Compounds for the treatment of alzheimer's disease

Compounds of general formula (I)

• wherein
• A denotes aryl or heteroaryl,
• wherein the group A, besides the groups L, may optionally be substituted by one or more fluorine atoms,
• L in each case independently of one another denote hydrogen, fluorine, chlorine, bromine, iodine, hydroxy, carboxy, formyl, cyano, nitro, F3C, HF2C, FH2C, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkyl-S, C1-6-alkyl-S—C1-3-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C3-7-cycloalkyl-C2-6-alkenyl, C3-7-cycloalkyl-C2-6-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-6-alkyl, C3-7-cycloalkenyl-C2-6-alkenyl, C3-7-cycloalkenyl-C2-6-alkynyl, heterocyclyl, heterocyclyl-C1-6-alkyl, heterocyclyl-C2-6-alkenyl, heterocyclyl-C2-6-alkynyl, aryl, aryl-C1-6-alkyl, aryl-C2-6-alkenyl, aryl-C2-6-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-6-alkyl, heteroaryl-C2-6-alkenyl, heteroaryl-C2-6-alkynyl, heteroaryl-C3-7-cycloalkyl, R13—O, R13—O—C1-3-alkyl, (R12)2N, (R12)2N—CO, R12—CO—(R12)N, (R12)2N—CO—(R12)N, R12—SO2—(R12)N, (R12)2N—SO2 or C1-6-alkyl-SO2,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F3C, HF2C, FH2C, hydroxy-C1-6-alkyl, C1-3-alkyl, C1-6-alkoxy, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO— and HOSO2—,
• i denotes 0, 1, 2 or 3,
• B denotes a C1-4-alkylene bridge,
• while the C1-4-alkylene bridge may optionally be substituted by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, cyano, nitro, F3C, HF2C, FH2C, C1-4-alkyl, C1-6-alkyl-S—C1-3-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, aryl, aryl-C1-3-alkyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-3-alkyl, heteroaryl-C3-7-cycloalkyl, R13—O, (R12)2N—SO2, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO, R12—SO2, R12—CO—(R12)N, R12—SO2(R12)N, (R12)2N—SO2, R12—CO— and R12—SO—, and
• wherein two C1-4-alkyl groups bound to the same carbon atom of the C1-4-alkylene bridge may be joined together, forming a C3-7-cycloalkyl group, and
• wherein the above mentioned C1-4-alkyl groups and the C3-7-cycloalkyl group formed from the C1-4-alkyl groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F3C, C1-3-alkyl, C1-3-alkoxy, R13—O—C1-3-alkyl, R12—CO(R12)N, R12—SO2(R12)N, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO, (R12)2N—SO2— and HOSO2—,
• R1 denotes hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C3-7-cycloalkyl-C2-6-alkenyl, C3-7-cycloalkyl-C2-6-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-6-alkyl, C3-7-cycloalkenyl-C2-6-alkenyl, C3-7-cycloalkenyl-C2-6-alkynyl, heterocyclyl, heterocyclyl-C1-6-alkyl, heterocyclyl-C2-6-alkenyl, heterocyclyl-C2-6-alkynyl, aryl, aryl-C1-6-alkyl, aryl-C2-6-alkenyl, aryl-C2-6-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-6-alkyl, heteroaryl-C2-6-alkenyl, heteroaryl-C2-6-alkynyl or heteroaryl-C3-7-cycloalkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, F3C, C1-3-alkyl, C1-3-alkoxy, hydroxy-C1-6-alkyl, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO, (R12)2N—SO2, R12—CO—(R12)N, R12—SO2(R12)N— and HOSO2—,
• R2 denotes C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkoxy-C1-3-alkyl, C1-6-alkyl-S—C1-3-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-3-alkyl, C3-7-cycloalkyl-C2-3-alkenyl, C3-7-cycloalkyl-C2-3-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-3-alkyl, C3-7-cycloalkenyl-C2-3-alkenyl, C3-7-cycloalkenyl-C2-3-alkynyl, heterocyclyl, heterocyclyl-C1-3-alkyl, heterocyclyl-C2-3-alkenyl, heterocyclyl-C2-3-alkynyl, aryl, aryl-C2-3-alkenyl, aryl-C2-3-alkyl, aryl-C2-3-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-3-alkyl, heteroaryl-C2-3-alkenyl, heteroaryl-C2-3-alkynyl or heteroaryl-C3-7-cycloalkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, F3C, HF2C, FH2C-hydroxy, oxo, carboxy, formyl, cyano, nitro, (R12)2N, (R12)2N—C1-3-alkyl, HOSO2, C1-3-alkyl, C1-6-alkyl-S—C1-3-alkyl, (R12)2N—SO2, R12—CO—(R12)N, R12—SO2(R12)N, (R12)2N—C1-3-alkyl, (R12)2N—CO, R13—O and R13—O—C1-3-alkyl-,
• R3, R4 in each case independently of one another denote hydrogen, C1-6-alkyl, fluorine, F3C, HF2C or FH2C,
• R5 denotes hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C3-7-cycloalkyl-C2-4-alkenyl, C3-7-cycloalkyl-C2-4-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-4-alkyl, C3-7-cycloalkenyl-C2-4-alkenyl, C3-7-cycloalkenyl-C2-4-alkynyl, heterocyclyl, heterocyclyl-C1-4-alkyl, heterocyclyl-C2-4-alkenyl, heterocyclyl-C2-4-alkynyl, aryl, aryl-C1-4-alkyl, aryl-C2-4-alkenyl, aryl-C2-4-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-4-alkyl, heteroaryl-C2-4-alkenyl, heteroaryl-C2-4-alkynyl or heteroaryl-C3-7-cycloalkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl, C1-6-alkoxy, C1-3-alkyl-S, aryl, heteroaryl, heteroaryl-C1-3-alkyl, aryl-C1-6-alkyl, R12—CO—(R12)N, R12—SO2(R12)N—(R12)2N—SO2, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO— and HOSO2—,
• R6 denotes hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C3-7-cycloalkyl-C2-6-alkenyl, C3-7-cycloalkyl-C2-6-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-6-alkyl, C3-7-cycloalkenyl-C2-6-alkenyl, C3-7-cycloalkenyl-C2-6-alkynyl,
• heterocyclyl, heterocyclyl-C1-6-alkyl, heterocyclyl-C2-6-alkenyl, heterocyclyl-C2-6-alkynyl, aryl, aryl-C1-6-alkyl, aryl-C2-6-alkenyl, aryl-C2-6-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-6-alkyl, heteroaryl-C2-6-alkenyl, heteroaryl-C2-6-alkynyl or heteroaryl-C3-7-cycloalkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, R13—O, R13—O—C1-3-alkyl, aryl, heteroaryl, heteroaryl-C1-3-alkyl, aryl-C1-6-alkyl, (R12)2N, (R12)2N—C1-3-alkyl, (R12)2N—CO, (R12)2N—CO—N(R12), (R12)2N—SO2— and HOSO2—,
• R7 denotes hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkoxy-C1-3-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-3-alkyl, heterocyclyl-C1-3-alkyl, aryl, aryl-C1-3-alkyl, heteroaryl or heteroaryl-C1-3-alkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, cyano, hydroxy, C1-3-alkyl, C1-6-alkoxy and (R12)2N,
• R8 denotes hydrogen, fluorine, chlorine, bromine, iodine, cyano, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C3-7-cycloalkyl-C2-6-alkenyl, C3-7-cycloalkyl-C2-6-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-6-alkyl, C3-7-cycloalkenyl-C2-6-alkenyl, C3-7-cycloalkenyl-C2-6-alkynyl, heterocyclyl, heterocyclyl-C1-6-alkyl, heterocyclyl-C2-6-alkenyl, heterocyclyl-C2-6-alkynyl, aryl, aryl-C1-6-alkyl, aryl-C2-6-alkenyl, aryl-C2-6-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-6-alkyl, heteroaryl-C2-6-alkenyl, heteroaryl-C2-6-alkynyl, heteroaryl-C3-7-cycloalkyl, R13—O, R13—O—C1-3-alkyl, R10—SO2—(R11)N or R10—CO—(R11)N,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among C1-6-alkyl, fluorine, chlorine, bromine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkyl-S, C1-6-alkyl-S—C1-3-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, heterocyclyl, heterocyclyl-C1-6-alkyl, heteroaryl, heteroaryl-C1-6-alkyl, R13—O, R13—O—CO, R13—CO, R13—O—CO—(R12)N, (R12)2N—CO—O, R13—O—C1-3-alkyl, (R12)2N, (R12)2N—CO, R12—CO—(R12)N, (R12)2N—CO—(R12)N, (R12)2N—SO2, (R12)2N—SO2—(R12)N, R12—SO2, F3C, HF2C, FH2C, F3C—O, HF2C—O, FH2C—O— and R12—SO2—(R12)N,
• R9 in each case independently of one another denote hydrogen, fluorine, chlorine, bromine, iodine, C1-3-alkyl, R13—O or (R12)2N,
• while the above mentioned C1-3-alkyl group may optionally be substituted by one or more fluorine atoms,
• R10 denotes C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C3-7-cycloalkyl-C2-4-alkenyl, C3-7-cycloalkyl-C2-4-alkynyl, C3-7-cycloalkenyl, C3-7-cycloalkenyl-C1-4-alkyl, C3-7-cycloalkenyl-C2-4-alkenyl, C3-7-cycloalkenyl-C2-4-alkynyl, heterocyclyl, heterocyclyl-C1-4-alkyl, heterocyclyl-C2-4-alkenyl, heterocyclyl-C2-4-alkynyl, aryl, aryl-C1-4-alkyl, aryl-C2-4-alkenyl, aryl-C2-4-alkynyl, aryl-C3-7-cycloalkyl, heteroaryl, heteroaryl-C1-4-alkyl, heteroaryl-C2-4-alkenyl, heteroaryl-C2-4-alkynyl, heteroaryl-C3-7-cycloalkyl- or (R12)2N,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, R13—O, R13—O—C1-3-alkyl, R12—CO(R12)N, R12—SO2(R12)N, (R12)2N—SO2, R12—SO2, R12—SO, R12—S, (R12)2N, (R12)2N—C1-3-alkyl- and (R12)2N—CO,
• R11 denotes hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, heterocyclyl-C2-3-alkenyl, heterocyclyl-C2-3-alkynyl, aryl, aryl-C1-3-alkyl, heteroaryl, heteroaryl-C1-3-alkyl, heteroaryl-C2-3-alkenyl or heteroaryl-C2-3-alkynyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, R13—O, R13—O—C1-3-alkyl, (R12)2N—SO2, R12—SO2, R12—SO, R12—S, (R12)2N, (R12)2N—C1-3-alkyl- and R12CO,
• or
• R10 and R11 together form a C2-6-alkylene bridge, so that a heterocyclic ring is formed with the inclusion of the nitrogen atom linked to R11 and the SO2— or CO— group linked to R10,
• wherein one or two —CH2 groups of the C2-6-alkylene bridge may be replaced independently of one another by O, S, SO, SO2 or —N(R12)— such that in each case two O or S atoms or an O and an S atom are not directly connected to one another, and
• wherein the C atoms of the above mentioned C2-6-alkylene bridge may optionally be substituted by one or more groups selected from among fluorine, chlorine, bromine, hydroxy, carboxy, formyl, cyano, F3C, C1-6-alkyl, C1-6-alkoxy, oxo and nitro,
• R12 in each case independently of one another denote hydrogen, C1-6-alkyl, C1-6-alkoxy-C1-3-alkyl, C3-6-cyclyoalkyl, C3-6-cyclyoalkyl-C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, aryl, aryl-C1-3-alkyl, heteroaryl or heteroaryl-C1-3-alkyl, while two C1-6-alkyl groups bound to the same nitrogen atom may together form a C2-6-alkylene bridge, so that with the inclusion of the nitrogen atoms linked to the groups R12 a heterocyclic ring is formed,
• while a —CH2 group of the C2-6-alkylene bridge may be replaced by O, S or —N(R13)—, and
• wherein the above mentioned groups and the heterocyclic ring may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl, hydroxy-C1-3-alkyl, C1-3-alkoxy, (R13)2N—CO— and (R13)2N—, and
• R13 in each case independently of one another denote hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-7-cycloalkyl, C3-7-cyclyoalkyl-C1-3-alkyl, heterocyclyl, heterocyclyl-C1-3-alkyl, aryl, aryl-C1-3-alkyl, heteroaryl or heteroaryl-C1-3-alkyl,
• wherein the above mentioned groups may optionally be substituted independently of one another by one or more groups selected from among fluorine, chlorine, bromine, iodine, hydroxy, oxo, carboxy, formyl, cyano, nitro, C1-3-alkyl- and C1-3-alkoxy,
• the pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates thereof.