Di-propargyl-containing aryl/alkylsulfonyl-terminated alanine am

Details Di-propargyl-containing aryl/alkylsulfonyl-terminated alanine am Di-propargyl-containing aryl/alkylsulfonyl-terminated alanine am

1992-07-20

1993-09-21

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

564154, D61K 3116, C07C32341

Patent

active

052469697

ABSTRACT:
Compounds characterized generally as di-propargyl-containing aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, nethyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylnethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein each of R.sup.5 and R.sup.8 is independently propargyl or a propargyl-containing moiety; and wherein R.sup.7 is cyclohexylmethyl.

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Kokubu et al, Biochm. Biophys. Res. Commun., 118, 929 (1984).
Castro et al, FEBS Lett., 167, 273 (1984).
Hanson et al, Biochm. Biophys. Res. Comm., 132, 155-161 (1985), 146, 959-963 (1987).

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