CAS: 75755-10-1; (2-(Pyridin-3-yl)Ethane-1,1-Diyl)Bis(Phosphonic Acid)

相似化合物

105462-24-6 115436-72-1 924628-44-4

上下游产品

[2-(3-pyridyl)ethyl]-1,1-bis(diethylphosphonate) 3-picolyl bromide

📜3-溴甲基吡啶置于三甲基溴硅烷,Sodium Hydride体系中,化学反应生成 P,P'-[2-(3-吡啶基)亚乙基]二膦酸
参考文献:双膦酸盐激活γδt细胞的定量结构-活性关系.
标题:双膦酸盐激活γδt细胞的定量结构-活性关系.
摘要:γt细胞是抵御许多传染性生物的第一道防线,并且还参与肿瘤细胞的监视和杀死.它们受到各种各样的小型含磷抗原(磷酸抗原)以及骨吸收疗法中常用的双膦酸盐(如帕米膦酸盐和利塞膦酸盐)的刺激.在这里,我们报告了广泛的双膦酸酯对γ-δt细胞的激活,并开发了γ-δt细胞激活的药效团模型,此外还使用了比较分子相似性指数分析(comsia)方法来对γ-δt细胞激活之间进行定量关系由双膦酸酯及其三维结构组成.comsia分析得出的r(2)值约为0.8-0.9,Q(2)值约为0.5-0.6个,用于一组45种化合物的训练.使用外部测试集,平均预测了16种化合物的活性(ic(50)值)在4.5倍之内.comsia场由大约40%的疏水性,大约40%的静电性和大约20%的空间相互作用组成.由于已知双膦酸盐是强效的甲羟戊酸/异戊二烯途径酶法尼基焦磷酸合酶(fpps)的纳摩尔抑制剂,因此,我们还使用catalyst程序比较
DOI:10.1021/jm0303709

专利信息

专利号:US-8431714-B2
优先权日:2007-04-16
标题:Synthesis of drug conjugates via reaction with epoxide-containing linkers
发明人：MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F
权利人:MCKENNA CHARLES E; KASHEMIROV BORIS A; BALA JOY LYNN F; UNIV SOUTHERN CALIFORNIA
摘要:The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.

专利号:US-2008312440-A1
优先权日:2007-04-16
标 题:Synthesis of drug conjugates via reaction with epoxide-containing linkers

专利号:US-2013203998-A1
优先权日:2007-04-16
标题:Synthesis of Drug Conjugates Via Reaction With Epoxide-Containing Linkers

专利号:RU-2086556-C1
优先权日:1990-12-20
标题:Methylene-bis-phosphonic acid derivatives and a method of their synthesis