Department of Pharmaceutical Sciences, Università del Piemonte Orientale, Largo Donegani 2, 28100 Novara, Italy.
J Med Chem. 2021 Apr 22;64(8):4410-4429. doi: 10.1021/acs.jmedchem.1c00181. Epub 2021 Apr 13.
The World Health Organization assigns international nonproprietary names (INN), also known as common names, to compounds upon request from drug developers. Structures of INNs are publicly available and represent a source, albeit underused, to understand trends in drug research and development. Here, we explain how a common drug name is composed and analyze chemical entities from 2000 to 2021. In the analysis, we describe some changes that intertwine chemical structure, newer therapeutic targets (e.g., kinases), including a significant increase in the use of fluorine and of heterocycles, and some other evolutionary modifications, such as the progressive increase in molecular weight. Alongside these, small signs of change can be spotted, such as the rise in spirocyclic scaffolds and small rings and the emergence of unconventional structural moieties that might forecast the future to come.
世界卫生组织(WHO)应药物开发商的请求,为化合物指定国际非专利名称(INN),又称通用名称。INN 的结构是公开的,虽然未被充分利用,但它是了解药物研究和开发趋势的一个来源。在这里,我们解释了通用药物名称的组成,并分析了 2000 年至 2021 年的化学实体。在分析中,我们描述了一些变化,这些变化交织着化学结构和更新的治疗靶点(如激酶),包括氟和杂环的使用显著增加,以及其他一些进化上的改变,如分子量的逐渐增加。除此之外,还可以发现一些微小的变化迹象,如螺环支架和小环的增加,以及非常规结构部分的出现,这些可能预示着未来的发展。