| abstract |
SUMMARY OF THE INVENTION The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1 is H, OH, C1-C4 alkyl, C1-C4 alkoxy, or C2-4alkenyl, R2 is C1-6alkyl. - optionally substituted with one of the following groups: fluoro, indolyl, imidazolyl, SO2 (1-4C) alkyl, C5-7 cycloalkyl or optionally protected OH, SH, CONH2, CO2H, NH2 or NHC (= NH ) NH 2, a cycloalkyl group having 5 to 7 carbon atoms, optionally substituted with C 1-6 alkyl, or benzyl, optionally substituted with an optionally protected OH group, 1-6 carbon atoms, benzyloxy or benzylthio, R 3, R 5, and R6 is independently H or F, R4 is CH3, Cl or F, X; is OH or HONH, Y is a bond or O is Z is wherein R10 is C1-C4 alkyl, C1-C4 alkoxymethyl, hydroxy (2-4C) alkyl, carboxy. (C 1 -C 4) alkyl, or (amino or dimethylamino) C 2-4 alkyl, and R 11 is phenyl, naphthyl or pyridyl, optionally having up to max. can be substituted by a triple halogen or methyl group, or a group of formula (b) wherein R14 is H, OH, CH3 or halogen, Ar is (c), (d) or (e) wherein A is N or CR12; B is N or CR13, with the proviso that A and B cannot simultaneously be N, R7 and R9 are independently H or F, R8, R12 and R13 independently of one another H, CN, C1-6alkyl, hydroxy (1-6 carbon atoms) alkyl, hydroxy (C 1 -C 6) alkoxy, C 1-6 alkoxy (C 1 -C 6) alkoxy, (amino or dimethylamino) -1-6 carbon atoms, CONH 2, OH, halogen, 1-6 C 1-4 alkoxy, (1-6 carbon atoms) methyl, piperazinylcarbonyl, piperidinyl, C (NH 2) = NOH or C (= NH) NHOH, with the proviso that at least two of R 8, R 12 and R 13 are H The invention further relates to the compounds of formula (I) above for the preparation of precursors, the method of preparation of the compounds and the intermediates used in the preparation. HE |