首页> 外国专利> Substituted 3amp;prime;,4amp;prime;-di-O-camphanoyl-(amp;plus;)-cis-khellactone analogs, compositions thereof, and methods for using thereof

Substituted 3amp;prime;,4amp;prime;-di-O-camphanoyl-(amp;plus;)-cis-khellactone analogs, compositions thereof, and methods for using thereof

机译:取代的3′,4′ -di-O-樟脑酰基-(&plus)-顺式-甲壳酮类似物,其组合物及其使用方法

摘要

3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: embedded image;or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.
机译:已经发现根据本发明的3′,4′-二-O-樟脑酰基-(+)-顺式-甲壳酮类似物具有抗HIV活性。本发明的化合物具有下式:<化学id =“ CHEM-US-00001”> <图像alt =“嵌入式图像” file =“ US06768007-20040727-C00001.GIF” he =“ 163.21095” id =“ EMI-C00001“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 166.10265“ /> ;或其药学上可接受的盐,酯或前药,其中R 规格中设置了1 ,R 2 ,R 3 ,R 4 ,X和Z。本发明还涉及药物组合物,其包含一种或多种式I的化合物,任选地进一步包含一种或多种抗病毒剂或免疫刺激剂。此外,本发明涉及式I化合物在抑制动物细胞或组织中的逆转录病毒感染,治疗患有逆转录病毒相关病理的患者,预防HIV传播中的用途。从感染了HIV的孕妇到胎儿的感染,并防止在性交期间传播HIV感染。

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