Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-06-14
2009-02-03
Wilson, James (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C544S251000
Reexamination Certificate
active
07485648
ABSTRACT:
In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
REFERENCES:
patent: 6232320 (2001-05-01), Stewart et al.
patent: 2002/0151544 (2002-10-01), Masahiko et al.
patent: 2006/0167029 (2006-07-01), Matasi et al.
patent: 2006/0189639 (2006-08-01), Stewart et al.
patent: WO 01/32632 (2001-05-01), None
patent: WO 02/062803 (2002-08-01), None
patent: WO 2006/081072 (2006-08-01), None
Kamble, D. G., et al.: “Synthesis of some new heterocyclic systems bearing (3H)-benzofuropyrimidin- 4-one-3-yl moiety as antibacterial agents”, Indian Journal of Heterocyclic Chemistry, 1999, p. 23-26, 9(1).
Russo, F., et al.: “New nitrogenous polycyclic systems. Synthesis and pharmacological properties of benzofuro and thienothiadiazolopyrimidine derivatives”, Farmaco, Edizione Scientifica, 1983, p. 762-774, 38(10). + English Abstract (1pg.).
Merour, J. Y.: “Specific synthesis of pyrimidines. Concurrent formation of pyrimidines and triazepines”, Journal of Heterocyclic Chemistry, 1982, p. 1425-1431, 19(6). + English Abstract (1pg.).
Mahajan, S. B., et al.: “Studies in benzofurans: Part VIII—Synthesis of Some 3-N-aryl-, 3-N-Alkyl- & 3-Amino-3,4-dihydro-4-oxobenzofuro[3,2-d]pyrimidines”, Indian Journal of Chemistry, 1980, p. 402-404. 19B(5).
Kadushkin, A. V., et al.: DMF diethyl acetal as a one-carbon component in the synthesis of isomeric pyridothienopyrimidines, Khimiko-Farmatsevticheskii Zhurnal, 1993, p. 40-43, 27(3). + English Abstract (1pg.).
International Search Report for International Application No. PCT/US2005/020972, mailed Oct. 26, 2005 (5pgs.).
El-Kouhen, O, et al., Research Paper—“Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist”, British Journal of Pharmacology, 2006, pp. 761-774, vol. 149.
Morè, Lorenzo, et al., “Comparison of the mGluR1 antagonist A-841720 in rat models of pain and cognition”, Behavioural Pharmacology, 2007, pp. 273-281, vol. 18, No. 4.
Zhu, Chang Z., et al., “Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats”, European Journal of Pharmacology, 2008, pp. 314-321, vol. 580.
Zheng, Guo Zhu, et al., “Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists”, Bioorganic & Medicinal Chemistry Letters, 2006, pp. 4936-4940, vol. 16.
Zheng, Guo Zhu, et al., “Structure—Activity Relationship of Triazafluorenone Derivatives as Potent and Selective mGluR1 Antagonists”, J. Med. Chem., 2005, pp. 7374-7388, vol. 48, No. 23.
Burnett Duane A.
Domalski Martin S.
Korakas Peter
Matasi Julius J.
Qiang Li
Leeser Erich A
MacMillan Keith D.
Schering Corporation
Wilson James
LandOfFree
mGluR1 antagonists as therapeutic agents does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with mGluR1 antagonists as therapeutic agents, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and mGluR1 antagonists as therapeutic agents will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4105242