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    Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors
    4.
    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。

    PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS
    9.
    发明申请
    PYRAZOLOPYRIMIDINES AS LIPID KINASE INHIBITORS 审中-公开
    作为脂质激酶抑制剂的吡唑并嘧啶

    公开(公告)号：US20090286779A1

    公开(公告)日：2009-11-19

    申请号：US12442606

    申请日：2007-09-27

    申请人： Patricia Imbach ,  Frederic Stauffer ,  Pascal Furet ,  Hans-Georg Capraro

    发明人： Patricia Imbach ,  Frederic Stauffer ,  Pascal Furet ,  Hans-Georg Capraro

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  C07D401/12 ,  C07D413/14 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： The invention relates to novel—at least 3,5-disubstituted-pyrazolo[1,5-a]pyrimidines of the formula I, wherein the symbols R1 to R4 are as defined in the specification, tautomers thereof or N-oxides thereof, or (preferably pharmaceutically acceptable) salts thereof, or hydrates or solvates thereof, as well as to related embodiments. The compounds are useful inter alia as protein kinase inhibitors, and thus e.g. useful in the treatment of diseases that respond to an inhibition of kinases of the PI3-kinase-related protein kinase family, especially lipid kinases and/or PI3 kinase (PI3K) and/or mTOR and/or DNA protein kinase and/or ATM and/or ATR and/or hSMG-1.

    摘要翻译： 本发明涉及式I的至少3,5-二取代 - 吡唑并[1,5-a]嘧啶，其中符号R1至R4如本说明书中所定义，其互变异构体或其N-氧化物，或 （优选药学上可接受的）盐，或其水合物或溶剂化物，以及相关实施方案。 所述化合物尤其可用作蛋白激酶抑制剂， 可用于治疗响应抑制PI3激酶相关蛋白激酶家族，特别是脂质激酶和/或PI3激酶（PI3K）和/或mTOR和/或DNA蛋白激酶和/或ATM的激酶的疾病，以及 /或ATR和/或hSMG-1。