- Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof
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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.
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Page/Page column 37-38
(2010/12/29)
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- Design of a practical fluorescent probe for superoxide based on protection-deprotection chemistry of fluoresceins with benzenesulfonyl protecting groups
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A strategy for designing probes based on protection-deprotection chemistry involving fluoresceins and their benzenesulfonyl (BES) derivatives has led to the development of a much more practical superoxide (O2-.) probe than the previously reported bis(2,4-dinitro-BES) tetrafluorofluorescein (6a). Examination of various BES derivatives, developed from the starting point of the prototype probe 6a. yielded 4,5-dimethoxy-2-nitro-BES tetrafluorofluorescein (BESSo; 7j) as the optimal reagent. A microtiter plate assay with BESSo showed a tenfold improved detection limit for O 2-. compared with such an assay based on 6a. BESSo showed markedly better specificity for O2-. than for GSH or other reactive oxygen species, and this specificity was significantly higher than that of Fe2+ and some reducing enzymes. These features have resulted in the development of an assay based on BESSo that is capable of providing more unambiguous results for O2. release from neutrophils, with or without stimulation by phorbol myristate acetate, as compared with an assay based on 6a. Intracellular generation of O2. in human Jurkat T cells stimulated by butyric acid has been measured by using flow cytometry and fluorescence microscopy utilizing the acetoxymethyl derivative of BESSo.
- Maeda, Hatsuo,Yamamoto, Kayoko,Kohno, Iho,Hafsi, Leila,Itoh, Norio,Nakagawa, Shinsaku,Kanagawa, Naoko,Suzuki, Keiichiro,Uno, Tadayuki
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p. 1946 - 1954
(2008/02/03)
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- Studies of Reactions of Amines with Sulfur Trioxide. VI. Thermal Reactions of Anilinium, Dimethylanilinium, and Trimethylanilinium Salts of Butylamidosulfuric Acid
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When the title compounds were heated in an evacuated reaction vessel, both transsulfonation and rearrangement occurred.At lower temperatures (80-120 deg C) the corresponding phenylamidosulfates and sulfophenylamidosulfates (transsulfonation products) were the main products.Increasing temperature led to the formation of ring mono- and disulfonates (rearrangement products) at the expense of the transsulfonation products.The sulfonate group always migrated to the ortho and/or para position(s) to the amino group.In no case was any meta-product detected.There was no significant difference in the ease of transsulfonation among the anilinium salts studied exept 2,6-dimethyl- and 2,4,6-trimethylanilinium salts.On the other hand, the ease of rearrangement and the orientation of ring sulfonation depended strongly on the structure of the substrate anilines.The thermal reactions of 2,4,6-trimethylanilinium butylamidosulfate produced (2,4,6-trimethylphenylimido)bis(sulfate) in addition to (2,4,6-trimethylphenylamido)sulfate.This is the first isolation of an arylimidobis(sulfate) from such reactions.Mechanisms of the transsulfonation and rearrangement have been discussed.
- Kanetani, Fujio,Yamaguchi, Hachiro
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p. 3048 - 3058
(2007/10/02)
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