152665-68-4

Upstream product

• 52423-62-8 1-bromo-2-cyclopentyl-2-oxoethane 
• 108895-98-3 benzyl 2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-ylcarbamate 
• 2835-77-0 (2-aminophenyl)(phenyl)methanone 
• 161365-74-8 benzyl N-[[(2-benzoylphenyl)carbamoyl](1H-1,2,3-benzotriazol-1-yl)methyl]carbamate 
• 124676-19-3 2-(benzotriazol-1-yl)-N-(benzyloxycarbonyl)glycine 

Downstream Products

• 155488-19-0 (R)-3-Amino-1-(2-cyclopentyl-2-oxo-ethyl)-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 
• 150007-40-2 3-Amino-1-(2-cyclopentyl-2-oxo-ethyl)-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one 

Relevant academic research and scientific papers

Synthesis and biological activity of 5-heteroaryl benzodiazepines: Analogues of YM022

A novel series of analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared which incorporate 5- and 6-membered heteroaromatic rings in the benzodiazepine 5-position. The 5-(2-pyridyl) derivatives in particular retained good in vitro and in vivo potency and one such compound 9i was shown to inhibit acid secretion after oral dosing in dogs. Improved bioavailability for 9i over the 5-phenyl analogue, 9h was demonstrated in rats.

Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

A novel series of 1-alkylcarbonylmethyl analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared. A number of analogues retained good affinity for the gastrin/CCK-B receptor and one compound (6d) showed improved binding and enhanced selectivity for this receptor over CCK-A. A second compound (6j) gave improved in vivo inhibition of gastric acid secretion in rats. Both analogues were shown to have significantly better activity in the same model following i.d. dosing than either YM022 or L-365,260.