56961-99-0Relevant articles and documents
Copper(0)/Selectfluor System-Promoted Oxidative Carbon-Carbon Bond Cleavage/Annulation of o-Aryl Chalcones: An Unexpected Synthesis of 9,10-Phenanthraquinone Derivatives
Bao, Hanyang,Xu, Zheng,Wu, Degui,Zhang, Haifeng,Jin, Hongwei,Liu, Yunkui
, p. 109 - 118 (2017/04/26)
A general and efficient protocol for the synthesis of 9,10-phenanthraquinone derivatives has been successfully developed involving a copper(0)/Selectfluor system-promoted oxidative carbon-carbon bond cleavage/annulation of o-aryl chalcones. A variety of substituted 9,10-phenanthraquinones were synthesized in moderate to good yields under mild reaction conditions.
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
Cote, Bernard,Boulet, Louise,Brideau, Christine,Claveau, David,Ethier, Diane,Frenette, Richard,Gagnon, Marc,Giroux, Andre,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.
, p. 6816 - 6820 (2008/04/03)
Phenanthrene imidazole 3 (MF63) has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor. This new series was developed by lead optimization of a hit from an internal HTS campaign. Compound 3 is significantly more potent than the previously reported indole carboxylic acid 1 with an A549 whole cell IC50 of 0.42 μM (50% FBS) and a human whole blood IC50 of 1.3 μM. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally dosed at 30 and 100 mg/kg.
2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS
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Page/Page column 38, (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
2-(PHENYL OR HETEROCYCLIC) - 1H-PHENANTHRO [9,10-D] IMIDAZOLES
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Page/Page column 56, (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 43, (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.
2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS
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Page/Page column 29, (2008/06/13)
The invention encompasses novel compounds of Formula I INSERT FORMULA I FROM CLAIM 1 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.