| abstract |
PURPOSE: To provide novel compds. which have renin inhibition activity and are useful for a hypertension procedure. n CONSTITUTION: The compd. of formula I [R 1 is formula II, formula III, formula IV (P is 1, 2; B is phenylmethyl; cyclohexylmethyl, etc.; R 10 is H, 1 to 3C alkyl, etc.), etc.; q is 0, 1; R 2 is phenylmethyl, cyclohexylmethyl, etc.; R 3 is H, methyl; R 4 is 1 to 8C alkyl, phenyl methyl, etc.; R 5 is the same as R 3 ; R 6 is 1 to 6C alkyl, phenylmethyl, etc.; W is 0, formula NR 3 ; A is formula V (Z is O, S, etc.)] and its analog. For example, 4,7-anhydro-2-(3-cyclohexyl-N-(diethoxyphosphynyl)- L-aranyl-L-leucilamino]-1,2,5,6-tetradeoxy-L-arabino (and D-xylo)-peptitol. The compd. of the formula I is obtd. by bringing, for example, the compd. of formula VI into reaction with a coupling agent of a peptide, then bringing the reaction product into reaction with the compd. of formula VII. n COPYRIGHT: (C)1992,JPO |