abstract |
The present invention relates to indazole derivatives of the formula (I), in which: R is H, alkyl, - (CH2) n (cycloalkyl), where n is 0 to 2, (alkoxy) alkyl, alkenyl, - (CH2) n (heterocyclyl), where n is 0 to 2 or - (Z ') b (Z' ') c (aryl), where b and c are independently 0 or 1, Z' is alkylene or alkenylene and Z '' is O, S, SO2; R1 is H, alkyl, alkenyl, phenyl, cycloalkyl; R2 is selected from the group of substituents presented in fig. 2; in which the broken lines in formulas (Ia) and (Ib) represent a single or double bond; m is 0 to 4; R3 is H, halogen, cyano, alkyl, cyclopropyl; R4 is H, COOH, CN,, tetrazolyl, thiazolyl, imidazolyl, pyrazolyl, oxazolyl, triazolyl, isoxazolyl; R5 is H, alkyl, CH2OH, CN, C (O) H, COOH, CONH2 or NH2; R6 is methyl, ethyl; R7 is OH, SH, SO2NH2, tetrazolyl, thiazolyl, imidazolyl, oxazolyl, isoxazolyl; and to the pharmaceutically acceptable salts thereof. The invention furthermore relates to intermediates for the preparation of the compounds of formula (I), to the pharmaceutical compositions containing them and to the methods of use, to the compounds of formula (I) or to the pharmaceutically acceptable salts of they are for the inhibition of type IV phosphodiesterase (PDE) and the production of tumor necrosis factor (TNF) in a mammal and as such are useful in the treatment of asthma, bronchitis, arthritis. Non-limiting eg 1- (1-cyclopentyl-3-ethyl-1H-indazol-6-yl) -4-oxo-cyclohexanecarbonitrile |