431990-03-3Relevant academic research and scientific papers
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats
Cameron, Kimberly O.,Lefker, Bruce A.,Chu-Moyer, Margaret Y.,Crawford, David T.,Jardine, Paul DaSilva,DeNinno, Shari L.,Gilbert, Sandra,Grasser, William A.,Ke, HuaZhu,Lu, Bihong,Owen, Thomas A.,Paralkar, Vishwas M.,Qi, Hong,Scott, Dennis O.,Thompson, David D.,Tjoa, Christina M.,Zawistoski, Michael P.
, p. 1799 - 1802 (2007/10/03)
Heptanoic acid lactams, exemplified by 2, were identified as highly selective EP4 agonists via high throughput screening. Lead optimization led to the identification of lactams with a 30-fold increase in EP4 potency in vitro. Compounds demonstrated robust
EP4 receptor selective agonists in the treatment of osteoporosis
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, (2008/06/13)
This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.
