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US 5,314,910 AGranted
Ester inhibitors
AssigneeCortech, Inc.
InventorsGary P. Kirschenheuter, Raymond T. Cunningham, John C. Cheronis
Life of this patent
Estimating the term…
Abstract
2-Heteroaromatic alkanoate esters which are useful as inhibitors of human leukocyate or neutrophil elastase.
Claims8
A compound of the formula:
- ##STR11## wherein:
- R.sub.1 and R.sub.2, which may be the same or different, are selected from the group consisting of hydrogen, alkyl of 1-4 carbons, cycloalkyl of 3-6 carbons or together represent a methylene group --(CH.sub.2).sub.n -- where n is a whole number of 1 to 6;
- Ar is phenyl or phenyl substituted with a member of the group consisting of halogen, nitro, --C(O)CH.sub.3, --S(O).sub.p R.sub.9 where p is 0, 1 or 2 and R.sub.9 is hydroxy, --ONa, alkyl of 1-12 carbons, lower alkyl substituted with halogen, lower alkyl bearing a carboxylic group and cycloalkyl;
- and
- HET is furanyl, thienyl, benzfuranyl and benzthienyl, provided that R.sub.1 and R.sub.2 are not both hydrogen.
2 more elements
A method of inhibiting undesired elastase activity which comprises administering to a subject in need of such inhibition, an effective amount of a compound of the formula:
- ##STR12## wherein:
- R.sub.1 and R.sub.2, which may be the same or different, are selected from the group consisting of hydrogen, alkyl of 1-4 carbons, cycloalkyl of 3-6 carbons or together represent a methylene group --(CH.sub.2).sub.n -- where n is a whole number of 1 to 6;
- Ar is phenyl or phenyl substituted with a member of the group consisting of halogen, nitro, --C(O)CH.sub.3, --S(O).sub.p R.sub.9 where p is 0, 1 or 2 and R.sub.9 is hydroxy, --ONa, alkyl of 1-12 carbons, lower alkyl substituted with halogen, lower alkyl bearing a carboxylic group and cycloalkyl;
- and
- HET is furanyl, thienyl, benzfuranyl and benzthienyl.
2 more elements
Dependencies are inferred from the claim text.