申请人:SUNTORY LIMITED
公开号:EP0393457A1
公开(公告)日:1990-10-24
A proteinase inhibitory compound represented by the following general formula (1):
wherein R₁ represents a straight-chain or branched acyl group having 2 to 10 carbon atoms, a branched-, cyclic- or polycyclic-alkyloxycarbonyl group having 4 to 15 carbon atoms, a substituted- or unsubstituted-benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluenesulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group or a 2-benzoly-1-methylvinyl group;
R₂ represents a hydrogen atom; or R₁ and R₂ may together form a phthaloyl group;
R₃ represents an isobutyl group, a n-butyl group or an isopropyl group and the above-mentioned R₁ can be an unsubstituted-benzyloxycarbonyl group provided that R₃ is a n-butyl group; and
R₄ represents a n-butyl group.
由以下通式(1)代表的蛋白酶抑制剂化合物:
其中 R₁ 代表具有 2 至 10 个碳原子的直链或支链酰基,具有 4 至 15 个碳原子的支链、环或多环烷氧基羰基,取代或未取代的苄氧基羰基,2、2,2-三氯乙基氧羰基、2-(三甲基硅基)乙基氧羰基、对甲苯磺酸基、邻硝基苯磺酰基、二苯基膦酰基、三苯基甲基或 2-苯甲酰基-1-甲基乙烯基;
R₂ 代表氢原子;或 R₁ 和 R₂ 可共同形成邻苯二甲酰基;
R₃ 代表异丁基、正丁基或异丙基,上述 R₁ 可以是未取代的苄氧羰基,条件是 R₃ 是正丁基;以及
R₄ 代表一个正丁基。