Phenanthryl piperazinyl dicarboxylic acids as selective NMDA...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S255010, C514S255020, C514S255030, C514S255060, C544S380000, C544S391000

Reexamination Certificate

active

06916816

ABSTRACT:
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2or C═O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4and R5are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof. Compounds of formula (I) are selective NMDA receptor modulating agents and, therefore, may be used to advantage in vitro in neuroassays and in vivo in the treatment of disorders of the CNS

REFERENCES:
patent: 5595983 (1997-01-01), Watkins et al.
patent: 5985586 (1999-11-01), Daggett et al.
patent: 0 159 889 (1985-10-01), None
Buller, A.L. et al. “Pharmacological heterogeneity of NMDA receptors: characterization of NR1 a/NR2D heteromers expressed inXenopusoocytes”; European Journal of Pharmacology, 320: 87-94 (1997).
Hrabetova, S. et al. “Distinct NMDA Receptor Subpopulations Contribute to Long-Term Potentiation and Long-Term Depression Induction”; The Journal of Neuroscience, 20: 1-6 (2000).

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