802916-68-3Relevant academic research and scientific papers
Discovery and structure-activity relationships of trisubstituted pyrimidines/pyridines as novel calcium-sensing receptor antagonists
Yang, Wu,Ruan, Zheming,Wang, Yufeng,Van Kirk, Katy,Zhengping, Ma.,Arey, Brian J.,Cooper, Christopher B.,Seethala, Ramakrishna,Feyen, Jean H. M.,Dickson Jr., John K.
supporting information; experimental part, p. 1204 - 1208 (2009/12/25)
The trisubstituted pyrimidine 1 was identified through high-throughput screening as a novel calcium-sensing receptor (CaSR) antagonist. Small molecule CaSR antagonists and/or negative allosteric modulators have the potential to act as an anabolic agent for the treatment of osteoporosis. The investigation of structure-activity relationships around 1 resulted in the identification of 18c and 18d, which showed efficacy at promoting PTH release in vivo and exhibited improved potency and solubility over the original lead 1.
TRISUBSTITUTED HETEROAROMATIC COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS
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Page 60, (2010/02/09)
Trisubstituted heteroaromatic compounds having the structure Formula (I) are provided, wherein X is C or N; A and B are each independently CH or N, with the proviso that A and B cannot both be CH; R is Ar-L-; R is hydrogen or alkyl; or R and R can be joined together to form a 4- to 7-membered cycloheteroalkyl ring; R to R, Ar and L are as defined herein. A method for using these compounds to treat diseases associated with abnormal bone or mineral homeostasis is also provided.
