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Phosphono:methoxy:alkylene-purine and -pyrimidine derivs. - with antiviral activity against DNA viruses and retro:viruses

机译:膦基:甲氧基:亚烷基-嘌呤和-嘧啶衍生物。 -对DNA病毒和Retro:Virus具有抗病毒活性

摘要

Phosphono methoxyalkylene purine and pyrimidine derivs. of formula (I) and salts, zwitterions and/or solvates are claimed, where B = purine or pyrimidine base form adenine, xanthine, hypoxanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-aminoguanine, 8-hydroazinoguanine, 8-hydroxyguanine, 8-methylguanine, 8-thioguanine, 2-aminopurine, 2,6-diaminopurine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-bromouracil, 5-iodouracil, 5-ethyluracil, 5-propyluracil, 5-vinyluracil or 5-bromovinyluracil; A1-3 = a bond or 1-4C alkylene, provided that when B = adenine and A1 = CH2, then A2 is not a bond; Q = H or oH, provided that when B = adenine and Q = H, then A1 = -C4H8-; R1,R2 = H or 1-4C alkyl; and R3,R4 = H, 1-6C alkyl, phenyl or phenyl-1-4-C-alkylene. 18 cpds. (I) e.g. 9-(3-hydroxy-2 -(phosphonomethoxy propyl) guanine; 8-bromo-9-(2- (phosphonomethoxy) ethyl)guanine; 9-(2-hydroxymethyl -3-(phosphonomethoxy) propyl)adenine; and 1-(4-phosphonomethoxy) butyl)thymine are specifically claimed.
机译:膦氧基甲氧基亚烷基嘌呤和嘧啶衍生。要求保护式(I)的式(I)的化合物及其盐,两性离子和/或溶剂化物,其中B =嘌呤或嘧啶碱基形式的腺嘌呤,黄嘌呤,次黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-氨基鸟嘌呤,8-氢叠氮鸟嘌呤,8-羟基鸟嘌呤,8-甲基鸟嘌呤,8-硫鸟嘌呤,2-氨基嘌呤,2,6-二氨基嘌呤,胞嘧啶,5-乙基胞嘧啶,5-甲基胞嘧啶,胸腺嘧啶,尿嘧啶,5-溴尿嘧啶,5-碘尿嘧啶,5-乙基尿嘧啶,5-丙基尿嘧啶, 5-乙烯基尿嘧啶或5-溴乙烯基尿嘧啶; A1-3 =键或1-4C亚烷基,条件是当B =腺嘌呤且A1 = CH2时,则A2不是键; Q = H或oH,条件是当B =腺嘌呤且Q = H时,则A1 = -C4H8-; R1,R2 = H或1-4C烷基; R3,R4 = H,1-6C烷基,苯基或苯基1-4-4-C-亚烷基。 18 cpds。 (I)例如9-(3-羟基-2-(膦酰基甲氧基丙基)鸟嘌呤; 8-溴-9-(2-(膦酰基甲氧基)乙基)鸟嘌呤; 9-(2-羟基甲基-3-(膦酰基甲氧基)丙基)腺嘌呤;和1-特别要求保护(4-膦基甲氧基)丁基)胸腺嘧啶。

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