1151833-03-2

Upstream product

• 1151832-34-6 ethyl 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxylate 
• 1151833-59-8 ethyl 4-(4-oxotetrahydro-2H-thiopyran-3-carboxamido)benzoate 
• 17766-28-8 cyclohexylpiperazine 
• 1151832-35-7 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxylic acid 

Relevant academic research and scientific papers

Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)

A series of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxamide derivatives, were successfully synthesized and their PARP-1 inhibitory activity was evaluated. These compounds were prepared from carboxylic acid 7 and the appropriate amines, and a number of the synthesized compounds were found to have significant PARP-1 activity. Among them, 9m showed potent activity in a PARP-1 enzymatic assay and cell-based assay (IC50 = 0.045 μM, ED 50 = 0.54 μM). Molecular modeling studies confirmed the obtained biological results. Springer Science+Business Media, LLC 2011.

NOVEL TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to novel tricyclic derivatives having an excellent inhibitory activity on poly (ADP-ribose) polymerase, or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The tricyclic derivatives of the present invention inhibit the activity of poly (ADP-ribose) polymerase, thereby being used for the prevention or treatment of diseases that are caused by excessive activation of PARP, in particular, neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic neuropathic pain, inflammatory diseases, osteoporosis, and cancer.