The Article related to benzenesulfonamide preparation trap1 modulator, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 1014631-89-0
On September 23, 2021, Holson, Edward; Blum, Charles published a patent.Electric Literature of 1014631-89-0 The title of the patent was Preparation of benzenesulfonamide derivatives as TRAP1 modulators and uses thereof. And the patent contained the following:
The disclosure provides compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“”TNF””) receptor associated protein 1 (“”TRAP1″”) modulators (e.g., TRAP1 activators). The provided compounds of formula I may also rescue the activity in PTEN-induced kinase 1 (“”PINK1″”) loss of function contexts. The provided compounds of formula I may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds of formula I may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof). Compounds of formula I wherein A and E are independently aryl and heteroaryl; dashed bonds are single and double bonds are valency permits; m is 0, 1 and 2; n and p are independently 0 – 13; each R1 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; R3 and R6 are independently H, (un)substituted alkyl and nitrogen protecting group; R1R3 may be taken together to form (un)substituted heterocyclyl; each R4 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted aryl, etc.; R5 and R9 are independently H, halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; each R7 is independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted aryl, etc.; and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of oxazole-5-carboxylic acid with 5-amino-N-(4-bromophenyl)-2-methoxybenzenesulfonamide. The invention compounds were evaluated for their TRAP1 modulatory activity. From the assay, it was determined that compound II exhibited an EC50 value in the range of 20μM to 100μM and an Emax value in the range of 160 – 199%. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Electric Literature of 1014631-89-0
The Article related to benzenesulfonamide preparation trap1 modulator, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 1014631-89-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics