[摘要]:Synthesis and structure-activity relationship (SAR) studies on 5-trifluoromethylpyrido[4,3-d] pyrimidin-4(3H)-ones, a novel class of calcium receptor antagonists is described with particular emphasis on optimization of the pharmacokinetic/pharmacodynamic parameters required for a short duration of action compound. Orally-active compounds were identified which displayed the desired animal pharmacology (rapid and transient stimulation of parathyroid hormone) essential for bone anabolic effects. (C) 2009 Elsevier Ltd. All rights reserved.