发明名称 Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists
摘要 A conjugated compound of Formula I: Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II:;
申请公布号 US9295732(B2) 申请公布日期 2016.03.29
申请号 US201313774155 申请日期 2013.02.22
申请人 INVIVOGEN 发明人 Lioux Thierry;Drocourt Daniel;Vernejoul Fabienne;Tiraby Gerard;Perouzel Eric
分类号 A61K31/52;A61K47/48 主分类号 A61K31/52
代理机构 Young & Thompson 代理人 Young & Thompson
主权项 1. A conjugated compound of Formula I: Q-Z—R4  Formula I wherein Q is a tautomer thereof or a pharmaceutically acceptable salt, of said compound or tautomer, wherein: R2 is a C1-C10 alkylamino; Z—R4 is a TLR2 agonist of formula III: wherein: R5 is the specific side chain of L or D isomers of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, phenylalanine, tryptophan, methionine, glycine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, proline and histidine; j and l, identical or different, are 0 or 1; p is integer from 0 to 6; m, n, o, and q, identical or different, are integers from 1 to 4; and R4 is a lipid of Formula XI: wherein: R7 and R8 are independently from each other H, C1-C30alkyl, C2-C30lkylenyl, —C(O)—C1-C30alkyl, —C(O)—C2-C30alkylenyl, or —C(O)—O—C1-C30alkyl; R9 is H, C1-C30alkyl or C2-C30alkylenyl; R10 is H, C1-C30alkyl or C2-C30alkylenyl; R9 and R10 are not both H; L1 is absent, —OC(O)—, —O—, —NR11C(O)—, —OC(O)NR11— or —CH2- wherein R11 is H, C1-C30alkyl or C2-C30alkylenyl; If L1 is present, L2 is —CH2OC(O)—, —CH2O—, —CH2NR11C(O)— or —CH2—, and if L1 is absent, L2 is —OC(O)—, —O—, —NR11C(O)—, —NR10R11, —OC(O)NR11— or —CH2- wherein R11 is as defined above.
地址 Toulouse FR