Benzimidazolidinone derivatives as muscarinic agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S322000, C546S199000, C548S304700

Reexamination Certificate

active

11188295

ABSTRACT:
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1and/or M4receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

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Bonner, et al., “Identification of a family of muscarinic acetylcholine receptor genes”,Science, (1987) 237:527.
Braüner-Osborne, et al., “Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): high throughput assays in mammalian cells”,Eur. J. Pharamacol., (1996) 295:93-102.
Bymaster, et al., “Potential role of muscarinic receptors in schizophrenia”,Life Science, (1999) 64:527.
Bymaster, et al., “Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-y1)-1-azabicyclo[3.2.1]octane”,Eur. J. Pharmacol., (1998) 356:109.
Cakir, et al., “Synthesis and antinociceptive activity of some 3-subsitiuted benzothiazolone derivatives”II Farmaco, (1999) 54:846.
Chahine, et al., “Functional expression and properties of the human skeletal muscle sodium channel”,Pfluegers Arch., (1994) 427:136-142.
Felder, et al., “Therapeutic opportunities for muscarinic receptors in the central nervous system”,J. Med. Chem., (2000) 43:4333.
Friedman, et al., “Pharmacologic strategies for augmenting cognitive performance in schizophrenia”,Biol. Psychiatry, (1999) 45:1.
Itani, et al., “Novel Potent Antagonists of Human Neuropeptide Y Y5 Receptors”,Bioorganic&Medicinal Chemistry Letters, (2002) 12:799-802.
Rowley, et al., “Current and novel approaches to the drag treatment of schizophrenia”,J. Med. Chem., (2001) 44:477.
Sauerberg, et al., “Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity”,J. Med. Chem., (1998) 41:4378.
Shannon, et al., “Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M receptors”,J. Pharmacol. Exp. Ther., (1994) 269:271.
Shannon, et al., “Muscarinic receptor agonists, like dopamine receptors antagonist antipsychotics, inhibit conditioned avoidance response in rats”,J. Pharmacol. Exp. Ther., (1999) 290:901.
Shannon, et al., “Xanomeline, an M1/M4preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice”,Schizophrenia Res., (2000) 42:249.
Stormann, et al., “Molecular cloning and expression of a dopamine D2 receptor from Human retina”,Mol. Pharmacol., (1990) 37:1-6.
Supplementary European Search Report for Application No. EP 02 76 3824, Sep. 22, 2005.
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