Compounds of Formula I are provided.
In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
[EN] Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CBl activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CBl modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such Iigands for receptor localization studies and various in vitro assays. [FR] L'invention concerne des composés de formule (I). Dans ces formules, les variantes sont telles que décrites dans la description. Ces composés peuvent être utilisés afin de moduler l'activité in vivo ou in vitro de CB1, et sont particulièrement utiles dans le traitement de troubles réagissant à la modulation CB1 chez les humains, les animaux de compagnie domestiqués et le bétail, notamment les troubles de l'appétit, l'obésité et les troubles de dépendance. L'invention concerne également des compositions pharmaceutiques et des procédés d'utilisation de celles-ci afin de traiter ces troubles, ainsi que des procédés d'utilisation de ses ligands dans des études de localisation de récepteur et divers dosages in vitro.
YbCl3-catalyzed one-pot synthesis of dihydropyrazines, piperazines, and pyrazines
作者:Liyan Fan、Wen Chen、Changtao Qian
DOI:10.1016/j.tetlet.2012.11.005
日期:2013.1
A simple and efficient synthetic approach to dihydropyrazines via YbCl3-catalyzed reaction of α-hydroxyketones with diamines under mild conditions was developed. The corresponding 2,3-subsitituted piperazines and pyrazines were obtained through tandem conversion of dihydropyrazines with good yields.