Novel IL-5 inhibiting 6-azauracil derivatives

The present invention is concerned with the compound 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 subst...

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Hauptverfasser: LACRAMPE, JEAN F. A, FREYNE, EDDY JEAN EDGARD, BOECKX, GUSTAAF MARIA, VENET, MARC G
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention is concerned with the compound 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 C1-6 alkyl, C1-6 alkyloxy, C3-7 cycloalkyl or aryl; R2 is aryl, Het1, C3-7 cycloalkyl, optionally substituted C1-6 alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4 alkyl; R4 and R5 independently are optionally substituted C1-6 alkyl, halo, hydroxy, mercapto, C1-6 alkyloxy, C1-6 alkylthio, C1-6 alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8, R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4 alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7 cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4 alkyloxy, carboxyl, C1-4 alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(=O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7 cycloalkyl, C3-7 cycloalkyloxy, phhalimide-2-yl, Het3 and C(=O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4 alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent C3-7 and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to pocesses for thei preparation and compositions comprising them. It further relates to their use as a medicine.