利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

43 条记录 (耗时 0.022 秒)

    3-SUBSTITUTED N-(ARYL- OR HETEROARYL)-PYRAZO[1,5-a]PYRIMIDINES AS KINASE INHIBITORS
    22.
    发明公开
    3-SUBSTITUTED N-(ARYL- OR HETEROARYL)-PYRAZO[1,5-a]PYRIMIDINES AS KINASE INHIBITORS 有权
    3-取代的N-（芳基 - 或杂芳基）吡唑并[1,5-A]嘧啶类作为激酶抑制剂的

    公开(公告)号：EP2004653A1

    公开(公告)日：2008-12-24

    申请号：EP07723895.4

    申请日：2007-04-02

    申请人： NOVARTIS AG

    发明人： MASUYA, Keiichi ,  VAUPEL, Andrea ,  IMBACH, Patricia ,  FURET, Pascal

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： The invention relates to 3-substituted N-(aryl- or heteroaryl)-pyrazolo[1 ,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warmblooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.

    USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS
    23.
    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.