883106-51-2

Upstream product

• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 1392490-93-5 [1-(4-nitrobenzenesulfonyl)piperidin-4-yl]carbamic acid tert-butyl ester 
• 98-74-8 4-Nitrobenzenesulfonyl chloride 

Downstream Products

• 1392490-94-6 N-[1-(4-nitrobenzenesulfonyl)piperidin-4-yl]acrylamide 
• 1392490-95-7 N-[1-(4-aminobenzenesulfonyl)piperidin-4-yl]acrylamide 
• 1392490-56-0 [4-(4-Acryloylamino-piperidine-1-sulfonyl)-phenyl]carbamic acid benzyl ester 
• 1414967-80-8 N-{1-[4-(Isoquinolin-3-ylamino)-benzenesulfonyl]-piperidin-4-yl}-acrylamide 

Relevant academic research and scientific papers

Structure-based design of benzo[e]isoindole-1,3-dione derivatives as selective GSK-3β inhibitors to activate Wnt/β-catenin pathway

Deregulation of Wnt/β-catenin pathway is closely related to the pathogenesis of neurodegenerative diseases such as Alzheimer's disease (AD), and glycogen synthase kinase 3β (GSK-3β), the central negative regulator of Wnt pathway, is regarded as an important target for these diseases. Here, we report a series of benzo[e]isoindole-1,3-dione derivatives as selective GSK-3β inhibitors by rational-design and synthesis, which show high selectivity against GSK-3β over Cyclin-dependent kinase 2 (CDK2), and significantly activate the cellular Wnt/β-catenin pathway. The structure-activity relationship of these GSK-3β inhibitors was also explored by in silico molecular docking.

Irreversible 4-aminopiperidine transglutaminase 2 inhibitors for Huntington's disease

A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure-activity relationship of this new series and report on the transglutaminase selectivity and in vitro ADME properties of selected compounds. We demonstrate that the compounds do not conjugate glutathione in an in vitro setting and have superior plasma stability over our previous series.

TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.