Novel IL-5 inhibiting 6-azauracil derivatives for marking and identifying receptors and imaging organs

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, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR³ or a direct bond; R¹ is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C_1-6alkyl, C_1-6alkyloxy, C_3-7cycloalkyl or aryl; R² is aryl, Het¹, C_3-7cycloalkyl, optionally substituted C_1-6alkyl; and if X is O, S or NR³, then R² may also be a carbonyl or thiocarbonyl linked substituent; R³ is hydrogen or C_1-4allyl; R⁴ and R⁵ independently are optionally substituted C_1-6alkyl, halo, hydroxy, mercapto, C_1-6alkyloxy, C_1-6alkylthio, C_1-6alkylcarbonyloxy, aryl, cyano, nitro, Het³, R⁶ or NR⁷R⁸; R⁶ is substituted sulfonyl or sulfinyl; R⁷ and R⁸ are hydrogen, optionally substituted C_1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C_3-7cycloalkyl, Het³ and R⁶; R⁹ and R¹⁰ are each independently selected from hydrogen, optionally substituted C_1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C_3-7cycloalkyl, Het³ and R⁶; R¹¹ is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C_1-4alkyloxy, carboxyl, C_1-4alkyloxycarbonyl, trihaloC_1-4alkylsulfonyloxy, R⁶, NR⁷R⁸, C(-O)NR⁷R³, aryl, aryloxy, arylcarbonyl, C_3-7cycloalkyl, C_3-7cycloalkyloxy, phthalimide-2-yl, Het³ and C(-O)Het³; R¹² and R¹³ are each independently selected from hydrogen, optionally substituted C_1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C_3-7cycloalkyl and R⁶; aryl is optionally substituted phenyl; Het¹, Het² and Het³ are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.