[EN] PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES [FR] DÉRIVÉS DE PYRIDOPYRAZINONE COMME STIMULATEURS DE LA SÉCRÉTION D'INSULINE, LEURS PROCÉDÉS D'OBTENTION ET LEUR UTILISATION POUR LE TRAITEMENT DU DIABÈTE
N-(cyclopropylmethyl)-3-nitropyridin-2-amine 在
钯氢气 作用下,
以
甲醇 为溶剂,
反应 3.0h,
以to give 3.1 g of N2-(cyclopropylmethyl)pyridine-2,3-diamine as a solid的产率得到N2-(cyclopropylmethyl)pyridine-2,3-diamine
参考文献:
名称:
PYRIDOPYRAZINONES DERIVATIVES INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES
Pyridopyrazinones derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
申请人:Merck Patent Gesellschaft MIT Beschraenkter Haftung
公开号:US08178556B2
公开(公告)日:2012-05-15
Described are pyridopyrazinone derivatives of formula (I),
wherein X, Y, Z, W, A and R1 are as defined in claim 1, as insulin secretion stimulators. Also described is the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
Imidazopyridines: A novel class of hNav1.7 channel blockers
作者:Clare London、Scott B. Hoyt、William H. Parsons、Brande S. Williams、Vivien A. Warren、Richard Tschirret-Guth、McHardy M. Smith、Birgit T. Priest、Erin McGowan、William J. Martin、Kathryn A. Lyons、Xiaohua Li、Bindhu V. Karanam、Nina Jochnowitz、Maria L. Garcia、John P. Felix、Brian Dean、Catherine Abbadie、Gregory J. Kaczorowski、Joseph L. Duffy
DOI:10.1016/j.bmcl.2008.01.047
日期:2008.3
A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4 h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10 mg/kg. (C) 2008 Elsevier Ltd. All rights reserved.