IL-5 inhibiting 6-azauracil derivatives

摘要

The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR⁵ or a direct bond; Y is O, S, NR⁵ or S(O)₂; R¹ independently is C_1-6alkyl, halo, polyhaloC_1-6alkyl, hydroxy, mercapto, C_1-6alkyloxy, C_1-6alkylthio, C_1-6alkylcarbonyloxy, aryl, cyano, nitro, Het³, R⁶, NR⁷R⁸ or substituted C_1-4alkyl; R² is Het¹, C_3-7cycloalkyl or optionally substituted C_1-6alkyl and if X is O, S or NR⁵, then R² may also represent aminocarbonyl, aminothiocarbonyl, C_1-4alkylcarbonyl, C_1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het¹carbonyl or Het¹thiocarbonyl; R³ and R⁴ independently are hydrogen, C_1-6alkyl or C_3-7cycloalkyl; R³ and R⁴ form a C_2-6alkanediyl; R⁵ is hydrogen or C_1-4alkyl; R⁶ is a sulfonyl or sulfinyl derivative; R⁷ and R⁸ are independently hydrogen, optionally substituted C_1-4alkyl, aryl, a carbonyl containing moiety, C_3-7cycloalkyl, -Y-C_1-4alkanediyl-C(-O)-O-R¹⁴, Het³, Het⁴ and R⁶; R¹¹ is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C_1-4alkyloxy, formyl, trihaloC_1-4alkylsulfonyloxy, R⁶, NR⁷R⁸, C(-O)NR⁷R⁸, C_1-4alkanediyl-C(-O)-O-R¹⁴, -C(-O)-O-R¹⁴, -Y-C_1-4alkanediyl-C(-O)-O-R¹⁴, aryl, aryloxy, arylcarbonyl, C_3-7cycloalkyl, C_3-7cycloalkyloxy, phthalimide- 2 -yl, Het³ and C(-O)Het³; R¹⁴ is hydrogen, C_1-4alkyl, C_3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C_1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het¹, Het², Het³ and Het⁴ are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.