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    • 8. 发明申请
    • Nobel compounds having selective inhibiting effect at gsk3
    • 诺贝尔化合物在gsk3具有选择性抑制作用
    • US20060116362A1
    • 2006-06-01
    • US10539543
    • 2003-12-15
    • Stefan BergSven HellbergPeter Soderman
    • Stefan BergSven HellbergPeter Soderman
    • A61K31/497A61K31/4965C07D403/02C07D241/26
    • C07D401/12
    • The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclicc ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
    • 本发明涉及新的式(I)化合物,其中:Z是N,X是CH或N; Y为CONR 5; P是苯基或含有一个或多个选自N,O或S的杂原子的5或6元杂芳环; Q是苯基或含有一个或多个氮原子的5或6元芳族杂环环; R是C 1-6烷基,R 10,或C 1-6烷基氮杂环丁烷; R 10是氢,C 1-6烷基,C 2-6 - 烯基,C 2-6 - 炔基 ,C 0-6-6烷基C 3-6环烷基,C 0-6烷基芳基,C 0-6-烷基杂芳基 或C 1-6烷基N R 8 R 9; R 11是C 1-6烷基,R 8,R 9,C 0-6, 烷基C 3-6环烷基或C 0-6-6烷基杂环烷基; 作为其盐的游离碱或其药学上可接受的盐,溶剂化物或溶剂化物,其制备方法和其中使用的新中间体,含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。