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Expert Opinion on Therapeutic Patents Volume 20, 2010 - Issue 3
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Patent Evaluations

Novel heterocyclic compounds as mGlu5 antagonists: WO2009015897

Dario Doller Department of Medicinal Chemistry, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA +1 201 350 0341; +1 201 261 0623; [email protected]
, PhD,
Guiying Li Department of Medicinal Chemistry, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA +1 201 350 0341; +1 201 261 0623; [email protected]; Department of Medicinal Chemistry, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA
, PhD,
Robbin M Brodbeck Department of Medicinal Chemistry, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA +1 201 350 0341; +1 201 261 0623; [email protected]; Department of Biological Research, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA
, PhD &
Christian Thomsen Department of Medicinal Chemistry, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA +1 201 350 0341; +1 201 261 0623; [email protected]; Department of Biological Research, Lundbeck Research USA, 215 College Road, Paramus, NJ 07652, USA
, MScPhD
Pages 435-439 | Published online: 24 Feb 2010
 
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Abstract

Metabotropic glutamate receptor 5 (mGlu5) negative allosteric modulators (NAMs) have previously been implicated in a number of pathophysiological conditions, based on preclinical, and to some extent clinical, proof of concept for migraine, gastroesophageal reflux disease, Parkinson's disease and anxiety. In the past, the potential use of known mGlu5 antagonists for the treatment of lower urinary tract disorders was disclosed. In the patent evaluated herein, novel derivatives of 4-(prop-2-ynylidene)piperidine are described and claimed by Recordati Ireland Ltd, Ireland, as NAMs at mGlu5 for the treatment of lower urinary tract disorders. Selected compounds reported in this application were efficacious in the cystometry model of bladder dysfunction in conscious rats, and mGlu5 NAMs are, therefore, suggested to have potential for the treatment of lower urinary tract disorders.

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