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    • 41. 发明专利
    • IL-5 INHIBITING 6-AZAURACIL DERIVATIVES
    • CA2352503A1
    • 2000-06-02
    • CA2352503
    • 1999-11-22
    • JANSSEN PHARMACEUTICA NV
    • LACRAMPE JEAN FERNAND ARMANDLIGNY YANNICKFREYNE EDDY JEAN EDGARDDEROOSE FREDERIK DIRK
    • C07D253/06A61K31/53A61P11/06A61P27/14A61P29/00A61P37/08A61P43/00C07D253/075C07D403/10C07D405/10C07D413/10C07D413/14C07D417/10C07D417/14
    • The present invention is concerned with the compounds of formula (I) the N- oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; - A- B- represents -(CH2)r-, -(CH2)t-O-, -(CH2)t-S(=O)u- or -(CH2)t-NR3-; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1- 6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, -C(=Q)-X2-R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 i s a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also b e hydroxy; where X2 is C(=O)-NH-NH or NH-NH-C(=O), R15 may be replaced by R11; Q is O, S or NR3; X2 is O, S, NR5, C(=O)-NH-NH, NH-NH-C(=O) or a direct bond; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, - Y- C1-4alkanediyl-C(=O)-O-R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonylox y, 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, Het3, Het4 and C(=O)Het3; aryl is optional ly 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.