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    • 37. 发明授权
    • Enzyme inhibiting peptide derivatives
    • 酶抑制肽衍生物
    • US5126326A
    • 1992-06-30
    • US361895
    • 1989-06-06
    • Paul C. AndersonYvan GuindonChristiane Yoakim
    • Paul C. AndersonYvan GuindonChristiane Yoakim
    • C12N9/99A61K38/55A61P9/00A61P9/12A61P43/00C07K1/06C07K1/113C07K5/02C07K5/06C07K14/81
    • C07K5/0227
    • Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.
    • 本文公开了抑制人免疫缺陷病毒(HIV)蛋白酶和肾素的活性的肽衍生物。 肽衍生物可以由通式R 1 -R 2 -Y-R 3 -R 4表示,其中R 1是基于O 4 - (羧甲基) - 酪氨酰残基R2的衍生氨基酸,并且是氨基酸或类似氨基酸残基(R3可以 任选地不存在),Y是非肽连接单元,例如 辛基,R4是[-NR17CHR18-C(O)] pZ,其中R17是氢或低级烷基,R18是氨基酸或类似的氨基酸侧链,p是0或1,Z是末端基团(例如羟基或 氨基),或R 4是-NR 17 CR 18(R 21)CH 2 OH,其中R 17和R 18如上所述,R 21是氢,低级烷基或羟基(低级)烷基。 该衍生物可用作抗艾滋病毒感染和治疗肾素相关性高血压和充血性心力衰竭的药剂。