3,4-DIHYDRO-PYRROLO[1,2-A]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

The present invention relates to novel 3,4-dihydro-pyrrolo[l,2-a]pyrazin-1-ylamine derivatives as 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, t...

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Bibliographic Details
Main Authors DELGADO-JIMENEZ, FRANCISCA, TRABANCO-SUAREZ, ANDRES AVELINO
Format Patent
LanguageEnglish
French
Published 23.04.2019
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to novel 3,4-dihydro-pyrrolo[l,2-a]pyrazin-1-ylamine derivatives as 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-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid. La présente invention concerne de nouveaux dérivés de 3,4-dihydro-pyrazolo[1,2-a]pyrazin-1-yl-amine en tant qu'inhibiteurs de bêta-sécrétase, également appelée enzyme de clivage d'amyloïde de site bêta, BACE, BACE1, Asp2 ou mémapsine 2. L'invention concerne en outre des compositions pharmaceutiques comprenant de tels composés, des procédés pour préparer de tels composés et compositions, et l'utilisation de tels composés et compositions pour la prévention et le traitement de troubles dans lesquels la bêta-sécrétase est impliquée, tels que la maladie d'Alzheimer (AD), un trouble cognitif léger, la sénilité, la démence à corps de Lewy, le syndrome de Down, la démence associée à un accident vasculaire cérébral, la démence associée à la maladie de Parkinson ou la démence associée au bêta-amyloïde.
Bibliography:Application Number: CA20122825620