| abstract |
A compound of general formula I ** (See formula) ** wherein R 1 is halogen, hydroxy, mercapto, trifluoromethyl, amino, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-4 alkoxy, alkylthio C1-4, C1-6 amino alkyl, C1-4 alkoxycarbonyl, cyano, -CONH2 or nitro; R2 is halogen, amino, C1-4 alkyl or nitro; R3 represents one or more same or different substituents selected from the group consisting of hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy; R4 is fluoro; one of R5 and R6 is -COOH, -C (O) NHOH, -C (O) NHNH2, Y2R9, Y2R9Y3R10, C1-6-Y2R9 alkyl, C1-6-Y2R9 Y3R10 alkyl, C2-6-Y2R9 alkenyl, alkenyl C2-6-Y2R9 Y3R10, Y2R9-C1-6-Y3R10 alkyl, Y2R9-C2-6l-Y3R10 alkenyl, C3-12-Y2R9 carbocyclyl, C3-12-Y2R9Y3R10 carbocyclyl, C1-12-Y2R9 heterocyclyl C1-12 -Y2R9Y3R10, C3-12 carbocyclyl-C 1-6 alkyl-Y2R9, C3-12 carbocyclyl-C 1-6 alkyl-Y2R9 Y3R10, C 1-12 heterocyclyl-C 1-6 alkyl-Y2R9, C 1-12 heterocyclyl-C 1-6 alkyl- Y2R9Y3R10, C3-12 carbocyclyl-C1-6-Y3R10 alkyl, C1-12 heterocyclyl-C1-6-Y3R10 alkyl, C1-12 heterocyclyl-C1-10 alkyl, C3-12 carbocyclyl C1-10 alkyl, C 2-10 alkyl - C1-12 heterocyclyl, C1-10 alkyl-C3-12 carbocyclyl, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocyclyl or C1-12 heterocyclyl, each optionally substituted by one or more substituents, the same or different represented by R7, and the other is hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, C1-4 alkylthio, C1-6 amino alkyl, C1-4 alkoxycarbonyl, cyano, -CONH2 or nitro; with the proviso that when R5 or R6 is phenyl, C1-5 alkyl or C2-3 alkenyl, said R5 or R6 is substituted by one or more substituents, the same or different represented by R7 (except three fluoro when R5 or R6 is methyl ), R7 is halogen, hydroxy, mercapto, trifluoromethyl, amino, C1-4 alkyl, C1-6 hydroxyalkyl, C1-4 alkoxy, C1-4 alkylthio, C1-6 alkylamino, C1-4 carbonyl alkoxy, C1-9 trialkylammonium in association with an anion, cyano, azido, nitro, -S (O) 2NH2, -S (O) 2NRaRb, -S (O) 2R, -COOH, -CONH2, -NRaC (O) R ', -CONHR' or -CONRR ', in which R and R' are the same or different, each representing hydrogen or C1-3 alkyl; Ra, Rb and Rc are the same or different, each representing hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 carbocyclyl, C1-12 heterocyclyl, or aryl, each being C1- alkyl 4, C2-4 alkenyl, C2-4 alkynyl, C3-6 carbocyclyl, C1-12 heterocyclyl, or aryl optionally substituted by one or more substituents, the same or different represented by R7; Y2 is -O-, -S-, -S (O) -, -S (O) 2-, -NRa-, -NRaC (O) NRb-, -NRaC (O) -, -C (O) NRa -, -C (O) NRaO-, -C (O) -, -NRaC (O) O-, -NRaS (O) 2-, -OC (O) -, -C (O) O-, -C (O) NRaNRbC (S) NRc-, -C (O) NRaNRb-, or -S (O) 2NRa-; R9 is C1-10 alkyl-C1-12 heterocyclyl, C1-10 alkyl-C3-12 carbocyclyl, C1-10 alkyl-C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocyclyl, C1-12 heterocyclyl, C3- carbocyclyl 12-C 1-10 alkyl, or C 1-12 heterocyclyl, C 1-10 alkyl, C 3-6 carbocyclyl, C 1-6 alkenyl, C 3-6 carbocyclyl, C 2-6 alkynyl, each optionally substituted by one or more substituents , the same or different represented by R7, with the proviso that when Y2 is -O-, -NRa-, -S- or -C (O) O-, and R9 is C1-6 alkyl, said C1-6 alkyl is substituted by one or more substituents, the same or different represented by R7; Y3 is -O-, -S-, -S (O) -, -S (O) 2-, -NRa-, -NRaC (O) NRb-, -NRaC (O) -, -C (O) NRa -, -C (O) NRaO-, -C (O) -, -NRaC (O) O-, -NRaS (O) 2-, -OC (O) - or -C (O) O-; R10 is C1-10 alkyl-C1-12 heterocyclyl, C1-10 alkyl-C3-12 carbocyclyl, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocyclyl or C1-12 heterocyclyl, each being of them optionally substituted by one or more substituents, the same or different represented by R7; or, when one of R5 or R6 is the group -C (O) NRaR9, Ra and R9, together with the nitrogen atom to which they are attached, form a C1-12 heterocyclic ring optionally comprising one or more additional heteroatoms selected from the group consisting of O, 5 and N, optionally substituted with one or more substituents represented by R7; or its pharmaceutically acceptable salt, solvate, or ester. |