Diamino acid derivatives

Details Diamino acid derivatives Diamino acid derivatives

C - Chemistry, Metallurgy

07

K

167/100, 260/468

C07K 5/00 (2006.01) A61K 31/195 (2006.01) C07K 5/02 (2006.01) C07K 5/04 (2006.01)

Patent

CA 1268597

Diamino acid derivatives 26474-54 Abstract The invention relates to new diamino acid deri- vatives of the formula I X-Z-NH-CH(CH2R1)-CH(NH2)-CH2-CO-E-G-Y I wherein X is H, R2-O-Cn2n-CO-, R2-CnH2n-O-CO-, R2-CnH2n-CO-, R2-SO2, (R2-CnH2n)-L(R2-CrH2r)-CtH2t-CO- H-(NHCH2CH2)n-NH-CH2CO- or 9-fluorenyl-CnH2n-O-CO-, Z is 0 to 4 amino acid radicals, bonded to one another in a peptide-like manner,se1ected from the group consisting of Abu, Ada, Ala, Arg, Dab, Gly, His, Ile, Leu, tert.-Leu, Lys, Met, Nbg, Nle, N-Me-His, N-Me-Phe, Orn, Phe, Pro, Ser, Thr, Tic, Trp, Tyr and Val, R1 is H, A, cycloalkyl,with 3 - 7 C atoms, Ar or CpH2p-W, E is absent or is Ala, Gly, Ile, Leu, tert.-Leu, Met, Ser, Thr or Val, G is absent or is His, Phe, Trp, Tyr or -NH-CH(CH2R1)- CH(NH2)-CH2CO-, Y is -OCmH2m-R3, -NH-CmH2m-R3, -NH-CmH2m-1(R3)2 or NA2, R2 is A, cycloalkyl with 3 -7 C atoms, benzyl or Ar, L is CH or N, R3 is H, A, cycloalkyl with 3 - 7 C atoms, Ar, pyridyl, imidazolyl, piperidyl, N-benzyl-piperidyl or piperazinyl, W is OH, NH2, OA, HHA or NA2, A is alkyl with 1-6 C atoms, Ar is unsubstituted phenyl, phenyl which is mono- or poly- substituted by A, AO, F, Cl, Br, I, CF3 and/or NH2, or unsubstituted naphthyl and m, n, p, r and t are each 0, 1, 2,3,4 or 5, and salts thereof. These compounds inhibit the activity of human plasma renin.

481660

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