发明授权
- 专利标题: Proline ester and preparation containing the same for percutaneous administration
- 专利标题(中): 脯氨酸酯和含有相同用于经皮给药的制剂
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申请号: US10527062申请日: 2003-09-08
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公开(公告)号: US07323489B2公开(公告)日: 2008-01-29
- 发明人: Takayuki Furuishi , Kunihiro Minami , Takayuki Minowa , Miho Komine , Kunihiko Kimura
- 申请人: Takayuki Furuishi , Kunihiro Minami , Takayuki Minowa , Miho Komine , Kunihiko Kimura
- 申请人地址: JP Tokyo
- 专利权人: Toaeiyo Ltd.
- 当前专利权人: Toaeiyo Ltd.
- 当前专利权人地址: JP Tokyo
- 代理机构: Oblon, Spivak, McClelland, Maier & Neustadt, P.C.
- 优先权: JP2002-265276 20020911
- 国际申请: PCT/JP03/11420 WO 20030908
- 国际公布: WO2004/024754 WO 20040325
- 主分类号: A61K31/40
- IPC分类号: A61K31/40 ; C07D207/00
摘要:
A proline ester represented by the following formula (I): wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.
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