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Quinolinas and its therapeutic use.

2008 
1st. A compound of formula (I) or a pharmaceutically acceptable salt thereof: in which: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently -OR6, C1-C6 alkyl or C3-C6 cycloalkyl, the last two groups being optionally substituted with one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1-C6 alkyl or C3-C6 cycloalkyl, any of which is optionally substituted with one or more halogen atoms; X is -CH2 -, -S-, or -O-; one of the groups Y and Y1 is hydrogen and the other is OR6, -C (= O) R7, NR8SO2R6 or a heterocyclic group selected from furan, thiophene, pyrrole, oxazole, thiazole, imidazole, pyrazole, isoxazole, isothiazole, 1, 2, 3-oxadiazol, 1, 2, 4-oxadiazol, 1, 3, 4oxadiazol, furazano, 1, 2, 3-triazol, 1, 2, 4-triazol, 1, 2, 3-thiadiazole, 1, 2, 5-thiadiazole, 1, 3, 4-thiadiazole, tetrazol, pyridine, pyridazine, pyrimidine, pyrazine, 1, 2, 4-triazine and 1, 3, 5-triazine, any of which may be optionally substituted with one or more substituents chosen from halogen; cyano; C1-C6 alkyl optionally substituted with one or more halogen atoms; C3-C6 cycloalkyl optionally substituted with one or more halogen atoms; hydroxy; C1-C6 alkoxy optionally substituted with one or more halogen atoms; C1-C6 alkyl -O-CH2-, C1-C6-O-CH (RX) alkyl -and C1-C6 -OC alkyl (RX RY) -in which the C1-C6 alkyl part is optionally substituted with one or more halogen atoms; NH2 C (= O) -; RXNHC (= O) -; RX RY NC (= O) -; RX RY NS (= O) 2-; RX NHS (= O) 2-; NH2 S (= O) 2-; NH2-; RX NH-; RX RY N-; RX S (= O) 2-; RX C (= O) -; RX S (= O) 2 NH-; RX S (= O) 2 N RY -; RX C (= O) NH-y RX C (= O) N (RY) -; wherein RX and RY are independently C1-C4 alkyl or C3-C6 cycloalkyl, any of which is optionally substituted with one or more halogen atoms; or RX and RY, when attached to the same nitrogen atom, form a cyclic amino ring; R7 is C1-C6 alkyl or C3-C6 cycloalkyl being any of which optionally substituted with one or more halogen atoms; or phenyl or monocyclic heteroaryl having 5 or 6 ring atoms, optionally substituted with one or more substituents independently selected from halogen; cyano; C1-C6 alkyl optionally substituted with one or more halogen atoms; C3-C6 cycloalkyl optionally substituted with one or more halogen atoms; hydroxy; C1-C6 alkoxy optionally substituted with one or more halogen atoms; C1-C6-O-CH2- alkyl, C1-C6 alkyl -O-CH (RX) -and C1-C6 -OC alkyl (RX RY) -in which the C1-C6 alkyl part is optionally substituted with one or more halogen atoms; NH2C (= O) -; RX NHC (= O) -; RX RY NC (= O) -; RX RY NS (= O) 2-; RX NHS (= O) 2 -; NH2 S (= O) 2 -; NH2 -; RX NH-; RX RY N-; RX S (= O) 2 -; RX C (= O) -; RX S (= O) 2 NH-; RX S (= O) 2 N RY -; RX C (= O) NH-y RX C (= O) N (RY) -; wherein RX and RY are independently C1-C4 alkyl or C3-C6 cycloalkyl, any of which is optionally substituted with one or more halogen atoms; or RX and RY when attached to the same nitrogen atom form an amino cyclic ring; and R8 is hydrogen, C1-C6 alkyl or C3-C6 cycloalkyl, the last two groups being optionally substituted with one or more halogen atoms.
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