384832-33-1

Upstream product

• 180340-57-2 5,6,7,8-tetra-hydro-4H-thieno[3,2-b]azepine 
• 1160759-52-3 4-cyano-3-methylbenzoyl chloride 
• 73831-13-7 4-cyano-3-methylbenzoic acid 

Downstream Products

• 384832-34-2 4-(4-Aminomethyl-3-methylbenzoyl)-5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine 

Relevant academic research and scientific papers

benzamide derivatives as oxytocin agonists and vasopressin antagonists

Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or Via receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Fused azepine derivatives and their use as antidiuretic agents

Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Non-peptide oxytocin agonists

The first non-peptide, low molecular weight agonists of the hormone oxytocin (OT) are reported. The most potent compound, 39, showed an EC 50 = 33 nM and was selective for the OT receptor. A library of compounds targeted to the vasopressin/oxytocin family of receptors was screened for activity at a cloned human oxytocin receptor using a reporter gene assay. Potency and selectivity were optimised to afford compound 39, EC50 = 33 nM. This series of compounds represents the first disclosed, non-peptide, low molecular weight agonists of the hormone oxytocin (OT).