Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.

Sang-Phyo Hong, Kevin G Liu, Gil Ma, Michael Sabio, Michelle A Uberti, Maria D Bacolod, John Peterson, Zack Z Zou, Albert J Robichaud, Darío Doller

Chemical & Pharmacokinetic Sciences, Lundbeck Research USA, 215 College Road, Paramus, New Jersey 07652, USA.

Journal of medicinal chemistry 2011 Jul 28

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There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. As part of our efforts in identifying therapeutics for central nervous system (CNS) diseases such as Parkinson's disease, we have been focusing on metabotropic glutamate receptors. Herein we report our studies with a series of tricyclic thiazolopyrazoles as mGlu4 PAMs.

Citation

Sang-Phyo Hong, Kevin G Liu, Gil Ma, Michael Sabio, Michelle A Uberti, Maria D Bacolod, John Peterson, Zack Z Zou, Albert J Robichaud, Darío Doller. Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. Journal of medicinal chemistry. 2011 Jul 28;54(14):5070-81