| abstract |
The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a -(CH2)n -Y or -CH = CH-Y group, in which Y is halogen, -OH, -OR, -COH, -COR, -COOH, -COOR, -COH, -COR, -CONH2, -CON(Rx, Ry) -CH = NOH, -CO- -CH = NOH, -NH2, -N(Rx, Ry), -NO2, -PO(OR)2-SH2, -SR, -SO2R, -SO2NHR, CN, or Z(Rc) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, Rx and Ry, identical or different are C1-C5 alkyl, Z an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5, Rb can further represent a hydrogen, and when Y is -COOH or -COOR in Rc, Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a -(CH2)n- group in which n is a whole number between 1 and 5: or a -CH(Rd)-CH(Re) group, Rd and Re, identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a -(CH2)n, -O-C-(CH2)m-, -(CH2)n, -C(O)-O-(CH2)m, -(CH2)n, -O-(CH2)m-, -(CH2)n, -N(Q)-(CH2)m-, or -(CH2)n, -S(O)t-(CH2)m-, group, in which n = 1 to 8, m = 0 to 8, t = 0, 1 or 2, and Q = H, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect. |