Abstract: A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

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 subject invention concerns compounds of formula (I): whereinn=1 or 2;R.sup.1 is H, NH.sub.2 or halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 represents the group CR.sup.6 R.sup.7 R.sup.8 where R.sup.6, R.sup.7 and R.sup.8 are the same or different and are each H, C.sub.1-6 alkyl or C.sub.1-6 haloalkyl;R.sup.4 and R.sup.5 are the same or different and are selected from the group consisting of H, CO.sub.2 H, CO.sub.2 C.sub.1-6, NHSO.sub.2 CF.sub.3, tetrazole and (CR.sup.9 R.sup.10).sub.p (Y).sub.q (CR.sup.9 R.sup.10).sub.t Z where (CR.sup.9 R.sup.10), or (CR.sup.9 R.sup.10).sub.t is straight or branched chain bearing the substituents R.sup.9 and R.sup.10 when p or t>1;R.sup.9 and R.sup.10 are the same or different and are each C.sub.0-6 alkyl-Z;p=1-3;q=0 or 1;t=0-4, provided that t>0 when q=1;Y=O, NH or S(O).sub.m where m=0-2; andZ is selected from a group consisting of H, CN, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3 tetrazole, triazole, CONH.sub.2, CON(C.sub.1-6 alkyl).sub.2, CONH(C.sub.

Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.

Abstract: A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl is reacted with the compound of the formulaZ.sub.1 --Xto yield the purine of the formula ##STR2## wherein x is a leaving group, and Z.sub.1 is a protected form of the carbohydrate surrogate Z.

Abstract: Compounds of the Formula I ##STR1## where one of R.sub.1 and R.sub.2 is --C(O)CH(CH(CH.sub.3).sub.2)NH.sub.2 or --C(O)CH(CH(CH.sub.3)CH.sub.2 CH.sub.3)NH.sub.2;the other of R.sub.1 and R.sub.2 is --C(.dbd.O)C.sub.3 -C.sub.21 saturated or monounsaturated, optionally substituted alkyl; andR.sub.3 is OH or H;and pharmaceutically acceptable salts thereof have utility as enhanced bioavailability antivirals against herpes and retroviral infections.

Abstract: Conformationally locked 4',6'-cyclopropane-fused carboxylic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine, and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.

Abstract: A 2,6,9-trisubstituted purine composition having the following formula: ##STR1## where X is a amino, oxo, thio, of sulfone moiety, R.sub.1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl, each having from 1 to 20 carbon atoms; R.sub.2 is hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl; and R.sub.3 is halogen, hydroxyl, thio, alkoxy, alkylthio, lower alkyl, --NR.sub.4 R.sub.5 or a component having the formula: ##STR2## wherein when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is methyl, R.sub.

Abstract: Compounds of formula (I) ##STR1## wherein n=1 or 2;R.sup.1 is H, NH.sub.2 or halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 represents the group ##STR2## where m=0 or 1; R.sup.4 and R.sup.5 are the same or different and are each H, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3, tetrazole, (CR.sup.6 R.sup.7).sub.p (Y).sub.q (CR.sup.6 R.sup.7).sub.t Z where (CR.sup.6 R.sup.7)p or (CR.sup.6 R.sup.7).sub.t may be straight or branched chain bearing the substituents R.sup.6 and R.sup.7 when p and t>1; R.sup.6 and R.sup.7 are the same or different and are each C.sub.0-6 alkyl-Z;p=1-3;q=0 or 1;t=0-4, provided that t>0 wgeb q=1;Y is NH, O, S(O)u where u=0-2;Z is H, CN, CO.sub.2 H, CO.sub.2 C.sub.1-6 alkyl, NHSO.sub.2 CF.sub.3, tetrazole, triazole, CONH.sub.2, CON(C.sub.1-6 alkyl).sub.2, CONH(C.sub.1-6 alkyl), SO.sub.2 NH (C.sub.1-6 alkyl) or SO.sub.2 N(C.sub.1-6 alkyl).sub.2 ; or a salt, soluate or hydrate thereof.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein HET is ##STR2## m is an integer from 1 to 4; R.sup.1 and R.sup.

Abstract: The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract: Process and novel intermediates for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for mono-esterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir in high yield and purity. These products are of value as antiviral agents with improved absorption.

Abstract: The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract: Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.

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: Antihypertensive and bronchodilating phosphoclusterose inhibitory compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is fluoro, chloro or bromo.

Abstract: This invention relates to an improved regiospecific process for the synthesis of acyclic nucleosides such as, acyclovir and ganciclovir, anti-viral compounds especially effective against herpes virus, and intermediates thereof starting from dyacylguanine and an alkylating agent, selected from 2-oxa-1,4-butanediol diacetate (OBDDA), 1,4-diacetoxy-3-acetoxymethyl-2-oxa-butane, 1,4-dibenzyloxy-3-acetoxymethyl-2-oxabutane. The reaction is carried out in the absence of an acid catalyst and a solvent.

Abstract: Processes are described for preparing substituted N-ethylglycine derivatives of the formula ##STR1## in which PG is an amino protecting group which is labile towards weak acids and is of the urethane type or the trityl type, X is NH or O, and B' represents bases which are customary in nucleotide chemistry and whose exocyclic amino and/or hydroxyl groups are protected by suitable known protecting groups, and the salts thereof.

Abstract: Disclosed herein are methods directed generally to the control of neural activity and for selectively and controllably inducing the in vivo genetic expression of one or more naturally occurring genetically encoded molecules in mammals. More particularly, the present invention selectively activates or derepresses genes encoding for specific naturally occurring molecules such as neurotrophic factors through the administration of carbon monoxide dependent guanylyl cyclase modulating purine derivatives. The methods of the present invention may be used to affect a variety of cellular and neurological activities and to therapeutically or prophylactically treat a wide variety of neurodegenerative, neurological, and cellular disorders.

Abstract: Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.

Abstract: Disclosed are novel prodrugs represented by the following structural formulas: ##STR1## Z is oxygen or sulfur; n is 1 or 2; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a group which can be metabolized in vivo to a give a modified A such that the phosphoester bond (modified A)--O undergoes cleavage in vivo. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.

Abstract: Immunostimulating 7,8-disubstituted guanine derivatives that also contain a 9-alkyl, 9-alkoxy or 9-aralkyl substituent are disclosed whose structures are represented by Formula I ##STR1## wherein X is O or S; R.sup.1 is a hydrocarbyl or substituted hydrocarbyl group having a length of about one to about seven carbon atoms; R.sup.2 is a hydrocarbyl or hydroxyl- or ether-substituted hydrocarbyl group having a length of about four to about ten carbon atoms; and the pharmaceutically acceptable base addition salts thereof. Also disclosed are compositions containing an immunostimulating guanine derivative and processes for using the same.

Abstract: (1R,trans) Diprotected 3-methylene-1,2-cyclopropanedimethanol is oxidized to an optically active diol ##STR1## which is then cyclized to an orthoester ##STR2## This orthoester is then treated with a Lewis acid catalyst to give the cyclobutanone ##STR3## which is useful as an intermediate in the preparation of the antiviral agent ?1R-(1.alpha.,2.beta.,3.alpha.)!-2-amino-9-?2,3-bis(hydroxymethyl)cyclobut yl!-1,9-dihydro-6H-purin-6-one.

Abstract: A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

Abstract: Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process provides an N,O-bis-trityl intermediate of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol which allows for mono-esterification by an L-valine derivative. These products are of value as antiviral agents with improved absorption.

Abstract: A process for the preparation of acyclovir by alkylation of N.sup.2 -formylguanine with 2-oxa-1,4-diacyloxybutane and hydrolysis of the resulting intermediate is described.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. Also provided is a process of making compounds of Formula I. Compounds of the present invention are represented by Formula I: ##STR1## its pharmaceutically acceptable salts, hydrochloride salts, or prodrug forms thereof, wherein:X.sub.1a, X.sub.1b are independently selected from --NH and --N-lower alkyl;X.sub.2a, X.sub.2b are optionally present and are independently selected from S(O)n, O, CH.sub.2, and NH;P.sub.1a, P.sub.1b, P.sub.2a, P.sub.2b, P.sub.4a, and P.sub.4b are independently selected from N, or CH;R.sub.1a, R.sub.1b, R.sub.2a, R.sub.2b, R.sub.3a and R.sub.3b are independently selected from H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 branched alkyl, C.sub.3 -C.sub.

Abstract: A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino;R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; andB is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio;and the pharmaceutically acceptable acid addition, metal, and amine salts thereof.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

Abstract: Compounds of formula I ##STR1## where n=0-2;R.sup.1 is H, NH.sub.2 or a halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 is any of the four groups ##STR2## where m=0 or 1; andX is O, NR.sup.5, or S(O).sub.0-2 and, in group (b), the X's may be the same or different.Compounds of the invention have utility as inhibitors of purine nucleoside phosphyorylase (PNP).

Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## wherein R.sub.2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R.sub.5 is alkyl; R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.

Abstract: The compound of the formula: ##STR1## where R.sub.1 is H, alkyl, perhaloalkyl, arylalkyl, alkenyl or alkynyl; R.sub.2 is H when R.sub.4 is other than H, and, when R.sub.4 is H, R.sub.2 is ##STR2## in which R.sub.5 is hydrogen or alkyl; R.sub.3 is hydrogen or halogen; R.sub.4 is H or ##STR3## X and Y are nitrogen and Z is carbon; n is 1 or 2; n.sub.1 is 0, 1, 2, 3, 4, or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.

Abstract: Process for preparing the L-monovaline ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts. The present process relates to an improved process whereby ganciclovir is esterified with an L-valine derivative to provide a di-valine ganciclovir intermediate. Removal of one of the valine groups with a lower alkyl amine, benzylamine or benzyl methylamine provides the mono-valine ester compound of Formula I. These products are of value as antiviral agents with improved absorption.

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: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.

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: Novel O.sup.6 -substituted guanine compounds and pharmaceutical compositions thereof are useful for effectively reducing O.sup.6 -alkylguanine-DNA alkyltransferase (AGT). The novel compounds are useful for treating tumors and when used with anti-neoplastic alkylating agents enhance the chemotherapeutic treatment of tumor cells in a host.

Abstract: Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.

Abstract: In order to produce a purine of the general formula (I), ##STR1## in which R.sup.1 and R.sup.2 can be the same or different and denote H, OH, SH, NH.sub.2, N-(di)-alkyl, halogen, O-alkyl, S-alkyl, alkyl or aryl and alkyl represents an aliphatic residue with 1 to 4 carbon atoms and aryl represents a phenyl residue which is substituted if desired by CH.sub.3, OH, NH.sub.2 or halogen, from the corresponding 4-amino-5-nitrosopyrimidine of formula (II), ##STR2## in which R.sup.1 and R.sup.2 have the above-mentioned meaning, the compound of formula (II) is reductively formylated in a solvent at a temperature of 80.degree. to 220.degree. C. in the presence of formic acid and a catalyst based on a noble metal and the 4-amino-5-formylaminopyrimidine formed as an intermediate is cyclized.

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: 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: 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: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

Abstract: The present invention provides a process for the synthesis of penciclovir and famciclovir by 9-substituting the compound 2-amino-6-chloropurine (ACP) with 2-acetoxymethyl-4-(leaving group)-but-1-yl acetate, followed by displacement of the 6-chloro moiety with a hydroxy moiety (i.e. to form a guanine derivative) or with hydrogen (to form the 2-aminopurine derivative), respectively.

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: Antivirally active compounds of formula (I), wherein R.sup.1 is hydrogen, hydroxy, mercapto or amino; R.sup.2 is hydrogen, hydroxy, fluoro, chloro or amino; R.sup.3 and R.sup.4 are independently selected from (II), (III), amino, hydroxy or an ether or ester residue thereof, or R.sup.3 together with R.sup.4 is (IV), wherein M is hydrogen or a pharmaceutically acceptable counterion; and n is 1 or 2; with the proviso that, when R.sup.2 is amino and R.sup.3 and R.sup.4 are hydroxy, R.sup.1 is not hydroxy and in addition, when n=1, R.sup.1 is not hydrogen, and pharmaceutically acceptable salts thereof; processes for preparation of said compounds, a pharmaceutical composition comprising said compounds, methods for treatments of virus infections as well as use of compounds of formula (I) without the proviso for the manufacture of a medicament for treatment of AIDS.

Abstract: A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxy-ethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ("DHPG") where the N.sup.2,N.sup.9 -diprotected guanine is reacted with CH.sub.3 C(O)OCH.sub.2 O(CH.sub.2).sub.2)OC(O)CH.sub.3 or 2-acetoxymethoxy-1,3-diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.

Abstract: N.sup.2 -substituted alkylguanine and N.sup.2 -substituted phenylguanine compounds which prevent recurrent herpes simplex infections are disclosed. By virtue of their ability to inhibit herpes virus thymidine kinase in vivo, such compounds will prevent, reduce the frequency of, or reduce the severity of recurring HSV infections in humans. The N.sup.2 -alkylguanine compounds are of the formula: ##STR1## where R.sub.1 is a normal or branched chain C.sub.n H.sub.2n+1 (where n is 1-12); R.sub.2 is H, 2-deoxyribofuranosyl, (CH.sub.2).sub.n OH (where n is 2-5), CH.sub.2 CH(OH)CH.sub.2 OH, (CH.sub.2).sub.n --COOH (where n is 1-4), CH.sub.2 CH(OH)CH.sub.2 --O--COR.sub.4, (CH.sub.2).sub.n --O--COR.sub.4 (where n is 2-5), or (CH.sub.2).sub.n CO--OR.sub.4 (where n is 1-4); R.sub.4 is CH.sub.3, CH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or CH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.3 is OH, H, Cl or NH.sub.2, or a tautomer or a pharmaceutically acceptable salt thereof. The N.

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: Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituentsCompounds of the formulae I and II ##STR1## in which the substituents A, R.sup.1, R.sup.2 and R.sup.3 and n have the meanings given, have an antiviral and antiparasitic action.