| abstract |
A compound of formula ** Formula ** in which A is - (C = O) NH- or-NH (C = O) -; X, Y and Z are = (CR6) -, = (CR7) - y = (CR8) -; R1 is ** Formula ** in which R10 is selected from the group consisting of hydrogen, (C1-C6) alkyl, HO-(C2-C6) alkyl or cycloalkyl (C3-C8) group; n is an integer from zero to two; q is the whole number one or two; s is an integer from one to three; R2 is chloro-, bromo-, (C1-C4) alkyl, -CF3 or -CN; R3 is selected from the group consisting of (C4-C10) alkyl, (C3-C12) cycloalkyl - (CR11R12) 8-, aryl (C6-C10) - (CR11R12) q- (CH2) -; heterocyclyl (C1-C10) - (CR11R12) 8- and heteroaryl (C1-C10) - (CR11R12) 8-; the said (C4-C10) alkyl being optionally substituted with one to three substituents independently selected from halo, hydroxyl, -CN, (C1-C4) alkyl, (C1-C4) alkoxy, -CF3, CF3O-, (C1-) alkyl C4) -S-, (C1-C4) alkyl - (S = O) -, (C1-C4) alkyl - (SO2) -, -CO2-(C1-C4) alkyl, formyl, (C1-C4) alkyl - (C = O) -, aryl (C6-C10), cycloalkyl (C3-C8), heteroaryl (C1-C10), heterocyclyl (C1-C10), aryl (C6-C10) -O-, cycloalkyl (C3- C8) -O-, heteroaryl (C1-C10) -O- and heterocyclyl (C1-C10) -O-; each of the aforementioned members of the group R3 heterocyclyl (C1-C10) - (CR11R12) 8- and heteroaryl (C1-C10) - (CR11R12) 3- containing one to three heteroatoms independently selected from -O- and -S ( O) n-; each of the aforementioned members of the R3 cycloalkyl (C3-C12) - (CR11R12) 4-, aryl (C6-C10) - (CR11R12) q- (CH2) -, heterocyclyl (C1-C10) group may be optionally substituted. (CR11R12) 8- and heteroaryl (C1-C10) - (CR11R12) 8-, in any carbon atom of the ring that may carry an additional substituent, with one to four substituents per ring selected from the group consisting of halo-, hydroxyl , -CN, (C1-C4) alkyl, (C1-C4) alkoxy, - CF3, CF3O-, (C1-C4) alkyl -S-, (C1-C4) alkyl - (S = O) -, alkyl ( C1-C4) - (SO2) -, (C1-C4) alkyl -O- (C = O) -, formyl, (C1-C4) alkyl - (C = O) -, aryl (C6-C10), [ aryl (C6-C10)] 2-CH-, cycloalkyl (C3-C8), heteroaryl (C1-C10), heterocyclyl (C1-C10), aryl (C6-C10) -O-, benzyl-O-, cycloalkyl ( C3-C8) -O-, heteroaryl (C1-C10) -O- and heterocyclyl (C1-C10) -O-; the aforementioned members of the R3 cycloalkyl (C3-C8) - (CR11R12) 5- and heterocyclyl (C1-C10) - (CR11R12) 8- group may also be optionally substituted with oxo; each of the aryl (C6-C10), cycloalkyl (C3-C8), heteroaryl (C1-C10) and heterocyclyl (C1-C10) above-mentioned may optionally be substituted, in any place of said substituents R3, in any atom carbon ring, with one to three moieties per ring, independently selected from the group consisting of halo-, hydroxyl, amino, -CN, (C1-C4) alkyl, (C1-C4) alkoxy, -CF3, CF3O-, (C1-C4) alkyl -NH-, [(C1-C4) alkyl] 2-N-, (C1-C4) alkyl - S-, (C1-C4) alkyl - (S = O) -, (C1-alkyl) -C4) - (SO2) -, (C1-C4) alkyl -O- (C = O) -, formyl and (C1-C4) alkyl - (C = O) -; R8, R7 and R8 are each independently selected from the group consisting of hydrogen, halogen, cyano-, hydroxyl, (C1-C6) alkyl optionally substituted with one to four chloro- or fluoro-, and (C1-C8) oxy optionally substituted with one to four chloro- or fluoro-; R11 and R12 are each independently selected from the group consisting of hydrogen, fluoro-, cyano-, hydroxyl, - CF3, CF3O-, (C1-C6) alkyl, cycloalkyl (C3-C8), alkyl (C1-C6) oxy , cycloalkyl (C3-C8) oxy, phenyl, heteroaryl (C1-C10) and heterocyclyl (C1-C10); the aforementioned (C1-C6) alkyl, (C3-C8) cycloalkyl, (C1-C6) alkyl oxy, cycloalkyl (C3-C8) oxy, phenyl, heteroaryl (C1-C10) and heterocyclyl (C1-C10) may optionally be substituted ) with one to three substituents independently selected from chloro-, fluoro-, cyano-, hydroxyl, -CF3, CF3O-, (C1-C4) alkyl -S-, (C1-C4) alkyl - (S = O) -, (C1-C4) alkyl - (SO2) -, (C1-C4) alkyl -O- (C = O) -, formyl or (C1-C4) alkyl - (C = O) -; with the proviso that when said R3 is cycloalkyl (C3-C12) - (CR11R12) 5-, R11 and R12 are each hydrogen and s is one or two; then said cycloalkyl (C3-C12) must be different from optionally substituted adamantyl; or a pharmaceutically acceptable salt or solvate thereof. |