- NON-STEROIDAL SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTIC MODULATORS (SEGRAMs) AND USES THEREOF
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The present invention relates to the two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated
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- Discovery of quinolines as selective glucocorticoid receptor agonists
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The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respec
- Jaroch, Stefan,Berger, Markus,Huwe, Christoph,Krolikiewicz, Konrad,Rehwinkel, Hartmut,Sch?cke, Heike,Schmees, Norbert,Skuballa, Werner
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scheme or table
p. 5835 - 5838
(2010/11/19)
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- Identification of dissociated non-steroidal glucocorticoid receptor agonists
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A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To iden
- Kuzmich, Daniel,Kirrane, Tom,Proudfoot, John,Bekkali, Younes,Zindell, Renee,Beck, Laura,Nelson, Richard,Shih, Cheng-Kon,Kukulka, Alison J.,Paw, Zofia,Reilly, Patty,Deleon, Rodney,Cardozo, Mario,Nabozny, Gerald,Thomson, David
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p. 5025 - 5031
(2008/02/11)
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- 1-PROPANOL AND 1-PROPYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANDS
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Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page 144-147
(2008/06/13)
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- Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7,and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceu
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- Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceu
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- GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocortic
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- GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate,or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 107-108
(2010/02/07)
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- 4-(ARYL OR HETEROARYL) -2-BUTYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANS
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A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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