CAS: 2450-08-0; Methyl Pyrimidine-4-Carboxylate

上下游产品

methanol pyrimidine-4-carboxylic acid 4-Methylpyrimidine3-Oxo-3-pyrimidin-4-yl-propionic acid methyl ester 1-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-3-pyrimidin-4-yl-propan-1,3-dione pyrimidine-4-carboxylic acid hydrazide 2-chloro-3-methyl-6-(pyrimidin-4-yl)-pyrimidine-4-one

📜4-甲基嘧啶置于吡啶,Selenium(Iv) Oxide,硫酸体系中,化学反应 22.0H,反应生成嘧啶-4-甲酸甲酯
参考文献:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
标题:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
摘要:用于心力衰竭的一类新型治疗药物,高效和选择性的grk2抑制剂,在体外研究中表现出增强的β-肾上腺素信号传导能力.Hts将衍生物5和1,2,4-三唑衍生物24A鉴定为命中化合物.新一代的脚手架和所有部分的sar研究都产生了带有n-苄基羧酰胺部分的4-甲基-1,2,4-三唑衍生物,对grk2的活性很高,对其他激酶的选择性更高.在亚型选择性方面,这些化合物对grk1,5,6和7表现出足够的选择性,并且对grk3具有几乎相同的抑制作用.我们的药物化学努力导致发现了115H(grk2 Ic 50= 18 Nm),获得了与人grk2和grk2抑制剂的共晶体结构,该抑制剂增强了β-肾上腺素能受体(βar)介导的camp积累,并防止了用异丙肾上腺素处理过的表达β2Ar的hek293细胞中βar的内在化.因此,115H似乎是心力衰竭治疗的一种新型疗法.
Doi:10.1021/acs.Jmedchem.7B00443

专利信息

专利号:WO-2004111011-A2
优先权日:2003-05-30
标 题:Synthesis of 2-aryl pyrimidine 4-carboxylic acid amides

专利号:US-2008200475-A1
优先权日:2005-03-28
标题:4-Piperazinothieno[2,3-D] Pyrimidine Compounds As Platelet Aggregation Inhibitors
发明人：ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; TENBRINK RUTH ELIZABETH
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: (I) wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , X 4 , X 6 , R 2a , R x , R 4 , R 5 , and R 6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:CN-116874433-A
优先权日:2023-06-16
标 题:A kind of pyrimidine compound and its synthesis method and application