Metabotropic glutamate receptor antagonists

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C546S159000

Reexamination Certificate

active

07629468

ABSTRACT:
The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2represents hydrogen; halo; C1-6alkyl or amino; R3and R4each independently represent hydrogen or C1-6alkyl; or R2and R3may be taken together to form —R2—R3—, which represents a bivalent radical of formula -Z4-CH2—CH2—CH2— or -Z4-CH2—CH2— with Z4being O or NR11wherein R11is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3and R4may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5represents 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.

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