Patent ID: 6462074
Filing Date: 2002-10-08
Classification: A61P,C07D

Abstract:
Compounds of the general formula (I) in whichA represents radicals of the formulae â€”CH2â€”, â€”COâ€”, â€”CR4(OH)â€” or â€”(CH2)aâ€”CHR5â€”, â€ƒin which a represents a number 0, 1, 2, 3 or 4, R4 represents hydrogen or (C1-C6)-alkyl and R5 represents phenyl, or â€ƒrepresents (C2-C8)-alkanediyl, (C2-C6)-alkenediyl or (C2â€”C6)â€” or (C2â€”C6)-alkinediyl, R1 represents hydrogen, (C3-C6)-cycloalkyl or represents a 5- to 6-membered heterocycle which may contain up to 3 O atoms or a S atom or â€ƒrepresents a 5-to 6-membered benzo-fused heterocycle which may contain up to 2 O atoms or a S atom or â€ƒrepresents radicals of the formulae â€ƒin which b and c are identical or different and represent a number 1 or 2, or â€ƒrepresents (C6-C10)-aryl, â€ƒwhere all of the ring systems listed above are optionally mono- to polysubstituted by identical or different substituents selected from the group consisting of halogen, cyano, nitro, trifluoromethyl, hydroxyl, (C1-C6)-alkoxy, (C1-C6)-alkyl-carbonyl and (C3-C6)-cycloalkyl, phenyl, phenoxy, benzyloxy and a 5- to 6-membered aromatic heterocycle having up to 3 O atoms or a S atom which for their part may be substituted up to three times by identical or different substituents from the group consisting of cyano and halogen, â€ƒand/or are substituted by (C1-C6)-alkyl and (C2-C6)-alkylene, which for their part may be substituted by halogen, (C6-C1o)-aryl or by radicals of the formula SR8,â€”OR9or â€”NR10R11 â€ƒin which R8 represents (C1-C6)-alkyl or phenyl, R9 represents hydrogen or (C1-C6)-alkyl, and R10and R11 are identical or different and represent hydrogen, phenyl or (C1-C6)-alkyl, which is optionally substituted by phenyl, which for its part may be mono- to polysubstituted by identical or different substituents from the group consisting of halogen, nitro, hydroxyl and (C1-C6)-alkoxy, â€ƒand/or are substituted by groups of the formulae â€”CO2â€”R13, â€”NR14R15, â€”NR16COâ€”R17, â€”NR18O2â€”R19 and â€”COâ€”NR20R21, â€ƒin which R13 represents hydrogen, or â€ƒrepresents (C1-C9)-alkyl or (C2-C6)-alkenyl, which for their part may be substituted by radicals of the formulae â€ƒ(C6-C10)-aryl or by a 5- to 7-membered aromatic heterocycle having up to 3 O atoms or a S atom â€ƒin which d represents a number 1 or 2, or â€ƒrepresents (C6-C1o)-aryl, which is optionally substituted by phenyl, which for its part may be substituted by cyano or halogen, R14 and R15 are identical or different and represent hydrogen, (C3-C6)-cycloalkyl, phenyl or (C1-C6)-alkyl, which is optionally substituted by (C3-C6)-cycloalkyl or phenyl, which for its part may be mono- to polysubstituted by identical or different substituents from the group consisting of halogen, hydroxyl or (C1-C6)-alkoxy, R16 represents hydrogen or (C1-C6)-alkyl, R17 represents hydrogen, adamantyl, (C3-C8)-cycloalkyl, (C2-C6)-alkenyl or (C1-C12)-alkyl which is optionally substituted by adamantyl, (C3-C6)-cycloalkyl, (C6-C10)-aryl, phenoxy or a 5- to 6-membered aromatic heterocycle having up to 4 O atoms or a S atom where aryl and the heterocycle for their part may be mono- to polysubstituted by identical or different substituents from the group consisting of (C1-C6)-alkyl, (C1-C6)-alkoxy, hydroxyl, nitro or halogen, â€ƒand/or alkyl is optionally substituted by a radical of the formula â€ƒin which e represents a number 0 or 1 and R22 represents (C1-C6)-alkyl or (C1-C10)-aryl, which is optionally mono- to polysubstituted by identical or different substituents from the group consisting of halogen, nitro, hydroxyl and (C1-C6)-alkoxy, or â€ƒrepresents (C6-C10)-aryl or a 5- to 6-membered aromatic heterocycle having up to, 3 O atoms or a S atom which for their part may optionally be mono- to polysubstituted by identical or different substituents from the group consisting of (C1-C6)-alkoxy, (C1-C6)-alkyl, hydroxyl, nitro and halogen, or â€ƒrepresents a radical of the formula â€ƒin which L and M are identical or different and represent hydrogen or halogen, R23 and R24 have the meaning of R10 and R11 given above and are identical to or different from this meaning, R18 has the meaning of R16 given above and is identical to or different from this meaning, R19 represents (C3-C8)-cycloalkyl, or represents (C1-C8)-alkyl or (C2-C8)-alkenyl, which for their part are optionally substituted by substituents selected from the group consisting of halogen, phenyl, hydroxyl, (C3-C8)-cycloalkyl and by a group of the formula â€”SiR25 R26 R27, â€ƒin which R25, R26 and R27 are identical or different and represent (C1-C6)-alkyl, R20 and R21 are identical or different and represent hydrogen, adamantyl, (C3-C8)-cycloalkyl, phenyl, phenoxy-substituted phenyl or a 5- to 6-membered, aromatic heterocycle having up to 3 O atoms or a S atom â€ƒor â€ƒrepresent (C2-C8)-alkenyl, (C1-C12)-alkyl or (C2-C6)-alkinyl, which are optionally substituted by hydroxyl, (C3-C6)-cycloalkyl, (C1-C6)-alkoxy, halogen, hydroxyl, trifluoromethyl, phenyl or by a 5- to 6-membered aromatic heterocycle having up to 3 O atoms or a S atom where the ring systems are optionally substituted up to 2 times by identical or different substituents from the group consisting of (C1-C6)-alkoxy, (C1-C6)-alkoxycarbonyl, halogen, phenoxy, hydroxyl and (C1-C6)-alkyl, â€ƒand/or the alkyl listed under R20/R21 is optionally substituted by radicals of the formulae â€”SCF3. â€ƒor â€”NR28R29, â€ƒin which R28 and R29 are identical or different and represent hydrogen or (C1-C6)-alkyl, R2 and R3 are identical or different and represent hydrogen or (C1-C6)-alkyl, and D and E together form radicals of the formulae â€ƒin which R31, R32, R33, R34, R35, R36, R37 and R38 are identical or different and represent hydrogen, phenyl or (C1-C6)-alkyl, and their pharmaceutically acceptable salts.