Substituted 6,7-dihydropyrazolo[1,5-a] pyrazines as negative allosteric modulators of mGlUR2 receptors
US-10005785-B2 · Jun 26, 2018 · US
US11045562B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11045562-B2 |
| Application number | US-201616061674-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 16, 2016 |
| Priority date | Dec 18, 2015 |
| Publication date | Jun 29, 2021 |
| Grant date | Jun 29, 2021 |
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The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.
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The invention claimed is: 1. A compound having the Formula or a pharmaceutically acceptable salt or a solvate thereof. 2. The compound according to claim 1 , having the Formula 3. A compound having the Formula or a pharmaceutically acceptable salt or a solvate thereof. 4. A process for the synthesis of compound comprising (a) the steps of (a-1) reacting a compound of Formula (P-1) with methanesulfonic anhydride in the presence of a base and an inert solvent, and (a-2) reacting the compound obtained in step (a-1) with [ 18 F]F − in the presence of a base in an inert solvent) or (b) the step of reacting a compound of Formula (P-2) with [ 18 F]F − in the presence of a base in an inert solvent or (c) the step of reacting a compound of Formula (P-3) with [ 18 F]F − in the presence of a base in an inert solvent
Ortho-condensed systems · CPC title
condensed with carbocyclic rings or ring systems · CPC title
with hetero atoms directly attached to ring nitrogen atoms · CPC title
Heterocyclic compounds · CPC title
Antidepressants · CPC title
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