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    • 7. 发明授权
    • Use of pyrazolo [3,4-b] pyridine as cyclin dependent kinase inhibitors
    • 吡唑并[3,4-b]吡啶作为细胞周期蛋白依赖性激酶抑制剂
    • US6107305A
    • 2000-08-22
    • US209575
    • 1998-12-11
    • Raj N. MisraS. David KimballDavid B. RawlinsKevin R. WebsterIsia Bursuker
    • Raj N. MisraS. David KimballDavid B. RawlinsKevin R. WebsterIsia Bursuker
    • A61K31/437A61P1/00A61P19/02A61P25/00A61P25/28A61P29/00A61P31/10A61P31/12A61P31/18A61P35/00A61P37/06A61P43/00C07D471/04A61K31/435
    • C07D471/04A61K31/437
    • Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein:X is O, S(O).sub.m ;Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl, --NR.sub.4 R.sub.5 ;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl;R.sub.5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, --O-alkyl, --O-aryl; andm is 0, 1 or 2.The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
    • 用作细胞周期依赖性激酶抑制剂的式及其可药用盐的化合物,其中:X为O,S(O)m; Y是烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,环烷基,环烷基烷基,杂环烷基,杂环烷基烷基; R1是氢或低级烷基; R2是烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,环烷基,环烷基烷基,杂环烷基,杂环烷基烷基,-O-烷基,-O-芳基,-NR4R5; R3是氢或低级烷基; R4是氢,烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,环烷基,环烷基烷基,杂环烷基,杂环烷基烷基,-O-烷基,-O-芳基。 R5是氢,烷基,芳基,烷基芳基,杂芳基,烷基杂芳基,环烷基,烷基环烷基,杂环烷基,烷基杂环烷基,-O-烷基,-O-芳基; 并且m为0,1或2.式I化合物为蛋白激酶抑制剂,可用于治疗和预防增殖性疾病,例如癌症,炎症和关节炎。 它们也可用于治疗神经变性疾病如阿尔茨海默病,心血管疾病,病毒性疾病和真菌性疾病。