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

1989-06-12

1991-05-21

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

544158, 544 90, 544 92, 544177, 546216, 546309, 546312, 548252, 548337, 548495, 548539, 548542, 549362, 560 12, 560 13, 560 34, 560138, 560 10, 560142, A61K 3122

Patent

active

050176102

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 be the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X-- .circle.A --(R.sup.4).sub.n wherein X is a single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by ##STR3## -- .circle.A -- is carbocyclic or heterocyclic 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, (10) the formula: --CONR.sup.41 R.sup.42 (11) the formula: --COO--Z.sup.42 --COOR.sup.43 wherein Z.sup.42 is C1-4 alkylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (12) the formula: --COO--Z.sup.42 --CONR.sup.41 R.sup.42 (13) the formula: --OCO--R.sup.45 wherein R.sup.45 is C1-8 alkyl or p-guanidinophenyl, (14) the formula: --CO--R.sup.46 wherein R.sup.46 is C1-4 alkyl, (15) the formula: --O--Z.sup.43 --COOR.sup.450 wherein Z.sup.43 is C1-6 alkylene, R.sup.450 represents a hydrogen, C1-8 alkyl or p-guanidinophenyl, (16) the formula: ##STR4## wherein ##STR5## is an amino acid residue, R.sup.47 is bond, C1-4 alkyl, R.sup.48 is --H or C1-4 alkyl, R.sup.49 is --OH, C1-4 alkoxy, --NH.sub.2, amino substituted by one or two C1-4 alkyl, carbamoylmethoxy or carbamoylmethoxy substituted by one or two C1-4 alkyl at N atom of carbamoyl, wherein ##STR6## is C3-6 heterocyclic ring, (ii) R.sup.1, R.sup.2 and N atom bonded to R.sup.1 and R.sup.2 together represents heterocyclic ring containing at least a N atom(s) and substituted by --COOH or unsubstituted heterocyclic ring containing at least a N atom(s), R.sup.3 is (1) --H, (2) --OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4.
or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating and/or preventing agent for pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.

REFERENCES:
patent: 3793292 (1974-02-01), Yamamura et al.
patent: 4188390 (1980-02-01), Campbell

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