Patent ID: 6350907
Filing Date: 2002-02-26
Classification: A61P,C07B,C07C,C07D,Y02P

Abstract:
A compound of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, whereinR1 is H, OH, C1-4 alkyl, C1-4 alkoxy, or C2-4 alkenyl, R2 is C1-6 akyl optionally substituted by fluoro, indolyl, imidazolyl, SO2(C1-4 alkyl), C5-7 cycloalkyl, or by an optionally protected OH, SH, CONH2, CO2H, NH2 or NHC(&boxH;NH)NH2 group, C5-7 cycloalkyl optionally substituted by C1-6 alkyl,or is benzyl optionally substituted by optionally protected OH, C1-6 alkoxy, benzyloxy or benzylthio,wherein the optional protecting groups for said OH, SH, CONH2, NH2 and NHC(&boxH;NH)NH2 groups are selected from C1-6 alkyl, benzyl, C1-6 alkanoyl,and where the optional protecting groups for said CO2H is selected from C1-6 alkyl or benzyl,R3, R5 and R6 are each independently selected from H and F, R4 is CH3, Cl or F, X is HO or HONH, Y is a direct link or O, Z is either a group of formula (a): where R10 is C1-4 alkyl, C1-4 alkoxymethyl, hydroxy(C2-4 alkyl), carboxy(C1-4 alkyl) or (amino or dimethylamino)C2-4 alkyl,and R11 is phenyl, naphthyl or pyridyl optionally substituted by up to three substituents independently selected from halo and methyl;or(b) R14 is H, OH, CH, or halo, Ar is a group of formula (c), (d) or (e): whereinA is N or CR12, B is N or CR13, provided that A and B are not both N,R7 and R9 are each independently H or F, and R8, R12 and R13 are H, CN, C1-6 alkyl, hydroxy(C1-6 alkyl), hydroxy(C1-6)alkoxy, C1-6 alkoxy(C1-6)alkoxy,(amino or dimethylamino)C1-6 alkyl, CONH2, OH, halo, C1-6 alkoxy, (C1-6 alkoxy)methyl, piperazinylcarbonyl, piperidinyl, C(NH2)&boxH;NOH or C(&boxH;NH)NHOH, with the proviso that at least two of R8, R12 and R13 are H.