CAS: 16285-74-8; Thieno[3,2-D]Pyrimidin-4-Amine

相似化合物

1097040-23-7 16234-40-5 1301212-43-0

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CAS号16269-66-2 4-氯噻吩并[3,2-d]嘧啶

📜4-氯噻吩并[3,2-D]嘧啶置于ammonium Hydroxide体系中,用 乙醇 用作溶剂,化学反应 8.0H,以81.4%的收率获得4-氨基噻吩并[3,2-D]嘧啶
参考文献:新型kdr激酶抑制剂1-(4-氯-3-(三氟甲基)-苯基)-3-(2-(氨基)吡啶-3-基)脲的发现和优化
标题:新型kdr激酶抑制剂1-(4-氯-3-(三氟甲基)-苯基)-3-(2-(氨基)吡啶-3-基)脲的发现和优化
摘要:激酶插入物含域受体(kdr)是抗癌药物发现和开发的当前验证目标之一.在此,已经合成了一系列邻氨基-芳基脲衍生物,并评估了它们的激酶抑制活性.在生物学筛选和分子建模的基础上进行优化,与该命中化合物相比,可明显提高kdr激酶的抑制活性.最终,我们确定了针对kdr的1-(4-氯-3-(三氟甲基)苯基)-3-(2-((喹啉-4-基甲基)氨基)吡啶-3-基)脲支架的有效抑制剂5A( Ic 50 = 0.0689 µm),可以作为进一步优化kdr抑制剂和开发的非常好起点.
Doi:10.2174/1573406412666151215105149

专利信息

专利号:US-2008261823-A1
优先权日:2004-12-10
标 题 :Fluorescent Nucleoside Analogs That Mimic Naturally Occurring Nucleosides
发明人：TOR YITZHAK
权利人:TOR YITZHAK
摘要:The present invention provides fluorescent nucleoside analogs with conjugated membered heterocycles, including furan and thiophene. The fluorescent nucleoside analogs maintain structural similarity to naturally occurring nucleoside bases, mimicking shape, size, hybridization, and recognition properties. Incorporation of the fluorescent cyclic compounds confers specific photophysical characteristics including a bathochromic (red) shift of the absorption spectrum to minimize absorption overlap with naturally occurring nucleoside bases, and a shift to the long emission wavelength in the visible range. The invention also provides for various methods of synthesizing the fluorescent nucleoside analogs and incorporating the fluorescent analogs in DNA, RNA, or oligomer synthesis. Further, methods of detecting the fluorescent nucleoside analogs in an oligonucleotide or oligomer are provided. The subject compounds are useful as probes in the study of the structure and dynamics of nucleic acids and their complexes with proteins.

专利号:US-7648986-B2
优先权日:2002-01-10
标题:Substituted thieno[3,2-D]pyrimidines as Rho kinase inhibitors
发明人：NAGARATHNAM DHANAPALAN; KHIRE UDAY; ASGARI DAVOUD; SHAO JIANXING; LIU XIAO-GAO; WANG CHUNGUANG; HART BARRY; WEBER OLAF; LYNCH MARK; ZHANG LEI; WANG LEI
权利人:BAYER HEALTHCARE LLC
摘要:Disclosed are compounds and derivatives thereof their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.