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    • 10. 发明授权
    • Peptides useful for inhibition of renin
    • 可用于抑制肾素的肽
    • US4709010A
    • 1987-11-24
    • US789286
    • 1985-10-18
    • Gunter HolzemannPeter RaddatzAlfred JonczykClaus J. Schmitges
    • Gunter HolzemannPeter RaddatzAlfred JonczykClaus J. Schmitges
    • C07K14/81A61K38/00A61K38/55A61P9/12A61P43/00C07K1/113C07K5/00C07K5/02C07C103/52A61K37/02A61K49/00
    • C07K5/0227C07K5/0205Y10S530/86
    • New peptides of the formula IX--Z--NH--CHR--CHOH--CH.sub.2 --CO--NH--CHR.sup.1 --CH.sub.2 --NH--CHY--C.sub.n H.sub.2n --R.sup.2 Iin whichX is H, R.sup.3 --O--CH.sub.2 --CO--, R.sup.3 --O--CO--, R.sup.3 --CH.sub.2 --O--CO-- or R.sup.3 --C.sub.m H.sub.2m --CO--,Z is 1 to 4 aminoacid residues which are bonded together in the manner of peptides and are selected from the group comprising Abu, Ala, Arg, Asn, Dab, Gln, Gly, His, Ile, Leu, Lys, Met, NLeu, Orn, Phe, Pro, Trp, Tyr and Val,is A, Ar-alkyl (in which the group -alkyl contains 1-4 C atoms) or cycloalkyl-alkyl having 4-11 C atoms,R.sup.1 is H or A,Y is H, A, --C.sub.p H.sub.2p --OR.sup.4, --C.sub.p H.sub.2p --NHR.sup.4, --COOR.sup.4, --CONHR.sup.4 or --CONA.sub.2,R.sup.2 is A, cycloalkyl having 3-7 C atoms, Ar, pyridyl, indolyl, imidazolyl, piperidyl, N-benzylpiperidyl or piperazinyl,R.sup.3 is A, cycloalkyl having 3-7 C atoms or Ar,R.sup.4 is H, A or cycloalkyl having 3-7 C atoms,A is alkyl having 1-6 C atoms,Ar is phenyl which is unsubstituted or substituted once or several times by A, AO, F, Cl, Br, I, CF.sub.3 and/or NH.sub.2, or is unsubstituted naphthyl, andm, n and p each are 0, 1, 2, 3, 4 or 5, and their salts inhibit the activity of the renin in human plasma.
    • 式I XZ-NH-CHR-CHOH-CH2-CO-NH-CHR1-CH2-NH-CHY-CnH2n-R2Ⅰ的新肽,其中X是H,R3-O-CH2-CO-,R3-O -CO-,R3-CH2-O-CO-或R3-CmH2m-CO-,Z是1-4个氨基酸残基,其以肽的方式结合在一起,并且选自Abu,Ala,Arg,Asn ,Dab,Gln,Gly,His,Ile,Leu,Lys,Met,NLeu,Orn,Phe,Pro,Trp,Tyr和Val是A,Ar-烷基(其中烷基含有1-4个C原子 )或具有4-11个碳原子的环烷基 - 烷基,R1是H或A,Y是H,A,-CpH2p-OR4,-CpH2p-NHR4,-COOR4,-CONHR4或-CONA2,R2是A,具有3 -7个C原子,Ar,吡啶基,吲哚基,咪唑基,哌啶基,N-苄基哌啶基或哌嗪基,R3是A,具有3-7个C原子的环烷基或Ar,R4是H,A或具有3-7个C原子的环烷基,A 是具有1-6个C原子的烷基,Ar是未取代或被A,AO,F,Cl,Br,I,CF 3和/或NH 2取代或被取代一次或几次的苯基,或未取代的萘基,m,n和 p分别为0,1,2,3,4或5及其s 抑制人血浆中肾素的活性。