Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2008-06-06
2010-12-28
Wilson, James O. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S231800, C514S232200, C514S232800, C514S252110, C514S315000, C514S320000, C540S575000, C544S126000, C544S361000, C546S082000
Reexamination Certificate
active
07858614
ABSTRACT:
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAAreceptor and negatively modulating the α5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAAreceptor associated disorders. The general structure of formula I is shown below:The invention further provides a method of modulation of one or more GABAAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
REFERENCES:
patent: 4552874 (1985-11-01), Mardin et al.
patent: 4690930 (1987-09-01), Takeda et al.
patent: 4814450 (1989-03-01), Yokoyama
patent: 5334595 (1994-08-01), Wentland
patent: 6686373 (2004-02-01), Kawamura et al.
patent: 2005/0004159 (2005-01-01), Hibi et al.
patent: 2005/0245563 (2005-11-01), Boyle et al.
patent: 2006/0035919 (2006-02-01), Matthews et al.
patent: 2006/0100229 (2006-05-01), Hays et al.
patent: 2007/0078083 (2007-04-01), Barlow et al.
patent: 0 214 092 (1986-08-01), None
patent: WO 99/06401 (1999-02-01), None
Carotti et al., “High Affinity Central Benzodiazepine Receptor Ligands. Part 3: Insights Into the Pharmacophore and Pattern Recognition Study of Intrinsic Activities of Pyrazole[4,3-c]quinolin-3-ones”,Bioorg. &Med. Chem., 2003, 11(23): 5259-5272.
Jacobsen et al., “Piperazine imidazo[1,5-a]quinoxaline Ureas as High-Affinity GABAALigands of Dual Functionality”,J. Med. Chem., 1999, 42(7): 1123-1144.
Atack et al., “The proconvulsant effects of the GABAAα5 subtype-selective compound RY-080 may not be α5-mediated”, European Journal of Pharmacology, 548:77-82 (2006).
Barnard et al., “International Union of Pharmacology. XV. Subtypes of γ-Aminobutyric AcidAReceptors: Classification on the Basis of Subunit Structure and Receptor Function” Pharmacol. Rev. 50(2):291-313 (1998).
Low et al., “Molecular and Neuronal Substrate for the Selective Attenuation of Anxiety”, Science, 290:131-134 (2000).
McKernan et al., “Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAAreceptor α1subtype”, Nat. Neurosci. 3:587-592 (2000).
Muller, “New trends in benzodiazepine research”, Drugs of Today, 24:649-663 (1988).
Rudolph et al., “Benzodiazepine actions mediated by specific γ-aminobutyric acidAreceptor subtypes”, Nature, 401:796-800 (1999).
Takada et al., “Thienylpyrazoloquinolines: Potent Agonists and Inverse Agonists to Benzodiazepine Receptors”, J. Med. Chem., 31:1738-1746 (1988).
Yokoyama at al., “2-Arylpyrazolo[4,3-c]quinolin-3-ones: Novel agonist, Partial Agonist and Antagonist of Benzodiazepines” J. Med. Chem., 25:337-339 (1982).
International Search Report corresponding to PCT Application No. PCT/US08/66211 mailed Sep. 2, 2008.
International Written Opinion corresponding to PCT Application No. PCT/US08/66211 mailed Sep. 2, 2008.
Allen et al., “Synthesis of novel 2-Phenyl-2H-pyrazolo[4,3-c]isoquinolin-3-ols: Topological Comparisons with Analogues of 2-Phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones at benzodiazepine receptors,”J. Med. Chem., 1992, 35(2): 368-374.
Fryer et al., “Structure Activity Relationships of 2-Phenylpyrazolo[4,3-c]quinolin-3-ones and their N- and O-Methyl Analogs at Benzodiazepine Receptors,”Med. Chem. Res., 1993, 3: 122-130.
Lister et al., “A pharmacokinetic study of CGS-8216, a benzodiazepine receptor ligand, in the rat,”Psychopharmacology, 1984, 84: 420-422.
Gupta Varsha
Kaplan Alan P.
Wasley Jan W.F.
Helicon Therapeutics, Inc.
Knobbe Martens Olson & Bear LLP
Sackey Ebenezer
Wilson James O.
LandOfFree
Therapeutic pyrazolonaphthyridine derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Therapeutic pyrazolonaphthyridine derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Therapeutic pyrazolonaphthyridine derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-4155074