Patent ID: 6500817
Filing Date: 2002-12-31
Classification: A61P,C07D

Abstract:
A compound of the general formula (I), in whichR1 represents hydrogen, halogen, (C1-C6)-alkyl, (C1-C6)-alkoxy, amino(C1-C6)alkyl or halogeno(C1-C6)alkyl, R2 and R3 are identical or different and represent hydrogen, (C3-C8)-cycloalkyl or biphenylylaminocarbonyl, or represent (C1-C6)-alkyl which is optionally substituted by 1 to 3 substituents selected from the group consisting of (C3-C6)-cycloalkyl, (C1-C6)-alkoxy, halogen, hydroxyl, radicals of the formula a 5- to 6-membered aromatic heterocycle with up to 3 heteroatoms from the series S, N and/or O, it also being possible for a nitrogen-containing heterocycle to be bonded via the nitrogen atom, a 3- to 8-membered saturated or unsaturated, nonaromatic heterocycle which has up to 3 heteroatoms from the series S, N and/or O and is optionally bonded via a nitrogen atom, and (C6-C10)-aryl which in turn may be substituted by hydroxyl or (C1-C6)-alkoxy, or R2 and R3 form, together with the nitrogen atom, a 5- to 6-membered saturated heterocycle which optionally also has an oxygen atom, R4 represents hydrogen, (C1-C6)-acyl, (C2-C6)-alkenyl, or R4 represents (C1-C6)-alkyl which is optionally substituted by 1 to 3 substituents selected from the group consisting of halogen, hydroxyl, (C1-C6)-acyl, (C1-C6)-alkoxy, phenoxy, (C6-C10)-aryl and â€”NR7R8, in which R7 and R8 are identical or different and denote hydrogen, (C1-C6)-acyl, (C1-C6)-alkyl, carbamoyl, mono- or di(C1-C6)-alkylamino(C1-C6)alkyl, mono- or di(C1-C6)-alkylaminocarbonyl, (C6-C10)-aryl or (C1-C6)-alkoxycarbonyl, or R7 and R8 form, together with the nitrogen atom, a 5- to 6-membered saturated heterocycle which optionally contains another heteroatom from the series S or O or a radical of the formula â€”NR9 and may be substituted by oxo, in which R9 denotes hydrogen or (C1-C4)-alkyl, or R4 represents (C1-C6)-alkyl which is substituted by a 5- to 6-membered aromatic, optionally benzo-fused heterocycle with up to 3 heteroatoms from the series S, N and/or O, it also being possible for a nitrogen-containing heterocycle to be bonded via the nitrogen atom, or is substituted by radicals of the formulae â€ƒin which R10 denotes hydrogen or (C1-C6)-alkyl, R11 and R12 are identical or different and denote hydrogen, (C1-C6)-alkyl or (C6-C10)-aryl, said (C1-C6)-alkyl and (C6-C10)-aryl optionally substituted by 1 to 3 substituents selected from the group consisting of hydroxyl, (C1-C6)-alkoxy and halogen, R5 represents hydrogen or (C1-C6)-alkyl, R6 represents a radical of the formula orR6 represents phenyl which is optionally substituted by one to three substituents selected from the group consisting of halogen, (C6-C10)-aryl which is optionally substituted by 1 to 3 substituents selected from (C1-C6)alkanoyl, (C1-C6)-alkoxy, (C1-C6)-alkyl, halogen, (C1-C6)alkoxycarbonyl, nitro, halogeno(C1-C6)alkyl, halogeno(C1-C6)alkoxy, amino, (C1-C6)alkylthio, hydroxyl, carboxyl, carbamoyl, mono- or di(C1-C6)alkylaminocarbonyl, mono- or di(C1-C6)acylamino, (C1-C6)alkylsulphinyl, (C1-C6)alkylsulphonyl, and/or cyano, or (C1-C6)-alkoxy, (C1-C6)-alkoxycarbonyl, (C1-C6)-alkylthio, hydroxyl, carboxyl, partially fluorinated (C1-C6)-alkoxy with up to 6 fluorine atoms, radicals of the formulae â€ƒin which R13 denotes hydrogen or (C1-C6)-alkyl, (C1-C6)-alkyl which is optionally substituted by a radical of the formula a 5- to 6-membered aromatic heterocycle which has up to 3 heteroatoms from the series S, N and/or O, is optionally bonded via a nitrogen atom and is optionally substituted by 1 to 3 substituents selected from (C1-C6)alkanoyl, (C1-C6)-alkoxy, (C1-C6)-alkyl, halogen, (C1-C6)alkoxycarbonyl, nitro, halogeno(C1-C6)alkyl, halogeno(C1-C6)alkoxy, amino, (C1-C6)alkylthio, hydroxyl, carboxyl, carbamoyl, mono- or di(C1-C6)alkylaminocarbonyl, mono- or di(C1-C6)acylamino, (C1-C6)alkylsulphinyl, (C1-C6)alkylsulphonyl, and cyano, a 3- to 8-membered saturated or unsaturated, nonaromatic mono- or bicyclic heterocycle which has up to 3 heteroatoms from the series S, N and/or O, is optionally bonded via a nitrogen atom and is optionally substituted by 1 to 3 substituents selected from oxo, halogen, hydroxyl, (C1-C6)-alkoxycarbonyl, (C1-C6)alkoxycarbonylamino, (C1-C6)-alkyl, halogeno(C1-C6)-alkyl and hydroxy(C1-C6)-alkyl, and groups of the formulae â€”OR14, â€”NR15R16 or â€”COâ€”NR17R18, â€ƒin which R14 denotes a radical of the formula or denotes phenyl which in turn is optionally substituted by a group of the formula â€”NR19R20, â€ƒin which R19 and R20 are identical or different and denote hydrogen, (C1-C6)-alkyl or (C1-C6)-acyl, orR14 denotes (C1-C6)-alkyl which is optionally substituted once to three times by hydroxyl, R15 and R16 are identical or different and denote hydrogen, carbamoyl, mono- or di(C1-C6)alkylaminocarbonyl, phenyl, (C1-C6)-acyl or (C1-C6)-alkyl, where (C1-C6)-alkyl is optionally substituted by (C1-C6)-alkoxy, (C1-C6)-acyl, by phenyl or by a 5- to 6-membered aromatic heterocycle with up to 3 heteroatoms from the series S, N and/or O, where aforementioned phenyl and aforementioned aromatic heterocycle are optionally substituted once to three times, identically or differently, by halogen and/or hydroxyl, and R17 and R18 are identical or different and denote hydrogen or (C1-C6)-alkyl, and the salts thereof.