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

1994-04-29

1995-04-04

Dees, Jose G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514359, 514546, 546 1, 548250, 548400, 560250, 560251, A61K 3140, C07C 6702

Patent

active

054038502

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 ##STR3## wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR4## 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: 3694720 (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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