Claims for Patent: 8,642,076

Summary for Patent: 8,642,076

Title:	Lipid containing formulations
Abstract:	Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
Inventor(s):	Manoharan; Muthiah (Cambridge, MA), Rajeev; Kallanthottathil G. (Cambridge, MA), Akinc; Akin (Cambridge, MA), Jayaprakash; Narayanannair K. (Cambridge, MA), Jayaraman; Muthusamy (Cambridge, MA), Maier; Martin (Cambridge, MA)
Assignee:	Tekmira Pharmaceuticals Corporation (Burnaby, British Columbia, unknown)
Application Number:	13/211,094
Patent Claims:	1. A compound having the formula (XV): ##STR00170## wherein L.sup.1 and L.sup.2 are both a bond; each R.sup.1 and R.sup.2 are independently alkyl, alkenyl, or alkynyl, each of which is optionally substituted with one or more substituents; X is --C(O)NH--, C(S)NH, --C(O)--C.sub.1-3alkyl-C(O)NH--, or --C(O)--C.sub.1-3alkyl-C(O)O--; m is an integer from 0-11; and n is an integer from 1-500. 2. The compound of claim 1, wherein R.sup.1 and R.sup.2 are independently unsubstituted C.sub.6-C.sub.28 alkyl. 3. The compound of claim 1, wherein R.sup.1 and R.sup.2 are independently unsubstituted C.sub.10-C.sub.18 alkyl. 4. The compound of claim 1, wherein the substituents for R.sub.1 and R.sup.2 are selected from alkyl, cycloalkyl, haloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, alkenyl, alkynyl, cycloalkenyl, heterocycloalkenyl, alkoxy, haloalkoxy, halo, hydroxy, carboxy, carboxylate, cyano, nitro, amino, alkyl amino, SO.sub.3H, sulfate, phosphate, methylenedioxy (--O--CH.sub.2--O-- wherein oxygens are attached to same carbon (geminal substitution) atoms), ethylenedioxy, oxo, thioxo, imino, S(O).sub.nalkyl (where n of S(O).sub.nalkyl is 0-2), S(O).sub.naryl (where n of S(O),.sub.naryl is 0-2), S(O).sub.nheteroaryl (where n of S(O).sub.nheteroaryl is 0-2), S(O).sub.nheterocyclyl (where n of S(O).sub.nheterocyclyl is 0-2), amine, ester, amide, and sulfonamide. 5. A compound having the formula ##STR00171## wherein L.sup.1 and L.sup.2 are both a bond; each R.sup.1 and R.sup.2 are independently alkyl, alkenyl, or alkynyl; each of which is optionally substituted with one or more substituents; m is an integer from 0-11 and n is an integer from 1-500. 6. The compound of claim 5, wherein the substituents for R.sup.1 and R.sup.2 are selected from alkyl, cycloalkyl, haloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, alkenyl, alkynyl, cycloalkenyl, heterocycloalkenyl, alkoxy, haloalkoxy, halo, hydroxy, carboxy, carboxylate, cyano, nitro, amino, alkyl amino, SO.sub.3H, sulfate, phosphate, methylenedioxy (--O--CH.sub.2--O-- wherein oxygens are attached to same carbon (geminal substitution) atoms), ethylenedioxy, oxo, thioxo, imino, S(O).sub.nalkyl (where n of S(O).sub.nalkyl is 0-2), S(O).sub.naryl (where n of S(O).sub.naryl is 0-2), S(O).sub.nheteroaryl (where n of S(O).sub.nheteroaryl is 0-2), S(O).sub.nheterocyclyl (where n of S(O).sub.nheterocyclyl is 0-2), amine, ester, amide, and sulfonamide. 7. The compound of claim 5, wherein R.sup.1 and R.sup.2 are independently unsubstituted C.sub.6-C.sub.28 alkyl. 8. The compound of claim 5, wherein R.sup.1 and R.sup.2 are independently unsubstituted C.sub.10-C.sub.18 alkyl. 9. The compound of claim 7, wherein R.sup.1 and R.sup.2 are straight chain alkyl having the same length. 10. The compound of claim 8, wherein R.sup.1 and R.sup.2 are straight chain alkyl having the same length. 11. The compound of claim 5, wherein R.sup.1 and R.sup.2 are unsubstituted C.sub.14 alkyl. 12. The compound of claim 5, wherein R.sup.1 and R.sup.2 are unsubstituted C.sub.18 alkyl. 13. The compound of claim 5, wherein m is 2. 14. The compound of claim 5, wherein n is from 40 to 400. 15. The compound of claim 5, wherein n is from 40 to 50. 16. The compound of claim 5, wherein n is from 42 to 47. 17. The compound of claim 5, wherein L.sup.1 and L.sup.2 are both bonds, R.sup.1 and R.sup.2 are both alkyl, and n is an integer from about 40-400. 18. The compound of claim 17, wherein R.sup.1 and R.sup.2 are unsubstituted C.sub.6-C.sub.28 alkyl. 19. The compound of claim 17, wherein R.sup.1 and R.sup.2 are unsubstituted C.sub.10-C.sub.18 alkyl. 20. The compound of claim 17, wherein R.sup.1 and R.sup.2 are unsubstituted C.sub.14 alkyl. 21. The compound of claim 5, wherein the compound has the formula: ##STR00172## wherein each R is C.sub.14H.sub.29 and n is from 42 to 47. 22. The compound of claim 21, wherein the average molecular weight of the PEG moiety is 2000. 23. The compound of claim 5, wherein the compound has the formula: ##STR00173## wherein each R is C.sub.18H.sub.37 and n is from 42 to 47. 24. The compound of claim 23, wherein the average molecular weight of the PEG moiety is 2000. 25. The compound of claim 5, wherein the compound has the formula: ##STR00174## wherein n is an integer from 1-500. 26. The compound of claim 25, wherein n is between 42 and 47. 27. A lipid particle comprising a compound of claim 5. 28. The compound of claim 1, wherein, each of R.sup.1 and R.sup.2 are independently C.sub.6-C.sub.28 alkyl or C.sub.6-C.sub.30 alkenyl and X is --C(O)NH--.