5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)

Added on:
15 Dec, 2017

The present invention relates to novel 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine inhibitors of beta-secretase, having the structure shown in Formula (I)

wherein R1, R2, R3, R4, X1, X2, X3, X4, L and Ar are defined in the specification. 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, cerebrovascular amyloid angiopathy, multi-infarct dementia, Down’s syndrome, dementia associated with stroke, dementia associated with Parkinson’s disease or dementia associated with beta-amyloid.

  • Inventors: Andrés Avelino Trabanco-Suárez
  • Francisca Delgado-Jiménez
  • Juan Antonio Vega Ramiro
  • Gary John Tresadern
  • Henricus Jacobus Maria Gijsen
  • Daniel Oehlrich
  • Assignee: Janssen Pharmaceutica NV Janssen Cilag SA
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