213532-95-7Relevant articles and documents
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists
Elworthy, Todd R.,Brill, Emma R.,Caires, Christopher C.,Kim, Woongki,Lach, Leang K.,Tracy, Jahari Laurant,Chiou, San-San
, p. 2523 - 2526 (2007/10/03)
2-Piperidones were prepared bearing heptanoic acid or a thioether heptanoic acid at the 1-position as well as appropriately substituted at the 6-position to mimic the structure of prostaglandins. The stereochemical purity at the 6-position was determined to be ≥95% ee for an advanced synthetic intermediate. The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. They displayed a high affinity (K i 5-130 nM) at EP4 and subtype selectivity.
EP4 receptor agonist, compositions and methods thereof
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Page/Page column 11, (2010/02/08)
This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.