摘要
Janus激酶（JAKs）是一类非受体酪氨酸激酶，由四个成员JAK1，JAK2，JAK3和TYK2组成。 JAK通过激活JAK / STAT信号传导途径参与不同的炎症和自身免疫疾病以及恶性肿瘤。此外，JAK2中的V617F突变在受骨髓增生性肿瘤影响的患者中被鉴定。这一知识促使学术界和制药公司的研究人员研究这一领域，以发现小分子JAK抑制剂。这些努力最近得到了四种JAK抑制剂的市场认可。尽管所有这些药物都是吡咯并[2,3-d]嘧啶衍生物，但是在文献中已经报道了许多赋予不同杂环支架的化合物作为选择性或多JAK抑制剂，并且其中许多目前正在评估中。临床试验。在本综述中，我们将报告在过去五年（2013-2017期）中发表在文章或专利中的许多代表性化合物。抑制剂将根据其化学结构进行分类，在可能的情况下，重点关注其结构活性关系，选择性和生物活性。对于每类衍生物，还将简要报告2013年之前公开的已进入临床试验的化合物，以强调特定化学支架在寻找新抑制剂中的重要性。
关键词: JAK抑制剂，专利，抗癌剂，炎性疾病，自身免疫疾病，杂环化合物，共价抑制剂。
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