- NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES
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[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
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Page/Page column 30
(2010/01/29)
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- Trifluoromethyl group as a pharmacophore: Effect of replacing a CF 3 group on binding and agonist activity of a glucocorticoid receptor ligand
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Compound 1, a potent glucocorticoid receptor ligand, contains a quaternary carbon bearing trifluoromethyl and hydroxyl groups. This paper describes the effect of replacing the trifluoromethyl group on binding and agonist activity of the GR ligand 1. The r
- Betageri, Raj,Zhang, Yan,Zindell, Renee M.,Kuzmich, Daniel,Kirrane, Thomas M.,Bentzien, Joerg,Cardozo, Mario,Capolino, Alison J.,Fadra, Tazmeen N.,Nelson, Richard M.,Paw, Zofia,Shih, Daw-Tsun,Shih, Cheng-Kon,Zuvela-Jelaska, Ljiljana,Nabozny, Gerald,Thomson, David S.
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p. 4761 - 4769
(2007/10/03)
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- Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof
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A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds,
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