2-saccharinylmethyl aryl and aryloxy acetates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
AssigneeSterling Winthrop Inc.
InventorsLee H. Latimer, Richard P. Dunlap
Life of this patent
Estimating the term…
Abstract
4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.
Claims6
A compound having the formula:
- ##STR20## wherein:
- m is zero, n is one;
- R.sup.1 is hydrogen or lower-alkyl;
- R.sup.2 is hydrogen or lower-alkyl;
- R.sup.3 is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl, perfluorolower-alkyl, lower-alkoxy and halogen;
- R.sup.4 is hydrogen, or lower-alkyl;
- and
- R.sup.5 is hydrogen, lower-alkoxy, or polyalkoxy-alkoxy;
- or acid-addition salts of basic members thereof or base-addition salts of acidic members thereof.
A composition for the treatment of degenerative diseases which comprises a pharmaceutical carrier and an effective proteolytic enzyme-inhibiting amount of a compound having the formula:
- ##STR21## wherein:
- m is zero, n is one;
- R.sup.1 is hydrogen or lower-alkyl;
- R.sup.2 is hydrogen or lower-alkyl;
- R.sup.3 is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl, perfluorolower-alkyl, lower-alkoxy and halogen;
- R.sup.4 is hydrogen, or lower-alkyl;
- and
- R.sup.5 is hydrogen, lower-alkoxy, or polyalkoxy-alkoxy;
- or acid-addition salts of basic members thereof or base-addition salts of acidic members thereof.
A method for the treatment of degenerative diseases which comprises administering to a patient in need of such treatment a medicament containing an effective proteolytic enzyme-inhibiting amount of a compound having the formula:
- ##STR22## wherein:
- m is zero and n is one;
- R.sup.1 is hydrogen or lower-alkyl;
- R.sup.2 is hydrogen or lower-alkyl;
- R.sup.3 is phenyl or phenyl substituted by from one to three, the same or different, members of the group consisting of lower-alkyl, perfluorolower-alkyl, lower-alkoxy and halogen;
- R.sup.4 is hydrogen, or lower-alkyl:
- and
- R.sup.5 is hydrogen, lower-alkoxy, or polyalkoxy-alkoxy;
- or acid-addition salts of basic members thereof or base-addition salts of acidic members thereof.
Dependencies are inferred from the claim text.