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尽管用于药物开发的经费和时间逐年攀升,但近些年来被批准上市的新化学实体类药物却很少。随着计算化学学科的进展,辅助以X-射线晶体学和核磁共振技术,越来越多有前景的疾病治疗候选药物被发现。多种药物化学策略被发展用于药物早期评价研究。尽管如此,在药物开发的早期阶段,如何有效提高候选药物开发的成功率依然存在一些问题待解决。本文主要综述了药物开发早期阶段新化学实体发现和评价的代表性案例。
Although funding and time spent on drug development have been rising year by year, few new chemical entities have been approved for listing in recent years. As computational chemistry advances, more and more promising drug candidates for treatment of disease have been discovered, aided by X-ray crystallography and nuclear magnetic resonance (NMR) techniques. Multiple drug chemistry strategies have been developed for early drug evaluation studies. Nevertheless, there are still some problems to be solved on how to effectively improve the success rate of drug candidate development in the early stage of drug development. This article summarizes the representative cases of discovery and evaluation of new chemical entities in the early stages of drug development.