C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/218, 260/255
C07D 239/46 (2006.01) A61K 31/505 (2006.01) C07D 239/54 (2006.01) C07D 239/545 (2006.01) C07D 239/56 (2006.01) C07D 239/58 (2006.01) C07D 239/60 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2026226
A 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I'; Image wherein R1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group; R2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a halogen atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups; R3 represents a hydrogen atom, methyl, branched alkyl or -CH2-Z-(CH2)n-R5 group where R5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5, R4 represents a hydrogen atom, alkyl or aralkyl group, X represents an oxygen or sulfur atom, Y represents an oxygen or sulfur atom, provided that when R4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R5 does not represent a hydroxyl group, or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient. 147
Baba Masanori
de Clercq Erik Desire Alice
Miyasaka Tadashi
Tanaka Hiromichi
Ubasawa Masaru
Baba Masanori
de Clercq Erik Desire Alice
Mitsubishi Chemical Corporation
Miyasaka Tadashi
Ridout & Maybee Llp
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