Novel Orthopox Small Molecule Anti-Virals

说明(申请人提供)：确定能够治疗或阻止由正痘病毒引起的天花或其他疾病传播的制剂，将极大地减少正肢病毒被用作生物武器的风险。此外，对于意外接触其他正痘病毒，例如最近公布的由人类接触外来进口动物引起的猴痘病例，这些制剂将是有用的治疗药物。理想的治疗方法是一种有效和安全的口服小分子药物，暴露于正畸病毒或患有活动性疾病的人可以服用这种药物。最近的证据表明，正畸病毒基因组编码的一种新的蛋白水解酶的活性是病毒增殖的必备事件。TransTech Pharma利用一种名为TTP Translational Technology TM的专利药物发现过程，该过程将新型药物化学与计算机建模和一系列体外生物筛选分析相结合，建议发现在效力、安全性和药代动力学特征方面具有类似药物特性的正极蛋白水解酶的小分子抑制剂，作为开发用于治疗正极病毒引起的感染的治疗性抗病毒药物的第一步。

DESCRIPTION (provided by applicant): The identification of agents that can either treat or halt the spread of smallpox or other diseases caused by orthopox viruses would have great benefit in mitigating the risk of the orthopox virus being used as a biological weapon. Furthermore such agents would be useful as a therapeutic for accidental exposure to other orthopox viruses such as the recently publicized cases of monkey pox caused by human exposure to exotic imported animals. The ideal therapeutic would be an effective and safe orally available small molecule that could be taken by individuals who were exposed to an orthopox virus or had active disease. Recent evidence suggests that the proteolytic activity of a novel protease encoded by the orthopox virus genome is an obligatory event for viral proliferation. Using a proprietary process of drug discovery called TTP Translational Technology TM that combines novel medicinal chemistry with computer modeling and a series of in vitro biological screening assays, TransTech Pharma proposes to discover small molecule inhibitors of the orthopox protease that have drug like characteristics in terms of potency, safety and pharmacokinetic characteristics as a first step in developing a therapeutic anti-viral for the treatment of infections caused by the orthopox virus.