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filingDate 1992-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 1993-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0539976-A1
titleOfInvention Ethynyl-alanine-amino-diol compounds for treatment of hypertension
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 In n wherein A is selected from CO and SO₂ wherein X is selected from oxygen atom and methylene; wherein each of R₁ and R₉ is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R₁ and R₉ are attached may be combined with oxygen to form an N-oxide; wherein R₂ is selected from hydrido, methyl, ethyl and isopropyl; wherein R₃ is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R₅ is propargyl or a propargyl-containing moiety; wherein R₇ is cyclohexylmethyl; wherein each of R₄ and R₆ is independently selected from hydrido and methyl; wherein R₈ is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R₁₁ and R₁₂ 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.
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Total number of triples: 552.