Patents Assigned to Nektar Therapeutics AL
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Publication number: 20120195846Abstract: A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.Type: ApplicationFiled: April 13, 2012Publication date: August 2, 2012Applicant: Nektar Therapeutics AL, CorporationInventors: J. Milton Harris, Xuan Zhao
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Publication number: 20110009589Abstract: A heterobifunctional poly(ethylene glycol) is provided having a hydrolytically degradable linkage, a first terminus comprising an acrylate group, and a second terminus comprising a target such as a protein or pharmaceutical agent or a reactive moiety capable of coupling to a target. Hydrogels can be prepared. The hydrogels can be used as a carrier for a protein or a pharmaceutical agent that can be readily released in a controlled fashion.Type: ApplicationFiled: August 20, 2010Publication date: January 13, 2011Applicant: Nektar Therapeutics AL., CorporationInventors: J. Milton Harris, Xuan Zhao
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Publication number: 20100284960Abstract: The present invention provides compositions comprising an opioid agonist and a water-soluble, non-peptidic polymer-opioid antagonist conjugate. Among other things, dosage forms and methods of administering the dosage forms are also provided.Type: ApplicationFiled: November 7, 2007Publication date: November 11, 2010Applicant: Nektar Therapeutics AL, CorporationInventor: Jennifer Riggs-Sauthier
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Publication number: 20100210505Abstract: Conjugates of a GLP-I moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-I polymer conjugate may include a GLP-I moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached to a water-soluble polymer, wherein the GLP-I moiety possesses an N-methyl substituent. The GLP-I polymer conjugate may include a GLP-I moiety covalently attached at a polymer attachment site to a water-soluble polymer, wherein the GLP-I moiety is glycosylated at a site separate from the polymer attachment site.Type: ApplicationFiled: December 18, 2006Publication date: August 19, 2010Applicants: Nektar Therapeutics AL, Corporation, Nektar TherapeuticsInventors: Mary J. Bossard, Zhihao Fang, Tacey X. Viegas, Stewart A. Thompson, Mei-chang Kuo
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Publication number: 20090299050Abstract: The invention provides methods for making copolymers and multi-arm block copolymers useful as drug delivery vehicles. The multi-arm block copolymers comprise a central core molecule, such as a residue of a polyol, and at least three copolymer arms covalently attached to the central core molecule, each copolymer arm comprising an inner hydrophobic polymer segment covalently attached to the central core molecule and an outer hydrophilic polymer segment covalently attached to the hydrophobic polymer segment, wherein the central core molecule and the hydrophobic polymer segment define a hydrophobic core region. The solubility of hydrophobic biologically active agents can be improved by entrapment within the hydrophobic core region of the block copolymer. The invention further includes pharmaceutical compositions including such block copolymers, pharmaceutical compositions, and methods of using the block copolymers as drug delivery vehicles.Type: ApplicationFiled: August 7, 2009Publication date: December 3, 2009Applicant: Nektar Therapeutics AL, CorporationInventor: Xuan Zhao
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Publication number: 20090280550Abstract: Conjugates of a Factor IX moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided (among other things) are compositions comprising the conjugates, methods of making the conjugates, and methods of administering to a patient compositions comprising the conjugates.Type: ApplicationFiled: July 8, 2009Publication date: November 12, 2009Applicant: Nektar Therapeutics AL, CorporationInventors: Mary J. Bossard, Gayle Stephenson
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Publication number: 20090264600Abstract: A method is provided for preparing water-soluble polymer derivatives bearing a terminal carboxylic acid or ester thereof. The method involves the hydrolyzing an ortho ester of a water-soluble polymer so as provide the corresponding acid. In addition, the invention provides water-soluble polymers bearing a terminal carboxylic acid or ester thereof, intermediates and reagents useful in carrying out the method, as well as gels, pharmaceutical formulations, conjugates related to the described water-soluble polymer derivatives.Type: ApplicationFiled: July 1, 2009Publication date: October 22, 2009Applicant: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Publication number: 20090234070Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.Type: ApplicationFiled: January 28, 2009Publication date: September 17, 2009Applicant: Nektar Therapeutics Al, CorporationInventor: Antoni Kozlowski
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Patent number: 7589157Abstract: The invention provides methods for making copolymers and multi-arm block copolymers useful as drug delivery vehicles. The multi-arm block copolymers comprise a central core molecule, such as a residue of a polyol, and at least three copolymer arms covalently attached to the central core molecule, each copolymer arm comprising an inner hydrophobic polymer segment covalently attached to the central core molecule and an outer hydrophilic polymer segment covalently attached to the hydrophobic polymer segment, wherein the central core molecule and the hydrophobic polymer segment define a hydrophobic core region. The solubility of hydrophobic biologically active agents can be improved by entrapment within the hydrophobic core region of the block copolymer. The invention further includes pharmaceutical compositions including such block copolymers, pharmaceutical compositions, and methods of using the block copolymers as drug delivery vehicles.Type: GrantFiled: August 21, 2007Date of Patent: September 15, 2009Assignee: Nektar Therapeutics AL, CorporationInventor: Xuan Zhao
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Publication number: 20090221766Abstract: A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.Type: ApplicationFiled: April 19, 2007Publication date: September 3, 2009Applicant: Nektar Therapeutics AL, CorporationInventors: Lin Cheng, Michael D. Bentley
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Publication number: 20090215988Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.Type: ApplicationFiled: March 30, 2009Publication date: August 27, 2009Applicant: Nektar Therapeutics AL, CorporationInventor: J. Milton Harris
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Publication number: 20090215910Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.Type: ApplicationFiled: April 30, 2009Publication date: August 27, 2009Applicant: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Patent number: 7579444Abstract: Conjugates of a Factor IX moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided (among other things) are compositions comprising the conjugates, methods of making the conjugates, and methods of administering to a patient compositions comprising the conjugates.Type: GrantFiled: June 30, 2005Date of Patent: August 25, 2009Assignee: Nektar Therapeutics AL, CorporationInventors: Mary J. Bossard, Gayle Stephenson
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Patent number: 7569214Abstract: A method is provided for preparing water-soluble polymer derivatives bearing a terminal carboxylic acid or ester thereof. The method involves the hydrolyzing an ortho ester of a water-soluble polymer so as provide the corresponding acid. In addition, the invention provides water-soluble polymers bearing a terminal carboxylic acid or ester thereof, intermediates and reagents useful in carrying out the method, as well as gels, pharmaceutical formulations, conjugates related to the described water-soluble polymer derivatives.Type: GrantFiled: September 9, 2003Date of Patent: August 4, 2009Assignee: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Publication number: 20090186984Abstract: An activated, substantially water-soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated (polyethylene glycol) and the biologically active agent.Type: ApplicationFiled: March 24, 2009Publication date: July 23, 2009Applicant: Nektar Therapeutics AL, CorporationInventors: J. Milton Harris, Antoni Kozlowski
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Patent number: 7547509Abstract: The present invention provides variants of cyanovirin-N and water-soluble polymer conjugates thereof, and methods of preparing such conjugates. The cyanovirin-N of the invention are particularly suited for site-selective covalent attachment of one or more water soluble polymers, to provide polymer conjugates of cyanovirin-N variants exhibiting antiviral activity.Type: GrantFiled: August 2, 2007Date of Patent: June 16, 2009Assignees: Nektar Therapeutics AL, Corporation, National Institute of HeatlhInventors: M. Elizabeth Snell, Michael J. Roberts, Toshiyuki Mori, Barry R. O'Keefe, Michael R. Boyd
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Patent number: 7544738Abstract: The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non-peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcarbonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid, such as lysine, to form an amino acid derivative.Type: GrantFiled: April 25, 2008Date of Patent: June 9, 2009Assignee: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski
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Patent number: 7528202Abstract: An activated, substantially water-soluble poly(ethylene glycol) is provided having of a linear or branched poly(ethylene glycol) backbone and at least one terminus linked to the backbone through a hydrolytically stable linkage, wherein the terminus is branched and has proximal reactive groups. The free reactive groups are capable of reacting with active moieties in a biologically active agent such as a protein or peptide thus forming conjugates between the activated (polyethylene glycol) and the biologically active agent.Type: GrantFiled: April 30, 2007Date of Patent: May 5, 2009Assignee: Nektar Therapeutics AL, CorporationInventors: J. Milton Harris, Antoni Kozlowski
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Patent number: 7511095Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the ?-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ?-amine of a polypeptide having a cytokine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.Type: GrantFiled: February 13, 2006Date of Patent: March 31, 2009Assignee: Nektar Therapeutics AL, CorporationInventors: Michael J. Roberts, Zhihao Fang
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Patent number: 7511094Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.Type: GrantFiled: March 13, 2006Date of Patent: March 31, 2009Assignee: Nektar Therapeutics AL, CorporationInventor: Antoni Kozlowski