METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS

摘要

The present invention concerns compounds of formula (I-A) and (I-B). In a preferable embodiment of the invention, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form –R-R-, which represents a bivalent radical of formula –Z-CH-CH-CH- or –Z-CH-CH- with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula –CH-CH-CH-CH- ; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.