CALCIUM SALTS OF INDOLE DERIVED STATINS
    18.
    发明申请
    CALCIUM SALTS OF INDOLE DERIVED STATINS 审中-公开
    单位衍生统计的钙盐

    公开(公告)号:US20100249204A1

    公开(公告)日:2010-09-30

    申请号:US12768991

    申请日:2010-04-28

    CPC分类号: C07D209/24

    摘要: The present invention provides calcium salts of indole derived statins of the formula wherein R1 is alkyl, cycloalkyl or aralkyl; R2, R3 and R4 are independently hydrogen, halogen or alkyl; R5 and R6 are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3-position is in the R-configuration and at the 5-position 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 R1 is isopropyl, R2 is fluorine and R3, R4, R5 and R6 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.

    摘要翻译: 本发明提供下式的吲哚衍生的他汀类钙盐:其中R1是烷基,环烷基或芳烷基; R2,R3和R4独立地是氢,卤素或烷基; R5和R6独立地是氢,卤素,烷基,环烷基,芳烷基,烷氧基或芳烷氧基; 3位的羟基为R构型,S构型为5位; 或其对映体; 或其水合物; 如通过本发明的方法可获得的。 更具体地,本发明提供式IA的钙盐,其中R 1是异丙基,R 2是氟,并且R 3,R 4,R 5和R 6是氢,在本文中称为氟伐他汀钙,为高度结晶形式。 此外,本发明涉及制备结晶氟伐他汀钙的方法以及包含结晶形式的药物组合物。