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US 6,320,017 B1Granted
Polyamide oligomers
AssigneeInex Pharmaceuticals Corporation
InventorSteven Michial Ansell
Life of this patent
Estimating the term…
Abstract
The present invention relates to new polyamide oligomers. These oligomers can be conjugated to lipids, nucleic acids, peptides, proteins, etc. The oligomer-lipid conjugates can be used to form liposomes, virusomes, micelles, etc., optionally containing drugs or biological agents. The polyamide oligomers are heterobifunctional allowing the attachment of other suitable ligand compounds (e.g., a targeting moiety). In addition, methods of use for the liposomes, virusomes, micelles, etc., are provided.
Claims24
A compound of Formula I
- wherein:
- R is a member selected from the group consisting of hydrogen, alkyl and acyl;
- R1 is a member selected from the group consisting of hydrogen and alkyl;
- or optionally,
- R and R1 and the nitrogen to which they are bound form an azido moiety;
- R2 is a member of the group selected from hydrogen, optionally substituted alky, optionally substituted aryl and a side chain of an amino acid;
- R3 is a member selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, mercapto, hydrazino, amino and NR4R5, wherein R4 and R5 are independently hydrogen or alkyl;
- n is 4 to 80;
- m is 2 to 6;
- p is 1 to 4;
- and
- q is 0 or 1.
9 more elements
A compound of Formula II:
- wherein:
- R1 is member selected from the group consisting of hydrogen and alkyl;
- A is a member selected from the group consisting of hydrogen, alkyl, acyl and a ligand;
- or, optionally,
- R1, A, and the nitrogen to which they are bound form an azido moiety;
- R2 is a member of the group selected from hydrogen, optionally substituted alkyl, optionally substituted aryl and a side chain of an amino acid;
- B is a member selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, amino, NR4R5, wherein R4 and R5 are independently hydrogen or alkyl, mercapto, hydrazino, diacylglycerolyl, dialkylglycerolyl, N,N-dialkylamino, 1,2-diacyloxy-3-aminopropane, 1,2-dialkyloxy-3-aminopropane and a ligand;
- n is 4 to 80;
- m is 2 to 6;
- p is 1 to 4;
- and
- q is 0 or 1.
9 more elements
A compound of the Formula III
- wherein:
- R is a member selected from the group consisting of hydrogen, alkyl and acyl;
- R1 and R2 are independently selected from the group consisting of hydrogen and alkyl;
- or, optionally, R, R1, and the nitrogen to which they are bound form an azido moiety;
- R3 is a member selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, mercapto, hydrazino, amino and NR4R5, wherein R4 and R5 are independently selected from the group consisting of hydrogen and alkyl;
- R6 and R7 are independently selected from the group consisting of hydrogen, optionally substituted alkyl or optionally substituted aryl, wherein the substituents include aryl, amine, carboxyl, thiol and hydroxy groups;
- v is 2 to 40;
- m and r are independently 2 to 6;
- x and s are independently 1 to 4;
- and
- z and t are independently 0 or 1.
8 more elements
A compound of Formula IV:
- wherein:
- A is selected from the group consisting of hydrogen, alkyl, acyl and a ligand;
- R1 and R2 are independently selected from the group consisting of hydrogen and alkyl;
- R6 and R7 are independently selected from the group consisting of hydrogen, optionally substituted alkyl and optionally substituted aryl, wherein the substituents include aryl, amine, carboxyl, thiol and hydroxy groups;
- B is a member selected from the group consisting of hydrogen, halogen, hydroxy, alkoxy, amino, NR4R5, wherein R4 and R5 are independently hydrogen and alkyl, mercapto, hydrazino, diacylglycerolyl, dialkylglycerolyl, N,N-dialkylamino, 1,2-diacyloxy-3-aminopropane, 1,2-dialkyloxy-3-aminopropane and a ligand;
- and
- v is 2 to 40;
- m and r are independently 2 to 6;
- x and s are independently 1 to 4;
- and
- z and t are independently 0 or 1.
8 more elements
Dependencies are inferred from the claim text.