abstract |
The present invention relates to novel 5 as beta-secretase inhibitors, 6 glyoxalidine simultaneously [1,5 a] pyrazine 3 (2H) ketone derivatives, beta-secretase is also referred to as β sites amyloid lyases, BACE, particularly BACE1 and/or BACE2 (wherein BACE1 is also referred to as Asp2 or film aspartic protease 2, and BACE2 is also referred to as Asp1, film aspartic protease 1 or DRAP).The invention further relates to the pharmaceutical composition for including such compound, it is related to the method for preparing such compound and composition, and it is related to such compound and composition is used for the purposes that prevention and treatment are directed to the obstacle of beta-secretase, these obstacles are such as Alzheimer disease (AD), mild cognitive impairment, aging, it is dull-witted, dementia with Lewy body, Down syndrome, the dementia related to apoplexy, the dementia related to Parkinson's disease, alzheimer dementia, the dementia related to amyloid beta, AMD, diabetes B and other dysbolisms. |