745011-75-0Relevant articles and documents
Immunomodulators
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Paragraph 0152-0155, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL-17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of the compounds shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/orpreparing medicines for treating diseases related to IL-17A activity.
Synthesis of fluorinated analogues of sphingosine-1-phosphate antagonists as potential radiotracers for molecular imaging using positron emission tomography
Prasad, Vysakh Pushpa,Wagner, Stefan,Keul, Petra,Hermann, Sven,Levkau, Bodo,Sch?fers, Michael,Haufe, Günter
, p. 5168 - 5181 (2015/02/19)
Sphingosine-1-phosphate (S1P) receptors play major roles in cardiovascular, immunological and neurological diseases. The recent approval of the sphingolipid drug Fingolimod (Gilenya), a sphingosine-1-phosphate agonist for relapsing multiple sclerosis, in 2010 exemplifies the potential for targeting sphingolipids for the treatment of human disorders. Moreover, non-invasive in vivo imaging of S1P receptors that are not available till now would contribute to the understanding of their role in specific pathologies and is therefore of preclinical interest. Based on fluorinated analogues of the S1P1receptor antagonist W146 showing practically equal in vitro potency as the lead structure, the first S1P receptor antagonist [18F]-radiotracer has been synthesized and tested for in vivo imaging of the S1P1receptor using positron emission tomography (PET). Though the tracer is serum stable, initial in vivo images show fast metabolism and subsequent accumulation of free [18F]fluoride in the bones.