1227174-96-0Relevant articles and documents
Discovery of clinical candidate 1-(4-(3-(4-(1 H-benzo[ d ]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A)
Hu, Essa,Chen, Ning,Bourbeau, Matthew P.,Harrington, Paul E.,Biswas, Kaustav,Kunz, Roxanne K.,Andrews, Kristin L.,Chmait, Samer,Zhao, Xiaoning,Davis, Carl,Ma, Ji,Shi, Jianxia,Lester-Zeiner, Dianna,Danao, Jean,Able, Jessica,Cueva, Madelyn,Talreja, Santosh,Kornecook, Thomas,Chen, Hang,Porter, Amy,Hungate, Randall,Treanor, James,Allen, Jennifer R.
, p. 6632 - 6641 (2014/10/15)
We report the identification of a PDE10A clinical candidate by optimizing potency and in vivo efficacy of promising keto-benzimidazole leads 1 and 2. Significant increase in biochemical potency was observed when the saturated rings on morpholine 1 and N-a