首页> 外国专利> METHODS OF PREPARATION AND RESOLUTION OF E/Z ISOMERS OF VINYLFURO2,3-D PYRIMIDINE AND THEIR BIOLOGICAL ACTIVITIES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT

METHODS OF PREPARATION AND RESOLUTION OF E/Z ISOMERS OF VINYLFURO2,3-D PYRIMIDINE AND THEIR BIOLOGICAL ACTIVITIES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT

机译:乙烯基[2,3-D]嘧啶的E / Z异构体的制备和拆分方法及其生物学活性,组成和治疗方法

摘要

Stereoselective methods for preparing the individual isomers, E- and Z-2,4-substituted-5-vinylfuro[2,3-d]pyrimidine and pharmaceutically acceptable salts, solvates, and prodrugs thereof using selective synthetic conditions are provided. This class of pyrimidine compounds function as receptor tyrosine kinase inhibitors during angiogenesis and resists the development of new blood vessels in tumors as well as inhibit the folate pathway required for cell growth. The isomers of these compounds are separated by physical, chromatographic, and/or HPLC methods. Their biological activities are described. Also provided are methods of treating diseases associated with angiogenesis in a patient comprising administering the isolated E- and Z- isomers of the composition of the present invention.
机译:提供了使用选择性合成条件制备单独的异构体,E-和Z-2,4-取代的5-乙烯基呋喃[2,3-d]嘧啶及其可药用盐,溶剂化物和前药的立体选择性方法。这类嘧啶化合物在血管生成过程中起受体酪氨酸激酶抑制剂的作用,并抵抗肿瘤中新血管的发育,并抑制细胞生长所需的叶酸途径。这些化合物的异构体通过物理,色谱和/或HPLC方法分离。描述了它们的生物学活性。还提供了治疗患者中与血管生成有关的疾病的方法,其包括施用本发明组合物的分离的E-和Z-异构体。

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