898563-88-7

Upstream product

• 898563-86-5 4-[3-(4-benzyloxyphenyl)-1H-pyrazol-4-yl]pyridine 
• 898563-87-6 4-[3-(4-benzyloxyphenyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]pyridine 

Downstream Products

• 1301167-92-9 5-methoxy-2-[4-[4-(4-pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]phenoxymethyl]pyridine 
• 1301167-98-5 3-methoxy-2-[4-[4-(4-pyridinyl)-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]phenoxymethyl]pyridine 

Relevant academic research and scientific papers

RADIOLABELLED PDE10 LIGANDS

The present invention relates to novel, selective, radiolabelled PDE10 ligands which are useful for imaging and quantifying the PDE10A enzyme 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, and to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo.

Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging

We have recently reported the phosphodiesterase 10A (PDE10A) inhibitor 2-[4-[1-(2-[18F]fluoroethyl)-4-pyridin-4-yl-1H-pyrazol-3-yl]- phenoxymethyl]-quinoline ([18F]1a) as a promising candidate for in vivo imaging using positron emission tomography (PET). We now describe the synthesis and biological evaluation of a series of related pyridinyl analogues that exhibit high potency and selectivity as PDE10A inhibitors. The most interesting compounds were injected in rats to measure their levels of PDE10A occupancy through an in vivo occupancy assay. The 3,5-dimethylpyridine derivative 3 and the 5-methoxypyridine derivative 4 showed a comparable level of occupancy to that of 1a. Because these derivatives showed lower in vitro activity and are slightly less lipophilic than 1a, we hypothesized that they could behave as better PET imaging ligands. Compounds [18F]3, [ 18F]4, and [11C]4 were radiosynthesized and subjected to biodistribution studies in rats for a preliminary evaluation as candidate PET radioligands for in vivo imaging of PDE10A in the brain.

BICYCLIC HETEROARYL COMPOUNDS AS PDE10 INHIBITORS

The invention pertains to bicyclic heteroaryl compounds that serve as effective phosphodiesterase (PDE) inhibitors The invention also relates to compounds which are selective inhibitors of PDE-10. The invention further relates to intermediates for prepara

Heteroaromatic quinoline compounds

The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.