365413-00-9Relevant articles and documents
A novel class of potent NF-κB signaling inhibitors
Leban, Johann,Baierl, Marcel,Mies, Jan,Trentinaglia, Viola,Rath, Sandra,Kronthaler, Kerstin,Wolf, Kristina,Gotschlich, Astrid,Seifert, Markus H.J.
, p. 5858 - 5862 (2007)
A novel class of NF-κB pathway signaling inhibitors was discovered by virtual screening, medicinal chemistry, and QSAR analysis. An initial set of compounds inhibited NF-κB signaling in a whole cell reporter gene assay in the micro-molar range. Activity was improved step by step by medicinal chemistry to yield nano-molar signaling inhibitors.
Synthetic method and application of piperidyl thiazole formamide compound
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, (2020/06/09)
The invention relates to a 2-(4-piperidyl)-thiazole-4-formamide compound and a synthetic method and medicinal evaluation thereof. The synthetic method comprises the following steps: carrying out a substitution reaction between N-Boc-4-piperidine-carboxylic acid and ammonium chloride to prepare an intermediate 2; carrying out a thiolation reaction between the compound 2 and a Lawesson reagent to obtain an intermediate 3; carrying out a reaction between the compound 3 and ethyl bromopyruvate to obtain an intermediate 4; carrying out esterolysis on the compound 4 to obtain a compound 5; carryingout a reaction between the compound 5 and ammonia to obtain an intermediate 6; deprotecting the Boc protected compound 6 to obtain a compound 7; performing acid condensation on the compound 7 to obtain an intermediate 8; deprotecting the Boc protected intermediate 8 to obtain a compound 9; and carrying out a reaction between the compound 9 and different isocyanates to obtain a final product. An MTT method is adopted for tests, and it shows that part of the 2-(4-piperidyl)-thiazole-4-formamide compounds have certain anti-tumor activity, wherein the antitumor activity of a compound 10f-10m is superior to that of a compound 10a-10d.
NOVEL FUNGIDAL HETEROCYCLIC COMPOUNDS
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, (2019/04/10)
The present invention relates to a compound selected from Formula (I) and its salts, metal complexes, N-oxides, isomers, and polymorphs: Formula (I) wherein E, Z, R3, n, G, J & Q have the meaning as defined in the description.
HETEROCYCLIC COMPOUNDS WITH MICROBIOCIDAL PROPERTIES
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, (2018/11/22)
The present disclosure relates to a compound of Formula I, wherein the substituents T, A, W, R2, n, Z, G, Z1 and J are as defined in the description.
A class of nitrogen-containing heterocyclic thiazole derivative and its preparation and use
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Paragraph 0052-0054, (2018/02/23)
The invention provides a nitrogen heterocyclic ring thiazole derivative, a preparation method and applications thereof, and relates to isothiazole oxime ether compounds, which have a chemical construction general formula shown in the description. The inve
OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
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, (2012/03/26)
The present invention relates to compound of formula (I) and pharmaceutically acceptable salt thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Novel NIP Thiazole Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydroge-Nase-1
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, (2011/04/18)
The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
Thiazole-4-Carboxylic Acid Esters and Thioesters as Plant Protection Agents
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Page/Page column 32, (2011/05/08)
The use of thiazole-4-carboxylic esters and thioesters of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Y1, Y2, Y3, W, X and G have the me
Heteroarylpiperidine And-Piperazine Derivatives
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Page/Page column 45, (2012/01/03)
Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for
BENZIMIDAZOLE NF- KAPPAB INHIBITORS
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Page/Page column 30, (2009/04/25)
The present invention relates to compounds of the general formula (Ihb) or pharmaceutically acceptable salts thereof with an acid or a base or a stereoisomer thereof for the prevention and/or treatment of a disease associated with increased cytokine release, wherein Y' is O or NR2'; Z is N or CR2'; X is NR2', O or S; R2' is H, alkyl, -C(O)NR7, -C(O)Re, cycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl; R3 is H, methyl, ethyl, methoxy, amine, alkylamine, morpholino, N-methylpiperazine, CF3, or OCF3; R2a is substituted or unsubstituted aryl, benzyl or heteroaryl.