13791-03-2Relevant 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
scheme or table, 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 phenyl naphthalenes as estrogenic agents
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, (2008/06/13)
This invention provides estrogen receptor modulators of formula I, having the structure 1wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Fluoronaphthylones
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, (2008/06/13)
4-(6-Substituted naphthyl)butan-2-ols,-butan-2-ones,-pentan-2-ols and -pentan-2-ones bearing a fluoro group in the naphthyl ring, and pro-drugs thereof, are anti-inflammatory agents. A typical embodiment is 4-(4-fluoro-6-methoxy-2-naphthyl)-butan-2-one.