- Discovery of orally available 8-aza-5-thiaProstaglandin E1 analogs as highly selective EP4 agonists
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Analogs 8-aza-16-aryl prostaglandin E1 (PGE1) and 8-aza-5-thia-16-arylPGE1 were synthesized and evaluated with respect to their subtype receptor affinity and EP4 agonist activity for the purposes of identifying sub-type- selective EP
- Kambe, Tohru,Maruyama, Toru,Nakano, Masayuki,Yamaura, Yoshiyuki,Shono, Tomoyuki,Seki, Akiteru,Sakata, Kiyoto,Maruyama, Takayuki,Nakai, Hisao,Toda, Masaaki
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p. 1523 - 1534
(2012/01/13)
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- EP4 receptor selective agonists in the treatment of osteoporosis
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This invention is 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 comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists. This invention is especially directed to those methods wherein the EP4 receptor selective agonist is a compound of Formula I: wherein the variables are as defined in the specification.
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