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.
IMMUNOMODULATORY COMPOUNDS
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Paragraph 0291-0293, (2020/01/24)
Disclosed are immunomodulatory compounds, pharmaceutical compositions containing them, and methods of making and using the compounds to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.
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.
PYRIMIDO-DIAZEPINONE COMPOUNDS AND METHODS OF TREATING DISORDERS
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, (2016/02/16)
The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1,2,3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK,
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
A SIMPLE SYNTHESIS OF 7-SUBSTITUTED 1-ACETYL-2,3-DIHYDROINDOLES
Somei, Masanori,Kawasaki, Toshiya,Ohta, Toshiharu
, p. 2363 - 2366 (2007/10/02)
7-Cyano-, 7-hydroxy-, 7-methoxycarbonyl-, 7-methyl-, 7-nitro-, and 7-phenyl-1-acetyl-2,3-dihydroindoles are prepared in two steps (or one pot) from 1-acetyl-2,3-dihydroindole.
Cyclic carbamates and fungicidal use
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, (2008/06/13)
Fungicidally active cyclic carbamates of the formula STR1 in which X and Y each represent oxygen or sulfur, Z represents hydrogen, halogen, alkyl or nitro, and n is 2 or 3. Some intermediates are new.