1018678-55-1Relevant articles and documents
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists
Didiuk, Mary T.,Griffith, David A.,Benbow, John W.,Liu, Kevin K.C.,Walker, Daniel P.,Christopher Bi,Morris, Joel,Guzman-Perez, Angel,Gao, Hua,Bechle, Bruce M.,Kelley, Ryan M.,Yang, Xiaojing,Dirico, Kenneth,Ahmed, Syed,Hungerford, William,DiBrinno, Joseph,Zawistoski, Michael P.,Bagley, Scott W.,Li, Jianke,Zeng, Yuan,Santucci, Stephanie,Oliver, Robert,Corbett, Matthew,Olson, Thanh,Chen, Chiliu,Li, Mei,Paralkar, Vishwas M.,Riccardi, Keith A.,Healy, David R.,Kalgutkar, Amit S.,Maurer, Tristan S.,Nguyen, Hang T.,Frederick, Kosea S.
, p. 4555 - 4559 (2009)
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.
PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
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Page/Page column 24, (2008/06/13)
The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.
