Potent TLR9-Selective and TLR9/7 Dual Antagonists

Activation of toll -like receptors (TLRs) on immune syatem is one of the critical machanisk for self -nonself discrimination by the host immune response. Interstingly aberrent TLR98 activation is implicated in the pathogenesis of a number of autoimmune diseases(viz psoriasis,systemic lupis, sceloderma, rheumatoid arthritis, type1 diabites).TLR89 is establlished as an impotant therapeutic target in these different clinical contexts. 

A series of potent inhibitors of toll –like receptor (TLR) 9 as well as dual antagonists of TLR9 and TLR& with potential application in auto-immune disease and metabolic syndrome.

1. Potent ( nanomolar IC 50) small molecule inhibitora of TLR9 and TLR7: 'ABODINIBS' and 'ADADINIBS'

2. Demonstarated oral bioavailabity effiacy in human immune cells and pharmacokinetics in preclinal rodent model.

3. Demonstrated efficacy in apreclinical model of psoriasis