发明公开
EP0471493A1 N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase
失效
N，N'，N'-三取代-5,5-二氨基亚甲基-1,3-二恶烷-4,6-二酮α酰-CoA：胆固醇 - 酰基转移酶。
- 专利标题： N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase
- 专利标题（中）： N，N'，N'-三取代-5,5-二氨基亚甲基-1,3-二恶烷-4,6-二酮α酰-CoA：胆固醇 - 酰基转移酶。
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申请号： EP91307196.5申请日： 1991-08-06
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公开(公告)号： EP0471493A1公开(公告)日： 1992-02-19
- 发明人: Fobare, William Floyd , Strike, Donald Peter
- 申请人： AMERICAN HOME PRODUCTS CORPORATION
- 申请人地址： Five Giralda Farms Madison, New Jersey 07940-0874 US
- 专利权人： AMERICAN HOME PRODUCTS CORPORATION
- 当前专利权人： AMERICAN HOME PRODUCTS CORPORATION
- 当前专利权人地址： Five Giralda Farms Madison, New Jersey 07940-0874 US
- 代理机构： Wileman, David Francis, Dr.
- 优先权： US568384 19900816; US719873 19910624
- 主分类号： C07D319/06
- IPC分类号： C07D319/06 ; A61K31/335 ; C07D405/12 ; C07F7/18 ; A61K31/445 ; A61K31/695
摘要：
The compounds of the formula:
in which X, and Y are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R₁ is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethylphenethyl, 1-(t-butyl)dimenthylsilyloxy methylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R₁ is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R₂ is alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
in which X, and Y are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R₁ is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethylphenethyl, 1-(t-butyl)dimenthylsilyloxy methylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R₁ is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R₂ is alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
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