7-位取代吡咯并三嗪类化合物或其药学上可用的盐,及其制备方法和用途

文档序号:1409151 发布日期:2020-03-06 浏览:13次 >En<

阅读说明:本技术 7-位取代吡咯并三嗪类化合物或其药学上可用的盐,及其制备方法和用途 (7-substituted pyrrolotriazine compound or pharmaceutically acceptable salt thereof, and preparation method and application thereof ) 是由 杨春皓 蒙凌华 向皞月 李京 张希 王祥 谭村 贺茜 丁健 陈奕 于 2018-06-22 设计创作,主要内容包括:本发明涉7-位取代吡咯[2,1-f][1,2,4]并三嗪类化合物或其药学上可用的盐,及其制备方法和用途。该类化合物显示较好的PI3K抑制活性,能有效地抑制PI3K激酶活性,并且由于7-位基团的引入,生物利用度等药代动力学性质有较大提高和改善;此外,本发明中的化合物表现出了对PI3Kδ不可预期的高选择性和强抑制活性,因此这些化合物能用来治疗与PI3K通道相关的疾病,尤其是用来抗癌或者治疗肿瘤、白血病及自身免疫性疾病。经过进一步的优化和筛选后,有望研发成为新型的抗肿瘤药物。(The invention relates to a 7-substituted pyrrole [2,1-f ] [1,2,4] triazine compound or pharmaceutically usable salt thereof, and a preparation method and application thereof. The compound shows better PI3K inhibitory activity, can effectively inhibit PI3K kinase activity, and greatly improves and improves the pharmacokinetic properties such as bioavailability and the like due to the introduction of a 7-site group; in addition, the compounds of the present invention exhibit unexpectedly high selectivity and strong inhibitory activity against PI3K δ, and thus can be used for the treatment of diseases associated with PI3K channel, especially for the treatment of cancer or for the treatment of tumors, leukemia and autoimmune diseases. After further optimization and screening, the compound is expected to be developed into a novel anti-tumor medicament.)

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