| 主权项 |
1. A compound of the formula (I) wherein X1, X2, X3, X4 and X5, independently of each other, are N or CH; R1 is C1-C4-alkyl which carries a group —C(═O)R4 or fluorinated C1-C4-alkyl which carries a group —C(═O)R4; R2 is phenyl or a 5- or 6-membered heteroaromatic ring with 1, 2 or 3 heteroatoms selected from the group consisting of O, S and N as ring members, where phenyl or the 5- or 6-membered heteroaromatic ring may carry 1, 2 or 3 substituents R5; R3 is a 3-, 4-, 5- or 6-membered saturated or partially unsaturated carbocyclic ring which carries one substituent R6 and which may additionally carry 1 or 2 substituents R7; R4 is OR8 or —NR9R10; each R5 is independently halogen, cyano, nitro, hydroxyl, C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, where the 8 last-mentioned aliphatic and cycloaliphatic radicals may carry one or more radicals R15; C3-C8-cycloalkoxy, fluorinated C3-C8-cycloalkoxy, C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6-alkylthio, fluorinated C1-C6-alkylthio, C1-C6-alkylsulfinyl, fluorinated C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6-alkylsulfonyl, amino, C1-C6-alkylamino, di-(C1-C6-alkyl)-amino, C1-C6-alkylcarbonyl, fluorinated C1-C6-alkylcarbonyl, carboxyl, C1-C6-alkoxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, C1-C6-alkylcarbonyloxy, fluorinated C1-C6-alkylcarbonyloxy, aminocarbonyl, C1-C6-alkylaminocarbonyl, di-(C1-C6-alkyl)-aminocarbonyl, phenyl, phenyl-C1-C2-alkyl, or a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO and SO2 as ring members, where phenyl, phenyl-C1-C2-alkyl and the heterocyclic ring may carry one or more radicals R13; or
two radicals R5, bound on adjacent ring atoms, form together with the ring atoms to which they are bound a saturated or unsaturated 3-, 4-, 5-, 6-, 7-, 8- or 9-membered ring, wherein the ring may contain 1 or 2 heteroatoms or heteroatom groups selected from the group consisting of O, S, N, NO, SO and SO2 and/or 1 or 2 C═O groups as ring members, and wherein the ring may be substituted by one or more radicals R13; R6 is C1-C4-alkyl which carries a radical —NR11R12 or fluorinated C1-C4-alkyl, which carries a radical —NR11R12; each R7 is independently halogen, cyano, hydroxyl, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkoxy, or fluorinated C1-C4-alkoxy, or two radicals R7 bound on the same carbon ring atom form together a group ═O (oxo); R8 is hydrogen, C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, where the 8 last-mentioned aliphatic and cycloaliphatic radicals may carry one or more radicals R15; phenyl, phenyl-C1-C2-alkyl, or a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO and SO2 as ring members, where phenyl, phenyl-C1-C2-alkyl and the heterocyclic ring may carry one or more radicals R13; R9 and R10, independently of each other, are hydrogen, C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, where the 8 last-mentioned aliphatic and cycloaliphatic radicals may carry one or more radicals R15; C1-C6-alkoxy, fluorinated C1-C6-alkoxy, phenyl, phenyl-C1-C2-alkyl, or a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO and SO2 as ring members, where phenyl, phenyl-C1-C2-alkyl and the heterocyclic ring may carry one or more radicals R13; or
R9 and R10, together with the nitrogen atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the heterocyclic ring may additionally contain 1 or 2 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO, SO2 and C═O as ring members, and where the heterocyclic ring may carry 1, 2, 3 or 4 radicals R13; R11 and R12, independently of each other, are hydrogen, C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, where the 8 last-mentioned aliphatic and cycloaliphatic radicals may carry one or more radicals R15; C1-C6-alkoxy, fluorinated C1-C6-alkoxy, phenyl, phenyl-C1-C2-alkyl, or a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO and SO2 as ring members, where phenyl, phenyl-C1-C2-alkyl and the heterocyclic ring may carry one or more radicals R13; or
R11 and R12, together with the nitrogen atom they are bound to, form a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring, where the heterocyclic ring may additionally contain 1 or 2 heteroatoms or heteroatom groups selected from the group consisting of: O, S, N, NO, SO, SO2 and C═O as ring members, and where the heterocyclic ring may carry 1, 2, 3 or 4 radicals R13; each R13 is independently halogen, cyano, hydroxyl, C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6-alkylthio, fluorinated C1-C6-alkylthio, C1-C6-alkylsulfinyl, fluorinated C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6-alkylsulfonyl, amino, C1-C6-alkylamino, di-(C1-C6-alkyl)-amino, C1-C6-alkylcarbonyl, fluorinated C1-C6-alkylcarbonyl, carboxyl, C1-C6-alkoxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, C1-C6-alkylcarbonyloxy, fluorinated C1-C6-alkylcarbonyloxy, aminocarbonyl, C1-C6-alkylaminocarbonyl, di-(C1-C6-alkyl)-aminocarbonyl, phenyl, or phenyl-C1-C2-alkyl; or two radicals R13 bound to the same carbon ring atom together a group ═O or ═S; or
two radicals R13 bound to the same carbon ring atom may form together with this carbon ring atom a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated ring, where the ring may contain 1, 2, 3 or 4 heteroatoms or heteroatom-containing groups selected from the group consisting of O, S, N, NO, SO, SO2 and C═O as ring members, and where the ring may be substituted with one or more substituents R14; ortwo non-geminal radicals R13 form together a group —(CH2)k—, where k is 1, 2, 3 or 4, where 1 or 2 hydrogen atoms in this group may be replaced by a methyl group; ortwo vicinal radicals R13 form together a group —CH═CH—CH═CH—; each R14 is independently halogen, cyano, hydroxyl, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkoxy, or fluorinated C1-C4-alkoxy; and each R15 is independently cyano, hydroxyl, nitro, C3-C8-cycloalkyl, fluorinated C3-C8-cycloalkyl, C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6-alkylthio, fluorinated C1-C6-alkylthio, C1-C6-alkylsulfinyl, fluorinated C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6-alkylsulfonyl, amino, C1-C6-alkylamino, di-(C1-C6-alkyl)-amino, C1-C6-alkylcarbonyl, fluorinated C1-C6-alkylcarbonyl, carboxyl, C1-C6-alkoxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, C1-C6-alkylcarbonyloxy, fluorinated C1-C6-alkylcarbonyloxy, aminocarbonyl, C1-C6-alkylaminocarbonyl, di-(C1-C6-alkyl)-aminocarbonyl, phenyl, or a 3-, 4-, 5-, 6-, 7- or 8-membered saturated, partially unsaturated or maximally unsaturated heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of O, S, N, NO, SO and SO2 as ring members, where phenyl, phenyl-C1-C2-alkyl and the heterocyclic ring may carry one or more radicals R13; and
R15 as a substituent on a cycloaliphatic ring is additionally C1-C6-alkyl, fluorinated C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, fluorinated C2-C6-alkynyl, or phenyl-C1-C2-alkyl, where the phenyl moiety in phenyl-C1-C2-alkyl may carry one or more radicals R13; or an N-oxide, stereoisomer, or a pharmaceutically acceptable salt thereof, or the compound of the formula I, wherein at least one of the atoms has been replaced by its stable, non-radioactive isotope. |
