CAS: 1173204-81-3; Pki-402

上下游产品

1-methyl-piperazine 4-({[4-(3-ethyl-7-morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl]carbamoyl}amino)benzoic acid

📜N-甲基哌嗪,4-({[4-(3-Ethyl-7-Morpholin-4-Yl-3H-[1,2,3]Triazolo[4,5-D]Pyrimidin-5-yl)Phenyl]Carbamoyl}Amino)Benzoic Acid置于1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 四氢呋喃 用作溶剂,化学反应 6.0H,以79%的收率获得pki-402; 1-[4-[3-乙基-7-(吗啉-4-基)-3H-[1,2,3]三唑并[4,5-D]嘧啶-5-基]苯基]-3-[4-[(4-甲基哌嗪-1-基)羰基]苯基]脲
参考文献:Lead Optimization Of N-3-Substituted 7-Morpholinotriazolopyrimidines As Dual Phosphoinositide 3-Kinase/mammalian Target Of Rapamycin Inhibitors: Discovery Of Pki-402
标题:Lead Optimization Of N-3-Substituted 7-Morpholinotriazolopyrimidines As Dual Phosphoinositide 3-Kinase/mammalian Target Of Rapamycin Inhibitors: Discovery Of Pki-402
摘要:Herein We Describe The Identification And Lead Optimization Of Triazolopyrimidines As A Novel Class Of Potent Dual Pi3K/mtor Inhibitors,Resulting In The Discovery Of 3 (Pki-402). Compound 3 Exhibits Good Physical Properties And Pk Parameters,Low Nanomolar Potency Against Pi3K Alpha And Mtor,And Excellent Inhibition Of Cell Proliferation In Several Human Cancer Cell Lines. Furthermore,In Vitro And In Vivo Biomarker Studies Demonstrated The Ability Of 3 To Shut Down The Pi3K/akt Pathway And Induce Apoptosis In Cancer Cells. In Addition,3 Showed Excellent In Vivo Efficacy In Various Human Cancer Xenografts,Validating Suppression Of Pi3K/mtor Signaling As A Potential Anticancer Therapy.
Doi:10.1021/jm9014982

专利信息

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.