Excitatory amino acid receptor antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 217/26 (2006.01) C07D 401/00 (2006.01) C07D 403/06 (2006.01) C07F 9/62 (2006.01)

Patent

CA 2009578

The present invention provides novel bicyclic derivatives useful as excitatory amino acid receptor antagonists and in treating a variety of associated nervous system disorders. The bicyclic derivatives have the general formula: (see fig I) wherein: X is -COOH, (see fig II), (see fig. III), (see fig. IV), (see fig. V), -SO2R3, -PO3, (R4)2 or (see fig. VI); one of Y and Z is COOH, (see fig. VII), (see fig. VIII), (see fig. IX), (see fig. X), or (see fig. XI) and the other of Y and Z is hydrogen; each R3 is independently C1 - C16 alkoxy, phenyl-substituted C1 - C4 alkoxy, benzyloxy substituted on the phenyl ring with halogen, C1 - C4 alkyl or C1 - C4 alkoxy; C1 - C5 alkanoyloxymethyl; or C1 - C5 alkanoyloxymethyl substituted on the oxymethyl with C1 - C4 alkyl or C4 - C7 cycloalkyl, and each R4 is independently hydrogen, C1 - C16 alkyl, phenyl-substituted C1 - C4 alkyl, or phenyl; or a pharmaceutically acceptable salt thereof.

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