214699-26-0Relevant articles and documents
An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines
Guiadeen, Deodialsingh,Kothandaraman, Shankaran,Yang, Lihu,Mills, Sander G.,MacCoss, Malcolm
scheme or table, p. 6368 - 6370 (2009/04/07)
An expeditious and concise synthesis of 3-(difluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines is described. Starting from N-benzyl piperidone, the key intermediates leading to these two bio
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists
Shah, Unmesh,Lankin, Claire M.,Boyle, Craig D.,Chackalamannil, Samuel,Greenlee, William J.,Neustadt, Bernard R.,Cohen-Williams, Mary E.,Higgins, Guy A.,Ng, Kwokei,Varty, Geoffrey B.,Zhang, Hongtao,Lachowicz, Jean E.
scheme or table, p. 4204 - 4209 (2009/04/10)
SCH 58261 is a reported adenosine A2A receptor antagonist which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A1 receptor and does not demonstrate oral activity. Quinoline analogs have improved upon the selectivity and pharmacokinetics of SCH 58261, but were difficult to handle due to poor aqueous solubility. We report the design and synthesis of fused heterocyclic analogs of SCH 58261 with aqueous solubility as well as improved A2A receptor binding selectivity and pharmacokinetic properties. In particular, the tetrahydronaphthyridine 4s has excellent A2A receptor in vitro binding affinity and selectivity, is active orally in a rat in vivo model of Parkinson's Disease, and has aqueous solubility of 100 μM at physiological pH.
A facile synthesis of the 3-amino-5,6,7,8-tetrahydro[1,6]naphthyridine system and some alkylated and polycyclic homologues
Harling,Harrington,Thompson
, p. 787 - 797 (2007/10/03)
A facile, two step synthesis of the 3-amino-5,6,7,8-tetrahydro[1,6]naphthyridine system 1 and its more substituted homologues 2-5 via the condensation of mono- and bicyclic-4-piperidinones 11a-c, 12-14 with 3,5-dinitro-1-methyl-2-pyridone 6 in the presenc
Imidazole and imidazoline derivatives and uses thereof
-
, (2008/06/13)
This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human α2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where