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Expert Opin Ther Pat. 2014 Jan;24(1):121-5. doi: 10.1517/13543776.2014.851670. Epub 2013 Oct 23.
A series of pyrrolo[2,3-d]pyrimidine derivatives have previously been claimed as Janus kinase (JAK) 1 selective inhibitors. Introduction of a 4-aryl substituent onto this bicyclic scaffold modulates the JAK selectivity profile, thus providing JAK3 selective inhibitors. This patent application claims such compounds as JAK3 inhibitors. Many of the compounds exemplified show > 100,000-fold selectivity for JAK3 over JAK2. The inhibitors are claimed to be useful in the treatment of respiratory diseases, arthritis and cancer.
先前已有报道称,一系列吡咯并[2,3-d]嘧啶衍生物为 Janus 激酶(JAK)1 选择性抑制剂。在该双环骨架上引入 4-芳基取代基可调节 JAK 选择性谱,从而提供 JAK3 选择性抑制剂。本专利申请要求将此类化合物作为 JAK3 抑制剂。所举例说明的许多化合物对 JAK3 的选择性超过 JAK2 超过 100,000 倍。据称,这些抑制剂可用于治疗呼吸道疾病、关节炎和癌症。