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US 7,115,581 B2Granted
Chemically-defined non-polymeric valency platform molecules and conjugates thereof
AssigneeLa Jolla Pharmaceutical Company
InventorsStephen M. Coutts, David S. Jones, Douglas Alan Livingston, Lin Yu
Life of this patent
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Abstract
Chemically-defined, non-polymeric valency platform molecules and conjugates comprising chemically-defined valency platform molecules and biological or chemical molecules including polynucleotide duplexes of at least 20 base pairs that have significant binding activity for human lupus anti-dsDNA autoantibodies.
Claims46
A conjugate comprising:
- a polynucleotide bound to
- a chemically-defined valency platform molecule, wherein the chemically-defined valency platform molecule is formable by a reaction selected from the group consisting of:
- (a) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(6′-N′-carbobenzyloxyaminohexyl)acetamide]4″-nitrophenyl ester;
- (b) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(8′-N′-carbobenzyloxyamino-3′,6′-dioxaoctyl)acetamide]4″-nitrophenyl ester;
- or
- (c) reacting polyethylene glycol-bis-chloroformate with N,N-di(2-[6′-N′-carbobenzyloxyamino hexanoamido]ethyl)amine;
- wherein the product of reaction (a), (b) or (c) is derivatized to provide attachment sites at termini of the valency platform molecule prior to binding the polynucleotide;
- and
- the conjugate optionally comprises a linker moiety linking the polynucleotide and the chemically-defined valency platform molecule.
6 more elements
A conjugate of the formula:
- wherein r=0–300;
- X=O or S;
- and
- PN is a polynucleotide.
1 more element
A conjugate of the formula:
- wherein PN is a polynucleotide.
A conjugate of the formula
A method of making a conjugate of a valency platform molecule and a polynucleotide, wherein the method comprises:
- bonding the polynucleotide to the valency platform molecule at attachment sites on the valency platform molecule, wherein
- the conjugate optionally comprises a linker moiety linking the polynucleotide and the valency platform molecule and
- the valency platform molecule is formable by performing a reaction selected from the group consisting of:
- (a) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(6′-N′-carbobenzyloxyaminohexyl)acetamide]4″-nitrophenyl ester;
- (b) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(8′-N′-carbobenzyloxyamino-3′,6′-dioxaoctyl)acetamide]4″-nitrophenyl ester;
- or (c) reacting polyethylene glycol-bis-chloroformate with N,N-di(2-[6′-N′-carbobenzyl oxyaminohexanoamido]ethyl)amine, wherein the product of reaction (a), (b) or (c) is derivatized to provide attachment sites at termini of the valency platform molecule.
3 more elements
A conjugate of the formula:
- [(PN)-Linker]4-valency platform molecule, wherein:
- PN is double stranded polynucleotide duplex;
- Linker is a linker moiety;
- Valency platform molecule is a chemically-defined valency platform molecule formable by a reaction selected from the group consisting of:
- (a) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(6′-N′-carbobenzyloxyaminohexyl)acetamide]4″-nitrophenyl ester;
- (b) reacting an amino modified-polyethylene glycol with 3-carboxypropionamide-N,N-bis-[(8′-N′-carbobenzyloxyamino-3′,6′-dioxaoctyl)acetamide]4″-nitrophenyl ester;
- or
- (c) reacting polyethylene glycol-bis-chloroformate with N,N-di(2-[6′-N′-carbobenzyloxyamino hexanoamido]ethyl)amine;
- wherein the product of reaction (a), (b) or (c) is derivatized to provide attachment sites at termini of the valency platform molecule.
6 more elements
Dependencies are inferred from the claim text.