On February 21, 2013, Dineen, Thomas; Marx, Isaac E.; Nguyen, Hanh Nho; Weiss, Matthew published a patent.Recommanded Product: 5-Bromo-2-iodobenzotrifluoride The title of the patent was Preparation of indolesulfoamide derivatives as sodium channel inhibitors useful in the treatment of pain disorders. And the patent contained the following:
The invention relates to indolesulfoamide derivatives of formula I and II; pharmaceutical composition containing them; and their preparation and use as sodium channel inhibitors for the treatment of pain disorders. Indolesulfoamide derivatives of formula I and II, wherein X1, X2 and X3 are independently CH, Chalo, CC1-6 alkyl, COC1-6 alkyl, CCN and N; R1 is (un)substituted 5- and 6-membered (hetero)aryl and (hetero)cycloalkyl; R2 is (un)substituted 5- to 10-membered (hetero)cycloalkyl and (hetero)aryl; R3 is H, C1-6 alkyl, COC1-6 alkyl, CO2C1-6 alkyl and SO2C1-6 alkyl; R4 is H and C1-6 alkyl; and their pharmaceutically acceptable salt, are claimed. Example compound III was prepared by cross coupling of 3-bromo-N-(2,4-dimethoxybenzyl)-N-(1,2,4-thiadiazol-5-yl)-1H-indole-6-sulfonamide with (4-chloro-2-(1-methyl-1H-pyrazol-5-yl)phenyl)boronic acid to afford 3-(4-chloro-2-(1-methyl-1H-pyrazol-5-yl)phenyl)-N-(2,4-dimethoxybenzyl)-N-(1,2,4-thiadiazol-5-yl)-1H-indole-6-sulfonamide, which underwent debenzylation to give compound III. All the example compounds were evaluated for their sodium channel inhibitory activity. From the assay, it was determined that example compound III exhibited IC50 value of 0.445 渭M and > 10.0 渭M against Nav 1.7 and Nav 1.5 resp. The experimental process involved the reaction of 5-Bromo-2-iodobenzotrifluoride(cas: 364-12-5).Recommanded Product: 5-Bromo-2-iodobenzotrifluoride
The Article related to indolesulfoamide preparation sodium channel inhibitor treatment pain, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 5-Bromo-2-iodobenzotrifluoride
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com