892549-58-5Relevant articles and documents
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
Giroux, Andre,Boulet, Louise,Brideau, Christine,Chau, Anh,Claveau, David,Cote, Bernard,Ethier, Diane,Frenette, Richard,Gagnon, Marc,Guay, Jocelyne,Guiral, Sebastien,Mancini, Joseph,Martins, Evelyn,Masse, Frederic,Methot, Nathalie,Riendeau, Denis,Rubin, Joel,Xu, Daigen,Yu, Hongping,Ducharme, Yves,Friesen, Richard W.
scheme or table, p. 5837 - 5841 (2010/04/28)
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human whole blood IC50 of 0.20 and 0.14 μM, respectively. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model at oral doses as low as 14 mg/kg. Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development. Crown Copyright
2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS
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Page/Page column 68-69, (2008/06/13)
The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed
METHODS FOR TREATING OR PREVENTING NEOPLASIAS
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Page/Page column 47, (2008/06/13)
The present invention is directed to a method for treating or preventing a neoplasia in a human patient in need of such treatment comprising administering to the patient a compound that inhibits microsomal prostaglandin E synthase-1 in an amount that is effective for treating or preventing the neoplasia.