Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-03-16
1995-06-20
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514248, 544235, 544119, 544116, A61K 31495, C07D23728
Patent
active
054261066
ABSTRACT:
A class of 4-hydroxy-pyrrolo[1,2-b]pyridazin-2(1H)-one derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.
REFERENCES:
patent: 3973020 (1976-08-01), Connor et al.
patent: 4888347 (1989-12-01), Woodruff et al.
"R-(+)-HA-966, a glycine/NMDA receptor antagonist, selectively blocks the activation of the mesolimbic dopamine system by amphetamine", P. H. Hutson, et al., Br. J. Pharmacol. (1991), vol. 103, pp. 2037-2044.
Br. J. Pharmacol., 1990, 101, pp. 776-780 by G. Bagetta, et al., entitled "Prevention by the NMDA receptor antagonist, MK801 of neuronal loss produced by tetanus toxin in the rat hippocampus".
Society for Neuroscience Abstracts, 1990, 16, 128.11.
Science, 1990, 250, pp. 1276-1278, by A. N. VanDenPol, et al., entitled "Glutamate, the Dominant Excitatory Transmitter in Neuroendocrine Regulation".
Endocrinology, 1990, 127, pp. 2223-2228, by H. K. Urbanski, entitled "A Role for N-Methyl-D-Aspartate Receptors in the Control of Seasonal Breeding".
J. Neurochem., 1985, 45, pp. 477-482, by M. J. Christie, et al., entitled "An Excitant Amino Acid Projection from the Medial Prefrontal Cortex to the Anterior Part of Nucleus Accumbens in the Rat".
Neurochem. Int., 1983, 5, pp. 479-486, by M. I. Rudolph, et al., entitled "L-Glutamic Acid, A Neuromodulator of Dopaminergic Transmission in the Rat Corpus Striatum".
Life Sci., 1981, 28, pp. 1597-1603, by J. Arnt, entitled "Hyperactivity Following Injection of a Glutamate Agonist and 6,7-ADTN into Rat Nucleus Accumbens and its Inhibition by THIP".
Chem. Ber., 1969, 102, pp. 3268-3276, by Flitsch, et al.
Proc. Natl. Acad. Sci. USA, 1986, 83, pp. 7104-7108, by E. H. F. Wong, et al., entitled "The anticonvulsant MK-801 is a Potent N-Methyl-D-aspartate Antagonist".
Proceedings of the British Pharmacological Society, Jul. 1991, Abstract C78.
Kulagowski Janusz J.
Leeson Paul D.
DiPrima Joseph F.
Kilby Scalzo Catherine S.
Merck Sharp & Dohme Limited
North Robert J.
Richter Johann
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