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OwnerP. Jeffrey Conn, Anthony G. DiLella +4inventors
InventorsP. Jeffrey Conn, Anthony G. DiLella, Gene G. Kinney, Michael J. Marino, Guy R. Seabrook, David L. Williams
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An mGluR4 receptor positive allosteric modulator is useful, alone or in combination with a neuroleptic agent, for treating or preventing movement disorders such as Parkinson's disease, dyskinesia, tardive dyskinesia, drug-induced parkinsonism, postencephalitic parkinsonism, progressive supranuclear palsy, multiple system atrophy, corticobasal degeneration, parkinsonian-ALS dementia complex, basal ganglia calcification, akinesia, akinetic-rigid syndrome, bradykinesia, dystonia, medication-induced parkinsonian, Gilles de la Tourette syndrome, Huntington's disease, tremor, chorea, myoclonus, tick disorder, and dystonia.
A method of treatment of Parkinson's disease in a patient in need-thereof that comprises administering to the patient a therapeutically effective amount of an mGluR4 receptor positive allosteric modulator or a pharmaceutically acceptable salt thereof consisting of a selectivity for the mGluR4 receptor relative to other mGluR receptors of at least three fold as measured by the ratio of EC50.
A method of treatment of Parkinson's disease in a patient in need-thereof that comprises administering to the patient a therapeutically effective amount of an mGluR4 receptor positive allosteric modulator or pharmaceutically acceptable salt thereof having a binding of at least 1 nM for the mGluR4 receptor as measured by EC50 and as evaluated by the Fluorometric Imaging Plate Reader (FLIPR).
A method of positive allosteric modulation of a human mGluR4 receptor having a preferential selectivity of at least three fold as measured by the ratio of EC50 of the mGluR4 to other mGluR receptors and a binding for the mGluR4 receptor relative to the other mGluR receptors as measured by EC50 and evaluated by FLIPR of less than 1 nM.
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