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A pharmaceutical composition, a process for treatment of HIV and prevention of HIV infection in a human, and process for production of a composition

机译:药物组合物,用于在人中治疗HIV和预防HIV感染的方法以及用于生产组合物的方法

摘要

Compositions for the treatment of AIDS and ARC having the following compound as an active ingredient: IMAGE where R1 is OH, monophosphate, diphosphate, or triphosphate; or a pharmacologically acceptable salt thereof. The primary advantage of this compound is its highly selective anti-retroviral activity, i.e., it significantly decreases viral replication as measured as reverse transcriptase activity while demonstrating orders of magnitude less cytotoxicity than other anti-viral compounds such as AZT. In a preferred embodiment, the compound is present in an amount sufficient to inhibit the HIV reverse transcriptase activity but not significantly inhibit human DNA polymerase activity. Also included within the scope of this invention are 3'-azido-2',3'-dideoxyuridine mono-, di-, and triphosphate and compositions containing these compounds as the active agent.
机译:具有以下化合物作为活性成分的用于AIDS和ARC的治疗组合物:<IMAGE>其中R 1为OH,一磷酸,二磷酸或三磷酸;或其药理学上可接受的盐。该化合物的主要优点是其高度选择性的抗逆转录病毒活性,即,以逆转录酶活性衡量,它显着降低了病毒复制,同时显示出比其他抗病毒化合物(如AZT)低几个数量级的细胞毒性。在一个优选的实施方案中,化合物以足以抑制HIV逆转录酶活性但不显着抑制人DNA聚合酶活性的量存在。 3'-叠氮基-2',3'-二脱氧尿苷单,二和三磷酸酯以及包含这些化合物作为活性剂的组合物也包括在本发明的范围内。

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