- 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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Page/Page column 78; 79; 80
(2019/05/15)
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- Non-steroidal dissociated glucocorticoid agonists: Indoles as A-ring mimetics and function-regulating pharmacophores
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We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (R)-33 which showed high PR and MR selectivity, potent agonist activity, and reduced transactivation activity in the MMTV and aromatase assays. The compound is equipotent to prednisolone in the LPS-TNF model of inflammation. In mouse CIA, at 30 mg/kg compound (R)-33 inhibited disease progression with an efficacy similar to the 3 mg/kg dose of prednisolone.
- Betageri, Raj,Gilmore, Thomas,Kuzmich, Daniel,Kirrane, Thomas M.,Bentzien, J?rg,Wiedenmayer, Dieter,Bekkali, Younes,Regan, John,Berry, Angela,Latli, Bachir,Kukulka, Alison J.,Fadra, Tazmeen N.,Nelson, Richard M.,Goldrick, Susan,Zuvela-Jelaska, Ljiljana,Souza, Don,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Lee, Heewon,Pack, Edward,Harcken, Christian,Nabozny, Gerald,Thomson, David S.
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scheme or table
p. 6842 - 6851
(2011/12/22)
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- Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics
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Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene trans
- Riether, Doris,Harcken, Christian,Razavi, Hossein,Kuzmich, Daniel,Gilmore, Thomas,Bentzien, J?rg,Pack, Edward J.,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Nabozny, Gerald H.,Thomson, David S.
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experimental part
p. 6681 - 6698
(2010/12/19)
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- GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Compounds of Formula I wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, 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 62-63
(2009/12/28)
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- METHOD FOR PRODUCING OPTICALLY ACTIVE FLUORINE-CONTAINING CARBONYL-ENE PRODUCT
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An optically active, fluorine-containing carbonyl-ene product is produced by reacting a fluorine-containing α-ketoester with an alkene in the presence of a transition metal complex having an optically active ligand. There are Mode 1 of conducting this rea
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Page/Page column 18-19; 29-30
(2009/09/26)
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- Process for the manufacture of non-steroidal anti-inflammatory agents and intermediates thereof
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The current invention describes novel synthetic routes and intermediates for the manufacture of anti-inflammatory agents of general formula VIII in which one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which one of the groups Z1, Z2, Z3 is selected from -O-, -S-, -NH-, -N(-CH3)-, whereas the other groups Z1, Z2, Z3 have the meaning of a -CH2- group, and in which Ar is an aromatic group.
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Page/Page column 8
(2008/12/04)
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- NOVEL COMPOUNDS
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The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.
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Page/Page column 59-61
(2008/06/13)
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- 5-SUBSTITUTED QUINOLINE AND ISOQUINOLINE DERIVATIVES, A METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS ANTIPHLOGISTICS
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The invention relates to compounds of general formulas (IIa) or (IIb) and to their use as medicaments.
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Page/Page column 34-35
(2008/06/13)
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- 1,1,1-TRIFLUORO-4-PHENYL-4-METHYL-2-(1H-PYRROLO
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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), 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 195-196
(2010/02/11)
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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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- 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; pharmaceutical compositions containing such compounds, and methods of modulating the glucocortic
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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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- 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 106
(2010/02/07)
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- Nonsteroidal gestagens
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This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2and R3have the meanings that are indicated in more detail in the description. The new compounds show a very great affin
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Page column 16
(2010/11/29)
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