| 摘要 |
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,Ris 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; Ris selected from a group consisting of i) hydrogen atom, ii) halogen atom, Ris a lower alkyl; Ris selected from a group consisting of i) a hydrogen atom, and ii) lower alkyl; Ris 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 |
