[EN] N-HETEROCYCLYL-SUBSTITUTED AMINO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS<br/>[FR] DERIVES D'AMINO-THIAZOLE SUBSTITUES PAR N-HETEROCYCLYLE EN TANT QU'INHIBITEURS DE LA PROTEINE KINASE
申请人:PFIZER
公开号:WO2004074283A1
公开(公告)日:2004-09-02
Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, or pharmaceutically acceptable salt of said compound, modulate and/or inhibit the cell proliferation and activity of protein kinases.
[EN] 4—(1H— IMIDAZOL— 5— YL) -1H-PYRROLO [2, 3-B] PYRIDINES FOR USE IN THE TREATMENT OF LEUKAEMIAS, LYMPHOMAS AND SOLID TUMORS<br/>[FR] 4-(1H-IMIDAZOL-5-YL)-1H-PYRROLO [2,3-B] PYRIDINES DESTINÉES À ÊTRE UTILISÉES DANS LE TRAITEMENT DE LEUCÉMIES, DE LYMPHOMES ET DE TUMEURS SOLIDES
申请人:UNIV MASARYKOVA
公开号:WO2019185631A1
公开(公告)日:2019-10-03
The present invention relates to novel 4-(1H-imidazol-5-yl)-1H-pyrrolo[2,3-b]pyridine compounds which are useful in the treatment of lymphomas, leukaemias, and solid tumors.
N-containing cycloalkyl-substituted amino-thiazole derivatives and pharmaceutical compositions for inhibiting cell proliferation and methods for their use
申请人:Chu Shao Song
公开号:US20050101595A1
公开(公告)日:2005-05-12
Aminothiazole compounds with N-containing cycloalkyl at the 2-amino position which are represented by the Formula (I), or a pharmaceutically acceptable prodrug of said compound, pharmaceutically active metabolite or pharmaceutically acceptable salt of said compound, or metabolite thereof, modulate and/or inhibit the cell proliferation and activity of protein kinases.
The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating malignancies and other disorders by administering effective amounts of such compounds.
and CK1ϵ in cells as well as in vivo. Our observations suggest that the central scaffold can be used more broadly in compounds targeting other protein kinases, as evidenced by the highly selective p38α inhibitor MU1299.
新发现的化学生物学探针MU1250、MU1500和MU1742,基于 1 H-吡咯并[2,3- b ]吡啶-咪唑支架,允许高度特异性靶向细胞中的亚型 CK1α、CK1δ 和 CK1ε体内。我们的观察表明,中央支架可以更广泛地用于靶向其他蛋白激酶的化合物,高选择性 p38α 抑制剂MU1299证明了这一点。