19786-58-4Relevant articles and documents
Discovery of β-Arrestin Biased Ligands of 5-HT7R
Kim, Youngjae,Kim, Hyunguk,Lee, Jieon,Lee, Jae Kyun,Min, Sun-Joon,Seong, Jihye,Rhim, Hyewhon,Tae, Jinsung,Lee, Hyunjoo Jenny,Choo, Hyunah
, p. 7218 - 7233 (2018/08/01)
Though many studies have been published about therapeutic potentials of selective 5-HT7R ligands, there have been few biased ligands of 5-HT7R. The development of potent and selective biased ligands of 5-HT7R would be of great help in understanding the relationship between pharmacological effects and G protein/β-arrestin signaling pathways of 5-HT7R. In order to identify 5-HT7R ligands with biased agonism, we designed and synthesized a series of tetrahydroazepine derivatives 1 and 2 with arylpyrazolo moiety or arylisoxazolo moiety. Through several biological evaluations such as binding affinity, selectivity profile, and functions in G protein and β-arrestin signaling pathways, 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine 1g was discovered as the β-arrestin biased ligand of 5-HT7R. In an electroencephalogram (EEG) test, 1g increased total non-rapid eye movement (NREM) sleep time and decreased total rapid eye movement (REM) sleep time.
The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors
Neelamkavil, Santhosh F.,Boyle, Craig D.,Chackalamannil, Samuel,Greenlee, William J.,Zhang, Lili,Terracina, Giuseppe
scheme or table, p. 4563 - 4565 (2010/04/05)
Discovery of a series of azepine sulfonamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has
Pentacyclic kinase inhibitors
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Page/Page column 54, (2010/11/25)
The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.