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editorial
. 2013 Aug 6;4(9):819–821. doi: 10.1021/ml4002776

Trisubstituted Imidazoles as Positive Modulators of Metabotropic Glutamate Receptor Subtype 5

Gerard Rosse 1,*
PMCID: PMC4027227  PMID: 24900753

Title: Trisubstituted Imidazoles as Positive Modulators of Metabotropic Glutamate Receptor Subtype 5
Patent/Patent Application Number: US2013150347A1 Publication date: June 13, 2013
US2013150355A1
Priority Application: EP 2011–193132 Priority date: December 13, 2011
EP 2011–193133
Inventors: Rudolf, K.; Bischoff, D.; Dahmann, G.; Grauert, M.; Kuelzer, R.; Wellenzohn, B.
Assignee Company: Boehringer Ingelheim International GmbH, Germany
Disease Area: Neurological and/or psychiatric disorder Biological Target: Metabotropic Glutamate Receptor Subtype 5 (mGluR5)
Summary: These two application claim a series of trisubstituted imidazoles that may provide treatment for a wide variety of diseases and disorders such as schizophrenia, cognitive decline, dementia, cognitive impairment, and Alzheimer’s disease.
Important Compound Classes: graphic file with name ml-2013-002776_0001.jpg
Key Structures: graphic file with name ml-2013-002776_0003.jpg
Recent Review Articles: 1. Matosin N.; Newell K. A.. Metabotropic glutamate receptor 5 in the pathology and treatment of schizophrenia. Neurosci. Biobehav. Rev. 2013, 37 (3), 256–268.
2. Lindsley C. W.; Stauffer S. R.. Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004–2012). Pharm. Pat. Anal. 2013, 2 (1), 93–108.
Biological Assay: The positive modulation of mGluR5 is measured in HEK 293A cells expressing human recombinant mGluR5 and is detected with calcium based FLIPR assay.
Pharmacological Data: Activity of positive modulator of mGluR5graphic file with name ml-2013-002776_0004.jpg

The authors declare no competing financial interest.


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