Kurata, Haruto published the artcileDiscovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P1 and S1P5 Selective Agonist for the Treatment of Autoimmune Diseases, COA of Formula: C9H9ClO2, the main research area is sphingosinephosphate receptor agonist ceralifimod immunomodulator autoimmune disease.
The discovery of 1-({6-[(2-methoxy-4-propylbenzyl)oxy]-1-methyl-3,4-dihydronaphthalen-2-yl}methyl)azetidine3-carboxylic acid (I) (13n, ceralifimod, ONO-4641), a sphingosine-1-phosphate (S1P) receptor agonist selective for S1P1 and S1P5, is described. While it has been revealed that the modulation of the S1P1 receptor is an effective way to treat autoimmune diseases such as relapsing-remitting multiple sclerosis (RRMS), it was also reported that activation of the S1P3 receptor is implicated in some undesirable effects. The authors carried out a structure-activity relationship (SAR) study of hit compound 6 with an amino acid moiety in the hydrophilic head region. Following identification of a lead compound with a dihydronaphthalene central core by inducing conformational constraint, optimization of the lipophilic tail region led to the discovery of I as a clin. candidate that exhibited >30 000-fold selectivity for S1P1 over S1P3 and was potent in a peripheral lymphocyte lowering (PLL) test in mice (ED50 = 0.029 mg/kg, 24 h after oral dosing).
Journal of Medicinal Chemistry published new progress about Anti-multiple sclerosis agents. 99585-12-3 belongs to class chlorides-buliding-blocks, name is Methyl 4-chloro-2-methylbenzoate, and the molecular formula is C9H9ClO2, COA of Formula: C9H9ClO2.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics