MITCHELL, SCOTT A.,史考特 米特歇尔,史考特 米特歇爾,DANCA, MIHAELA DIANA,麦黑拉 丹卡,麥黑拉 丹卡,BLOMGREN, PETER A.,彼得 布朗格恩,DESIMONE, ROBERT W.,罗伯特 狄西门尼,羅伯特 狄西門尼,PIPPIN, DOUGLAS A. I.,道格拉斯 皮宾,道格拉斯 皮賓,BRITTELLI, DAVID,史考特 米特歇尔,史考特 米特歇爾,麦黑拉 丹卡,麥黑拉 丹卡,彼得 布朗格恩,罗伯特 狄西门尼,羅伯特 狄西門尼,道格拉斯 皮宾,道格拉斯 皮賓
申请号：
TW095101448
公开号：
TWI378925B
申请日:
2006.01.13
申请国别(地区):
TW
年份:
2012
代理人:
摘要：
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.本文中提供一些選自式1之化合物的化學個體和其醫藥上可接受的鹽、溶劑合物、晶形、螯合物、非共價錯合物、前驅藥、和混合物。本文中也提供一種醫藥組成物，其包含至少一種化學個體和一或多種選自載體、佐藥和賦形劑的醫藥上可接受之載劑。本發明揭示治療患有一些反應血管生成激酶調節之疾病或障礙的病人之方法，其包含將足以有效減少疾病或障礙的跡象或症狀的量之至少一種化學個體投予至該病人。這些疾病包括癌，包括乳房腫瘤形成、大腸直腸癌和頸部鱗狀細胞癌。本發明揭示之治療的方法包括投予作為單一活性劑之至少一種化學個體或投予該至少一種化學個體與一或多種治療劑之組合。本發明揭示一種測定樣品中血管生成激酶存在或不存在之方法，其包含在允許檢測血管生成激酶之活性的條件下使樣品與至少一種化學個體接觸，檢測血管生成激酶之含量，由此測定樣品中血管生成激酶存在或不存在。
