Propargyl-terminated cycloalkylalkyl-P2-site substituted aryl/alkylsulfonyl-terminated alanine amino-diol compounds for treatment of hypertension
US5268391A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jul 20, 1992 |
| Grant date | Dec 7, 1993 |
| Priority date | — |
| Expiry date | Jul 20, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2601/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds characterized generally as being propargyl-terminated aryl/alkylsulfonyl-terminated amino diol derivatives having a cycloalkylalkyl group at the P2 substitution site 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 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 cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is propargyl or a propargyl-containing moiety.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.