Patent ID: 6495555
Filing Date: 2002-12-17
Classification: A61P,C07D

Abstract:
A compound having the formula a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric forms thereof, wherein:Alk is C1-6alkanediyl; n is 1 or 2; X1 is â€”Oâ€”, â€”Sâ€”, â€”S(&boxH;O)â€” or â€”S(&boxH;O)2â€”; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is a radical of formula whereineach m independently is 0, 1 or 2; X2 is â€”Oâ€” or â€”NR11â€”; each X3 independently is â€”Oâ€”, â€”Sâ€” or â€”NR11â€”; X4 is â€”Oâ€”, â€”Sâ€”, â€”CH2â€”Sâ€” or â€”NR12â€”; X5 and X6 each independently are â€”CH2â€”,â€”Oâ€”, â€”Sâ€” or â€”NR11â€”; R2 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alalkylthio, amino or mono- or di(C1-6alkyl)amino; R4, R5, R6, R7, R8, R9, R10, R11 and R15 each independently are hydrogen or C1-6alkyl; R12 is hydrogen, C1-6alkyl, C1-6alkyloxyC1-6alkyl or pyridinylC1-6alkyl; R13, R14 sand R16 each independently are halo or C1-6alkyl; R3 and R4 taken together may form a bivalent radical â€”R3â€”R4â€” formula â€”CH2â€”CH2â€”CH2â€”â€ƒâ€ƒ(a-1); â€”CH2â€”CH2â€”CH2â€”CH2â€”â€ƒâ€ƒ(a-2); â€”CH&boxH;CHâ€”CH2â€”â€ƒâ€ƒ(a-3); â€”CH2â€”CH&boxH;CHâ€”â€ƒâ€ƒ(a-4) or â€”CH&boxH;CHâ€”CH&boxH;CHâ€”â€ƒâ€ƒ(a-5); wherein one or two hydrogen atoms of said radicals (a-1) to (a-5) each independently may be replaced by halo, C1-6alkyl, arylC1-6alkyl, trifluoromethyl, amino, hydroxy, C1-6alkyloxy or C1-10alkylcarbonyloxy; or where possible, two geminal hydrogen atoms may be replaced by C1-6alalkylidene or arylC1-6alkylidene; or â€”R3â€”R4â€” may also be â€”Sâ€”CH2â€”CH2â€”â€ƒâ€ƒ(a-6); â€”Sâ€”CH2â€”CH2â€”CH2â€”â€ƒâ€ƒ(a-7); â€”Sâ€”CH&boxH;CHâ€”â€ƒâ€ƒ(a-8); â€”NHâ€”CH2â€”CH2â€”â€ƒâ€ƒ(a-9); â€”NHâ€”CH2â€”CH2â€”CH2â€”â€ƒâ€ƒ(a-10); â€ƒâ€”NHâ€”CH&boxH;CHâ€”â€ƒâ€ƒ(a-11);â€”NHâ€”CH&boxH;Nâ€”â€ƒâ€ƒ(a-12); â€”Sâ€”CH&boxH;Nâ€”â€ƒâ€ƒ(a-13) or â€”CH&boxH;CHâ€”Oâ€”â€ƒâ€ƒ(a-14); wherein one or where possible two or three hydrogen atoms in said radicals (a-6) to (a-14) each independently may be replaced by C1-6alkyl or aryl; and aryl is phenyl or phenyl substtituted with one, two or three substtituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C1-6alkyl, C1-6alkyloxy, C1-6alalkylthio, mercapto, amino, mono- and di(C1-6alkyl)amino, carboxyl, C1-6alkyloxycarbonyl and C1-6alkylcarbonyl.