Anti-viral pyrimidine nucleoside analogues
AssigneesRega Foundation, University College Cardiff Consultants Limited
InventorsChristopher McGuigan, Jan Balzarini
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AssigneesRega Foundation, University College Cardiff Consultants Limited
InventorsChristopher McGuigan, Jan Balzarini
Estimating the term…
A compound having the formula (I) wherein Ar is an, optionally substituted, aromatic ring system, the aromatic ring system comprising one six-membered aromatic ring or two fused six-membered aromatic rings; R8 and R9 are each independently selected form the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH2)m where m is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N-alkyl; U″ is H and U′ is selected from H and CH2T, or U′ and U″ are joined so as to form a ring moiety including Q wherein U′—U″ together is respectively selected from the group comprising —CTH—CT′T″- and —CT=CT- and —CT′=CT′-, so as to provide ring moieties selected from the group comprising (a), (b) wherein: T is selected from the group comprising OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2 and N3; T′ is selected from the group comprising H and halogens and, where more than one T′ is present, they may be the same or different; T″ is selected from the group comprising H and halogens; and W is selected from the group comprising H, a phosphate group and a pharmacologically acceptable salt, derivative or pro-drug thereof; with the proviso that when T is OAc and T′ and T″ are present and are H, Ar is not 4-(2-benzoxazolyl)phenyl. C1 to C10 alkyl and alkoxy substituents on the aromatic ring system of Ar are preferred. Compounds show anti-viral activity, for example with respect to varicella zoster virus.
A compound having the formula:
A compound according to any one of the preceding claims wherein Ar comprises an aromatic ring system substituted by one or more moieties independently selected from the group comprising H, alkyl, aryl, cycloalkyl, chlorine, bromine, iodine, cyano, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthiol and arylthiol, any alkyl, cycloalkyl or aryl groups of which may be substituted by one or more members selected from the group comprising chlorine, bromine, iodine, CN, CO2alkyl (C1 to C6), CONH2, CONH alkyl (C1 to C6), SH, S alkyl (C1 to C6) and NO2.
A compound according to any one the preceding claims wherein the moiety or moieties substituted on the said aromatic ring system comprise one or more, optionally substituted, alkyl or alkoxy moieties wherein the said alkyl or alkoxy moiety or moieties, in total, comprise from 3 to 8 carbon atoms, calculated excluding any substituents that may be present on the said alkyl or alkoxy moiety or moieties.
A compound according to any one of the preceding claims wherein the aromatic ring system comprises one six-membered aromatic ring, preferably a carbocyclic aromatic ring, and one substituent, preferably one alkyl or one alkoxy moiety, at the para position on the six-membered aromatic ring.
Dependencies are inferred from the claim text.