| abstract |
Compounds that are toll-like receptor 7 (TLR7) agonists and can be used as adjuvants to stimulate the immune system. Some of these compounds can be used in conjugates for organ or tissue targeted delivery of intended action. Claim 1: A compound characterized in that it has a structure according to formula (1) or (2) in which R¹ is (C₁₋₅ alkyl) O, (C₁₋₂ alkyl) O (CH₂) ₂₋₃O, (C ₋₅ alkyl) C (= O) O, (C₁₋₅ alkyl) NH, (C₁₋₂ alkyl) O (CH₂) ₂₋₃NH or (C₁₋₅ alkyl) C (= O) NH; R² is, independently of each occurrence, H, C₁₋₃ alkyl, halo, O (C₁₋₃ alkyl), CN or NO₂; X is, independently of each occurrence, CR² or N; and Ar is a 5-membered heteroaromatic moiety selected from pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, tetrazolyl, 1,2,4-oxadiazolyl. , 1,2,4-thiadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-thiadiazolyl, 1,2,5-oxadiazolyl, 1,2,5-thiadiazolyl, 1,2,3,4-oxathiazolyl and 1,2,3,4-thiatriazolyl. |