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    • 10. 发明申请
    • COMPOUNDS, COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASES THROUGH INHIBITING TGF-&bgr; ACTIVITY
    • 化合物,组合物和通过抑制TGF-β的治疗疾病的方法 活动
    • WO2014183018A3
    • 2015-01-22
    • PCT/US2014037471
    • 2014-05-09
    • SOUTHERN RES INSTUAB RESEARCH FOUNDATION
    • SUTO MARK JMURPHY-ULLRICH JOANNE E
    • A61K38/06
    • C07K5/081A61K38/00A61K38/04A61K38/06C07K5/00C07K5/04C07K5/08C07K5/0804
    • The present disclosure relates to compounds, compositions and methods for the treatment of diseases through inhibiting the activity of the transforming growth factor beta (TGF-&bgr;). More specifically, the disclosed compounds, compositions and methods are useful in the treatment of certain cancers (e.g. multiple myeloma, hematologic malignancies), diseases associated with excessive TGF-&bgr; activity including fibrosis, dermal scarring, immune dysfunction, and bone loss by inhibiting the conversion of latent TGF-&bgr; to active TGF-&bgr;. A method of preventing the activation of TGF-&bgr; in pathology is also provided, comprising administering an amount of the compounds sufficient to inhibit conversion of latent TGF-&bgr; to active TGF-&bgr; by thrombospondin 1 (TSP1), resulting in reduced TGF-&bgr; activity and reduced adverse effects such as fibrosis, bone loss, and immune dysfunction.
    • 本公开涉及通过抑制转化生长因子β(TGF-β)的活性来治疗疾病的化合物,组合物和方法。 更具体地,所公开的化合物,组合物和方法可用于治疗某些癌症(例如多发性骨髓瘤,血液恶性肿瘤),与过量TGF-和bgr相关的疾病; 活性包括纤维化,皮肤瘢痕形成,免疫功能障碍和骨丢失,通过抑制潜伏性TGF-和bgr的转化; 活化TGF-β。 一种预防TGF-β的活化的方法 还提供了病理学,其包括给予一定量足以抑制潜伏性TGF-β1转化的化合物; 活化TGF- 通过血小板反应蛋白1(TSP1),导致TGF- 活动和减少的不良反应如纤维化,骨丢失和免疫功能障碍。