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    • 4. 发明公开
    • 6-번 위치에 아미노메틸기가 치환된3-하이드록시크로멘-4-온 구조를 갖는 사이클린 의존키나아제 저해제
    • CYPIN依赖性激酶(CDK)与6-位氨基甲酰基的3-羟基-4-酮结构的抑制剂
    • KR1020030064078A
    • 2003-07-31
    • KR1020020004512
    • 2002-01-25
    • 주식회사 엘지생명과학
    • 홍창용이진호이인상이성배김종현최세현김학중최환근김민형김정인홍상용
    • C07D413/06
    • PURPOSE: Inhibitors of cyclin dependent kinase(CDK) with a 3-hydroxychromen-4-one structure having aminomethyl group at 6-position are provided, thereby effectively inhibiting the activity of CDKs resulting in cancer. CONSTITUTION: Inhibitors of cyclin dependent kinase(CDK) with a 3-hydroxychromen-4-one structure having aminomethyl group at 6-position represented by the formula 1, and pharmaceutically acceptable salts, hydrate, solvate and isomers thereof are provided, wherein R1 and R2 are independently hydrogen or C1-C6 alkoxycarbonyl; 5 or 6 member ring heterocycle substituted or unsubstituted C1-C6 alkyl containing one or two hetero atoms selected from oxygen and nitrogen and optionally containing C1-C4 alkyl; 5 or 6 member ring heterocycle containing hydroxy, halogen or one or two hetero atoms selected from oxygen and nitrogen, and optionally containing C1-C4 alkyl, or one or two substituents which are selected from hydroxy-C1-C4 alkyl and C1-C4 alkyl substituted or unsubstituted amino substituted carbonyl-C1-C6 alkyl; 5 or 6 member ring heterocycle containing halogen, or one or two hetero atoms selected from oxygen and nitrogen, and optionally containing C1-C4 alkyl, or one or two substituents which are selected from hydroxy-C1-C4 alkyl and C1-C4 alkyl substituted or unsubstituted amino substituted or unsubstituted C1-C6 alkylcarbonyl; or R1 and R2 are 5 or 6 member ring heterocycle containing one or two hetero atoms selected from oxygen and nitrogen, and optionally containing C1-C4 alkyl together with substituted nitrogen; and R3 is halogen, amino substituted or unsubstituted phenyl, pyridine, C1-C4 alkyl substituted or unsubstituted piperidine, or pyridinium.
    • 目的:提供具有6-位氨基甲基的3-羟基色素-4-酮结构的细胞周期蛋白依赖性激酶(CDK)抑制剂,从而有效抑制导致癌症的CDKs的活性。 提供:具有由式1表示的6-位具有氨基甲基的3-羟基色烯-4-酮结构的细胞周期蛋白依赖性激酶(CDK)的抑制剂及其药学上可接受的盐,水合物,溶剂化物和异构体,其中R1和 R2独立地是氢或C1-C6烷氧基羰基; 5或6元环杂环取代或未取代的含有一个或两个选自氧和氮的杂原子和任选含有C 1 -C 4烷基的杂原子的C 1 -C 6烷基; 含有羟基,卤素或选自氧和氮的一个或两个杂原子,以及任选地含有C 1 -C 4烷基或选自羟基-C 1 -C 4烷基和C 1 -C 4烷基的一个或两个取代基的5或6元环杂环 取代或未取代的氨基取代的羰基-C 1 -C 6烷基; 含有卤素的5或6元环杂环,或选自氧和氮的一个或两个杂原子,以及任选地含有C 1 -C 4烷基或选自羟基-C 1 -C 4烷基和C 1 -C 4烷基取代的一个或两个取代基 或未取代的氨基取代或未取代的C 1 -C 6烷基羰基; 或R 1和R 2是含有一个或两个选自氧和氮的杂原子的5或6元环杂环,并且任选地含有C 1 -C 4烷基和取代的氮; 和R 3是卤素,氨基取代或未取代的苯基,吡啶,C 1 -C 4烷基取代或未取代的哌啶或吡啶鎓。