128102-80-7Relevant articles and documents
Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β
Wang, Yikai,Wach, Jean-Yves,Sheehan, Patrick,Zhong, Cheng,Zhan, Chenyang,Harris, Richard,Almo, Steven C.,Bishop, Joshua,Haggarty, Stephen J.,Ramek, Alexander,Berry, Kayla N.,O'Herin, Conor,Koehler, Angela N.,Hung, Alvin W.,Young, Damian W.
, p. 852 - 856 (2016/10/12)
Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based on diversity-oriented synthesis (DOS). A DOS-based fragment collection was able to produce initial hit compounds against the target GSK3β, allow the systematic synthesis of related fragment analogues to explore fragment-level structure-activity relationship, and finally lead to the synthesis of a more potent compound.
4-METHYL-2,3,5,9,9B-PENTAAZA-CYCLOPENTA[A]NAPHTHALENES
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Page/Page column 94-95, (2014/02/16)
The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
PYRIDINE COMPOUNDS AND USES THEREOF
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Page/Page column 18, (2013/03/26)
The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psych