CAS: 444902-32-3; 6-Chloro-5-Iodopyridin-3-Amine

相似化合物

25391-60-0 426463-09-4 351227-42-4

上下游产品

CAS号25391-60-0 2-氯-3-碘-5-硝基吡啶 | CAS号5418-51-9 2-羟基-5-硝基吡啶 | CAS号7439-89-6 铁粉 | CAS号25391-58-6 3-碘-2-羟基-5-硝基吡啶 | CAS号444902-34-5 6-氯-5-碘-3-吡啶醇

📜2-羟基-5-硝基吡啶置于喹啉,碘,铁粉,Potassium Carbonate,溶剂黄146,三氯氧磷体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 10.0H,反应生成 5-氨基-2-氯-3-碘吡啶
参考文献:合成和评估一系列新型的2-氯-5-((1-甲基-2-(S)-吡咯烷基)甲氧基)-3-(2-(4-吡啶基)乙烯基)吡啶类似物作为潜在的正电子发射断层扫描烟碱乙酰胆碱受体的显像剂.
标题:合成和评估一系列新型的2-氯-5-((1-甲基-2-(S)-吡咯烷基)甲氧基)-3-(2-(4-吡啶基)乙烯基)吡啶类似物作为潜在的正电子发射断层扫描烟碱乙酰胆碱受体的显像剂.
摘要:据报道,2-[((18)f] Fluoro-A-85380,1是一种很有前途的放射性示踪剂,可通过正电子发射断层扫描(pet)对人的烟碱型乙酰胆碱受体(nachr)进行成像,它显示出穿过血脑屏障的缓慢渗透(Bbb)由于其低亲脂性.亲脂性大于1的nachrs配体由于nbchr可以更快地穿透bbb,因此可能对pet成像更有利.在此,基于对nachr的高亲和力配体,2-氯-5-((1-甲基-2-(S)-吡咯烷基)甲氧基)-3-(2-(4-吡啶基)乙烯基)吡啶,3B.发现该新系列的体外结合亲和力在k(i)= 9-331Pm的范围内.分子建模研究表明,这些化合物的构型和电子特性存在差异,这提供了对nachr的构效关系的进一步了解.已经发现化合物3B-6B的亲脂性明显高于1.结果,化合物3B-6B的亲脂性可能比亲脂性较低的1更快地穿过bbb.n-甲基衍生物3B和6B证明了在nachrs处具有非常高的亲和力(分别为k(i)=
DOI:10.1021/jm010550N

专利信息

专利号:WO-2023071314-A1
优先权日:2021-10-29
标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound

专利号:US-12331058-B2
优先权日:2021-10-29
标 题:SHP2 and CDK4/6 dual-target inhibitory compound and pharmaceutical composition containing the same
发明人：WU XIAOXING; CHEN XIAOYU; LI WENQIANG; Shu Chengxia; LUO GUANGMEI; YANG KEXIN
权利人:UNIV CHINA PHARMA
摘要:The present invention belongs to the field of medicinal chemistry, and particularly relates to synthesis, a preparation method and the use of an inhibitor containing dual targets SHP2 and CDK4/6, wherein the inhibitor comprises three compounds of general formulas I-III and pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs thereof. According to the present invention, a class of brand-new SHP2 and CDK4/6 dual-target inhibitors are prepared by means of a pharmacophore fusion and reasonable drug design method, so that the problems of drug resistance, poor drug effect, etc., of the existing SHP2 inhibitor and CDK4/6 inhibitor are solved; the great significance of the present invention is providing the first SHP2 and CDK4/6 dual-target inhibitor, which provides a basis for solving the problem of drug resistance of kinase and phosphatase in the later period.

专利号:EP-4410794-A1
优先权日:2021-10-29
标题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound

专利号:CA-3236558-A1
优先权日:2021-10-29
标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound