916504-92-2Relevant academic research and scientific papers
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists
McDonald, Iain M.,Austin, Carol,Buck, Ildiko M.,Dunstone, David J.,Gaffen, John,Griffin, Eric,Harper, Elaine A.,Hull, Robert A. D.,Kalindjian, S. Barret,Linney, Ian D.,Low, Caroline M. R.,Patel, Dipa,Pether, Michael J.,Raynor, Michelle,Roberts, Sonia P.,Shaxted, Mark E.,Spencer, John,Steel, Katherine I. M.,Sykes, David A.,Wright, Paul T.,Xun, Wei
, p. 4789 - 4792 (2008/03/13)
A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.
BENZOTRIAZEPINONE DERIVATIVES
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, (2010/11/25)
The present invention is concerned with benzotriazepinone derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-l or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.
