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US 7,741,361 B2Granted
Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AssigneeBoehringer Ingelheim Pharmaceuticals, Inc.
InventorsDaniel Kuzmich, Darren DiSalvo, John Robinson Regan, David S. Thomson
Life of this patent
Estimating the term…
Abstract
Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 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.
Claims8
A compound of Formula (I)
- wherein:
- R1 is hydrogen or C1-C3 alkyl, each optionally independently substituted with one to three substituent groups selected from hydroxy, halogen, or oxo;
- R2 is aryl independently substituted with one to five substituent groups,
- wherein each substituent group of R2 is independently C1-C5 alkyl, C2-C3 alkenyl, C2-C3 alkynyl, C1-C5 alkoxy, hydroxy, nitro, trifluoromethyl, trifluoromethoxy, halogen, cyano, acylamino, C1-C5 alkoxycarbonylamino, C1-C5 alkylsulfonylamino, C1-C5 alkylthio, amino wherein the nitrogen atom is optionally independently mono- or di-substituted by C1-C5 alkyl, or ureido wherein either nitrogen atom is optionally independently substituted with C1-C5 alkyl,
- wherein each substituent group of R2 is optionally independently substituted with C1-C3 alkyl, halogen, hydroxyl, or amino;
- R3 is C1-C8 alkyl independently substituted with one to five substituent groups,
- wherein each substituent group of R3 is independently C3-C6 cycloalkyl, aryl, halogen, trifluoromethyl, trifluoromethoxy, or trifluoromethylthio and wherein at least one substituent is a halogen;
- R4 is a hydrogen or C1-C5 alkyl, each optionally independently substituted with one to three substituent groups,
- wherein each substituent group of R4 is independently selected from halogen, hydroxy, oxo, cyano, amino, or trifluoromethyl;
- R5 and R6 are each independently hydrogen, C1-C5 alkyl, or phenyl, or R5 and R6 together with the carbon atom they are commonly attached to form a C3-C8 spiro cycloalkyl ring, each optionally independently substituted with one to three substituent groups,
- wherein each substituent group of R5 and R6 is independently selected from halogen, hydroxy, oxo, cyano, amino, or trifluoromethyl;
- and
- R7 is a heteroaryl group optionally independently substituted with one to three substituent groups,
- wherein each substituent group of R7 is independently C1-C3 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, heterocyclyl, aryl, heteroaryl, C1-C5 alkoxy, aminocarbonyl, C1-C3 alkylaminocarbonyl, C1-C3 dialkylaminocarbonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, nitro, amino wherein the nitrogen atom is optionally independently mono- or di-substituted by C1-C5 alkyl, or C1-C5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone,
- wherein each substituent group of R7 is optionally independently substituted with one to three substituent groups selected from C1-C3 alkyl, C1-C3 alkoxy, aryl, acyl, acylamino, halogen, hydroxy, oxo, cyano, trifluoromethyl, or amino wherein the nitrogen atom is optionally independently mono- or di-substituted by C1-C5 alkyl,
- or a tautomer, ester or amide prodrug, or pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.