Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2008-10-31
2011-10-11
Padmanabhan, Sreeni (Department: 1627)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S309000, C514S416000, C514S418000, C540S461000, C540S523000, C546S113000, C546S141000, C548S453000, C548S484000
Reexamination Certificate
active
08034806
ABSTRACT:
In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
REFERENCES:
patent: 5731324 (1998-03-01), Fisher
patent: 6137002 (2000-10-01), Fisher
patent: 6656957 (2003-12-01), Allgeier et al.
patent: 2006/0235069 (2006-10-01), Duggan
patent: 43013473 (1998-06-01), None
patent: WO 96/11210 (1996-04-01), None
patent: WO 98/37068 (1998-08-01), None
patent: WO 00/75178 (2000-12-01), None
patent: WO 03/059886 (2003-07-01), None
patent: WO 2005/048953 (2005-06-01), None
patent: WO 2005/108370 (2005-11-01), None
patent: WO 2006/020879 (2006-02-01), None
patent: WO 2007/093364 (2007-02-01), None
patent: WO 2007/093364 (2007-08-01), None
patent: WO 2008/151184 (2008-12-01), None
patent: WO 2009/047303 (2009-04-01), None
patent: WO 2009/078983 (2009-06-01), None
Kew, Pharmacology & Therapeutics, 2004, Elsevier, vol. 104, pp. 233-244.
Kato et. al., Chemical Abstract Services STN, 1990.
Gazivoda et. al., Bioorganic & Medicinal Chemistry, 2007, Elsevier, vol. 15, pp. 749-758.
Alagarsamy, et al., “Coordinate regulation of metabotropic glutamate receptors,”Curr Opin Neurobiol11:357-362 (2001).
Alagarsamy, et al., “NMDA-Induced phosphorylation and regulation of mGluR5,”Pharmacol., Biochem, Behav. (special issue devoted to metabotropic glutamate receptors) 73:299-306 (2002).
Alagarsamy, et al., “NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin,”Neuropharm. 49:135-145 (2005).
Albin, et al., “The functional anatomy of basal ganglia disorders,”Trends Neurosci12:366-75 (1989).
Andreasen, “Scales for the Assessment of Negative Symptoms”, Iowa City, Iowa (1983).
Annoura, et al., “A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxycyclopropa[b]chromen-la-carboxylates,”Bioorg. Med. Chem. Lett. 6:763-766 (1996).
Awad-Granko, et al., “Activation of groups I and III metabotropic glutamate receptors inhibits excitatory transmission in the rat subthalamic nucleus,”Neuropharmacol. 41: 32-41 (2001).
Awad et al., “Activation of metabotropic glutamate receptor 5 has direct excitatory effects and potentiates NMDA receptor currents in neurons of the subthalamic nucleus,” J. Neurosci. 20:7871-7879 (2000).
Ayala, et al., “mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning.” Neuropsychopharmacology, 34(9):2057-7l(2009).
Berger, et al., Anil-Synthese. 20. Mitteilung . Über die Herstellung von Stilbenyl-Derivaten des 1,2,4,- Oxadiazols, Helvetica Chimica Acta, 62:1411-1428 (2004) (abstract).
Bevan, et al., “Move to the rhythm: oscillations in the subthalamic nucleus-external globus pallidus network,”Trends Neurosci25:525-31 (2002).
Boraud, et al., “From single extracellular unit recording in experimental and human Parkinsonism to the development of a functional concept of the role played by the basal ganglia in motor control,”Prog Neurobiol66:265-83 (2002).
Bradley, et al., “Immunohistochemical localization of subtype 4a metabotropic glutamate receptors in the rat and mouse basal ganglia,”J Comp Neurol407:33-46 (1999).
Braff, et al., “Sensorimotor gating and schizophrenia. Human and animal model studies,”Archives of general psychiatry, 47(2):181-8 (1990).
Braff, et al., “Human studies of prepulse inhibition of startle: normal subjects, patient groups, and pharmacological studies,”Psychopharmacology, 156(2-3), 234-258 (2001).
Brody, “Assessment of a prepulse inhibition deficit in a mutant mouse lacking mGlu5 receptors,” Molecular Psychiatry, 9:35-41 (2004).
Chan et al., “Attenuation of ketamine-evoked behavioral responses by mGluR5 positive modulators in mice,” Psychopharmacology (Berl), 198(1):141-8 (2008).
Chavez-Noriega et al., “Curr. Drug Targets: CNS & Neurological Disorders,” 1:261-281 (2002).
Chavez-Noriega, et al., “Novel potential therapeutics for schizophrenia: focus on the modulation of metabotropic glutamate receptor function,”Curr Neuropharmacol3:9-34 (2005).
Chen, et al., “Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses,” Mol Pharmacol, 71(5):1389-98 (2007).
Chen, et al., “20.N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindo1-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors,” Mol Pharmacol, 73(3):909-18 (2008).
Chiamulera et al. Nature Neurosci. 4:873-874 (2001).
Conn, et al., “Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders,” Nat Rev Drug Discov, 8(1):41-54 (2009).
Conn, et al., “Pharmacology and functions of metabotropic glutamate receptors,”Annu Rev Pharmacol Toxicol37:205-37 (1997).
Conn, “Physiological roles and therapeutic potential of metabotropic glutamate receptors,”Annals New York Acad. Sci. 1003:12-21 (2003).
Corti, et al., “Distribution and synaptic localisation of the metabotropic glutamate receptor 4 (mGluR4) in the rodent CNS,”Neuroscience110:403-20 (2002).
Daggett, et al., “Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5,”Neuropharmacology34:871-86 (1995).
Darrah, et al., “Interaction of N-methyl-D-aspartate and group 5 metabotropic glutamate receptors on behavioral flexibility using a novel operant set-shift paradigm,” Behav Pharmacol., 19(3):225-34 (2008).
De Blasi, et al., “Molecular determinants of metabotropic glutamate receptor signaling,”Trends Pharmacol Sci. 22: 114-120 (2001).
DeLong, “Primate models of movement disorders of basal ganglia origin,”Trends Neurosci13:281-5 (1990).
Doherty, et al., “Metabotropic glutamate receptors modulate feedback inhibition in a developmentally regulated manner in rat dentate gyrus,”J Physiol, 561.2:395-401 (2004).
Engers, et al., “Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago-potentiator ADX-47273,” ChemMedChem, 4:505-511 (2009).
Epping-Jordan et al., “In Vivo Characterization of mGluR5 Positive Allosteric Modulators as Novel Treatments for Schizophrenia and Cognitive Dysfunction,”Neuropharmacology, 49:243 (2005).
Fisher et al., “Non-Peptide RGD Surrogates Which Mimic a Gly-Asp β-Turn: Potent Antagonists of Platelet Glycoprotein IIb-IIIa,” J. Med. Chem., 40:2085-2101 (1997).
Gasparini et al., “2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist,” Neuropharmacol. 38:1493-1503 (1999).
Gass JT, et al., “Positive allosteric modulation of mGluR5 receptors facilitates extinction of a cocaine contextual memory,” Biol Psychiatry., 65(8):717-20 (2009).
Gazivoda, et al., Bioorganic & Medicinal Chemistry, 2007, Elsevier, vol. 15, pp. 749-758.
Geyer, et al., “Mouse genetic models for prepulse inhibition: an early review,”Molecular Psychiatry, 7(10):1039-1053 (2002).
Geyer, M. A. ‘Behavioral studies of hallucinogenic drugs in animals: implications for schiz
Conn P. Jeffrey
Jones Carrie K.
Lindsley Craig W.
Niswender Colleen M.
Rodriguez Alice L.
Ballard Spahr LLP
Padmanabhan Sreeni
Pihonak Sarah
Vanderbilt University
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