Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti

Details Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti

1991-08-16

1993-07-20

Lee, Lester L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 19, 514400, 530330, 530331, 5483381, A61K 3702, C07K 506, C07K 508, C07K 510

Patent

active

052293696

ABSTRACT:
Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl 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 each of R.sub.1 and R.sub.9 is independently selected from hydrido, methyl, ethyl, t-butyloxycarbonyl; and methoxymethylcarbonyl; 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.11 and R.sub.12 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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