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US 2004/0006203 A1Published application
Method for sequential support-bound synthesis of conjugated oligomeric compounds
AssigneeIsis Pharmaceuticals, Inc.
InventorsMartin A. Maier, Andrei P. Guzaev, Muthiah Manoharan
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Abstract
A sequential support-bound synthesis method is disclosed for preparing a conjugated oligomeric compound, preferably a PNA-peptide conjugate or an oligonucleotide-peptide conjugate, using a bridging molecule having at least two N-protecting amino groups. A conjugated oligomeric compound for therapeutic or prophylactic delivery is also disclosed.
Claims45
A method of preparing a conjugated oligomeric compound comprising the steps of:
- providing a bridging unit bound to a support medium, said bridging unit comprising at least two orthogonally protected amino groups;
- deblocking one of said at least two orthogonally protected amino groups and covalently attaching to said deblocked amino group a conjugate group or an oligomeric compound;
- and
- deblocking another of said at least two orthogonally protected amino groups and covalently attaching to said another deblocked amino group a conjugate group or an oligomeric compound;
- wherein at least one conjugate group and at least one oligomeric compound are attached to said bridging unit.
2 more elements
A method of preparing a conjugated oligomeric compound comprising the steps of:
- providing a bridging unit bound to a support medium, said bridging unit comprising at least two orthogonally protected amino groups;
- deblocking one of said at least two orthogonally protected amino groups and covalently attaching a conjugate group to said deblocked amino group;
- deblocking another of said at least two orthogonally protected amino groups and covalently attaching a spacer unit comprising a protected hydroxyl group to said another deblocked amino group;
- deprotecting said protected hydroxyl group;
- and
- covalently attaching an oligomeric compound.
3 more elements
Dependencies are inferred from the claim text.