MORPHOLINE TYPE CINNAMIDE DERIVATIVE Russian patent published in 2010 - IPC C07D413/10 C07D413/14 C07D498/04 A61K31/5377 A61K31/5383 A61P25/28 

FIELD: chemistry.

SUBSTANCE: present invention relates to a morpholine type cinnamide derivative with general formula I or its pharmacologically acceptable salt, where (a) R¹, R² , R³ and R⁴ are identical or different and each represents a hydrogen atom or C_1-6alkyl group; X₁ represents a C_1-6alkylene group, where the C_1-6alkylene group can be substituted with 1-3 hydroxyl groups or C_1-6alkyl groups, or a C_3-8cycloalkyl group formed by two C_1-6alkyl groups all bonded to the same carbon atom of the C_1-6alkylene group; X_a represents a methoxy group or a fluorine atom; X_b represents an oxygen atom or a methylene group, under the condition that X_b represents only an oxygen atom when X_a represents a methoxy group; and Ar₁ is an aryl group, pyridinyl group which can be substituted with 1-3 substitutes selected from A1 group of substitutes; (b) Ar₁-X₁- represents a C_5-7cycloalkyl group condensed with a benzene ring, where one methylene group in the C_5-7cycloalkyl group can be substituted with an oxygen atom, the C_5-7cycloalkyl group can be substituted with 1-3 hydroxyl groups and/or C_1-6alkyl groups, and R¹, R², R³, R⁴, X_a and X_b assume values given in (a); (d) Ar₁-X₁- and R⁴ together with the nitrogen atom bonded to the Ar₁-X₁- group and the carbon atom bonded to the R⁴ group form a 5-7-member nitrogen-containing heterocyclic group which is substituted with an aryl group or a pyridinyl group, where one methylene group in the 5-7-member nitrogen-containing heterocyclic group can be substituted with an oxygen atom, and the aryl or pyridinyl group can be substituted with 1-3 substitutes selected from A1 group of substitutes, X_b is an oxygen atom, and R¹, R², R³ and X_a assume values given in (a) and (b); group A1 of substitutes: (1) halogen atom. The invention also relates to a pharmaceutical composition containing a formula I compound, which is useful in treating Alzheimer's disease, senile dementia, Down syndrome or amyloidosis.

EFFECT: obtaining novel morpholine type cinnamide derivatives with inhibitory effect on amyloid-β production.

17 cl, 9 tbl, 113 ex