| 摘要 |
<p>The present invention provides calcium salts of indole derived statins of the formula (IA) wherein R<SUB>1</SUB>, is alkyl, cycloalkyl or aralkyl; R<SUB>2</SUB>, R<SUB>3 </SUB>and R<SUB>4 </SUB>are independently hydrogen, halogen or alkyl; R<SUB>5 </SUB>and R<SUB>6 </SUB>are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3position is in the R-configuration and at the 5position in the S-configuration; or an enantiomer thereof; or a hydrate thereof; as obtainable by the methods of the present invention. More specifically, the invention provides a calcium salt of formula (IA) wherein R<SUB>1</SUB>, is isopropyl, R<SUB>2 </SUB>is fluorine and R<SUB>3</SUB>, R<SUB>4</SUB>, R<SUB>5 </SUB>and R<SUB>6 </SUB>are hydrogen, designated herein as Fluvastatin calcium, in a highly crystalline form. Furthermore, the present invention is directed to methods for the preparation of the crystalline Fluvastatin calcium, and to pharmaceutical compositions comprising the crystalline form.</p> |
