a):--(CH.sub.2).sub.m --A (a)wherein m represents zero or an integer 1, 2 or 3; A represents a substituted or unsubstituted cyclic hydrocarbon radical; andR.sup.3 represents a halogen atom, a nitro group, or a group --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each independently represents hydrogen, alkyl or alkylcarbonyl or R.sup.4 and R.sup.5 together with the nitrogen to which they are attached forming an optionally substituted, heterocyclic group; certain novel compounds falling within formula (I) and compositions comprising such compounds.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.8 are independently alkyl, aryl or aralkyl, and R.sup.2 is selected from the group consisting of S and O, R.sup.6 is selected from the group consisting of S and O, provided that R.sup.2 and R.sup.6 are not both O. The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition. Methods of treatment using the compounds are also disclosed.

Abstract: A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R).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 method for treating a mammal having a damaged central nervous system, as the result of trauma or disease, for reestablishing previously destroyed neurological functions in a traumatized or diseased mammal, or for controlling spasticity and for providing protection from such injury to the central nervous system. The method comprises administering to the mammal at least one neurologically active compound comprising two groups, one group providing alpha-adrenergic agonist activity, specifically a guanidino group, and the second group providing agonist activity selected from the group consisting of beta-adrenergic agonist activity, serotinergic agonist activity, and GABA-ergic agonist activity (for example a methylated xanthine group, having beta-adrenergic agonist activity) as the primary therapeutic agent. The neurologically active compound is administered in a dosage amount and at a dosage rate sufficient to at least partially restore the lost neurological function or to control spasticity.

Abstract: The present invention provides AGT inactivating compounds such as substituted O.sup.6 -benzylguanines of the formula ##STR1## wherein, for example, R.sub.1 is amino, hydroxy, or alkylamino, R.sub.2 is aminoalkyl, hydroxyalkyl, or alkylaminoalkyl, and R.sub.3 is halo, hydroxyalkyl, thiol or alkylthio, as well as pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine comprising administering to a mammal an effective amount of one of the aforesaid compounds and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.

Abstract: A process for preparing 7-benzylpurine derivatives is provided. An acetylpurine nucleoside is reacted with a benzyl halide to benzylate the 7-position of the purine base, and an acid is then added to the reaction mixture to hydrolyze the glycoside bond. The 7-benzylpurines may be used to prepare 9-substituted purine derivatives.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo?3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation.The invention relates to the use of xanthine derivatives of the formula I ##STR1## in which R.sup.2 is a (C.sub.1 -C.sub.4)-alkyl group and at least one of the symbols R.sup.1 and R.sup.3 is a radical of the formula II or III ##STR2## in which A is CHOH, CO or dioxolane, R.sup.4 is a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group and n is 0 to 5, and in which R.sup.5 and R.sup.6 are hydrogen atoms or (C.sub.1 -C.sub.4)-alkyl groups or, together with the nitrogen atom to which they are bonded, form a 5- to 7-membered ring, it being possible for one carbon atom to be replaced by an oxygen or nitrogen atom, m is 1 or 2 and the other radical R.sup.1 or R.sup.3, if appropriate, is a hydrogen atom, a (C.sub.1 -C.sub.6)-alkyl group or a (C.sub.3 -C.sub.

Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are defined herein.

Abstract: The present invention provides 8-substituted O.sup.6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. Thus, for example, the present invention provides a compound of the formula ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of amino, hydroxy, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.4 acylamino, R.sub.2 is a substituent selected from the group consisting of C.sub.1 -C.sub.4 aminoalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 dialkylamino alkyl, and C.sub.1 -C.sub.4 pivaloylalkyl, and R.sub.3 is a C.sub.1 -C.sub.4 alkyl. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lessons at the O.sup.

Abstract: A process for the preparation of 2-fluoro-9- (2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)adenine (I) is described. The process involves reacting a protected 2-fluoro adenine with a protected chlorosugar under controlled conditions of temperature (80-85.degree. C.) to produce (I), rather than using a process involving fluorinating a 2-substituted nucleoside precursor of (I).

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Abstract: Compounds and pharmaceutical compositions thereof comprise the formula:(R)j- (core moiety),including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, wherein J is an integer from one to three, the core moiety is non-cyclic or comprises at least one, five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, alkyl (C.sub.1-6) or alkenyl (C.sub.1-6), and at least one R has the formula I: ##STR1## wherein n is an integer from four to eighteen; each R'.sub.1 and R'.sub.2 is independently hydrogen, alkyl (C.sub.1-4) or alkenyl (C.sub.1-4), the alkyl or alkenyl groups being preferably substituted by a halogen, hydroxyl, ketone or dimethylamino group and/or may be interrupted by an oxygen or hydrogen atom or an alkyl (C.sub.1-4) group; and each R'.sub.3 and R'.sub.4 is independently hydrogen or methyl. Preferably, n is an integer from six to ten, R'.sub.1 and R'.sub.

Abstract: The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3, and R.sub.7 are methyl and X is one to three substituents, which may be the same or different and selected from the group consisting of amino, C.sub.1 -C.sub.4 alkylcarbonylamino, carboxy C.sub.2 -C.sub.4 alkylcarbonylamino, halo, C.sub.1 -C.sub.3 alkyloxy, amino C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkyloxy carbonylamino, amino C.sub.1 -C.sub.4 alkenyloxy, isothiocyanato, and diazonium tetrafluoroborate. In compound (b), R.sub.1, R.sub.3, and R.sub.7 are methyl, R.sub..beta. is hydrogen or methyl, and X is selected from the group consisting of R, C(.dbd.O)OR, and C(.dbd.O)NH--R, wherein R is a C.sub.1 -C.sub.6 alkyl.

Abstract: A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative.

Abstract: Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or derivatives thereof, then hydrolyzing the ribose moiety to form purine derivatives having the substituent in the 7-position, subsequently introducing the desired substituent in the 9-position, and then removing the substituent in the 7-position.

Abstract: 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: A method for screening a compound as a potential anti-obesity agent by determining whether the compound stimulates micro motion of cells in vitro is described

Abstract: Disclosed are therapeutic compounds having the formula:(R)j - (core moiety),including resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is either non-cyclic or comprises at least one five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C.sub.1-6 alkyl or C.sub.1-6 alkenyl, and at least one R has the formula I: ##STR1## n is an integer from seven to twenty and at least one of X or Y is --OH. The other of X or Y, which is not --OH, is hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --, and each W.sub.1, W.sub.2, and W.sub.3 is independently hydrogen, CH.sub.3 --, CH.sub.3 --CH.sub.2 --, CH.sub.3 --(CH.sub.2).sub.2 -- or (CH.sub.3).sub.2 --CH.sub.2 --. The X, Y, W.sub.1, W.sub.2, or W.sub.

Abstract: Acetal-and ketal-substituted compounds and pharmaceutical compositions thereof have the following formula:CORE MOIETY--(R).sub.j,including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof. j is an integer from one to three, the core moiety is non-cyclic or cyclic a monocyclic moiety having at least one nitrogen atom within the ring and R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted alkyl C.sub.(1-6), alkenyl C.sub.(2-6), cyclic or heterocyclic groups, and groups having a structure prescribed by formula I. At least one R has the formula I:--(CH.sub.2).sub.n --C--(R.sub.1).sub.3 Iwherein n is an integer from three to twenty; R.sub.1 is selected from among hydrogen; halogen; hydroxide; substituted or unsubstituted C.sub.(1-6) alkyl, C.sub.(1-6) alkoxy, C.sub.2-6) alkenyl, cyclic or heterocyclic group; --OR.sub.2, R.sub.2 being hydrogen or a substituted or unsubstituted C.sub.(1-6) alkyl, C.sub.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo?3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: Disclosed is a process for preparing compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises administering to the airways of the patient a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5')tetraphosphate, an analog of UTP, or any other analog, in an amount effective to promote drainage of fluid in the congested airways, including sinuses, by hydrating mucous secretions or by stimulating ciliary beat frequency in the airways. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or eye drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

Abstract: The present invention relates to novel xanthine derivatives of the formula (I) which are selectively antagonistic to an adenosine A.sub.2 receptor, and pharmaceutically acceptable salts thereof. Formula (I): ##STR1## In the formula, R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, a propyl group, a butyl group or an allyl group; R.sup.3 represents a hydrogen atom or a lower alkyl group; Y.sup.1 and Y.sup.2 are the same or different and each represents a hydrogen atom or a methyl group; and Z represents a substituted or unsubstituted phenyl group, a pyridyl group, an imidazolyl group, a furyl group or a thienyl group.

Abstract: A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or other disorders which method comprises the administration of an effective, non-toxic amount of a compound of formula (I): ##STR1## or if appropriate a pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 each independently represent alkyl or a moiety of formula (a):--(CH.sub.2).sub.m --A (a)whereinm represents zero or an integer 1, 2 or 3;A represents a substituted or unsubstituted cyclic hydrocarbon radical; andR.sup.3 represents a halogen atom, a nitro group, or a group --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each independently represents hydrogen, alkyl or alkylcarbonyl or R.sup.4 and R.sup.5 together with the nitrogen to which they are attached forming an optionally substituted, heterocyclic group; certain novel compounds falling within formula (I) and compositions comprising such compounds.

Abstract: Xanthine derivatives having general structure (I) including the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently (C.sub.1 -C.sub.4)lower alkyl or (C.sub.2 -C.sub.4)lower alkenyl, Z is (II) or (III) or (IV) wherein R.sub.3 is hydrogen, (C.sub.1 -C.sub.3)lower alkyl, nitro, amino, hydroxy, fluoro, bromo or chloro, R.sub.4 is (C.sub.1 -C.sub.4)lower alkyl and n is 1 or 2 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 selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.

Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.

Abstract: The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2.The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: The invention relates to new xanthine derivatives of general formula I, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl;B is a purine or pyrimidine base.optionally R is taken together with X' to complete a cyclic phosphonate having the formula ##STR2## A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR3## wherein X and X' are the same or different and are hydrogen or alkyl, the dashed line is an optional bond,Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z are taken together to form an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine.

Abstract: An improved method for the preparation of acyclic nucleotide analogues comprises first condensing a cyclic carbonate with a purine or pyrimidine base and then reacting the alkylated base with an activated phosphonate. Novel cyclic carbonates are employed to yield the desired phosphonylmethoxyalkyl nucleotide analogues.

Abstract: This invention relates to a process for preparing xanthine derivatives of formula I: ##STR1## characterized in that a uracil derivative of formula A or B ##STR2## is dissolved in a suitable organic-aqueous solvent and cyclized in the presence of LiOH.

Abstract: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo?2,3-d!pyrimidine and pyrazolo?3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.

Abstract: Disclosed are xanthine derivatives represented by the following Formula (I): ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen or lower alkyl;Q.sup.1, Q.sup.2, and Q.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy, or halogen;and X represents --COR.sup.4 (in which R.sup.4 represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or --SO.sub.2 R.sub.5 {in which R.sup.5 represents hydroxy, lower alkoxy, trifluoromethyl, ##STR2## in which R.sup.6 and R.sup.7 independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or ##STR3## (in which m represents an integer of 1 to 3; and R.sup.8 and R.sup.9 independently represent hydrogen or lower alkyl), or ##STR4## (in which Y represents a single bond, oxygen, or N--R.sup.10 in which R.sup.10 represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3)}, and pharmaceutically acceptable salts thereof.

Abstract: There is disclosed a compound having the formula: ##STR1## wherein n is an integer from 5 to 9, wherein the core moiety is a heterocylic moiety wherein C.sub.a, C.sub.b, and C.sub.c are an R or S enantiomer or racemic mixture and the C.sub.a, C.sub.b, and C.sub.c carbon atoms are bonded together by a single bond, double bond, ether or ester linkages, wherein R.sub.1, R.sub.2 and R.sub.3 are independently halo, hydroxy, hydrogen, keto, isothiocyano, azide or haloacetoxy with the proviso that at least one of R.sub.1, R.sub.2 or R.sub.3 must be a halo, isothiocyano, azide or haloacetoxy group, wherein R.sub.4 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, cyclo C.sub.4-6 alkyl, or phenyl, and wherein halo refers to fluoro, chloro, bromo and iodo and salts thereof and pharmaceutical compositions thereof.

Abstract: Adenosine and xanthine derivatives, and compositions comprising those compounds, are potent selective agonists and antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.

Abstract: Certain prodrugs such as ##STR1## are useful in the inhibition of herpes virus thymidine kinase, the prevention or treatment of recurrent infection by herpes virus, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating recurrent infection by herpes virus are also described.

Abstract: The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): ##STR1## wherein R.sub.1 is H, alkyl or aralkyl;Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group;R.sub.4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group;R.sub.5 and R.sub.6 are each independently H or alkyl;R.sub.3 is H, and R.sub.7 and R.sub.8 are combined together to be oxo, or else R.sub.3 and R.sub.7 are combined together to be another direct bond, and R.sub.5 and R.sub.8 are combined together to be a direct bond,or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.

Abstract: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.

Abstract: The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain vital infections.

Abstract: New xanthine compounds of formula I: ##STR1## wherein the substituents are defined herein, which xanthines are useful as adenosine antagonists.

Abstract: Xanthine derivatives, and compositions comprising those compounds, are potent selective antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias. The compounds, specifically, are C-8 epoxide derivatives of xanthine having the general formulae of: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and can be H or an alkyl group of 1-4 carbons, and n=0-4; and ##STR2## wherein R.sub.1 and R.sub.2 are the same or different, and can be H or an alkyl group of 1-4 carbons, R.sub.3 is either O or (CH.sub.2).sub.1-4, and n=0-4.

Abstract: There is disclosed compounds and pharmaceutical compositions that are a resolved R or S (preferably R) enantiomer of an .omega.-1 alcohol of a straight chain alkyl (C.sub.5-8) substituted at the 1-position of 3,7-disubstituted xanthine. The inventive compounds are effective in modulating cellular response to external or in situ primary stimuli, as well as to specific modes of administration of such compounds in effective amounts.

Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.

Abstract: Xanthines of the formula I ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group:R.sub.2 is a C.sub.1 -C.sub.4 alkyl group;R.sub.3 tetrahydropyran-4-yl or 1,3-dithiolan or;R.sub.3 represents one of the groups of formula ##STR2## and pharmaceutically acceptable acid addition salts thereof. These are adenosine antagonists, capable of acting as cholinomimetics, useful for the treatment of CNS disorders such as senile dementia and Alzheimer's disease.