NEW MATERIAL: The compd. of formula I [A is the acyl of formula II, etc., (R6 is 1 to 10C alkyl, etc.); B, C are a single bond, formula III (R1 is H, 1 to 5C alkyl; R11 is an amino acid side chain); D is a single bond, -O-, etc.; R2 is 1 to 10C alkyl, etc.; R3 is H, hydroxyl, etc.; R4, R5 are H, 1 to 5C alkyl, etc.; Y is formula IV, etc.].
EXAMPLE: (2S,3S)-3-(N-BOC-phenylalanyl histidyl)amide-1-(n- butylcarbamoylamino)-4-cyclohexyl-2-butanol.
USE: The compd. exhibits renin-inhibiting activity and is useful for the treatment of hypertension and cardiac insufficiency.
PROCESS: The compd. of the formula I is obtd. by bringing the compd. of the formula A-B-C-OH and the compd. of formula V (R3' is H, hydroxyl, etc.) into reaction at 0°C to room temp. in the presence of N,N-dicyclohexylcarbodimide, etc.; in a solvent, such as dimethylformamide.
METTERNICH RAINER
PFENNINGER EMIL
WEIDMANN BEAT
Next Patent: SESQUITERPENOID ISOCYANIDE COMPOSITION AND ITS METHOD OF USE