申请人:Mitchell A. Scott
公开号:US20060199846A1
公开(公告)日:2006-09-07
Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
本文提供了从式1化合物中选择的某些化学实体及其药学可接受的盐、溶剂化物、晶体形式、螯合物、非共价复合物、前药和混合物。本文还提供了包含至少一种化学实体和一种或多种药学可接受的载体、佐剂和赋形剂的制药组合物。本文还揭示了用于治疗对血管生成激酶调节有反应的某些疾病和障碍的患者的方法,包括向这些患者施用足够量的至少一种化学实体,以减少疾病或障碍的症状或体征。这些疾病包括癌症,包括乳腺肿瘤、子宫内膜癌、结肠癌和颈部鳞状细胞癌。治疗方法包括将至少一种化学实体作为单一活性剂施用或与一种或多种其他治疗剂联合使用。本文还揭示了一种用于确定样品中是否存在血管生成激酶的方法,包括在允许检测血管生成激酶活性的条件下,将样品与至少一种化学实体接触,检测血管生成激酶活性水平,并从中确定样品中是否存在血管生成激酶。