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    Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors
    17.
    发明申请
    Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors 审中-公开
    使用2,4-二氨基-3-羟基羧酸衍生物作为蛋白酶体抑制剂

    公开(公告)号：US20050026994A1

    公开(公告)日：2005-02-03

    申请号：US10035301

    申请日：2001-10-25

    申请人： Dennis France ,  Peter Furst ,  Johann Zimmermann ,  Carlos Garcia-Echeverria ,  Dieter Scholz ,  Pascal Furet ,  Patricia Imbach

    发明人： Dennis France ,  Peter Furst ,  Johann Zimmermann ,  Carlos Garcia-Echeverria ,  Dieter Scholz ,  Pascal Furet ,  Patricia Imbach

    IPC分类号： A61K38/00 ,  A61P17/06 ,  A61P35/00 ,  A61P43/00 ,  C07C237/12 ,  C07C271/22 ,  C07K5/00 ,  A61K31/381 ,  A61K31/165

    CPC分类号： C07C271/22 ,  Y02P20/55

    摘要： The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R1 represents hydrogen; an amino protecting group; or a group of formula R5Y— wherein R5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents —CO—; —NH—CO—; —NH—CS—; —SO2—; —O—CO—; or —O—CS—; R2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g., of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R2 represents arylalkyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R5 represents arylalkyl and Y represents —CO—; or R5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents —O—CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.

    摘要翻译： 本发明涉及式（I）的2,4-二氨基-3-羟基羧酸的新用途，其中A和B独立地表示键或未取代或取代的氨基酰基部分; R1表示氢; 氨基保护基; 烯基，炔基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环基或杂环基烷基;或其中R 5表示氢或未取代或取代的烷基，烯基，炔基，芳基， Y表示-CO-; -NH-CO-; -NH-CS-; -SO2-; -O-CO-; 或-O-CS-; R2表示天然氨基酸的侧链; 烷基，芳基烷基，杂芳基烷基或环烷基烷基; 或三甲基甲硅烷基甲基，2-噻吩基甲基或苯乙烯基甲基; R3表示卤素，烷基，烷氧基或羟基烷氧基; 并且R 4表示2（R） - 羟基茚满-1（S） - 基; （S）-2-羟基-1-苯基乙基; 或2-羟基苄基未被取代或在4-位上被甲氧基取代; 在制备用于治疗增殖性疾病例如实体瘤的药物组合物中; 涉及一种治疗温血动物的方法; 和式（I *）的2,4-二氨基-3-羟基羧酸，其中A和B独立地表示未取代或取代的氨基酰基部分; R2代表芳基烷基; R3表示卤素，烷基，烷氧基或羟基烷氧基; R4代表未取代的或在4位被甲氧基取代的2-羟基 - 苄基; R5表示芳基烷基，Y表示-CO-; 或R 5表示被环烷基，萘基，吡啶基或苯基取代的烷基，其中苯基被烷基或氨基取代; Y表示-O-CO; 其药学上可接受的盐; 以及使用这些式（I *）化合物来治疗人或动物体，特别是治疗增殖性疾病。