Abstract | INTRODUCTION: AREAS COVERED: This review begins with an update of the clinical trial efforts with mGlu5 NAMs. Following that update, the review summarizes small molecule mGlu5 NAM patent applications published between 2010 and 2012. These summaries are subdivided into three separate groups: inventions related to improvements in drug properties and/or developability, new chemical entities that contain a disubstituted alkyne, and new chemical entities that do not contain a disubstituted alkyne. EXPERT OPINION: Given the abundant promise found within the mGlu5 NAM field, optimism remains that a drug will emerge from this therapeutic class. Still, the launch of a new drug is far from a certainty. It is encouraging to observe the ever-increasing chemical diversity among mGlu5 NAMs. Finally, in spite of the mature nature of this field, room remains for new advancements.
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Authors | Kyle A Emmitte |
Journal | Expert opinion on therapeutic patents
(Expert Opin Ther Pat)
Vol. 23
Issue 4
Pg. 393-408
(Apr 2013)
ISSN: 1744-7674 [Electronic] England |
PMID | 23339457
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Review)
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Chemical References |
- Alkynes
- Excitatory Amino Acid Antagonists
- Receptor, Metabotropic Glutamate 5
- Receptors, Metabotropic Glutamate
- Glutamic Acid
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Topics |
- Alkynes
(chemistry, pharmacology, therapeutic use)
- Animals
- Binding Sites
- Drug Design
- Drug and Narcotic Control
- Excitatory Amino Acid Antagonists
(chemistry, pharmacology, therapeutic use)
- Glutamic Acid
(metabolism)
- Humans
- Molecular Structure
- Patents as Topic
- Receptor, Metabotropic Glutamate 5
- Receptors, Metabotropic Glutamate
(drug effects, metabolism)
- Structure-Activity Relationship
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