CAS: 1228013-15-7; 1-Ethyl-7-(2-Methyl-6-(1H-1,2,4-Triazol-5-yl)Pyridin-3-yl)-3,4-Dihydropyrazino[2,3-B]Pyrazin-2(1H)-One

📜Ethyl 2-(5-Bromo-3-(Ethylamino)Pyrazin-2-Ylamino)Acetate置于盐酸,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,溶剂黄146体系中,用 1,4-二氧六环,甲醇,水 用作溶剂,化学反应 20.33H,反应生成1-乙基-7-[2-甲基-6-(4H-1,2,4-三唑-3-基)吡啶-3-基]-3,4-二氢吡嗪并[2,3-B]吡嗪-2(1H)-酮
参考文献:Optimization Of A Series Of Triazole Containing Mammalian Target Of Rapamycin (Mtor) Kinase Inhibitors And The Discovery Of Cc-115
标题:Optimization Of A Series Of Triazole Containing Mammalian Target Of Rapamycin (Mtor) Kinase Inhibitors And The Discovery Of Cc-115
摘要:We Report Here The Synthesis And Structure Activity Relationship (Sar) Of A Novel Series Of Triazole Containing Mammalian Target Of Rapamycin (Mtor) Kinase Inhibitors. Sar Studies Examining The Potency,Selectivity,And Pk Parameters For A Series Of Triazole Containing 4,6-Or 1,7-Disubstituted-3,4-Dihydropyrazino[2,3-B]Pyrazine-2(1H)-Ones Resulted In The Identification Of Triazole Containing Mtor Kinase Inhibitors With Improved Pk Properties. Potent Compounds From This Series Were Found To Block Both Mtorc1(P56) And Mtorc2(Pakts473) Signaling In Pc-3 Cancer Cells,In Vitro And In Vivo. When Assessed In Efficacy Models,Analogs Exhibited Dose-Dependent Efficacy In Tumor Xenograft Models. This Work Resulted In The Selection Of Cc-115 For Clinical Development.
Doi:10.1021/acs.Jmedchem.5B00627

专利信息

专利号:EP-3103803-B1
优先权日:2008-10-27
标 题 :Intermediates for the synthesis of mtor kinase inhibitors

专利号:EP-3660020-A1
优先权日:2008-10-27
标题 :Process for the synthesis of mtor kinase inhibitors

专利号:ES-2794012-T3
优先权日:2008-10-27
标题 :Intermediaries for the synthesis of mTOR kinase inhibitors

专利号:EP-3103803-A1
优先权日:2008-10-27
标 题 :Intermediates for the synthesis of mtor kinase inhibitors

专利号:EP-3660020-B1
优先权日:2008-10-27
标题:Process for the synthesis of mtor kinase inhibitors

专利号:EP-3091021-B1
优先权日:2009-10-26
标题:Methods of synthesis and purification of heteroaryl compounds