The present invention relates to novel amino acid derivatives having an N, N-dialkylaminophenyl group represented by the general formula [I].
wherein
R1 represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkanoyl group or a benzoyl group, and each phenyl ring in the phenyl-lower alkyl group and the benzoyl group can be substituted by a halogen atom, a lower alkyl group or a lower alkoxy group;
R2 represents a carboxyl group which can be converted into an ester, an amide or a hydroxamic acid;
R3 represents a lower alkyl group;
R4 represents a lower alkyl group;
A1 represents a lower alkylene group which can be substituted by a phenyl group, and the phenyl group can be substituted by a halogen atom, a lower alkyl group or a lower alkoxy group;
A2 represents a lower alkylene group;
A3 represents a lower alkylene group; and
"Z" represents a sulfur atom or an oxygen atom.
The compounds have inhibitory effects on LTA4 hydrolase and are useful as medicines, in particular, therapeutic agents for inflammatory diseases such as rheumatic diseases, psoriasis, inflammatory intestinal diseases, gout and cystic fibrosis, in which LTB4 is concerned.
本发明涉及具有通式 [I] 所代表的 N,N-二烷基
氨基
苯基的新型
氨基酸衍
生物。
其中
R1 代表
氢原子、低级烷基、
苯基低级烷基、低级烷酰基或
苯甲酰基,
苯基低级烷基和
苯甲酰基中的每个
苯基环可被卤素原子、低级烷基或低级烷
氧基取代;
R2 代表可转化为
酯、
酰胺或羟
肟酸的羧基;
R3 代表低级烷基
R4 代表一个低级烷基;
A1 代表可被
苯基取代的低级亚烷基,
苯基可被卤素原子、低级烷基或低级烷
氧基取代;
A2 代表一个低级亚烷基
A3 代表一个低级亚烷基;以及
Z "代表
硫原子或
氧原子。
这些化合物对 L
TA4
水解酶有抑制作用,可用作药物,特别是治疗与 LTB4 有关的炎症性疾病,如风湿病、牛皮癣、肠道炎症性疾病、痛风和囊性纤维化。