| 主权项 |
1. A compound represented by Formula (1), Formula (2), Formula (3), Formula (4) or Formula (5): or an enantiomer, a diastereomer, a tautomer, an N-oxide, a solvate, a formulation or a pharmaceutically acceptable salt thereof; wherein: R1 is independently selected from C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C3-10-heterocycloalkyl, C1-10-alkylene-C3-10-cycloalkyl, C1-10-alkylene-C3-10-heterocycloalkyl, C1-10-alkylene-(5-membered heteroaryl) and SO2—C1-10-alkyl, wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl and heteroaryl is unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of oxo, CN, OR11, O—C2-6-alkylene-OR11, C1-6-alkyl, halo-C1-6-alkyl, halogen, CO2R11, CONR11R12, CONR11SO2R11, COR11, SOxR11, SO3H, SO2NR11R12, NR11COR11, NR11SO2R11, NR11—CO—NR11R12, NR11—SO2—NR11R12, C3-10-cycloalkyl, O—C3-10-cycloalkyl, C3-10-heterocycloalkyl, O—C3-10-heterocycloalkyl and NR11R12; R2 is R1 or H; or R1 and R2 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substitutents independently selected from the group consisting of halogen, oxo, CN, OR11, SOxR11, SO3H, NR11SO2R11, SO2NR11R12, C0-6-alkylene-CO2R11, CONR11R12, CONR11SO2R11, COR11, NR11—CO—R11, NR11—CO—NR11R12, NR11—SO2—NR11R12, NR11R12, C1-6-alkyl, halo-C1-6-alkyl, hydroxy-C1-6-alkyl, C3-8-cycloalkyl, O—C3-8-cycloalkyl, C3-8-heterocycloalkyl and O—C3-8-heterocycloalkyl,
wherein cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 4 substitutents independently selected from the group consisting of halogen, C1-3-alkyl, halo-C1-3-alkyl, OH, O—C1-3-alkyl, O-halo-C1-3-alkyl, SO2—C1-3-alkyl, COOH and oxo; R3 is a 6-10 membered mono- or bicyclic aryl or a 5-14 membered mono-, bi- or tricyclic heteroaryl containing 1 to 5 heteroatoms independently selected from the group consisting of N, O and S,
wherein aryl and heteroaryl is optionally substituted with 1 to 5 substituents independently selected from the group consisting of halogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, halo-C1-6-alkyl, OH, O—C1-6-alkyl, O-halo-C1-6-alkyl, C0-6-alkylene-C3-10-cycloalkyl, C0-6-alkylene-C3-10-heterocycloalkyl, C0-6-alkylene-(5- or 6-membered heteroaryl), C1-6-alkylene-O—R31, C0-6-alkylene-CN, C0-6-alkylene-N(R31)2, O—C3-10-cycloalkyl, O—C1-6-alkylene-O—R31, O—C3-10-heterocycloalkyl, C0-6-alkylene-COOR31, C0-6-alkylene-C(O)R31, C0-6-alkylene-C(O)N(R31)2, C0-6-alkylene-N(R31)C(O)R31, C0-6-alkylene-SO—R31, C0-6-alkylene-SO2—R31, C0-6-alkylene-SO2—N(R31)2, C0-6-alkylene-N(R31)SO2—R31, C0-6-alkylene-SO2—C3-10-heterocycloalkyl and C0-6-alkylene-SO2—C3-10-heterocycloalkyl,
wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl and the 5- or 6-membered heteroaryl is unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of halogen, CN, C1-3-alkyl, halo-C1-3-alkyl, OH, oxo, ═N—OR32, O—C1-3-alkyl and O-halo-C1-3-alkyl,or wherein two adjacent substituents completing a 3- to 8-membered saturated or partially unsaturated ring containing carbon atoms and optionally containing 1 to 3 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of halogen, C1-6-alkyl, halo-C1-6-alkyl, C3-6-cycloalkyl, C3-6-heterocycloalkyl, oxo, ═N—OR32, OH, O—C1-6-alkyl and O-halo-C1-6-alkyl; R4 is (CR8R9)R40, (C═O)R40, (C═O)NR13R14, O—R40, C3-10-cycloalkylidenemethyl, C3-cycloalkylene-R40 or SOy—R7; R5 is H, C1-3-alkyl, C3-6-cycloalkyl or halo-C1-3-alkyl,
wherein alkyl, cycloalkyl and haloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of OH, oxo, O—C1-6-alkyl and O-halo-C1-6-alkyl; R6 is independently H, halogen, CN, C1-3-alkyl, C3-6-cycloalkyl, halo-C1-3-alkyl or CONHR61R62,
wherein alkyl, cycloalkyl and haloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of OH, oxo, O—C1-6-alkyl and O-halo-C1-6-alkyl; R7 is C3-10-cycloalkyl or C3-10-heterocycloalkyl,
wherein cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of halogen, OH, oxo, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl, C3-7-cycloalkyl and 3 to 7-membered heterocycloalkyl; R8 is H, F, C1-3-alkyl, halo-C1-3-alkyl, OH, O—C1-3-alkyl or O-halo-C1-3-alkyl; R9 is H, F, C1-3-alkyl or halo-C1-3-alkyl; R11 is independently selected from H, C1-6-alkyl, C0-6-alkylene-C3-10-cycloalkyl and C0-6-alkylene-C3-10-heterocycloalkyl,
wherein alkyl, alkylene, cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 6 substituents selected from the group consisting of halogen, CN, OH, oxo, C1-3-alkyl, halo-C1-3-alkyl, O—C1-3-alkyl, O-halo-C1-3-alkyl, NH2, NH(C1-3-alkyl), N(C1-3-alkyl)2, C3-6-heterocycloalkyl, C3-6-cycloalkyl and SO2—C1-3-alkyl,wherein cycloalkyl and heterocycloalkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of F, OH, oxo, CH3 and CF3; R12 is independently selected from H, C1-6-alkyl, halo-C1-6-alkyl and C3-6-cycloalkyl; R13 and R14 taken together with the nitrogen to which they are attached complete a 3- to 10-membered ring containing carbon atoms, wherein this ring is unsubstituted or substituted with 1 to 5 substituents independently selected from the group consisting of halogen, OH, oxo, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl and C3-6-cycloalkyl; R31 is independently selected from H, C1-6-alkyl, halo-C1-6-alkyl, C0-6-alkylene-C3-8-cycloalkyl, C0-6-alkylene-C3-8-heterocycloalkyl, 5- or 6-membered heteroaryl and 6-membered aryl,
wherein alkyl, alkylene, cyclolalkyl, heterocycloalkyl, aryl and heteroaryl are unsubstituted or substituted with 1 to 6 substituents independently selected from the group consisting of halogen, CN, OH, oxo, ═N—OR32, C1-3-alkyl, halo-C1-3-alkyl, O—C1-3-alkyl, O-halo-C1-3-alkyl and SO2—C1-3-alkyl; and optionally when two R31 are attached to a nitrogen atom, they may complete a 3- to 8-membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, wherein the ring is unsubstituted or substituted with 1 to 4 substitutents independently selected from the group consisting of fluoro, OH, oxo, C1-4-alkyl and halo-C1-4-alkyl; R32 is independently selected from H, C1-6-alkyl, halo-C1-6-alkyl and C3-6-cycloalkyl; R40 is C3-10-cycloalkyl, which is unsubstituted or substituted with 1 to 5 substituents independently selected from the group consisting of halogen, OH, oxo, O—C1-6-alkyl, O-halo-C1-6-alkyl, C1-6-alkyl, halo-C1-6-alkyl, C3-8-cycloalkyl and C3-8-heterocycloalkyl; R61 and R62 are independently selected from the group consisting of H, C1-3-alkyl and halo-C1-3-alkyl; and x and y is independently selected from 0, 1 and 2; with the proviso that the compound is not 5-(cyclopentylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide and compounds of Formula (5) are not compound wherein R4 is OR40. |
