Abstract: Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.

Abstract: Deoxyuridine derivatives of Formula (I?); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.

Abstract: The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).

Abstract: A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(CR8R8?)n-D-(CR8R8?)m—; D is a bond, —NR9—, —O—, —S—, —S(?O)— or —S(?O)2—; n and m are independently 0, 1 or 2, R8 and R8? are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8? together with their adjacent C atom is —C(?O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(?O)—, —NR9—, —O—, —S—, —S(?O)2—; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q?2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.

Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.

Abstract: Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR1, NHS(?O)pR2, NHR3, NRaRb, C(?O)NHR3 or C(?O)NRaRb wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl or NRaRb; R3 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl, —OC1-C6alkyl, —OC0-C3alkylenecarbocyclyl, —OC0-C3alkyleneheterocyclyl; wherein any alkyl, carbocyclyl or heterocycylyl in R1, R2 or R3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Ry and Ry? are independently C1-C6alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is —CH2—, —O—, —OC(?O)NH—, —OC(?O)—, —S—, —NH—, —NRa, —NHS(?O)2—, —NHC(=0)NH— or —NHC(?O)—, —NHC(?S)NH— or a bond; R8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carbo

Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.

Abstract: This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.

Abstract: There is provided inter alia use of 2?,3?-dideoxy-3?-hydroxymethylcytosine or a prodrug or salt thereof in the manufacture of a medicament for the treatment of HIV infection wherein the reverse transcriptase of the HIV bears at least one mutation that allows an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.

Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, —O—, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.

Abstract: A topical composition comprising an antiinflammatory glucocorticoid and a nucleoside analogue antiviral agent in a pharmaceutical carrier characterized in that the carrier comprises about 15 to about 25 weight % propylene glycol and about 10 to about 25 weight percent isopropyl C12–C22 alkanoic ester. The compositions have utility in the treatment or prophylaxis of herpesvirus infections and exhibit superior antiviral and therapeutic efficacy and an improved shelf life.

Abstract: Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

Abstract: Compounds of the formula I: wherein Rx is cyano or bromo; R1 is halo; R2 is C114 C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.

Abstract: A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(C8R8)n-D-(C8C8?)m—; D is a bond, —NR9—, —O—, —S—, —S(?O)— or —S(?O)2; n and m are independently 0, 1 or 2, R8 and R8? are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8? together with their adjacent C atom is —C(?O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(?O)—, —NR9—, —O—, —S—, —S(?O)2—; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q?2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.

Abstract: A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig

Abstract: A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig

Abstract: A pharmaceutical preparation comprising a synergistic combination of abacavir and alovudine and a pharmaceutical carrier therefor. Use of abacavir and alovudine together for the treatment of multiresistant HIV, wherein the use comprises simultaneous, combined or sequential administration of alovudine and abacavir.

Abstract: A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig

Abstract: A method of treating HBV or HIV infections comprising administering to an individual an effective amount of the compound of formula IId?: wherein R2 is the residue of an aliphatic L-amino acid, p is 0, 1, or 2-20, and q is 0, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the prophylactic and curative treatment of herpesvirus infections in mammals including man. The invention also relates to the use of a combination of a topically acceptable antiviral substance and an antiinflammatory glucocorticoid for the manufacture of a medicament for said prophylactic and curative treatment.