| 摘要 |
EP--85424 A (A) 9-(2-acyloxy-1-hydroxymethyl ethoxymethyl) purine derivs. of formula (I) and their acid-addn. salts are new, (R1 is H or R7CO; R7 is H, 1-19C alkyl, 1-8C hydroxyalkyl, 2-9C alkoxyalkyl, 2-19C alkenyl, Ph, 1-adamantyl, 2-carboxyethyl, or carboxymethyl or their alkali metal salts; R2 is R7CO; R3 is H, halogen, SH, 1-6C alkylthio, N3, NR9R19 or NH-COR8; R8 is H, 1-19C alkyl or 1-adamantyl; R9 and R10 are H or 1-6C alkyl; and either (a) R4+R5 form a single bond and R6 is H, halogen, 1-6C alkoxy, N3, SH, 1-6C alkylthio, NR9R10 or NH-COR8; or (b) R4 is H and R5+R6 form a keto group). (B) Intermediates of formula (I) are new when (1) R1 and R2 are H; R3 is other than NY-COR8; R4 and R5 form a bond and R6 is other than NH-COR8; and (2) R1, R2 and R4 are H; R3 is NH-COR8; and R5+R6 form a keto gp. - Cpds. (I) are antivirals esp. effective against Herpes simplex virus I and II, cytomegalovirus, Epstein-Barr virus and varicella zoster virus and viral hepatitis B. Intermediates defined in paragraph (B) are also antivirals. Dose is 0.1-300 mg/kg. orally or parenterally. (0/0) USAB- US4612314 A Substd. 9-(1 or 3-monoacyloxy or 1,3-diacyloxy-2-propoxymethyl) purines of formula (I) are new. In (I), R1 and R2 are both -C(O)R7 in which R7 is 1-adamantyl; R3 is NH2 a R6 is H or NH2 and R4 with R5 is a bond or b R5 with R6 is keto and R4 is H. Esp. cpd. is 9-(1,3-di(1-adamantyl carboxy)-2-propoxy methyl)guanine. (I) may be prepd. e.g. by esterifying cpds. (X) and (IV). |
