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Substituted-2'-deoxy-4'-azido nucleosides, processes for their preparation and pharmaceutical composition containing the same

机译:取代的2'-脱氧-4'-叠氮核苷,其制备方法和含有该核苷的药物组合物

摘要

Nucleoside compounds of the formula CHEM wherein: B is guanine, adenine, thymine, uracil, cytosine, hypoxanthine, xanthine, 5-methylcytosine, 4-ethoxy-5-methyl-2-oxo-pyrimidine, 4-isopropoxy-5-methyl-2-oxo-pyrimidine, or 5-methyl-2-oxo-pyrimidine; X is H or F; Y min is H, OH, OCH3 or F; and Z is CHEM or (R min O) @@-CH2- where n is zero, one, or three and both R min are hydrogen or lower alkyl; or Y min and Z together form a cyclic phosphate ester; and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.
机译:的核苷化合物,其中:B为鸟嘌呤,腺嘌呤,胸腺嘧啶,尿嘧啶,胞嘧啶,次黄嘌呤,黄嘌呤,5-甲基胞嘧啶,4-乙氧基-5-甲基-2-氧代嘧啶,4-异丙氧基-5-甲基-2-氧代嘧啶或5-甲基-2-氧代嘧啶; X为H或F; Y min为H,OH,OCH3或F; Z为或(R min O)@-CH 2-,其中n为零,一或三,且R min均为氢或低级烷基; Ymin和Z一起形成环状磷酸酯;已经发现其药学上可接受的酯,醚和盐具有有效的抗病毒活性,并且具有很高的治疗率。

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