6-SUBSTITUTED-THIO (OR -OXO-)-2-AMINO-QUINOLINE DERIVATIVES USED AS β-SECRETASE INHIBITORS Russian patent published in 2013 - IPC C07D405/06 C07D405/14 A61K31/4709 A61P25/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to organic chemistry, namely to new 2-aminoquinoline derivatives of formula , or to pharmaceutically acceptable salts thereof, wherein R¹ represents 6-member heterocycloalkyl (tetrahydropyranyl); R² is specified in a group consisting of hydrogen and halogen; L¹ is specified in a group consisting of -CH₂-NR^A, -CH₂CH₂-NR^A, -CH₂-O- and -CH₂-S-; wherein R^A means hydrogen; R³ is specified in a group consisting of carboxy substituted C_1-4alkyl, aryl(phenyl), -(C_1-4alkyl)-aryl(phenyl), -(C_1-4alkyl)-heteroaryl(imidazolyl, pyridinyl); wherein aryl analysed either individually, or as a part of a substituting group, carries one to three substitutes independently specified in a group consisting of halogen, C_1-4alkyl, fluorinated C_1-4alkyl, -C_1-4alkoxygroup- and -C_1-4alkyl-CO₂H; either R^A and R³ together with a nitrogen atom whereto attached form a ring structure representing 6-member heterocycloalkyl (piperazinyl). Further, the invention refers specific compounds and , a pharmaceutical composition of the compounds of formula (I), (II-a) and (II-b), a method for preparing the pharmaceutical composition, a method for treating the above disorders, a method for inhibiting enzyme β-secretase activity and using the compounds of formulas (I), (II-a) and (II-b).

EFFECT: there are prepared new 2-amino-quinoline derivatives effective for treating the β-secretase mediated disorders.

25 cl, 3 tbl, 8 ex