Patent ID: 6635643
Filing Date: 2003-10-21
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 R1 and R2 taken together form a bivalent radical of formula â€”Oâ€”CH2â€”Oâ€” (a-1), â€”Oâ€”CH2â€”CH2â€” (a-2), â€”Oâ€”CH2â€”CH2â€”Oâ€” (a-3), â€”Oâ€”CH2â€”CH2â€”CH2â€” (a-4), â€”Oâ€”CH2â€”CH2â€”CH2â€”Oâ€” (a-5), â€”Oâ€”CH2â€”CH2â€”CH2â€”CH2â€” (a-6), wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl,R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, or C2-6alkenyl, Or L is a radical of formula â€”Alkâ€”R6 (b-1), â€”Alkâ€”Xâ€”R7 (b-2), â€”Alkâ€”Yâ€”C(&boxH;O)â€”R9 (b-3), or â€”Alkâ€”Yâ€”C(&boxH;O)â€”NR11R12 (b-4), wherein each Alk is C1-12alkanediyl; andR6 is hydrogen, hydroxy, cyano, C16alkylsulfonylamino, C3-6cycloalkyl, C56cycloalkanone, or Het1; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or Het2; X is O,S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said 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 C16alkyl; and Het1 and Het2 each independently are selected from furan; furan substituted with C1-6alkyl or halo; tetrahydrofuran a tetrahydrofuran substituted with C1-6alkyl; a dioxolane: a dioxolane substituted with C1-6alkyl a dioxane; a dioxane substituted with C1-6alkyl; tetrahydropyran; a 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; pyriniidinyl pyrimidinyl substituted with one or two substituents each indepentently 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 or 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 bearadical of formula Het1 and Het2 each independently can also be selected from the radicals of formula R13 and R14 each independently are hydrogen or C1-4 alkyl; and wherein the â€”OR4 radical is situated at the 4-position of the central piperidine moiety.