CAS: 14631-08-4; 2-Chloropyrimidine-4,5-Diamine

相似化合物

1920-66-7 130838-36-7 13754-19-3

上下游产品

CAS号1920-66-7 4-氨基-2-氯-5-硝基嘧啶 | CAS号14159-38-7 2-chloro-6,7-di... | CAS号1681-15-8 2-氯嘌呤 | CAS号13754-19-3 4,5-二氨基嘧啶

2-氯-4-氨基-5-硝基嘧啶置于铁粉,氯化铵体系中,用 四氢呋喃,乙醇,水 用作溶剂,以33%的收率获得2-氯-4,5-二氨基嘧啶
参考文献:新型pi3Ka抑制剂的设计,合成,抗肿瘤活性和理论计算.
标题:新型pi3Ka抑制剂的设计,合成,抗肿瘤活性和理论计算.
摘要:Pi3Kα已被确定为治疗pik3Ca基因突变疾病的理想靶标,包括alpelisib和copanlisib等药物.设计并合成了五个嘌呤类似物和四个噻唑类似物.分别测试了它们对pi3Ka /β/γ/δ的酶活性.所有化合物在调节pi3Ka活性上均表现出优异的选择性,部分化合物具有非常好的抑制作用.同时,我们使用autodock 4.2探索最有潜力的化合物tg与目标蛋白的结合模式.此外,Dft用于计算化合物tf,Tg和阳性对照的homo-Lumo图.本文将为pi3Kα抑制剂的进一步药物设计提供一些有用的信息.
Doi:10.1016/j.Bioorg.2020.103737

专利信息

专利号:US-2009318476-A1
优先权日:2006-08-09
标 题 :Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人：RAMTOHUL YEEMAM K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).

专利号:US-2010197692-A1
优先权日:2007-07-20
标 题 :Bicyclic heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：RAMTOHUL YEEMAN K; LI CHUN SING; LECLERC JEAN-PHILIPPE
权利人:MERCK FROSST CANADA LTD
摘要:Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.