申请人:BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
公开号:EP0443573A2
公开(公告)日:1991-08-28
Disclosed herein are compounds of the general formula X-A-B-C'-Y wherein X is lower alkanoyl optionally substituted with one or two hydroxyls, A is an amino acid residue having a lower alkyl side chain, e.g. Ala or Val, B is a non-peptide linking unit, e.g. statyl or PheΨ[CH₂NH]Leu, C' is an amino acid residue of α-amino-β-cycloalkylpropionic acid, glutamic acid or α-aminoadipic acid, or a related derivative thereof, and Y is alkoxy, cycloalkoxy, a substituted alkoxy or a substituted amino group, e.g. cycloalkylalkoxy, arylalkoxy, alkylamino, (cycloalkyl)alkylamino or arylalkylamino. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.
本文公开了通式 X-A-B-C'-Y 的化合物,其中 X 是可选被一个或两个羟基取代的低级烷酰基,A 是具有低级烷基侧链的氨基酸残基,例如 Ala 或 Val,B 是非肽连接单元,例如C'是α-氨基-β-环烷基丙酸、谷氨酸或α-氨基己二酸或其相关衍生物的氨基酸残基,Y 是烷氧基、环烷氧基、取代的烷氧基或取代的氨基,如环烷氧基、芳基烷氧基、烷基氨基、(环烷基)烷基氨基或芳基烷基氨基。这些化合物能抑制人体免疫缺陷病毒(HIV)蛋白酶的活性,干扰 HIV 在人体细胞中诱导的细胞致病作用。这些特性使这些化合物可用于防治 HIV 感染。