| 主权项 |
1. A compound of formula 1 wherein R1 is selected from the group consisting of hydrogen, C1-6-alkyl and C1-6-haloalkyl; R2 is selected from the group consisting of hydrogen, C1-6-alkyl, C1-6-haloalkyl, —(C1-3-alkylene)-O—(C1-3-alkyl) and three-, four-, five- or six-membered cycloalkyl, wherein this cycloalkyl may optionally be substituted by halogen; R3 is selected from the group consisting of hydrogen, C1-6-alkyl, halogen, —O—C1-6-alkyl, three-, four-, five- or six-membered cycloalkyl, —S—(C1-3-alkylene)-A, —S-A and -A, with A being a group selected from the group consisting of —CO—N(C1-3-alkyl)2, —CO—NH(C1-3-alkyl), —CO—NH2, five- or six-membered heteroaryl comprising 1, 2 or 3 heteroatoms each independently selected from S, O or N and five-, six- or seven-membered heterocycle comprising 1, 2 or 3 heteroatoms each independently selected from S, O or N, wherein A may optionally be further substituted by one, two or three groups each independently selected from —C1-3-alkyl, halogen, -oxo, —OH or C1-3-haloalkyl; R4 is selected from the group consisting of hydrogen, -halogen, SH, —OH, —NH2, —CO—Y, —CO—N(CH3)—Y, —CO—N(CH3)(C1-5-alkylene)-Y, —CO—N(ethyl)(C1-5-alkylene)-Y, —CO—N(ethyl)-Y, —CS—Y, —CS—N(CH3)—Y, —CS—N(CH3)—(C1-3-alkylene)-Y, —C1-6-alkyl, —C1-3-haloalkyl, —CO—NH—Y, —CO—NH—C1-6-alkylene-Y, —CO—N(CH3)—(C2-3-alkylene)-O—(C1-3-alkyl), —NH2, —C1-6-alkylene-L, —SO2-phenyl, —SO2—(C1-3-alkyl), —CO—N(C1-4-alkyl)2 and —CO—N(C2-4-alkylene-O—C1-3-alkyl)2, or wherein R4 is a five- or six-membered heteroaromatic group comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, wherein said heteroaromatic group on any atom available for substitution may optionally be further substituted by one, two or three groups each independently selected from —C1-3-alkyl halogen or C1-3-haloalkyl, with Y being a group selected from the group consisting of —NH2, —NH(CH3), —N(CH3)2, —C1-6-alkylene-N(CH3)2, —O—C1-3-alkyl, —C1-3-haloalkyl, —OH, —N(ethyl)2 and —C1-5-alkinyl, or with Y being a group selected from the group consisting of a four-, five-, six- or seven-membered monocyclic fully saturated or partially unsaturated heterocycle comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, a five- or six-membered monocyclic heteroaromatic group comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, —C6-10-aryl, and C3-6-cycloalkyl, or with Y being a 8- to 11-membered bicyclic annellated fully saturated, partially unsaturated or aromatic heterocycle comprising 1, 2, 3 or 4 heteroatoms each independently from each other selected from N, S or O, or with Y being an 8- to 11-membered bicyclic fully saturated spiro-heterocycle comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, with the proviso that this spiro-heterocycle comprises at least one N-atom and that this heterocycle is directly attached to the molecule via this N-atom, or with Y being a six- or seven-membered fully saturated heterocycle comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, which is bridged by an additional C1-3-alkylene-unit, whereby each Y may optionally be substituted by one, two or three groups Z each independently from each other selected from the group consisting of halogen, -oxo, OH, —CN, —C1-5-alkyl, —C1-5-alkanol, —O—C1-3-alkyl, a four-, five-, six- or seven-membered fully saturated or partially unsaturated heterocycle comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, a fully saturated or partially unsaturated C3-6-cycloalkyl, a five- to six-membered heteroaromatic group comprising 1, 2 or 3 heteroatoms each independently selected from N, S or O, —CO—(C1-3-alkyl), —CHO, —CO-L, —C1-3-alkylene-CO-L, —C1-4-alkylene-O—C1-3-alkyl, —N(CH3)2 and —N(ethyl)2, whereby each group Z may optionally be further substituted by one, two or three groups T each independently selected from the group consisting of -oxo, OH, halogen, —C1-3-alkyl, —O—C1-3-alkyl, —N(methyl)2, —N(ethyl)2, 5- to 6-membered fully saturated, partially unsaturated or aromatic heterocycle comprising 1 or 2 heteroatoms each independently selected from N, O or S, a C3-6-cycloalkyl and —CN, wherein each group T may also optionally be substituted by a group selected from the group consisting of C1-3-alkyl, halogen, OH, oxo and —O—C1-3-alkyl, whereby L denotes a 5- or 6-membered fully saturated or partially unsaturated heterocycle comprising 1 or 2 heteroatoms each independently selected from N, O or S, where the heterocycle may optionally be substituted by one, two or three groups independently selected from methyl, halogen, OH or -oxo; R5 is selected from the group consisting of hydrogen, C1-6-alkyl, C1-3-haloalkyl and —(C1-4-alkylene)-O—(C1-3-alkyl); or a pharmaceutically acceptable salt thereof. |
