Patent ID: 6465467
Filing Date: 2002-10-15
Classification: C07D

Abstract:
The compound according to the general formula (Ib):wherein:X1 and Y1 independently are â€”Oâ€”, â€”Sâ€” or â€”N(R27)â€”; Ra is aryl or heteroaryl, each of which may be substituted in one or more positions independently of each other by C1-6-alkyl, C1-6-alkoxy, fluoro-C1-6-alkoxy, 2,2,2-trifluoroethoxy, C3-5-alkynyloxy, C3-5-alkenyloxy, dimethylamino-C1-6-alkoxy, methylamino-C1-6-alkoxy, C1-6-arylthio, fluoromethyl, difluoromethyl, trifluoromethyl, fluoromethylthio, difluoromethoxy, difluoromethylthio, trifluoromethoxy, trifluoromethylthio, halogen, hydroxy, nitro, cyano, trifluoromethylsulphonyloxy, C1-6-alkylsulphonamido, C2-6-alkenyl, C2-6-alkynyl, C1-6-acyl, C1-6-alkylcarbonyl-C1-6-alkyl, C1-6-alkylsulphonyl, C1-6-alkylsulphon alkoxy-C1-6-alkyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, C1-6-acyloxy-C1-6-alkyl, hydroxy-C1-6-alkyl, hydroxy-C1-6-alkoxy, C1-6-alkoxy-C1-6-alkoxy, C1-6-alkoxy-C1-6-alkylthio, hydroxy-C1-6-alkylthio, heteroaryl-C1-6-alkylthio, aryl-C1-6-alkylthio, C1-6-alkoxy-C1-6-alkylarnino, N-(C1-6-alkoxy-C1-6-alkyl)â€”N-methylamino, C3-6-cycloalkyl-C1-6-alkoxy, aryl-C1-6-alkoxy, heterocyclyl-C1-6-alkoxy, C3-8-cycloalkyl, C3-8-cycloalkyloxy, aryl, aryloxy, arylthio, arylsulphonyl, aryl-C1-6-acyl, aryl-C1-6-alkyl, aryl-C2-6-alkenyl, aryl-C2-6-alkynyl, heterocycl C1-6-alkyl, heterocyclyl-C2-6alkenyl, heterocyclyl-C2-6-alkynyl, heterocyclyl, heterocyclyloxy, heterocyclylthio, heterocyclylsulphonyl, heterocyclylamino, heterocyclyl-C1-6acyl, â€”N(R2)(R3), â€”CON(R7)(R8) or, when Ra is optionally substituted C3-8cycloalkyl, oxo, wherein any cycloalkyl, aryl and heterocyclyl residues as substituents on C3-8-cycloalkyl, aryl or heteroaryl or as part of substituents on C3-8-cycloalkyl, aryl or heteroaryl in turn may be substituted in one or more positions independently of each other by C1-4-alkyl, C1-4-alkoxy, methanesulphonamido, C1-4-alkylthio, C1-4-alkylsulphonyl, C1-4-acyl, heterocyclyl, heterocyclyloxy, heterocyclylthio, aryloxy, arylthio, fluoromethyl, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, halogen, hydroxy, nitro, cyano, N(R2)(R3) or, for C3-8-cycloalkyl and partially or fully saturated heterocyclyl, oxo or hydroxy; R20 and R21 independently of each other are hydrogen, C1-4-alkyl, halogen, or together with the carbon atoms to which they are bound form benzene or thiophene, optionally mono- or di-substituted by halogen; R22 is hydrogen, hydroxy, or C1-4alkyl; R23 and R24 independently of each other are hydrogen or C1-4-alkyl; R25 is hydrogen or C1-4alkyl; R26 is hydrogen, C1-4-alkyl or is linked to a carbon atom in Ra adjacent to the atom binding to Y1 to form a 5- or 6-membered ring which may contain an additional heteroatom, R27 is hydrogen or C1-4-alkyl, preferably methyl or ethyl; and y and z independently of each other are 1 or 2, and pharmaceutically acceptable salts, hydrates, geometrical isomers, tautomers, optical isomers, N-oxides, and prodrug forms thereof.