Pyrimidine nucleoside derivative and antiviral agent...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/46 (2006.01) A61K 31/505 (2006.01) C07D 239/54 (2006.01) C07D 239/56 (2006.01) C07D 239/58 (2006.01) C07D 239/60 (2006.01)

Patent

CA 2039039

The invention is a pyrimidine nucleoside derivative represented by the following formula (I): Image wherein R1 represents ethyl group or isopropyl group; R2 and R3 independently represent hydrogen atom, an C1-C3 alkyl group or chlorine atom; X represents oxygen atom or sulfur atom; and Z represents sulfur atom or methylene group; with the proviso that R2 and R3 do not simultaneously represent hydrogen atoms when X represents oxygen atom and Z represents sulfur atom, or a pharmaceutically acceptable salt thereof. The pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof show a markedly higher anti-retroviral activity than conventional analogous compounds and have a relatively low toxicity against the host cells, and therefore, are useful as an active ingredient of antiviral agent.

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