Patent ID: 6593324
Filing Date: 2003-07-15
Classification: A61K,C07D

Abstract:
A compound of formula II, or a pharmaceutically acceptable salt or ester thereof,wherein, R1 is H or (C1-C6)alkyl; each R2 is independently OH, halogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, NO2, NH2, mono- or di(C1-C6)alkylamino, (C1-C6)alkyl-S- or hydroxy(C1-C6)alkyl; A is a benzene ring or (C5-C7)cycloalkyl; when A is a benzene ring each R3 is independently OH, halogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkoxy, halo-(C1-C6)alkyl, NO2, NH2, mono- or di(C1-C6)alkylamino, (C1-C6)alkyl-CO-, mono- or di(C1-C6)-alkylcarbamoyl, (C1-C6)alkyl-S-, hydroxy(C1-C6)alkyl or NH2â€”COâ€”; when A is (C5-C7)cycloalkyl each R3 is independently OH, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, mono- or di(C1-C6)alkylamino or hydroxy(C1â€”C6)alkyl; R4 and R5 form, together with the N-atom to which they are attached, wherein X is O or &boxH;NR6; R6 is H, OH, NH2, (C1-C6)alkyl, (C2-C6)alkenyl, CN-(C1-C6)alkyl, (C1-C6)alkoxy-CO-(C1-C6)alkyl, (C1-C6)alkyl-CO-, NH2â€”COâ€”, mono- or di(C1-C6)alkylcarbamoyl, hydroxy(C1-C6)alkyl, (C1-C6)cycloalkyl or benzyl, wherein the said benzyl is optionally substituted with one to three substituent(s) each independently being OH, halogen, NO2, NH2, (C1-C6)alkyl, (C1-C6)alkoxy, mono- or di(C1-C6)alkylamino or halo-(C1-C6)alkyl; or R4 and R5 form, together with the N-atom to which they are attached, wherein n=1 or 2; R6 is as defined above; and r=0 to 3; or R4 and R5 form, together with the N-atom to which they are attached, 1-imidazolyl, 1-imidazolinyl or 1-triazolyl, each of which can optionally be substituted with one to three substituent(s) R7 each independently being (C1-C6)alkyl or NH2; Ra is H, OH, halogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, NO2, NH2, mono- or di(C1-C6)alkylamino or (C1-C6)alkyl-Sâ€”; Rb is H, OH, halogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkynyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, NO2, NH2, mono- or di(C1-C6)alkylamino, (C1-C6)alkyl-Sâ€” or CN; m is 0 to 3; and t is 0 to 3, with the provisos, that when A is a benzene ring, then Ra and Rb are not at the same time H; and the compound is not 4-[4-[(7-Chloro-2-methyl-4-quinolinyl)amino]phenyl]-1-diethylcarbamoylpiperazine.