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US 5,229,381 AGranted
Substituted azetidinones as anti-inflammatory and antidegenerative agents
AssigneeMerck & Co., Inc.
InventorsJames B. Doherty, Conrad P. Dorn, Paul E. Finke, William K. Hagmann, Malcolm MacCoss, Shrenik K. Shah
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Abstract
New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1##
Claims17
A compound of the formula (A) ##STR51## wherein:
- R is C.sub.1-6 alkyl;
- R.sup.1 is C.sub.1-6 alkyl or alkoxy-C.sub.1-6 alkyl;
- M is
- (1) hydrogen,
- (2) C.sub.1-6 alkyl,
- (3) C.sub.2-6 alkenyl, or
- (4) C.sub.1-6 alkoxy-C.sub.1-6 alkyl;
- X.sub.5 is
- (1) hydrogen,
- (2) C.sub.1-6 alkyl,
- (3) halo-C.sub.1-6 alkyl,
- (4) C.sub.2-6 alkenyl,
- (5) C.sub.2-6 alkynyl,
- (6) carboxy,
- (7) carboxy-C.sub.1-6 alkyl,
- (8) carboxy-C.sub.1-6 alkylcarbonyl,
- (9) carboxy-C.sub.1-6 alkylcarbonylamino,
- (10) carboxy-C.sub.2-6 alkenyl,
- (11) hydroxy-C.sub.1-6 alkyl,
- (12) C.sub.1-6 alkylcarbonyl, or
- (13) C.sub.1-6 alkylcarbonylamino;
- and
- X.sub.6 is
- (1) hydrogen,
- (2) C.sub.1-6 alkyl,
- (3) halo
- (4) carboxy,
- (5) C.sub.1-6 alkoxy,
- (6) phenyl,
- (7) C.sub.1-6 alkylcarbonyl,
- (8) di-(C.sub.1-6 alkyl)amino,
- (9) phenoxy, or
- (10) methylenedioxy;
- or
- a pharmaceutically acceptable salt thereof.
32 more elements
Dependencies are inferred from the claim text.