Patent ID: 6544997
Filing Date: 2003-04-08
Classification: A61P,C07D,Y02P

Abstract:
A compound of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof, or a pharmaceutically acceptable acid or base addition salt thereof, wherein â€”R1â€”R2â€” is a bivalent radical of formula â€ƒwherein in said bivalent radicals optionally one or two hydrogen atoms on the same or a different carbon atom may be replaced by C1-6alkyl or hydroxy, R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, or C2-6alkenyl, or L is a radical of formula â€ƒwherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, amino, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or Het1; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C16alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond, NR10, O, S, Oâ€”(CH2)nâ€”, Sâ€”(CH2)nâ€”, or â€”NR10â€”(CH2)nâ€”, wherein n is an integer from 1 to 6, and R10 being hydrogen or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl; and each aryl represents unsubstituted phenyl or phenyl substituted with 1, 2 or 3 substituents each independently selected from halo, hydroxy, C1-6alkyl, C1-6alkyloxy, amino-sulfonyl, C1-6alkylcarbonyl, nitro, trifluoromethyl, amino or aminocarbonyl; and Het1 and Het2 each independently are selected from furan; furan substituted with C1-6alkyl or halo; tetrahydrofuran; tetrahydrofuran substituted with C1-6alkyl; dioxolane; dioxolane substituted with C1-6alkyl; dioxane; dioxane substituted with C1-6alkyl; tetrahydropyran; tetrahydropyran substituted with C1-6alkyl; pyrrolidinyl; pyrrolidinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano, or C1-6alkyl; pyridinyl; pyridinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano, C1-6alkyl; pyrimidinyl; pyrimidinyl substituted with one or two substituents each independently selected from halo, hydroxy, cyano, C1-6alkyl, C1-6alkyloxy, amino and mono and di(C1-6alkyl)amino; pyridazinyl; pyridazinyl substituted with one or two substituents each independently selected from hydroxy, C1-6alkyloxy, C1-6alkyl or halo; pyrazinyl; pyrazinyl substituted with one ore two substituents each independently selected from halo, hydroxy, cyano, C1-6alkyl, C1-6alkyloxy, amino, mono- and di(C1-6alkyl)amino and C1-6alkyloxycarbonyl; Het1 can also be a radical of formula Het1 and Het2 each independently can also be selected from the radicals of formula R13 and R14 each independently are hydrogen or C1-4alkyl.