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. |