发明申请
- 专利标题: ORGANIC COMPOUNDS
- 专利标题(中): 有机化合物
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申请号: US12528483申请日: 2008-02-22
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公开(公告)号: US20110015191A1公开(公告)日: 2011-01-20
- 发明人: Johannes Ludescher , Josef Wieser , Arthur Pichler , Ulrich Griesser , Doris Braun
- 申请人: Johannes Ludescher , Josef Wieser , Arthur Pichler , Ulrich Griesser , Doris Braun
- 申请人地址: CH Basel
- 专利权人: SANDOZ AG
- 当前专利权人: SANDOZ AG
- 当前专利权人地址: CH Basel
- 优先权: EP07103150.4 20070227
- 国际申请: PCT/EP2008/052192 WO 20080222
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D413/06 ; A61P1/08
摘要:
Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed.
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