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    Quinoline derivatives as caspase-3 inhibitor, preparation for producing the same and pharmaceutical composition comprising the same
    1.
    发明授权
    Quinoline derivatives as caspase-3 inhibitor, preparation for producing the same and pharmaceutical composition comprising the same 失效
    喹啉衍生物作为半胱天冬酶-3抑制剂，其制备方法和包含其的药物组合物

    公开(公告)号：US07009053B2

    公开(公告)日：2006-03-07

    申请号：US10493706

    申请日：2003-04-30

    申请人： Sung-Gyu Kim ,  Yoon Sung Jung ,  Jae Yang Kong ,  Woo Kyu Park

    发明人： Sung-Gyu Kim ,  Yoon Sung Jung ,  Jae Yang Kong ,  Woo Kyu Park

    IPC分类号： C07D215/38 ,  C07D215/44 ,  A61K31/47

    CPC分类号： C07D409/12 ,  C07D215/42 ,  C07D215/44 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R2 is H; halogen; C1-6alkyl; C1-6 alkoxy; C1-6 alkoxyalkyl; or C3-6cycloalkyl; R1 is formula (a); —CN; or formula (b); R is H; C6-14aryl unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; 5–15 membered heterocyclic group unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; or —(CH2)n—CHR4R5. The present invention relates to a pharmaceutical composition for treating caspase-associated diseases by inhibiting the activity of caspase-3 which comprises the compound of formula (1) or its pharmaceutically acceptable salt.

    摘要翻译： 本发明涉及式（1）的新喹啉衍生物或其与胱天蛋白酶-3抑制活性的药学上可接受的盐及其制备方法，其中R 2为H; 卤素; C 1-6烷基; C 1-6烷氧基; C 1-6烷氧基烷基; 或C 3-6环烷基; R 1是式（a）; -CN; 或式（b）; R为H; 未取代的或被卤素C 1-6烷基，C 1-6烷氧基或氨基取代的C 6-14芳基; 未取代或被卤素取代的5-15元杂环基，C 1-6烷基，C 1-6烷氧基或氨基; 或 - （CH 2）n-CHR 4 R 5 5。 本发明涉及通过抑制胱天蛋白酶-3的活性来治疗半胱氨酸蛋白酶相关疾病的药物组合物，其包含式（1）化合物或其药学上可接受的盐。