New N-acyl oligopeptide amide derivs. - used in inhibitors of renin, useful for control of hypertension and cardiac insufficiency

摘要

Peptides of formula (I) are new: R6=1-10C alkyl (opt. substd. by 1-5C alkoxy or 6-10C aryloxy); 3-7C cycloalkyl: 3-10C cyclo-alkyl (1-5C) alkyl; 6-10C aryl; 5 or 6 membered heteroaryl contg. 1 or 2 N, O or S or one N plus one O and/or 5; heteroaryl -(1-5C)alkyl; 1-5C alkoxy (opt. substd by 6-10C aryl), R10O(CH2CH2-O)n(CH2)m or the gp. (ii) R10=1-5C alkyl; n=1-20; m=1-5; R=H or acetyl; R7=1-5C alkyl or 6-10C aryl; R8 and R9=H, 1-5C alkyl or 6-10C aryl; R1=H or 1-5C alkyl; B and C=bond or are (iii) but not both bond; R11=hydrophilic or lipophilic aminoacid side chain; D=bond, O, NR, or CHR1; R2=1-10C alkyl; 3-10C cycloalkyl (1-5C) alkyl (opt. ring substd.); 6-10C aryl (1-5C) alkyl; heteroaryl (1-5C) alkyl or R15-S(O)s(CH2)p; R15=H, 1-4C alkyl or benzyl; S=O or 1; p=1 or 2; R3=H, OH, NH2 or OCOR2; R4 and R5=H, 1-5C alkyl (opt. substd.) or -CHR12. COR13; R12=1-5C alkyl, opt. substd. by OH; R13=OH, 1-5C alkoxy, NH2 (opt. substd) aminomethyl benzyl; NR4R5 may also be pyrrolidino, piperidino, morpholino or delta-R14-piperazino; R14=H, 1-5C alkyl, benzyl or R16CO; R16=1-4C alkyl or 1-4C alkoxy -(OCH2CH2)qCH2-; q=2-5; y=SO2,CO, (iv).