CAS: 1920-66-7; 2-Chloro-5-Nitropyrimidin-4-Amine

相似化合物

14631-08-4 31221-68-8 2164-84-3

上下游产品

CAS号49845-33-2 2,4-二氯-5-硝基嘧啶 | CAS号7664-41-7 氨 | CAS号14623-58-6 2-巯基-4,5-二氨基嘧啶 | CAS号13754-19-3 4,5-二氨基嘧啶 | CAS号14631-08-4 2-氯-4,5-二氨基嘧啶 | CAS号18620-73-0 2,4-二氨基-5-硝基嘧啶 | CAS号124732-29-2 2-(4-methylpipe... | CAS号5096-83-3 N2-甲基-5-硝基嘧啶-2,4-二胺 | CAS号5096-84-4 N2,N2-二甲基-5-硝基-...

2,4-二氯-5 硝基嘧啶置于ammonium Hydroxide体系中,用 乙醇 用作溶剂,化学反应 2.92H,以85%的收率获得2-氯-4-氨基-5-硝基嘧啶
参考文献:氟吡汀和瑞替加滨的硫化物类似物,具有纳摩尔kv 7.2 / Kv 7.3通道开放活性.
标题:氟吡汀和瑞替加滨的硫化物类似物,具有纳摩尔kv 7.2 / Kv 7.3通道开放活性.
摘要:钾通道开放剂氟吡汀和瑞替加滨已被证明是有价值的镇痛药或抗癫痫药.它们最近分别由于偶发的肝毒性和组织变色而退出治疗,这使得治疗领域没有被填补.两种药物的代谢氧化都会导致亲电子醌的形成.在长期摄入瑞替加滨后发生氟吡汀和蓝色组织变色的情况下,这些难以捉摸的,高反应性的代谢物可能引起肝损伤.我们研究了可以改变哪些结构特征,以避免芳香环的有害氧化,并使氧化向更良性代谢物的形成转移.进行了结构活性关系研究,以评估45种衍生物的kv 7.2 / 3通道开放活性.鉴定出硫化物类似物没有形成醌的风险,但具有有效的kv 7.2 / 3打开活性.例如,氟吡汀类似物3-(3,5-二氟苯基)-N-(6-(异丁硫基)-2-(吡咯烷-1-基)吡啶-3-基)丙酰胺(48)具有100倍的增强活性( Ec50 = 1.4 Nm),大大提高了毒性/活性比,并具有与体外瑞替加滨相同的功效.
Doi:10.1002/cmdc.201900112

专利信息

专利号:WO-2025128848-A1
优先权日:2023-12-12
标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

专利号:US-7196090-B2
优先权日:2002-07-25
标题 :Kinase inhibitors
发明人：CONNOLLY CLEO J CHIVIKAS; DEUR CHRISTOPHER JAMES; HAMBY JAMES MARINO; HOYER DENTON WADE; LIMBERAKIS CHRIS; REED JESSICA ELIZABETH; SCHROEDER MEL CONRAD; TAYLOR CLARKE
权利人:WARNER LAMBERT CO
摘要:This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: n nthat inhibit cyclin-dependent kinase and tyrosine kinase enzymes, methods and intermediate compounds for their synthesis, as well as pharmaceutical compositions and methods for their use in treating, inhibiting or preventing maladies associated with cell proliferative disorders, including angiogenesis, atherosclerosis, restenosis, and cancer.