171001-06-2

Upstream product

• 1486-50-6 4-(benzyloxy)benzoic acid chloride 
• 1486-51-7 p-(benzyloxy)benzoic acid 
• 108-89-4 picoline 
• 252199-28-3 4-(benzyloxy)-N-methoxy-N-methylbenzamide 

Downstream Products

• 171001-07-3 4'-benzyloxy-2-(4-pyridinyl)butyrophenone 
• 1351663-48-3 C₂₃H₂₂N₂O₂ 
• 1422841-34-6 C₂₆H₂₂N₄O₂ 
• 1422841-39-1 C₂₆H₂₂N₄O₂ 
• 1422841-40-4 C₂₆H₂₂N₄O₂ 
• 1422841-41-5 C₂₆H₂₂N₄O₂ 
• 1422841-58-4 C₂₆H₂₂N₄O₂ 
• 1422841-60-8 C₂₆H₂₂N₄O₂ 
• 1422841-62-0 C₂₆H₂₂N₄O₂ 
• 1422841-63-1 C₂₆H₂₂N₄O₂ 
• 1422841-66-4 C₂₆H₂₂N₄O₂ 
• 1422841-67-5 C₂₆H₂₂N₄O₂ 
• 898563-25-2 4-[3-(4-benzyloxy-phenyl)-1-methyl-1H-pyrazol-4-yl]-pyridine 
• 1351597-28-8 C₂₂H₁₉N₃O 

Relevant academic research and scientific papers

Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A

Twenty eight new analogues were synthesized by optimizing the structure of MP-10 and their in vitro binding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues, 10a, 10b, 10d, 11a, 11b and 11d are very potent towards PDE10A and have IC50 values of 0.40 ± 0.02, 0.28 ± 0.06, 1.82 ± 0.25, 0.24 ± 0.05, 0.36 ± 0.03 and 1.78 ± 0.03 nM respectively; these six compounds displayed high selectivity for PDE10A versus PDE3A/3B/4A/4B. The promising compounds will be further validated in vivo to identify PDE10A imaging tracers. The Royal Society of Chemistry.

RADIOLABELED PDE10A LIGANDS

Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emi

Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3- yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique "selectivity pocket" for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920). This PDE10A inhibitor is the first reported clinical entry for this mechanism in the treatment of schizophrenia.

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.

Derivatives of 4-styrylpyridines: Synthesis, estrogen receptor binding affinity, and photophysical properties

In order to develop novel ligands for the estrogen receptor (ER) that might have high binding affinity and fluorescence properties suitable for assaying ER levels in cells, we have prepared a series of substituted 4'- hydroxyl-styrylpyridines and phenylethylpyridines and studied their optical spectroscopy and receptor binding properties. Several derivatives that contain alkyl substituents on the internal ethene or ethane carbons were prepared. While most of these compounds have only modest affinity for ER, one fluorescent analog, (E)-l-(4-hydroxyphenyl)-1-phenyl-2-(4-pyridinyl)ethene (13), has reasonably good binding affinity for ER and shows long wavelength fluorescence emission that is sensitive to solvent polarity and pH. This compound may prove to be a useful probe for detecting ER in cells.