首页> 外国专利> compounds of formulas (i) and (ii), method of treating hiv-1, hiv-2, hbv or hcv infected host, method of preventing hiv-1, hiv-2, hbv or hcv infection, method for reduce biological activity of hiv-1, hiv-2, hbv or hcv infection and pharmaceutical composition

compounds of formulas (i) and (ii), method of treating hiv-1, hiv-2, hbv or hcv infected host, method of preventing hiv-1, hiv-2, hbv or hcv infection, method for reduce biological activity of hiv-1, hiv-2, hbv or hcv infection and pharmaceutical composition

机译:式(i)和(ii)的化合物,治疗HIV-1,HIV-2,HBV或HCV感染的宿主的方法,预防HIV-1,HIV-2,HBV或HCV感染的方法,降低其生物学活性的方法HIV-1,HIV-2,HBV或HCV感染和药物组合物

摘要

The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, HBV, and HCV, in human patients or other animal hosts. The compounds are 3-azido-2,3-dideoxy purine nucleosides or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 resistance mutants including HIV-1K65R, HTV-1K70E, HIV-1L74V, HIV-1M184V, HIV-1Q151M and inhibitory activity against HIV-1 RT harboring TAMS or insertion mutations including HIV-1AZT3, HIV-1AZT7, HIV-1AZT9, HIV-1Q151M, or HIV-169insertion. In one embodiment, the compounds are 3-azido-ddA, 3-azido-ddG, or combinations thereof, administered with one or more additional antiviral agents that select for TAM mutations and/or the M 184V mutation, along with a pharmaceutically acceptable carrier.
机译:本发明涉及用于治疗或预防人类患者或其他动物宿主中的病毒感染,尤其是HIV,HBV和HCV的化合物,组合物和方法。该化合物是3-叠氮基-2,3-二脱氧嘌呤核苷或膦酸酯,及其药学上可接受的盐,前药和其他衍生物。尤其是,这些化合物对HIV-1耐药突变体(包括HIV-1K65R,HTV-1K70E,HIV-1L74V,HIV-1M184V,HIV-1Q151M)显示出有效的抗病毒活性,并且对带有TAMS或包含HIV的插入突变的HIV-1 RT具有抑制活性-1AZT3,HIV-1AZT7,HIV-1AZT9,HIV-1Q151M或HIV-169插入。在一个实施方案中,化合物是3-叠氮基-ddA,3-叠氮基-ddG或其组合,与一种或多种选择TAM突变和/或M 184V突变的其他抗病毒剂以及药学上可接受的载体一起给药。

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