Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid der

Details Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid der Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid der

1991-12-16

1993-09-21

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514 19, 514489, 514616, 5483401, 560 25, 560 27, 560125, 564153, A61K 31415, A61K 3116, C07C23335, C07D23364

Patent

active

052469590

ABSTRACT:
Non-peptidyl compounds characterized generally as poly(aminoalkyl)aminocarbonyl aminoacyl 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.9 and R.sub.10 is independently selected from hydrido, ethyl and methyl; wherein R.sub.9 and R.sub.10 may be taken together to form a heterocyclic ring having five or six ring atoms and containing one or two nitrogen atoms as ring atoms; wherein each of R.sub.1 and R.sub.2 is independently 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 hydrido; wherein R.sub.7 is cyclohexylmethyl; wherein R.sub.8 is selected from ##STR2## with the carbon bearing the hydroxyl radical being in the S configuration; wherein R.sub.16 is selected from isopropyl, n-propyl, n-butyl and isobutyl; wherein each of R.sub.11, R.sub.12, R.sub.14 and R.sub.15 is hydrido; wherein m is zero or one and each of n and p is a number independently selected from zero through three; 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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