[EN] FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY [FR] DÉRIVÉS DE [1,2,4]THIADIAZINE FUSIONNÉS AGISSANT EN TANT QU'INHIBITEURS DE KAT DE LA FAMILLE DES MYST
Rapid Synthesis of Bicyclic N-Heterocyclic Cores from N-Terminal α,β-Unsaturated Diazoketones
作者:João Victor Santiago、Antonio C. B. Burtoloso
DOI:10.1002/ejoc.201800239
日期:2018.6.15
The synthesis of bicyclic N‐heterocyclic cores from N‐terminal α,β‐unsaturated diazoketones is described. The transformation consists of a three‐step domino process that involves a one‐pot N‐deprotection, intramolecular aza‐Michael, and photochemical Wolff rearrangement sequence of reactions.
The present invention relates to a novel process suitable for large-scale production of phenyl propane derivatives as well as to novel intermediates in the process.
本发明涉及一种适用于苯丙烷衍生物大规模生产的新工艺,以及在该过程中的新中间体。
[EN] DIAMINO-ALKYLAMINO-LINKED ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS<br/>[FR] COMPOSÉS D'ARYLSULFONAMIDE À LIAISONS DIAMINO-ALKYLAMINO PRÉSENTANT UNE ACTIVITÉ SÉLECTIVE DANS LES CANAUX SODIQUES SENSIBLES À LA TENSION
申请人:MERCK SHARP & DOHME
公开号:WO2018093694A1
公开(公告)日:2018-05-24
Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.