635702-23-7Relevant articles and documents
FUNGICIDAL OXADIAZOLES
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Paragraph 0578, (2020/06/07)
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
Syntheses and in vitro evaluation of new S1PR1 compounds and initial evaluation of a lead F-18 radiotracer in rodents
Luo, Zonghua,Rosenberg, Adam J.,Liu, Hui,Han, Junbin,Tu, Zhude
, p. 796 - 808 (2018/04/05)
Thirteen new sphingosine-1-phosphate receptor 1 (S1PR1) ligands were designed and synthesized by replacing azetidine-3-carboxylic acid moiety of compound 4 with new polar groups. The in vitro binding potency of these new analogs toward S1PR1 was determined. Out of 13 new compounds, four compounds 9a, 10c, 12b, and 16b displayed high S1PR1 binding potency with IC50 values of 13.2 ± 3.2, 14.7 ± 1.7, 9.7 ± 1.6, and 6.3 ± 1.3 nM, respectively; further binding studies of these four ligands toward S1PR2-5 suggested they are highly selective for S1PR1 over other S1PRs. The radiosynthesis of the lead radiotracer [18F]12b was achieved with good radiochemical yield (~14.1%), high radiochemical purity (>98%), and good specific activity (~54.1 GBq/μmol, decay corrected to the end of synthesis, EOS). Ex vivo autoradiography and initial biodistribution studies in rodents were performed, suggesting that [18F]12b was able to penetrate the blood-brain barrier (BBB) with high brain uptake (0.71% ID/g at 60 min post-injection) and no defluorination was observed. In vitro autoradiography study in brain slices of lipopolysaccharides (LPS)-induced neuroinflammation mice indicated that SEW2871, a specific S1PR1 ligand was able to reduce the uptake of [18F]12b, suggesting [18F]12b has S1PR1 specific binding. These initial results suggested that [18F]12b has potential to be an F-18 labeled radiotracer for imaging S1PR1 in the brain of the animal in vivo.
IMMUNE ADJUSTMENT COMPOUND, USE THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0042; 0043, (2016/08/29)
The present invention provides a compound represented by formula I, wherein R is a halogen element or a C1-C6 alkyl group. The compound has S1 P1 receptor agonist activity and selective specificity and has obviously-shortened half-life in-vivo, and therefore the compound is a high-quality second-generation S1P1 receptor agonist. The present invention also provides a use of the compound in preparing medicine for treating diseases or symptoms mediated by an S1P1 receptor, a pharmaceutical composition comprising the compound, and uses of the compound and the pharmaceutical composition in treating diseases or symptoms mediated by the S1 P1 receptor.