METHODS OF PREPARATION AND RESOLUTION OF E/Z ISOMERS OF VINYLFURO[2,3-D]PYRIMIDINE AND THEIR BIOLOGICAL ACTIVITIES AND RELATED COMPOSITIONS AND METHODS OF TREATMENT
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United States of America Patent
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app pub date -
Apr 13, 2007
filing date -
Mar 20, 2006
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Abstract
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.
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