Kangbaida (Sichuan) Biotechnology Co. Ltd. has synthesized pyrrolidine derivatives acting as Toll-like receptor 7 (TLR7) and/or (TLR8) antagonists reported to be useful for the treatment of autoimmune disease.

Jiangsu Hengrui Medicine Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have disclosed Toll-like receptor 7 (TLR7) and/or TLR8 and/or TLR9 antagonists reported to be useful for the treatment of rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus and Sjögren’s syndrome.

Chengdu Baiyu Pharmaceutical Co. Ltd. has disclosed pyrrolidine derivatives acting as IL-6 inhibitors and Toll-like receptor 7 (TLR7) and/or TLR8 antagonists reported to be useful for the treatment of autoimmune disease.

There is increasing evidence on the involvement of Toll-like receptor 7 (TLR7) in the pathogenesis of systemic lupus erythematosus (SLE). At the recent American College of Rheumatology meeting, researchers from Daiichi Sankyo Co. Ltd. presented preclinical data on DS-7011a, a TLR7 antagonist antibody with for the potential treatment of SLE.

Sichuan Kelun-Biotech Biopharmaceutical Co. Ltd. has identified immunostimulatory antibody-drug conjugates (ISAC) comprising immunomodulators (Toll-like receptor 7 [TLR7] and/or TLR8 agonists) bound to antibodies through cleavable or uncleavable linkers reported to be useful for the treatment of cancer.

Gilead Sciences Inc. has divulged thienopyrrole compounds acting as Toll-like receptor 7 (TLR7) and/or TLR8 antagonists reported to be useful for the treatment of systemic lupus erythematosus, cutaneous lupus erythematosus, lupus nephritis and inflammatory disorders, among others.

Shanghai Visonpharma Co. Ltd. has described Toll-like receptor 7 (TLR7) and/or TLR8 antagonists reported to be useful for the treatment of multiple sclerosis, lupus nephritis, psoriasis, rheumatoid arthritis, systemic scleroderma (systemic sclerosis), Sjogren syndrome and systemic lupus erythematosus.

Gilead Sciences Inc. has divulged thienopyrrole compounds acting as Toll-like receptor 7 (TLR7) and/or TLR8 antagonists reported to be useful for the treatment of systemic lupus erythematosus (SLE), cutaneous lupus erythematosus, lupus nephritis and inflammatory disorders, among others.