Folate conjugates

Details Folate conjugates Folate conjugates

A - Human Necessities

61

K

A61K 47/22 (2006.01) C12N 15/113 (2010.01) A61K 47/24 (2006.01) A61K 47/28 (2006.01) A61K 31/713 (2006.01) C07H 21/02 (2006.01)

Patent

CA 2708171

The present invention provides iRNA agent including at least one monomer having the structure shown in formula (I) wherein: A and B are each independently for each occurrence O, N(R) or S; X is H, a protecting group, a phosphate group, a phos- phodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite,a solid support, - P(Z')(Z")O-nu- cleoside, -P(Z)(Z")O-oligonucleotide, a lipid, a PEG, a steroid, a polymer, - P(Z' )(Z")O-L6-Q'-L7-OP(Z)(Z)O-oligonucleotide, a nucleotide, or an oligonucleotide; Y is H, a protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, - P(Z) (Z")O-nucleoside, -P(Z)(Z")O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, -P(Z)(Z")O-L -Q'-L6-OP(Z)(Z)O- oligonucleotide, a nucleotide, or an oligonu- cleotide; R is folate, a folate analog a folate mimic or a folate receptor binding ligand; L6 and L7 are each independently for each occurrence -(CH2)I1-, -C(R')(R")(CH2)n-, -(CH2)n C(R)(R")-, -(CH2CH2O)m CH2CH2- , or -(CH2CH2O)m CH2CH2NH-; Q'is NH, O, S, CH2, C(O)O, C(O)NH, -NH-CH(R')-C(O)-, -C(O)-CH(R')-NH-, CO, formula (A) where R a is H or amino acid side;;chain. R' and R" are each independently H, CH3, OH, SH, NH2, NH(Alkyl = Me, Et, Pr, isoPr, Bu, Bn) or N(diAlkyl = Me2, Et2, Bn2); Z', Z", Z"' and Z are independently O or S; n represent independently for each occurrence 1-20; and m represent independently for each occurrence 0-50.

La présente invention concerne un agent ARNi qui comprend au moins un monomère présentant une structure de formule (I'), dans laquelle A et B sont chacun, indépendamment pour chaque occurrence, O, N(R ) ou S; X est H, un groupe de protection, un groupe phosphate, un groupe phosphodiester, un groupe phosphate activé, un groupe phosphite activé, un phosphoramidite, un support solide, P(Z')(Z")O-nucléoside, -P(Z')(Z")O-oligonucléotide, un lipide, un PEG, un stéréoïde, un polymère, -P(Z' )(Z")O-L6-Q'-L7-OP(Z'")(Z"")O-oligonucléotide, un nucléotide ou un oligonucléotide; Y est H, un groupe de protection, un groupe phosphate, un groupe phosphodiester, un groupe phosphate activé, un groupe phosphite activé, un phosphoramidite, un support solide, P(Z')(Z")O-nucléoside, -P(Z')(Z")O-oligonucléotide, un lipide, un PEG, un stéréoïde, un lipophile, un polymère, -P(Z' )(Z")O-L6-Q'-L7-OP(Z'")(Z"")O-oligonucléotide, un nucléotide ou un oligonucléotide; R est folate, un analogue du folate, un mimétique du folate ou un ligand de liaison au récepteur du folate; L6 et L7 sont chacun, indépendamment pour chaque occurrence, -(CH2)I1-, -C(R')(R")(CH2)n-, - (CH2)nC(R')(R")-, (CH2CH2O)mCH2CH2- ou -(CH2CH2O)mCH2CH2NH-; Q' est NH, O, S, CH2, C(O)O, C(O)NH, -NH-CH(Ra)-C(0)-, -C(0)-CH(Ra)-NH-, CO, de formule (A) dans laquelle Ra est H ou une chaîne latérale aminoacide; R' et R" sont chacun, indépendamment, H, CH3, OH, SH, NH2, NH(alkyle = Me, Et, Pr, isoPr, Bu, Bn) ou N(dialkyle = Me2, Et2, Bn2); Z', Z", Z' " et Z"" sont chacun, indépendamment, 0 ou S; n représente indépendamment, pour chaque occurrence, 1-20; et m représente indépendamment, pour chaque occurrence, 0-50.

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