888952-52-1Relevant articles and documents
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain
Frost, Jennifer M.,Degoey, David A.,Shi, Lei,Gum, Rebecca J.,Fricano, Meagan M.,Lundgaard, Greta L.,El-Kouhen, Odile F.,Hsieh, Gin C.,Neelands, Torben,Matulenko, Mark A.,Daanen, Jerome F.,Pai, Madhavi,Ghoreishi-Haack, Nayereh,Zhan, Cenchen,Zhang, Xu-Feng,Kort, Michael E.
, p. 3373 - 3391 (2016/05/19)
The genetic validation for the role of the Nav1.7 voltage-gated ion channel in pain signaling pathways makes it an appealing target for the potential development of new pain drugs. The utility of nonselective Nav blockers is often li
The synthesis of (S)-5-fluoro-1-(2-fluorophenyl)-3-(piperidin-3-ylmethoxy)- 1H-indazole, a norepinephrine/serotonin reuptake inhibitor for the treatment of fibromyalgia
Magano, Javier,Waldo, Michael,Greene, Derek,Nord, Eric
, p. 877 - 883 (2013/01/03)
Compound 1, a norepinephrine/serotonin reuptake inhibitor (NSRI) for the treatment of fibromyalgia, has been synthesized in optically pure form in six linear steps and 48% overall yield with no chromatography. This route features a novel and efficient intramolecular cyclization to generate the indazolone core via a diazotization reaction and the preparation of a stable polymorph of the tartaric acid salt as the desired final form. The original synthetic route has been modified to avoid the use of toxic and expensive reagents, thus enabling the preparation of multigram quantities of API for toxicology studies.