Use of ethynyl alanine amino diol compounds for treatment of hyp

Details Use of ethynyl alanine amino diol compounds for treatment of hyp Use of ethynyl alanine amino diol compounds for treatment of hyp

1998-03-24

1999-08-24

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...

514255, 514315, 514317, 514357, 514365, 514374, 514378, 514400, 514427, 514428, 514438, 514471, 514478, 514484, 514485, 514489, 514517, 514588, 514595, 514601, 514608, A61K 31165

Patent

active

059425482

ABSTRACT:
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

REFERENCES:
patent: 5227401 (1993-07-01), Hanson et al.
patent: 5484811 (1996-01-01), Hanson et al.

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