发明公开
EP0726247A1 Aniline derivatives having a polyunsaturated fatty acid residue and use thereof
失效
苯胺衍生物轴承的多不饱和脂肪酸残基和它的应用
- 专利标题： Aniline derivatives having a polyunsaturated fatty acid residue and use thereof
- 专利标题（中）： 苯胺衍生物轴承的多不饱和脂肪酸残基和它的应用
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申请号： EP96101650.8申请日： 1996-02-06
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公开(公告)号： EP0726247A1公开(公告)日： 1996-08-14
- 发明人: Yazawa, Kazunaga , Watanabe, Kazuo , Ijuin, Yasuharu , Shikano, Mayumi , Soda, Yasuji , Kosaka, Tetsuya , Matsuyama, Naoto , Mizuno, Koji
- 申请人： NIPPON SHOJI KAISHA, LIMITED , SAGAMI CHEMICAL RESEARCH CENTER
- 申请人地址： 2-9 Kokumachi 2-chome, Chuo-ku Osaka-shi, Osaka 540 JP
- 专利权人： NIPPON SHOJI KAISHA, LIMITED,SAGAMI CHEMICAL RESEARCH CENTER
- 当前专利权人： NIPPON SHOJI KAISHA, LIMITED,SAGAMI CHEMICAL RESEARCH CENTER
- 当前专利权人地址： 2-9 Kokumachi 2-chome, Chuo-ku Osaka-shi, Osaka 540 JP
- 代理机构： von Kreisler, Alek, Dipl.-Chem.
- 优先权： JP20741/95 19950208
- 主分类号： C07C233/27
- IPC分类号： C07C233/27 ; C07C233/15 ; C07C233/09 ; C07C233/38 ; C07C275/28 ; C07C275/40 ; C07D295/18 ; A61K31/16
摘要：
An aniline derivative of the formula (1)
wherein R 1 is an eicosapentaenoyl or docosahexaenoyl; R 2 and R 3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R 4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, -C(=O)NH-(CH 2 ) n -NH- wherein n is 2 or 3, or a bivalent group of the following formula
wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.
wherein R 1 is an eicosapentaenoyl or docosahexaenoyl; R 2 and R 3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R 4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, -C(=O)NH-(CH 2 ) n -NH- wherein n is 2 or 3, or a bivalent group of the following formula
wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.
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