627526-70-9Relevant articles and documents
Novel 3-oxazolidinedione-6-aryl-pyridinones as potent, selective, and orally active EP3 receptor antagonists
Jin, Jian,Morales-Ramos, Angel,Eidam, Patrick,Mecom, John,Li, Yue,Brooks, Carl,Hilfiker, Mark,Zhang, David,Wang, Ning,Shi, Dongchuan,Tseng, Pei-San,Wheless, Karen,Budzik, Brian,Evans, Karen,Jaworski, Jon-Paul,Jugus, Jack,Leon, Lisa,Wu, Charlene,Pullen, Mark,Karamshi, Bhumika,Rao, Parvathi,Ward, Emma,Laping, Nicholas,Evans, Christopher,Leach, Colin,Holt, Dennis,Su, Xin,Morrow, Dwight,Fries, Harvey,Thorneloe, Kevin,Edwards, Richard
, p. 316 - 320 (2010/11/18)
High-throughput screening and subsequent optimization led to the discovery of novel 3-oxazolidinedione-6-aryl-pyridinones exemplified by compound 2 as potent and selective EP3 antagonists with excellent pharmacokinetic properties. Compound 2 was orally active and showed robust in vivo activities in overactive bladder models. To address potential bioactivation liabilities of compound 2, further optimization resulted in compounds 9 and 10, which maintained excellent potency, selectivity, and pharmacokinetic properties and showed no bioactivation liability in glutathione trapping studies. These highly potent, selective, and orally active EP3 antagonists are excellent tool compounds for investigating and validating potential therapeutic benefits from selectively inhibiting the EP3 receptor.
Substituted imidazol-pyridazine derivatives
-
Page 20, (2010/02/05)
The present invention relates to compounds of formula wherein A is an unsubstituted or substituted cyclic group; and R is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.
