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    USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS
    2.
    发明公开
    USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS 有权
    2,4-二氨基-3-HYDROXYCARBOXYLSÄUREDERIVATEALS蛋白酶体抑制剂

    公开(公告)号：EP1173413A1

    公开(公告)日：2002-01-23

    申请号：EP00927038.0

    申请日：2000-04-25

    申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

    发明人： FRANCE, Dennis ,  FÜRST, Peter ,  ZIMMERMANN, Johann ,  GARCIA-ECHEVERRIA, Carlos ,  SCHOLZ, Dieter ,  FURET, Pascal ,  IMBACH, Patricia

    IPC分类号： C07C271/22 ,  A61P43/00 ,  A61K31/325

    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.

    PHENYL-(4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES
    4.
    发明授权
    PHENYL-(4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES 有权
    苯基 - （4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基）胺衍生物

    公开(公告)号：EP1521749B1

    公开(公告)日：2010-05-19

    申请号：EP03762663.7

    申请日：2003-07-08

    申请人： Novartis AG

    发明人： FURET, Pascal ,  IMBACH, Patricia ,  RAMSEY, Timothy, Michael ,  SCHLAPBACH, Achim ,  SCHOLZ, Dieter ,  CARAVATTI, Giorgio

    IPC分类号： C07D403/04 ,  A61K31/505

    CPC分类号： C07D403/04 ,  A61K31/505

    摘要： The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives - alone or in combination with one or more other pharmaceutically active compounds - for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.

    摘要翻译： 本发明涉及苯基 - [4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基） - 胺衍生物及其制备方法，涉及包含此类衍生物的药物组合物和用途 的这些衍生物 - 单独或与一种或多种其它药物活性化合物组合用于制备用于治疗增殖性疾病（例如肿瘤）的药物组合物。