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US 2009/0023673 A1Published application
Lipid containing formulations
AssigneeAlnylam Pharamaceticals, Inc.
InventorsMuthiah Manoharan, Kallanthottathil G. Rajeev, Akin Akinc, Narayanannair K. Jayaprakash, Muthusamy Jayraman, Martin Maier
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Abstract
Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.
Claims26
1-395. (canceled)
An association complex comprising:
- a. cationic lipid having the structure shown in formula (I)
- wherein:
- each Xa and Xb, for each occurrence, is independently C1-6 alkylene;
- n is 0, 1, 2, 3, 4, or 5;
- each R is independently H,
- wherein:
- at least n+2 of the R moieties in at least about 80% of the molecules of the compound of formula (I) in the preparation are not H;
- m is 1, 2, 3 or 4;
- Y is O, NR2, or S;
- R1 is alkyl alkenyl or alkynyl;
- each of which is optionally substituted with one or more substituents;
- and
- R2 is H, alkyl alkenyl or alkynyl;
- each of which is optionally substituted each of which is optionally substituted with one or more substituents;
- provided that, if n=0, then at least n+3 of the R moieties are not H.
- b. PEG-lipid having the structure shown in formula (XV)
- wherein:
- each L1 and L2 are independently a bond or C(O);
- each R1 and R2 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)C1-3alkylC(O)NH—;
- or —C(O)C1-3alkyl-C(O)O—;
- m is an integer from 0-11 and
- n is an integer from 1-500.
- c. structural lipid;
- and
- d. therapeutic agent.
24 more elements
Dependencies are inferred from the claim text.