Novel betalactam elastase inhibitors containing phosphorous acid derivatives at the 4-position of the 2-azetidinone

Claim 1

A compound Formula (A) ##STR7## or a pharmaceutically acceptable salt thereof wherein: R is H, C 1-6 alkyl, or C 2-6 alkenyl; R 1 is H, C 1-6 alkyl, C 2-6 alkenyl or C 1-6 alkoxy-C 1-6 alkyl; M is (1) hydrogen, (2) C 1-6 alkyl, (3) hydroxy C 1-6 -alkyl, (4) halo C 1-6 -alkyl, (5) C 2-6 alkenyl, or (6) C 1-6 alkoxy-C 1-6 alkyl; R 2 and R 3 are each independently (1) hydrogen, (2) C 1-6 alkyl, (3) halo, (4) carboxy, (5) C 1-6 alkoxy, (6) phenyl, (7) C 1-6 alkylcarbonyl, (8) C 1-6 alkyloxycarbonyl, (9) di-(C 1-6 alkyl)amino, (10) phenoxy, or R 2 and R 3 are joined together with the carbon atoms to which they are attached to form a ring selected from furan, thiophene, and dioxacyclopentane; R 4 is (a) hydrogen, (b) C 1-6 alkyl, (c) halo, or (d) C 1-6 alkoxy; n is 0, 1, 2, 3, or 4; R 5 and R 6 are each independently (a) hydrogen, (b) C 1-6 alkyl, (c) substituted C 1-6 alkyl wherein the substituent is halo, hydroxy, C 1-6 alkoxy, C 1-6 alkylcarbonyloxy, amino, C 1-6 alkylamino, or di-(C 1-6 alkyl)- amino, (d) C 6-10 aryl wherein the aryl group is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) pyridyl, (4) furyl, (5) pyrryl, (6) thienyl, (7) imidazolyl, (8) benzimidazolyl, (9) pyrazinyl, (10) pyrimidyl, (11) quinolyl, (12) isoquinolyl, (13) benzofuryl, and (14) benzothienyl, and mono and di-substituted C 6-10 aryl as defined above in items (1) to (14) wherein the substituents are independently C 1-6 alkyl, halo, hydroxy, C 1-6 alkyloxy, C 1-6 alkylcarbonyl, C 1-6 alkoxy C 1-6 alkyl; (e) C 1-6 alkyl carbonyloxy-C 1-6 alkyl.