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US 7,803,399 B2Granted
Delivery system for nucleic acids
AssigneesThe Scripps Research Institute, The Board of Trustees of the Leland Stanford Jr. University
InventorsDavid A. Cheresh, John Hood, Mark Bednarski
Life of this patent
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Abstract
αvβ3 Integrin receptor targeting liposomes comprise a cationic amphiphile such as a cationic lipid, a neutral lipid, and a targeting lipid. The targeting lipid includes a non-peptidic αvβ3 integrin antagonist.
Claims7
An αvβ3 integrin receptor targeting liposome comprising
- a cationic lipid;
- a neutral lipid;
- a trivalent targeting lipid having a targeting domain and a hydrophobic domain bound to the targeting domain;
- and
- a nucleic acid complexed with the cationic lipid;
- the cationic lipid being present in an amount in the range of about 1 to about 50 mole percent, and said targeting lipid being present in an amount in the range of about 1 to about 20 mole percent, the mole percent values being based on total moles of lipid in the liposome, and the targeting domain including three non-peptidic αvβ3 integrin antagonists represented by formula (II):
- wherein in formula (II), R4 and R5 are each hydrogen, or together form a covalent bond;
- Y is —C(O)— or —CH2—;
- Z2 is —C(O)—R6;
- —C(O)OR6, or SO2R6;
- R6 is phenyl, substituted-phenyl, pyridyl, benzyl, substituted-benzyl;
- C1-C4 haloalkyl, C2-C30 alkyl, C2-C30 alkenyl, C2-C30 alkynyl, or cholesteryl;
- and Het is 2-pyridyl or 2-imidazolyl.
10 more elements
Dependencies are inferred from the claim text.