56441-84-0Relevant 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
PYRAZINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
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Page/Page column 68, (2010/06/15)
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.
Hypolipidemic analogues of ethyl 4 benzyloxybenzoate
Baggaley,Fears,Hindley,Morgan,Murrell,Thorne
, p. 1388 - 1393 (2007/10/05)
A series of compounds related to ethyl 4-benzyloxybenzoate was synthesized and evaluated for potential hypolipidemic activity in rats. Structure-activity relationships are discussed in terms of cholesterol-lowering activity together with effects on body weight gain and liver lipids. A number of the compounds inhibited cholesterol and free fatty acid biosynthesis from [1-14C]acetate in rat liver slices in vitro. Ethyl 4-benzyloxybenzoate, ethyl 4-benzyloxybenzoic acid, ethyl 4-p-bromobenzyloxybenzoate, and ethyl 4-o-methoxybenzyloxyphenyl acetate exhibited the most favorable spectrum of activity.
