112106-91-9Relevant articles and documents
HETEROBICYCLIC AMIDES AS INHIBITORS OF CD38
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Paragraph 0650, (2021/02/05)
The present invention relates to heterobicyclic amides and related compounds which are inhibitors of CD38 and are useful in the treatment of cancer.
A Continuous Flow Strategy for the Facile Synthesis and Elaboration of Semi-Saturated Heterobicyclic Fragments
Luise, Nicola,Wyatt, Eleanor W.,Tarver, Gary J.,Wyatt, Paul G.
, p. 1341 - 1349 (2019/01/14)
An efficient hydrogenation protocol under continuous flow conditions was developed for the synthesis of underrepresented semi-saturated bicyclic fragments containing highly sp3-rich skeletons for fragment-based drug discovery (FBDD) programs. Excellent yields were generally achieved by using Pd/C (10 % w/w) and RaNi at 25–150 °C under 4–100 bar of hydrogen pressure. The generated fragments, with appropriate physicochemical properties, present diverse hydrogen-bonding pharmacophores and useful vectors for their synthetic elaboration in the optimization stage. Successive, simple functionalizations in continuous flow were accomplished to demonstrate the opportunity to develop multi-step continuous flow synthesis of valuable starting points for FBDD campaigns. A conclusive quality control (QC) was essential to discard those structures which do not fit the typical fragment library parameters.
A novel series of potent and selective EP4 receptor ligands: Facile modulation of agonism and antagonism
Boyd, Michael J.,Berthelette, Carl,Chiasson, Jean-Franois,Clark, Patsy,Colucci, John,Denis, Danielle,Han, Yongxin,Lévesque, Jean-Francois,Mathieu, Marie-Claude,Stocco, Rino,Therien, Alex,Rowland, Steve,Wrona, Mark,Xu, Daigen
scheme or table, p. 484 - 487 (2011/02/27)
A novel series of EP4 ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic