IL-5 inhibiting 6-azauracil derivatives

Details IL-5 inhibiting 6-azauracil derivatives IL-5 inhibiting 6-azauracil derivatives

2005-05-17

2005-05-17

Raymond, Richard L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S236200, C514S227800, C544S182000, C544S112000, C544S058600

Reexamination Certificate

active

06894046

ABSTRACT:
The present invention is concerned with the compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5or a direct bond; Y is O, S, NR5or S(O)2; R1independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8or substituted C1-4alkyl; R2is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3and R4independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3and R4form a C2-6alkanediyl; R5is hydrogen or C1-4alkyl; R6is a sulfonyl or sulfinyl derivative; R7and R8are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(═O)—O—R14, Het3, Het4and R6; R11is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y—C1-4alkanediyl-C(═O)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3and C(═O)Het3; R14is hydrogen, C1-4alkyl, C3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het1, Het2, Het3and Het4are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

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