发明申请
- 专利标题: CALCIUM SALTS OF INDOLE DERIVED STATINS
- 专利标题(中): 单位衍生统计的钙盐
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申请号: US12768991申请日: 2010-04-28
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公开(公告)号: US20100249204A1公开(公告)日: 2010-09-30
- 发明人: Guang-Pei Chen , Prasad Koteswara Kapa , Paul Allen Sutton
- 申请人: Guang-Pei Chen , Prasad Koteswara Kapa , Paul Allen Sutton
- 主分类号: A61K31/404
- IPC分类号: A61K31/404 ; C07D209/18 ; A61P9/00 ; A61P9/10
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.
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