.beta.-alanineamide aryl/alkylsulfide/sulfonyl-terminated amino-diol compounds for treatment of hypertension
AssigneeG. D. Searle & Co.
InventorsBarbara B. Chen, Gunnar J. Hanson, John S. Baran
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AssigneeG. D. Searle & Co.
InventorsBarbara B. Chen, Gunnar J. Hanson, John S. Baran
Estimating the term…
Compounds characterized generally as .beta.-alanineamide aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from methyl and ethyl; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
A compound of Formula I:
A pharmaceutical composition comprising a therapeutically-effective amount of a renin-inhibiting compound and a pharmaceutically-acceptable carrier or diluent, said renin-inhibiting compound selected from a family of compounds of Formula I:
A therapeutic method for treating a circulatory-related disorder, said method comprising administering to a hypertensive patient a therapeutically-effective amount of a compound of Formula I:
The method of claim 28 wherein said compound is N-[3-[[1S,1R*-(cyclohexylmethyl)-2S*,3R-dihydroxy-5-methylhexyl]amino]-2S* -methyl-2-3-oxopropyl]-.alpha.-[[(1,1-dimethylethyl)thio]methyl]benzeneprop anamide.
The method of claim 28 wherein said compound is N-[[1S,1R*-(cyclohexylmethyl)-2S*,3R*-dihydroxy-5-methylhexyl]-2R*-methyl- 3-[[1-oxo-3-(phenylsulfonyl)propyl]amino]propanamide.
Dependencies are inferred from the claim text.