CAS: 42754-96-1; 4,6-Dichloro-1H-Pyrazolo[3,4-D]Pyrimidine

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2,4,6-三氯-5-嘧啶甲醛置于hydrazine Hydrate,三乙胺体系中,用 乙醇 作为反应溶剂,以71 %的收率获得产物4,6-二氯-1H-吡唑并[3,4-C]嘧啶
参考文献:具有 1H-吡唑并 [3,4-D] 嘧啶支架的强效 Plk4 抑制剂 Wy29 的设计,合成和生物学评价
标题:具有 1H-吡唑并 [3,4-D] 嘧啶支架的强效 Plk4 抑制剂 Wy29 的设计,合成和生物学评价
摘要:中心粒复制在每个细胞周期发生一次,并受 Polo 样激酶 4 (Plk4) 调节.plk4在体细胞中的过度表达会导致中心粒的过度形成,直接导致染色体分离错误和肿瘤发生.在这项研究中,我们描述了我们开发一系列具有 1 H-吡唑并 [3,4-D] 嘧啶核心的 Plk4 抑制剂的努力,并且进一步基于结构和受体的设计和优化产生了有效的抑制剂wy29 (Ic 50 = 0.027 μm),对其他 Plk 家族成员 (Plk1-3) 表现出非常好的选择性.在细胞水平上,化合物wy29对三种乳腺癌细胞系(mcf-7,Bt474 和 Mda-Mb-231)表现出优异的抗增殖活性,而对正常细胞系 Huvec 的抑制活性较弱.此外,化合物wy29的体外初步类药性评价表明,其在人血浆和肝微粒体中具有突出的稳定性,对人细胞色素p450的主要亚型具有较弱的抑制活性.此外,化合物wy29的类药性预测显示出显着的类药性(类药性模式评分:1
DOI:10.1002/ardp.202200490

专利信息

专利号:WO-2023086801-A1
优先权日:2021-11-09
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-2023010886-A1
优先权日:2019-09-23
标 题 :Shp2 inhibitors and uses thereof
发明人：XIE YINONG; BABISS LEE E
权利人:SUZHOU PUHE BIOPHARMA CO LTD
摘要:Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.

专利号:US-10561655-B2
优先权日:2018-03-21
标 题 :SHP2 inhibitors and uses thereof
发明人：XIE YINONG; BABISS LEE E
权利人:SYNBLIA THERAPEUTICS INC
摘要:Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.