CPG-52364 a small molecule TLR7/8/9 antagonist, has recently completed phase 1 clinical trial for SLE therapy. Toll-like receptors (TLRs) are a family of type I transmembrane receptors and the central components of the innate immune system. Human TLR3, TLR7, TLR8, and TLR9 are expressed on endosomal membranes in the cells and recognize pathogenderived nucleic acid molecular patterns.5 However, recognition of endogenous immune complexes containing self-nucleic acids as PAMPs or DAMPs contributes to certain autoimmune diseases, such as systemic lupus erythematosus (SLE), psoriasis,7 arthritis, and multiple sclerosis.8 Therefore, inhibition of these recognition signals is expected to have therapeutic value. References: Watanabe M, Kasai M, Tomizawa H, Aoki M, Eiho K, Isobe Y, Asano S. Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts. ACS Med Chem Lett. 2014 Oct 2;5(11):1235-9. doi: 10.1021/ml5003184. eCollection 2014 Nov 13. PubMed PMID: 25408837; PubMed Central PMCID: PMC4233361.

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CAS：1093135-60-4