专利号:WO-2023071314-A1 优先权日:2021-10-29 标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:US-12331058-B2 优先权日:2021-10-29 标 题:SHP2 and CDK4/6 dual-target inhibitory compound and pharmaceutical composition containing the same 发明人:WU XIAOXING; CHEN XIAOYU; LI WENQIANG; Shu Chengxia; LUO GUANGMEI; YANG KEXIN 权利人:UNIV CHINA PHARMA 摘要:The present invention belongs to the field of medicinal chemistry, and particularly relates to synthesis, a preparation method and the use of an inhibitor containing dual targets SHP2 and CDK4/6, wherein the inhibitor comprises three compounds of general formulas I-III and pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs thereof. According to the present invention, a class of brand-new SHP2 and CDK4/6 dual-target inhibitors are prepared by means of a pharmacophore fusion and reasonable drug design method, so that the problems of drug resistance, poor drug effect, etc., of the existing SHP2 inhibitor and CDK4/6 inhibitor are solved; the great significance of the present invention is providing the first SHP2 and CDK4/6 dual-target inhibitor, which provides a basis for solving the problem of drug resistance of kinase and phosphatase in the later period.
专利号:EP-4410794-A1 优先权日:2021-10-29 标题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:CA-3236558-A1 优先权日:2021-10-29 标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:CN-117143026-A 优先权日:2023-08-31 标题:A kind of synthesis method of heteroaryl trifluoromethyl compound
专利号:US-10858359-B2 优先权日:2016-06-07 标题 :Heterocyclic ring derivatives useful as SHP2 inhibitors 发明人:MA CUNBO; GAO PANLIANG; CHU JIE; WU XINPING; WEN CHUNWEI; KANG DI; BAI JINLONG; PEI XIAOYAN 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:Provided are certain novel pyrazine derivatives (I) as SHP2 inhibitors which is shown as formula (I), their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided are fused heterocyclic derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
参考文献:10.1016/j.str.2025.07.016 摘要:Hope I, Martin MP, Jiang Z, Waring MJ, Noble MEM, Endicott JA, Tatum NJ. Crystallographic fragment screening of CDK2-cyclin A: FragLites map sites of protein-protein interaction. Structure. 2025 Nov 06;33(11):1971–1983.e3. doi: 10.1016/j.str.2025.07.016. 参考文献:10.1038/s41556-025-01833-4 摘要:Scourzic L, Izzo F, Teater M, Polyzos AP, Cucereavii L, Chin CR, Papin A, Pinto HB, Mlynarczyk C, Tsialta I, Xia M, Lidoski A, Myers RM, Israel EM, Venturutti L, Mackay SP, Hoehn KB, Skoultchi AI, Béguelin W, Stadtfeld M, Chen Z, Landau DA, Melnick AM, Apostolou E. T follicular helper cells transiently unlock a plasticity state in germinal centre B cells during the humoral immune response. Nat Cell Biol. 2025 Dec 29;28(1):35–48. doi: 10.1038/s41556-025-01833-4.