Ethynyl alanine amino diol compounds for treatment of hypertensi

Details Ethynyl alanine amino diol compounds for treatment of hypertensi Ethynyl alanine amino diol compounds for treatment of hypertensi

1991-10-29

1993-07-13

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

N-c doai

514255, 514315, 514317, 514357, 514365, 514374, 514378, 514400, 514427, 514428, 514438, 514471, 514478, 514484, 514485, 514517, 514588, 514595, 514601, 514608, 514616, 544400, 546231, 546233, 546332, 546336, 548204, 548235, 548247, 548561, 548568, 5483751, 5483451, 5483361, 5483381, 5483385, 549 76, 549 77, 549492, 549496, 558 50, 558 61, 560 13, 560 27, 560 29, 560115, 560148, 560159, 564 32, 564 47, 564 57, 564 86, 564 95, 564 96, 564 97, 564102, 564153, 564154, 564155, 564152, 564159, A61K 3127

Patent

active

052274012

ABSTRACT:
Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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: 4902706 (1990-02-01), Hanson et al.
patent: 5032577 (1991-07-01), Fung et al.
Umezawa et al., in J. Antibiot. (Tokyo), 23, 259-262 (1970).
Gross et al., Science, 175, 656 (1971).
Boger et al, Nature, 303, 81 (1983).
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