6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

摘要

Disclosed is a compound of formula (I) wherein R1 is selected from the group consisting of C1-4alkyl, C3-8cycloalkyl, 5-6 membered heteroaryl, -(C1-4alkyl)-(5-6 membered heteroaryl), 5-6 membered heterocycloalkyl and -(C1-4alkyl)-5-6 membered heterocycloalkyl; R2 is selected from the group consisting of hydrogen and halogen; L1 is selected from the group consisting of -CH2-NRA-, -CH2CH2-NRA, - CH2-O- and -CH2-S-; wherein RA is selected from the group consisting of hydrogen, C1-4alkyl, -C(O)-C1-4alkyl, -C(O)O-C1-4alkyl and -SO2-C1-4alkyl; R3 is selected from the group consisting of C1-4alkyl, carboxy substituted C1-4alkyl, C4-8cycloalkyl, -(C1-4alkyl)-C4-scycloalkyl, partially unsaturated carbocyclyl, -(C1-4alkyl)-(partially unsaturated carbocyclyl), aryl, -(C1-4alkyl)-aryl, heteroaryl, -(C1-4alkyl)-heteroaryl, heterocycloalkyl and -(C1-4alkyl)heterocycloalkyl; wherein the C4-8cycloalkyl, aryl, heteroaryl or heterocycloalkyl, whether alone or as part of a substituent group is optionally substituted with one or more substituents independently selected from the group consisting of halogen, hydroxy, carboxy, C1-4alkyl, fluorinated C1-4alkyl, - C1-4alkoxy-, fluorinated -C1-4alkoxy, -C1-4alkyl-OH, -C1-4alkyl-CO2H and phenyl; alternatively, RA and R3 are taken together with the nitrogen atom to which they are bound to form a ring selected from the group consisting of 5 to 6 membered heteroaryl and 5 to 6 membered heterocycloalkyl; or a pharmaceutically acceptable salt thereof.