Derivatives of p-substituted phenyl ester of pivalic acid

Details Derivatives of p-substituted phenyl ester of pivalic acid Derivatives of p-substituted phenyl ester of pivalic acid

1992-10-13

1994-08-09

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514352, 514357, 514424, 514426, 514427, 546294, 546309, 546312, 546334, 546318, 548543, 548544, 548557, 548558, A61K 3140, A61K 3144, C07D21370, C07D20712

Patent

active

053366816

ABSTRACT:
A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X--A-- (R.sup.4)n wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR3## --A-- is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy, 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula: --SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H, C1-4 alkyl or benzyl;
or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.

REFERENCES:
patent: 2694720 (1954-11-01), Denton
patent: 3793292 (1974-02-01), Yamamura et al.
patent: 4074059 (1978-02-01), Bullock
patent: 4188390 (1980-02-01), Campbell
patent: 4289865 (1981-09-01), Wilson
patent: 4310682 (1982-01-01), Ozawa
patent: 4335254 (1982-06-01), Wilson

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