CAS: 23002-51-9; 6-Chloro-1H-Pyrazolo[3,4-D]Pyrimidine

相似化合物

42754-96-1 871254-63-6 1547960-36-0

上下游产品

CAS号871254-61-4 2,4-二氯-5-嘧啶甲醛

📜2,4-二氯-5-嘧啶甲醛置于一水合肼体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,以44%的收率获得6-氯-1H-吡唑并[3,4-D]嘧啶
参考文献:Discovery Of Novel Dual Extracellular Regulated Protein Kinases (Erk) And Phosphoinositide 3-Kinase (Pi3K) Inhibitors As A Promising Strategy For Cancer Therapy
标题:Discovery Of Novel Dual Extracellular Regulated Protein Kinases (Erk) And Phosphoinositide 3-Kinase (Pi3K) Inhibitors As A Promising Strategy For Cancer Therapy
摘要:Mapk和pi3K信号通路的同时抑制已被认为是癌症治疗的一种有前途的策略,可以有效地克服mapk信号通路相关抑制剂的药物抗性.在这里,我们报告了一系列1H-吡唑[3,4-D]嘧啶双erk/pi3K抑制剂的骨架跳跃生成.化合物32D是最有前途的候选药物,对erk2和pi3Kα均具有强大的抑制活性,对hct116和hec1B癌细胞显示出优越的抗增殖特性.与此同时,化合物32D具有可接受的药代动力学特性,并且在hct-116移植瘤模型中显示出比gddc-0980和相应的药物组合(bvd-523 + Gddc-0980)更有效的抗肿瘤活性,肿瘤生长抑制率为51%,且没有造成明显的毒性效应.所有结果表明,32D是一种高效的抗癌化合物,并为进一步优化向双erk/pi3K抑制剂提供了有前途的基础.
Doi:10.3390/molecules25235693

专利信息

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.