C07D277/40

BENZENE SULFONAMIDE THIAZOLE COMPOUNDS AND THEIR USE FOR THE TREATMENT OF CANCERS
20250353821 · 2025-11-20 ·

The present inventors have shown that specific benzene sulfonamide thiazole compounds (I) have the ability to induce an early endoplasmic reticulum stress. These compounds also lead to cancerous cells growth inhibition and death.

##STR00001##

NOVEL INHIBITORS

Compounds of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is monocyclic and bicyclic heteroaryl; B is alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl, or alkylene; D is aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine, or sulfamoyl; and E is aryl, heteroaryl, cycloalkyl, or heterocyclyl.

These compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

NOVEL INHIBITORS

Compounds of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is monocyclic and bicyclic heteroaryl; B is alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl, or alkylene; D is aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine, or sulfamoyl; and E is aryl, heteroaryl, cycloalkyl, or heterocyclyl.

These compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).