[EN] INHIBITORS OF KINASE ACTIVITY WITH 1,2-DI-CYCLYL SUBSTITUTED ALKYNE STRUCTURES<br/>[FR] INHIBITEURS DE L'ACTIVITÉ KINASE AVEC STRUCTURES ALCYNE À SUBSTITUTION 1,2-DI-CYCLYLE
申请人:METHYLGENE INC
公开号:WO2009100536A1
公开(公告)日:2009-08-20
This invention relates to compounds that inhibit protein kinase activity. More particularly, the invention relates to compounds, compositions, and methods fo inhibiting Ret receptor kinase activity, c-Raf kinase activity and/or VEGF receptor kinase activity. These compounds are alkynes substituted by carbocyclic or heterocyclic rings at both ends with further substitutions thereon. They further show in vivo activity against solid tumor disease models.
这项发明涉及抑制蛋白激酶活性的化合物。更具体地说,该发明涉及抑制Ret受体激酶活性、c-Raf激酶活性和/或VEGF受体激酶活性的化合物、组合物和方法。这些化合物是炔烃,在两端被碳环或杂环取代,并在其上进一步取代。它们还显示对实体肿瘤疾病模型具有体内活性。