Novel lipids and compositions for the delivery of therapeutics

Details Novel lipids and compositions for the delivery of therapeutics Novel lipids and compositions for the delivery of therapeutics

C - Chemistry, Metallurgy

07

C

C07C 271/12 (2006.01) C12N 15/113 (2010.01) C12N 15/117 (2010.01) A61K 9/127 (2006.01) A61K 31/7088 (2006.01) A61K 39/00 (2006.01) C07C 211/21 (2006.01) C07C 211/22 (2006.01) C07C 229/12 (2006.01) C07C 229/48 (2006.01) C07C 237/06 (2006.01) C07C 251/38 (2006.01) C07C 251/78 (2006.01) C07C 271/20 (2006.01) C07C 323/27 (2006.01) C07D 317/34 (2006.01) C07D 317/44 (2006.01) C07F 9/06 (2006.01) C07F 9/28 (2006.01) C07H 15/00 (2006.01)

Patent

CA 2743136

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure (I) wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C 30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkyl- hetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, .omega.-aminoalkyls, .omega. -(substituted)aminoalkyls, .omega.-phosphoalkyls, .omega. -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O),NS(O)2N(Q),S(O)2, N(Q)S(O)2,SS,O=N,aryl,heteroaryl,cyclic or heterocycle;and, Q is H, .omega.- aminoalkyl, .omega.-(substituted) aminoalky, .omega.-phosphoalkyl or .omega.-thiophosphoalkyl.

La présente invention concerne des lipides qui sont utilisés avantageusement dans des particules lipidiques pour ladministration in vivo dagents thérapeutiques aux cellules. En particulier, linvention concerne des lipides ayant la structure (I) suivante dans laquelle : R1 et R2 représentent chacun indépendamment à chaque apparition un groupe alkyle en C10 à C30 éventuellement substitué, alcényle en C10 à C30 éventuellement substitué, alcynyle en C10 à C30 éventuellement substitué, acyle en C10 à C30 éventuellement substitué, ou -lieur-ligand; R3 représente H, un groupe alkyle en C1 à C10 éventuellement substitué, alcényle en C2 à C10 éventuellement substitué, alcynyle en C2 à C10 éventuellement substitué, alkylhétérocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonate, alkylamine, hydroxyalkyle, ?-aminoalkyle, ?-aminoalkyle (substitué), ?-phosphoalkyle, ?-thiophosphoalkyle, polyéthylène glycol éventuellement substitué (PEG, mm 100 à 40 K), mPEG éventuellement substitué (mm 120 à 40 K), hétéroaryle, hétérocycle ou lieur-ligand; E représente O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O=N, aryle, hétéroaryle, cyclique ou hétérocycle; et, Q représente H, un groupe alkyle, ?-aminoalkyle, ?-aminoalkyle (substitué), ?-phosphoalkyle ou ?-thiophosphoalkyle.

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