24590-51-0Relevant articles and documents
Substituted thiazole derivative and application thereof
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Paragraph 0247-0251, (2019/02/13)
The invention provides a compound represented by a general formula (I), or a stereoisomer, pharmaceutically acceptable salt, solvate, hydrate, chemically protective form or prodrug thereof. The compound has an effect of inhibiting adenosine receptor 2a (A2a), and can be used as an antagonist of the adenosine receptor 2a (A2A) for treating tumors.
Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 Receptor
Moldovan, Rare?-Petru,Teodoro, Rodrigo,Gao, Yongjun,Deuther-Conrad, Winnie,Kranz, Mathias,Wang, Yuchuan,Kuwabara, Hiroto,Nakano, Masayoshi,Valentine, Heather,Fischer, Steffen,Pomper, Martin G.,Wong, Dean F.,Dannals, Robert F.,Brust, Peter,Horti, Andrew G.
, p. 7840 - 7855 (2016/10/12)
Cannabinoid receptors type 2 (CB2) represent a target with increasing importance for neuroimaging due to its upregulation under various pathological conditions. Encouraged by preliminary results obtained with [11C](Z)-N-(3-(2-methoxyethyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetramethyl-cyclopropanecarboxamide ([11C]A-836339, [11C]1) in a mouse model of acute neuroinflammation (induced by lipopolysaccharide, LPS), we designed a library of fluorinated analogues aiming for an [18F]-labeled radiotracer with improved CB2 binding affinity and selectivity. Compound (Z)-N-(3-(4-fluorobutyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetramethyl-cyclopropanecarboxamide (29) was selected as the ligand with the highest CB2 affinity (Ki = 0.39 nM) and selectivity over those of CB1 (factor of 1000). [18F]29 was prepared starting from the bromo precursor (53). Specific binding was shown in vitro, whereas fast metabolism was observed in vivo in CD-1 mice. Animal PET revealed a brain uptake comparable to that of [11C]1. In the LPS-treated mice, a 20-30% higher uptake in brain was found in comparison to that in nontreated mice (n = 3, P 0.05).
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00343; 00344, (2013/08/28)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.