Amino acyl amino propargyl diol compounds for treatment of a renin-mediated disease
AssigneeG.D. Searle & Co.
InventorsGunnar J. Hanson, J. Timothy Keane
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AssigneeG.D. Searle & Co.
InventorsGunnar J. Hanson, J. Timothy Keane
Estimating the term…
Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful as renin inhibitors for the treatment of a renin-mediated disease Compounds of particular interest are those of Formula I 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, β,ββ-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 selected from hydrido, alkyl, pyrazolealkyl, pyridylalkyl, thiazolylalkyl, imidazolealkyl, thienylalkyl, furanylalkyl, oxazolylalkyl, isoxazolylalkyl, pyrimidinylalkyl, pyridazinylalkyl and pyrazinylalkyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R7 is cyclohexylmethyl; wherein R8 is propargyl or a propargyl-containing moiety; 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.
A therapeutic method for treating a disease mediated by renin inhibition, said method comprising administering to a patient a therapeutically-effective amount of a compound of Formula I:
Dependencies are inferred from the claim text.