550367-75-4Relevant academic research and scientific papers
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups
Lescop, Cyrille,Müller, Claus,Mathys, Boris,Birker, Magdalena,De Kanter, Ruben,Kohl, Christopher,Hess, Patrick,Nayler, Oliver,Rey, Markus,Sieber, Patrick,Steiner, Beat,Weller, Thomas,Bolli, Martin H.
, p. 222 - 238 (2016)
In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound class is phototoxic in vitro. Here we describe a new class of potent S1PR1 agonists wherein the exocyclic nitrogen was moved away from the pyridine ring (e.g. 11c). Further structural modifications led to the identification of novel alkylaminomethyl substituted phenyl and thienyl derivatives as potent S1PR1 agonists. These new alkylaminomethyl aryl compounds showed no phototoxic potential. Based on their in vivo efficacy and ability to penetrate the brain, the 5-alkyl-aminomethyl thiophenes appeared to be the most interesting class. Potent and selective S1PR1 agonist 20e, for instance, maximally reduced the blood lymphocyte count (LC) for 24 h after oral administration of 10 mg/kg to rat and its brain concentrations reached >500 ng/g over 24 h.
Reduction response containing double-disulfide bond of chemical connector and its preparation and use (by machine translation)
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Paragraph 0083; 0085, (2018/01/11)
Reduction response containing double-disulfide bond of chemical connector and its preparation and use thereof, relates to a double-mercapto compound and its forming with double-disulfide bond of chemical linker, based on the non-coherent double-two-sulfur of the synergistic effect of the tenon, construction with unique oxidation-reduction response dynamic covalent linkage. The covalent linkage with traditional single disulfide bond completely different oxidation-reduction response; its low reducing agent concentration or extracellular conditions having ultra high stability, such as in the cell in the strong reducing conditions can occur under rapid reduction of the fracture. It is expected to be applied to the drug release and biological sensing field, constructing the oxidation-reduction responsive drug delivery system, such as the monoclonal antibody - such as the drug in the sample. (by machine translation)
NOVEL AMINOMETHYL BENZENE DERIVATIVES
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Page/Page column 42, (2009/10/22)
The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. (I) wherein A represents one of the groups (I), (I), (I) and
