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NEW DISPIRO-INDOLINONES, MDM2/p53 INTERACTION INHIBITORS, METHOD FOR PRODUCTION AND APPLICATION

机译:新型双螺茚酸酯,MDM2 / p53相互作用抑制剂,生产方法和应用

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to new derivatives of formula 1 dispiro-indolinones or pharmaceutically acceptable salts thereof, or optical isomers, where R1 is selected from the group including phenyl optionally substituted with 1-2 substituents selected from halogen atom, lower alkoxy group; R2 is selected from the group consisting of hydrogen, unsubstituted pyridyl or phenyl optionally substituted with a substituent selected from halogen, lower alkoxy, C1-C6alkyl or -O-C5cycloalkyl; R3 is selected from the group incuding a hydrogen or halogen atom; R4 represents C1-C5alkyl; R5 is selected from the group consisting of hydrogen, methyl or propargyl HC≡C-CH2-. The invention also relates to the active ingredient, based on formula 1 compounda, pharmaceutical composition based of the said active ingredient, a drug based on this active ingredient or pharmaceutical composition, method for MDM2/p53 protein-protein interaction inhibition.;EFFECT: new dispiro-indolinone derivatives are obtained, that are useful for cancer treatment.;10 cl, 1 tbl, 15 ex
机译:技术领域本发明涉及式1的新衍生物。<图像文件=“ 00000016.JPG” he =“ 70” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 63” /> dispiro-indolinones或或其药学上可接受的盐,或旋光异构体,其中R Sub 1选自任选被1-2个选自卤素原子,低级烷氧基的取代基取代的苯基; R 2 选自氢,未取代的吡啶基或任选地被选自卤素,低级烷氧基,C 1 -C 6 <的取代基取代的苯基。 / Sub>烷基或-OC 5 环烷基; R 3 选自氢或卤素原子; R 4 代表C 1 -C 5 烷基; R 5 选自氢,甲基或炔丙基HC≡C-CH 2 -。本发明还涉及基于式1化合物的活性成分,基于所述活性成分的药物组合物,基于该活性成分的药物或药物组合物,抑制MDM2 / p53蛋白-蛋白相互作用的方法。获得双螺吲哚酮衍生物,可用于癌症治疗。; 10 cl,1 tbl,15 ex

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