208519-37-3Relevant articles and documents
(-)-6-Chloro-2-[(1-furo[2,3-c]pyridin-5-yl-ethyl)thio]-4- pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor
Wishka,Graber,Kopta,Olmsted,Friis,Hosley,Adams,Seest,Castle,Dolak,Keiser,Yagi,Jeganathan,Schlachter,Murphy,Cleek,Nugent,Poppe,Swaney,Han,Watt,White,Poel,Thomas,Voorman,Stefanski,Stehle,Tarpley,Morris
, p. 1357 - 1360 (1998)
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6-alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds
R?ver, Stephan,Andjelkovic, Mirjana,Bénardeau, Agnès,Chaput, Evelyne,Guba, Wolfgang,Hebeisen, Paul,Mohr, Susanne,Nettekoven, Matthias,Obst, Ulrike,Richter, Wolfgang F.,Ullmer, Christoph,Waldmeier, Pius,Wright, Matthew B.
, p. 9874 - 9896 (2014/01/17)
We identified 6-alkoxy-5-aryl-3-pyridinecarboxamides as potent CB1 receptor antagonists with high selectivity over CB2 receptors. The series was optimized to reduce lipophilicity compared to rimonabant to achieve peripherally active molecules with minimal central effects. Several compounds that showed high plasma exposures in rats were evaluated in vivo to probe the contribution of central vs peripheral CB1 agonism to metabolic improvement. Both rimonabant and 14g, a potent brain penetrant CB1 receptor antagonist, significantly reduced the rate of body weight gain. However, 14h, a molecule with markedly reduced brain exposure, had no significant effect on body weight. PK studies confirmed similarly high exposure of both 14h and 14g in the periphery but 10-fold lower exposure in the brain for 14h. On the basis of these data, which are consistent with reported effects in tissue-specific CB1 receptor KO mice, we conclude that the metabolic benefits of CB1 receptor antagonists are primarily centrally mediated as originally believed.
CRYSTALLINE FUMARATE SALTS OF 1-AZABICYCLO[2.2.2]OCT SUBSTITUTED FURO[2,3-C]PYRIDINYL CARBOXAMIDE AND COMPOSITIONS AND PREPARATIONS THEREOF
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, (2008/06/13)
The invention provides fumarate salts of N-[1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, compositions, racemic mixtures, or pure enantiomers thereof, and preparation thereof. The fumarate salts are useful to treat diseases or conditions in which α7 nAChR is known to be involved. Formula (I).