2-AMINO-5,5-DIFLUORO-5,6-DIHYDRO-4H-OXAZINES AS BACE1 AND(OR) BACE2 INHIBITORS Russian patent published in 2014 - IPC C07D265/08 C07D413/12 A61K31/535 A61K31/5355 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to 2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amide derivatives of formula I, having BACE1 and/or BACE2 inhibiting activity, pharmaceutical compositions based thereon and use thereof as therapeutically active substances. In general formula

,

R¹ is selected from a group consisting of i) a 5-6-member heteroaryl containing 1-2 heteroatoms selected from nitrogen and oxygen, and ii) 5-6-member heteroaryl containing 1-2 heteroatoms selected from nitrogen and oxygen, substituted with 1-4 substitutes, individually selected from amide, cyano, cycloalkyl, cycloalkyl-lower alkynyl, cycloalkyl-lower alkyl, cycloalkyl-lower alkoxy, halogen atom, lower haloalkoxy, lower haloalkyl, lower alkyl and nitro; iii) lower alkyl; iv) lower alkyl substituted with 1-5 substitutes individually selected from a halogena tom and hydroxy; v) lower alkenyl substituted with furanyl; vi) cycloalkyl substituted with 1-4 substitutes individually selected from a halogen atom, lower haloalkyl; R² is selected from a group consisting of i) hydrogen atom, ii) halogen atom, R³ is a lower alkyl; R⁴ is selected from a group consisting of i) a hydrogen atom, and ii) lower alkyl; R⁵ is selected from a group consisting of i) a hydrogen atom, and ii) lower alkyl; n equals 0, 1 or 2.

EFFECT: active compounds in the present invention are useful in therapeutic and/or preventive treatment, for example, of Alzheimer's disease and type 2 diabetes.

29 cl, 10 tbl, 83 ex