CAS: 252917-06-9; 6-((2-((4-(2,4-Dichlorophenyl)-5-(5-Methyl-1H-Imidazol-2-yl)Pyrimidin-2-yl)Amino)Ethyl)Amino)Nicotinonitrile

2,4-二甲基咪唑置于盐酸,Sodium Ethanolate,溶剂黄146,N,N-二异丙基乙胺体系中,用 乙醇,二氯甲烷,水 用作溶剂,化学反应 11.5H,反应生成6-[[2-[[4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)-2-嘧啶]氨基]乙基]氨基]-3-吡啶甲腈
参考文献:糖原合酶激酶3的强效和选择性(5-咪唑-2-基-4-苯基嘧啶-2-基)[2-(2-吡啶基氨基)乙基]胺抑制剂的合成,结合模式和降血糖活性
标题:糖原合酶激酶3的强效和选择性(5-咪唑-2-基-4-苯基嘧啶-2-基)[2-(2-吡啶基氨基)乙基]胺抑制剂的合成,结合模式和降血糖活性
摘要:为了鉴定新的抗糖尿病药,我们发现了一种新型的(5-咪唑-2--2-基-4-苯基嘧啶-2-基)[2-(2-吡啶基氨基)乙基]胺类似物,它们是人类的抑制剂.糖原合酶激酶3(gsk3).我们开发了有效的合成路线来探索各种取代模式,并会聚各种类似物.化合物1(chir-911,Ct-99021或chir-73911)来自对c-5位置的杂环,C-4的苯基以及c处连接的各种不同取代的连接基和氨基吡啶部分的探索-2位置.这些化合物表现出gsk3 Ic 50在低纳摩尔范围内和出色的选择性.它们激活表达胰岛素受体的cho-Ir细胞和原代大鼠肝细胞中的糖原合酶.在2型糖尿病的啮齿动物模型中对先导化合物1和2(chir-611或ct-98014)的评估表明,单次口服剂量可在60分钟内降低高血糖症,增强胰岛素刺激的葡萄糖转运,并改善葡萄糖的处置而不增加胰岛素水平.
Doi:10.1021/acs.Jmedchem.7B00922

专利信息

专利号:US-2025043248-A1
优先权日:2023-08-04
标题:Preparation method and use of hydrogel material for growth of blood vessel organoids
发明人：SUN DI; SUN JIAMING; WANG ZHENXING; LEI SHIZE
权利人:UNION HOSPITAL TONGJI MEDICAL COLLEGE HUST
摘要:The present disclosure provides a preparation method and use of a hydrogel material for growth of blood vessel organoids (BVOs). The preparation method of the hydrogel material includes: (1) synthesis of gelatin methacryloyl (GelMA), and (2) synthesis of ns-GelMA-PEO. The hydrogel material may be used for in vitro cultivation of BVOs. The hydrogel material ns-GelMA-PEO prepared by the present disclosure may significantly improve the survival and budding abilities of BVOs. The ns-GelMA-PEO provides a novel solution for in vitro cultivation of BVOs, and may well support the growth and differentiation of organoids.

专利号:WO-2022191130-A1
优先权日:2021-03-08
标 题:Method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent
发明人：YAMASHITA JUN; YOSHIOKA MIKI
权利人:UNIV KYOTO
摘要:Provided are a method for proliferating cardiomyocytes, a method for producing cardiomyocytes, and a cardiomyocyte proliferating agent capable of contributing to cardiac regenerative medicine, that make it possible to induce proliferation of human cardiomyocytes by a drug. The method for proliferating cardiomyocytes, method for producing cardiomyocytes, and cardiomyocyte proliferating agent, including a step for culturing cardiomyocytes in the presence of one or more compounds selected from the group consisting of ALK inhibitors, cytochrome P450 omega hydroxylase inhibitors, and fatty acid synthesis inhibitors