Ethereal N-terminal aminodiol amino acid derivatives as anti-hyp

Details Ethereal N-terminal aminodiol amino acid derivatives as anti-hyp Ethereal N-terminal aminodiol amino acid derivatives as anti-hyp

1991-11-27

1993-07-20

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

5483381, 560160, 564153, 514616, C07D23364, A61K 3116, C07C27116, C07C23322

Patent

active

052294200

ABSTRACT:
Non-peptidyl compounds characterized generally as ethereal N-terminal aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein X is selected from oxygen atom and methylene; wherein R.sub.1 is selected from methyl, ethyl, t-butyloxycarbonyl and 2-(N-piperidinyl)ethyl; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.7 is cyclohexylmethyl; wherein R.sub.8 is isobutyl; wherein each of R.sub.9 and R.sub.11 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R.sub.5 is selected from imidazolemethyl, thiazolemethyl and isobutyl; and with the further proviso that when m is one, then R.sub.5 is methyl or ethyl.

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