Excitatory amino acid receptor modulators

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

Reexamination Certificate

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C514S562000, C560S115000, C560S157000, C560S222000, C562S506000

Reexamination Certificate

active

07081481

ABSTRACT:
Compounds of the formula (I) in which: R1is (CH2)nY; n is 1 or 2; Y is NHSO2R2or X1—W—X2—R3; X1is O or NH; W is C═O, C═S, C═NH, or SO2; X2is O or NH, provided that X1and X2are not both O; R2is C1-10alkyl; C2-10alkenyl; C2-10alkynyl; aryl; aryl-C1-10alkyl; aryl-C2-10alkenyl; aryl-C2-10alkynyl; C3-8cycloalkyl or C3-8-cycloalkyl-C1-10alkyl; and R3is hydrogen, C1-10alkyl; C2-10alkenyl; C2-10alkynyl; aryl; aryl-C1-10alkyl; aryl-C2-10alkenyl; aryl-C2-10alkynyl; C3-8cycloalkyl; or C3-8-cycloalkyl-C1-10alkyl; or a salt or ester thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.

REFERENCES:
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patent: 6498180 (2002-12-01), Collado et al.
patent: 6504052 (2003-01-01), Collado et al.
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patent: WO 01/92212 (2001-12-01), None
Baskys et al., Understanding regulation of nerve cell death by mGluRs as a method for development of successful neuroprotective strategies, Journal of the Neurological Sciences 229-230 (2005) 201-209.
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Pellicciari et al: “Synthesis and Pharmacological Characterization of All Sixteen Stereoisomers of 2-(2′-Carboxy-3′-phenylcyclopropyl)glycine . Focus on (2S, I'S,2'S,3'R)-2-(2′-Carboxy-3′-phenylcy clopropyl)glycine, a Novel and Selective Group II Metabotropic Glutamate Receptor Antagonist” Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 39, No. 11, 1996, pp. 2259-2269, XP002122695 ISSN: 0022-2623 cited in the application pp. 2259-2269.
Collado, Ivan et A., (2S,1'S,2′ R,3′R)-2-(2′-Carboxy-3′-hydroxymethylcyclopropyl) Glycine Is a Highly Potent Group 2 and 3 Metabotropic Glutamate Receptor Agonist with Oral Activity, J. Med. Chem, 2004, 456-466, vol. 47.
Johnson, Byran G. et al, [2H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate {mGlu} receptors: characterization of binding to membranes of mGlu receptors subtype expressing cells, Neuropharmacology, 1999, 1519-1529 vol. 38.

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