2(1h)-quinolone derivatives, their preparation and their use...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) C07D 215/22 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2228038

Compounds of formula (I) Image in which A represents a 4-(thieno[3,2-c]pyridin-4-yl)-1- piperazinyl or 4-(4-fluorobenzoyl)-1-piperidyl group, R1 and R2 each represent, independently of one another, either a hydrogen or halogen atom, or an amino, hydroxyl, nitro, cyano, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, trifluoromethoxy or -COOH group, a group -COOR4, a-CONH2 group or a group -CONHR4, -CONR4R5, -SR4, -SO2R4, -NHCOR4, -NHSO2R4 or -N(R4) 2, where R4 and R5 are each a(C1-C4) alkyl group, R3 represents either a hydrogen atom, or a (C1-C4)alkyl group, or a group -(CH2)POH, -(CH2)p NH2, - ( CH2 ) n COOH, - ( CH2 ) n COOR4 , - ( CH2 ) n CONH2 , - ( CH2 ) n CONHOH, - (CH2)p SH, - (CH2)n SO3H, - (CH2)n SO2NH2, - (CH2)n SO2NHR4, - (CH2)n SO2NH4R5, - (CH2)CONHR24, - (CH2)n CONR4R5, -(CH2)p NHSO2R4, -(CH2)p NHCOR4 or -(CH2)p OCOR4, where R4 and R5 are each a(C1-C4)alkyl group, n is equal to 1, 2, 3 or 4, p is equal to 2, 3 or 4 and m is equal to 2, 3 or 4. Use in therapy.

Composés de formule (I), dans laquelle A représente un groupe 4-(thiéno[3,2-c]pyridin-4-yl)pipérazin-1-yle ou 4-(4-fluorobenzoyl)pipéridin-1-yle, R1 et R2 représentent chacun indépendamment l'un de l'autre, soit un atome d'hydrogène ou d'halogène, soit un groupe amino, hydroxy, nitro, cyano, (C1-C6)alkyle, (C1-C6)alcoxy, trifluorométhyle, trifluorométhoxy, -COOH, -COOR4, -CONH2, -CONHR4, -CONR4R5, -SR4, -SO2R4, -NHCOR4, -NHSO2R4, -N(R4)2 où R4 et R5 sont chacun un groupe (C1-C4)alkyle, R3 représente soit un atome d'hydrogène, soit un groupe (C1-C4)alkyle, -(CH2)pOH, -(CH2)pNH2, -(CH2)nCOOH, -(CH2)nCOOR4, -(CH2)nCONH2, -(CH2)nCONHOH, -(CH2)pSH, -(CH2)nSO3H, -(CH2)nSO2NH2, -(CH2)nSO2NHR4, -(CH2)nSO2NR4R5, -(CH2)nCONHR4, -(CH2)nCONR4R5, -(CH2)pNHSO2R4, -(CH2)pNHCOR4, -(CH2)pOCOR4, où R4 et R5 sont chacun un groupe (C1-C4)alkyle, n est égal à 1, 2, 3 ou 4, p est égal à 2, 3 ou 4 et m est égal à 2, 3 ou 4. Application en thérapeutique.

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