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US 2002/0058639 A1Published application
Targeted oligonucleotide conjugates
AssigneeIsis Pharmaceuticals, Inc.
InventorMuthiah Manoharan
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Abstract
The present invention provides improved ingress of therapeutic and other moieties into cellular targets. In accordance with preferred embodiments, complexes are provided which carry primary moieties, chiefly therapeutic moieties, to such target cells. Such complexes preferably feature cell surface receptor ligands to provide specificity. Such ligands are preferably bound to primary moieties through polyfunctional manifold compounds.
Claims40
A complex comprising:
- a primary moiety for modulating a cellular function;
- and
- at least two cell surface receptor ligands covalently connected to said primary moiety.
A chemical complex having the formula:
- 8
- wherein
- said primary moiety is a nucleotide, nucleoside, oligonucleotide or oligonucleoside;
- each of said linkers are, independently, bi-or trifunctional;
- said manifold is derivatized at a plurality of sites;
- each of said cell surface receptor ligands is a carbohydrate;
- and
- n is an integer from 2 to about 8.
5 more elements
A method of facilitating cellular uptake of a primary moiety comprising:
- identifying a cell surface receptor on a target cell;
- attaching a plurality of cell surface receptor ligands on said primary moiety to form a complex;
- and
- contacting said cell with said complex.
1 more element
Dependencies are inferred from the claim text.