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US Patent 5863916 - 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor

US Patent Issued on January 26, 1999
Estimated Patent Expiration Date: Icon_subject February 4, 2017Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
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Abstract

Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof; wherein n is zero or 1; R4, R5, R6 are independently hydrogen, nitro, amino, halo, haloalkyl, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, azido, acylamino, alkylsulfonyl, aryl, substituted aryl, heteroaryl, alkoxy, trialkylsilyl-substituted alkoxy, aryloxy, substituted aryloxy, heteroaryloxy, a heterocyclic group, a heterocyclicoxy group, aralkoxy, or haloalkoxy; and Rc and Rd are defined in the specification. These compounds have high binding to the glycine site of the NMDA receptor. Also disclosed are methods of treating pathophysiologic conditions associated with neuronal degeneration, convulsions, anxiety, chronic pain, pyschosis, opiate tolerance, and inducing anesthesia.

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Inventors

Assignee

Application

No. 795387 filed on 02/04/1997

US Classes:

514/249, 1,4-diazine as one of the cyclos544/345Three or more ring hetero atoms in the tricyclo ring system

Field of Search

514/249, 1,4-diazine as one of the cyclos544/345Three or more ring hetero atoms in the tricyclo ring system

Examiners

Primary: Grumbling, Matthew V.

Attorney, Agent or Firm

US Patent References

4296114, 3,4-Dihydro-3-oxopyrido[2,3-b]-pyrazines, compositions and use thereof
Issued on: 10/20/1981
Inventor: Appleton ,   et al.
5055465, Imidazoquinoxalinones, their aza analogs and process for their preparation
Issued on: 10/08/1991
Inventor: Davey
5283244, Fused pyrazine derivatives
Issued on: 02/01/1994
Inventor: Sakamoto, et al.
5424311Azaquinoxalines and their use
Issued on: 06/13/1995
Inventor: Billhardt-Troughton, et al.

Foreign Patent References

  • 0 008 864 EP. 03/09/1980
  • 0 039 920 EP. 11/09/1981
  • 0 283 162 EP. 09/09/1988
  • 0 290 819 EP. 11/09/1988
  • 0 320 136 EP. 06/09/1989
  • 0 347 146 EP. 12/09/1989
  • 0 374 534 EP. 06/09/1990
  • 4-178385 JP. 06/09/1992
  • WO 91/13878 WO. 09/09/1991
  • WO 92/07847 WO. 05/09/1992

International Classes

A61K 031/495
C07D 403/12

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