- Selective sodium channel regulator as well as preparation and application thereof
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The invention provides a compound serving as a selective sodium channel regulator and a synthesis and use method, and particularly provides a compound shown as a formula (I), a preparation method of the compound and application of the compound serving as the selective sodium channel regulator. The compounds exhibit excellent activity as a regulator of sodium channels.
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Paragraph 0228-0233
(2021/02/10)
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- 1,2,4-TRIAZINE-6-CARBOXAMIDE KINASE INHIBITORS
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Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
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- NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
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- Novel indole inhibitors of IMPDH from fragments: Synthesis and initial structure-activity relationships
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The elaboration of previously reported indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II, PBMC proliferation and physicochemical properties are discussed.
- Beevers, Rebekah E.,Buckley, George M.,Davies, Natasha,Fraser, Joanne L.,Galvin, Francis C.,Hannah, Duncan R.,Haughan, Alan F.,Jenkins, Kerry,Mack, Stephen R.,Pitt, William R.,Ratcliffe, Andrew J.,Richard, Marianna D.,Sabin, Verity,Sharpe, Andrew,Williams, Sophie C.
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p. 2539 - 2542
(2007/10/03)
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- 3-Cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: Synthesis and initial structure-activity relationships
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A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immuno
- Dhar, T. G. Murali,Shen, Zhongqi,Gu, Henry H.,Chen, Ping,Norris, Derek,Watterson, Scott H.,Ballentine, Shelley K.,Fleener, Catherine A.,Rouleau, Katherine A.,Barrish, Joel C.,Townsend, Robert,Hollenbaugh, Diane L.,Iwanowicz, Edwin J.
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p. 3557 - 3560
(2007/10/03)
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