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    3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATEMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA
    14.
    发明专利
    3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATEMENT OF ALZHEIMER'S DISEASE AND OTHER FORMS OF DEMENTIA 未知

    公开(公告)号：NZ603896A

    公开(公告)日：2013-08-30

    申请号：NZ60389611

    申请日：2011-06-27

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  DELGADO-JIMENEZ FRANCISCA ,  TRESADERN GARY JOHN

    IPC: C07D241/08 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61P25/28 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10

    Abstract: Abstract - 603896 Disclosed are 3-amino-5-[3-(aryl / heteroaryl)-phenyl]-5,6-dihydro-1H-pyrazin-2-one derivatives as represented by the general Formula (I) or stereoisomeric forms thereof, wherein R1 is selected from the group consisting of hydrogen, alkyl, mono- and polyhalo-alkyl, aryl and heteroaryl; R2 is selected from the group consisting of hydrogen, alkyl, mono- and polyhalo-alkyl, aryl and heteroaryl; X1, X2, X3, X4 are independently C(R3) or N, provided that no more than two thereof represent N; each R3 is selected from the group consisting of hydrogen, halo, alkyl, mono- and polyhalo-alkyl, cyano, alkyloxy, mono- and polyhalo-alkyloxy; L is a bond or -N(R4)CO-, wherein R4 is hydrogen or alkyl; Ar is homoaryl or heteroaryl; wherein homoaryl is phenyl or phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono and polyhalo-alkyl; heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, oxazolyl, and oxadiazolyl, each optionally substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono- and polyhalo-alkyl; or an addition salt or a solvate thereof. Representative compounds include 3'-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydropyrazin-2-yl)-biphenyl-3-carbonitrile, 3-amino-5-[3-(5-methoxy-pyridin-3-yl)-phenyl]-1,5-dimethyl-5,6-dihydro-1H-pyrazin-2-one, 5-chloro-pyridine-2-carboxylic acid [3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydro-pyrazin-2-yl)-phenyl]-amide, 5-chloro-pyridine-2-carboxylic acid [3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydro-pyrazin-2-yl)-phenyl]-amide, 5-amino-3-(2,4-difluoro-biphenyl-5-yl)-1,3-dimethyl-2H-pyrazin-6-one, 5-amino-3-[2,4-difluoro-5-(5-methoxy-3-pyridyl)phenyl]-1,3-dimethyl-2H-pyrazin-6-one, 5-amino-3-(2,4-difluoro-5-pyrimidin-5-yl-phenyl)-1,3-dimethyl-2H-pyrazin-6-one, 5-chloro-pyridine-2-carboxylic acid [3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydro-pyrazin-2-yl)-4-fluoro-phenyl]-amide, 5-amino-1,3-dimethyl-3-(biphenyl-3-yl)-2H -pyrazin-6-one and 5-amino-1,3-dimethyl-3-(3-(pyrimidin-5-yl)phenyl)-2H-pyrazin-6-one. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above and a pharmaceutically acceptable carrier for the treatment of Alzheimer's disease, mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.

    4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
    15.
    发明专利
    4,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-6-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 未知

    公开(公告)号：SG188338A1

    公开(公告)日：2013-04-30

    申请号：SG2013015136

    申请日：2011-09-20

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  TRESADERN GARY JOHN ,  DELGADO-JIMENEZ FRANCISCA

    Abstract: The present invention relates to novel 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-yl- aminederivativesas inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretaseis involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associatedwith stroke, dementia associated with Parkinson's disease or dementia associated with beta- amyloid.

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