Pyridazinedione-based heterobicyclic covalent linkers and methods and applications thereof
US-2024425465-A1 · Dec 26, 2024 · US
US8933094B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8933094-B2 |
| Application number | US-201314055047-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 16, 2013 |
| Priority date | Dec 17, 2009 |
| Publication date | Jan 13, 2015 |
| Grant date | Jan 13, 2015 |
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The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R 4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
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The invention claimed is: 1. A compound selected from the group consisting of: 6-Phenylethynyl-[1,2,4]triazolo[1,5-a]pyridine; 2-tert-Butyl-6-phenylethynyl-[1,2,4]triazolo[1,5-a]pyridine; 2-Methyl-2-(6-phenylethynyl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-propan-1-ol; 6-Phenylethynyl-pyrazolo[1,5-a]pyridine; 2-tert-Butyl-6-phenylethynyl-pyrazolo[1,5-a]pyridine; and 6-Phenylethynyl-[1,2,3]triazolo[1,5-a]pyridine, or a pharmaceutically acceptable salt thereof.…
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