Patent ID: 6423690
Filing Date: 2002-07-23
Classification: A61K,A61P,C07C,C07D,C07K

Abstract:
A method for inhibiting the growth of bacteria in humans and non-human mammals suffering bacterial infections, which comprises administering to a subject suffering such infection an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof: wherein:R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10â€”(X)nâ€”(ALK)mâ€” wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo, trifluoromethyl, cyano, nitro, â€”COOH, â€”CONH2, â€”COORA, â€”NHCORA, â€”CONHRA, â€”NHRA, â€”NRARB, or â€”CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent â€”NHâ€”, â€”Oâ€” or â€”Sâ€” linkages, X represents â€”NHâ€”, â€”Oâ€” or â€”Sâ€”, and m and n are independently 0 or 1; and A represents (i) a group of formula (IA), (IB), (IC) or (ID) â€ƒwherein: R3 represents hydrogen and R4 represents the side chain of a natural or non-natural alpha amino acid or R3 and R4 when taken together with the nitrogen and carbon atoms to which they are respectively attached form an optionally substituted saturated heterocyclic ring of 5 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring, R5 and R6, independently represent hydrogen, or optionally substituted C1-C8 alkyl, cycloalkyl, aryl, aryl(C1-C6 alkyl), heterocyclic, or heterocyclic(C1-C6 alkyl), or R5 and R6 when taken together with the nitrogen atom to which they are attached form an optionally substituted saturated heterocyclic ring of 3 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring, wherein substituted means substituted with up to four substituents, each of which independently may be (C1-C6)alkyl, benzyl, (C1-C6)alkoxy, phenoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo, trifluoromethyl, nitro, â€”COOH, â€”CONH2, â€”CORA, â€”COORA, â€”NHCORA, â€”CONHRA, â€”NHRA, NRARB, or CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and R7 represents hydrogen, C1-C6 alkyl, or an acyl group.