39216-68-7Relevant articles and documents
Ligand based design of novel histamine H4 receptor antagonists; Fragment optimization and analysis of binding kinetics
Smits, Rogier A.,Lim, Herman D.,Van Der Meer, Tiffany,Kuhne, Sebastiaan,Bessembinder, Karin,Zuiderveld, Obbe P.,Wijtmans, Maikel,De Esch, Iwan J.P.,Leurs, Rob
, p. 461 - 467 (2012/02/04)
The histamine H4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl) quinazolin-2-amine (VUF11489), as a new H4R antagonist. Analysis of its binding kinetics at the human H4R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.
Novel norepinephrine reuptake inhibitors for the treatment of central nervous system disorders
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Page/Page column 33, (2010/02/11)
This invention relates to compounds of the formula 1 wherein R1, R2, and R3 and R4 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.
Synthesis and bioactivities of novel piperidylpyrimidine derivatives: Inhibitors of tumor necrosis factor-alpha production
Fujiwara, Norio,Fujita, Hitoshi,Iwai, Kiyotaka,Kurimoto, Ayumu,Murata, Shinobu,Kawakami, Hajime
, p. 1317 - 1320 (2007/10/03)
New piperidylpyrimidine derivatives, including quinazolines, were prepared, and their abilities to inhibit TNF-α production evaluated. Some compounds showed potent inhibitory activity in mouse macrophages stimulated with LPS. The synthesis and structure-activity relationships of these compounds are described. (C) 2000 Elsevier Science Ltd. All rights reserved.