- 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)
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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
- 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.
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p. 6632 - 6641
(2014/10/15)
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- PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
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Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 201
(2010/06/15)
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