135338-27-1Relevant academic research and scientific papers
Dipyridyl amides: Potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
Bonnefous, Celine,Vernier, Jean-Michel,Hutchinson, John H.,Chung, Janice,Reyes-Manalo, Grace,Kamenecka, Theodore
, p. 1197 - 1200 (2005)
The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amides as small molecules mGluR5 antagonists.
SUBSTITUTED 2-AZABICYCLO[3.1.1]HEPTANE AND 2-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
-
, (2019/03/17)
There is provided a compound of formula (I), wherein L1 to L3, R1 to R4, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
Highly regioselective ring opening of quinolinic[2,3]anhydrides under mild conditions
Metobo, Sammy E.,Jabri, Salman Y.,Aktoudianakis, Evangelos,Evans, Jared,Jin, Haolun,Kim, Choung U.
, p. 6782 - 6784 (2013/11/19)
We report a study of the influence of Lewis acids upon the regioselectivity of ring opening of quinolinic[2,3]anhydrides to provide 2-(isopropoxycarbonyl)- nicotinic acids. In the presence of stoichiometric amounts of indium trifluoromethanesulfonate or lanthanum trifluoromethanesulfonate, the desired 2-position ester was generated with greater than 95:5 regioselectivity. This methodology was also applied to 6-methyl-[2,3]-quinoline to provide similar results.
AZABICYCLO [4.1.0] HEPT - 4 - YL DERIVATIVES AS HUMAN OREXIN RECEPTOR ANTAGONISTS
-
Page/Page column 41, (2012/07/14)
This invention relates to azabicyclo[4.1.0]hept-4-yl derivatives and their use as pharmaceuticals.
NOVEL COMPOUNDS WITH A 3A-AZABICYCLO [4.1.0] HEPTANE CORE ACTING ON OREXIN RECEPTORS
-
Page/Page column 50, (2012/07/14)
This invention relates to azabicyclo[4.1.0]hept-4-yl derivatives and their use as pharmaceuticals.
5-METHYL-PIPERIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SLEEP DISORDER
-
Page/Page column 26-27, (2011/04/14)
This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals.
NOVEL COMPOUNDS
-
Page/Page column 26, (2010/06/19)
Disclosed are N-{[(1R,4S,6R)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
PIPERIDINE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS
-
Page/Page column 44, (2010/07/09)
This invention relates to imidazopyridylmethylene substituted piperidine derivatives orexin antagonists and their use as pharmaceuticals.
3 -AZABICYCLO [4.1.0] HEPTANES USED AS OREXIN ANTAGONISTS
-
Page/Page column 41, (2010/11/05)
This invention relates to 3-azabicyclo[4.1.0] heptane derivatives (I) and their use as orexin receptor antagonists.
N-{[(IR,4S,6R-3-(2-PYRIDINYLCARBONYL)-3-AZABICYCLO [4.1.0] HEPT-4-YL] METHYL}-2-HETEROARYLAMINE DERIVATIVES AND USES THEREOF
-
Page/Page column 38; 39, (2010/06/20)
This invention relates to N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
