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Nektar Therapeutics

Nektar Therapeutics Patent applications
Patent application numberTitlePublished
20120123065Hydrolytically Stable Maleimide-Terminated Polymers - The present invention is directed to conjugates of hydrolytically stabilized maleimide-functionalized water soluble polymers and to methods for making and utilizing such polymers and their precursors.05-17-2012
20120122871Oligomer-Containing Substituted Aromatic Triazine Compounds - The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.05-17-2012
20120118284NEGATIVELY BIASED SEALED NEBULIZERS SYSTEMS AND METHODS - Methods, systems, and devices are described for creating a negative bias pressure within a liquid reservoir. Embodiments may include providing a liquid reservoir coupled with an aerosol generator. The liquid reservoir may be sealed to create the sealed reservoir. An ambient pressure may be maintained while the liquid reservoir is being sealed and the ambient pressure may be maintained in the sealed liquid reservoir until a portion of the liquid is dispensed. Further, embodiments may include vibrating the aperture plate to dispense the portion of the liquid. The portion of the liquid dispensed may decreases the amount of the liquid in the sealed reservoir. By decreasing the amount of liquid in the sealed reservoir, a negative bias pressure between an air side and a liquid side of the aperture plate may be created.05-17-2012
20120111963SYSTEMS AND METHODS FOR DRIVING SEALED NEBULIZERS - Various methods, devices, and systems are described for aerosolizing a liquid. Embodiments may include sealing the liquid within a reservoir. An output waveform signal may be generated. A nebulizer element may be vibrated to aerosolize the liquid. A negative pressure may be produced within the reservoir as the liquid is aerosolized. The output waveform signal may cause the nebulizer element to vibrate. Embodiments may involve determining a phase shift between a current of the output waveform signal and a voltage of the output waveform signal. Also, embodiments may involve adjusting a frequency of the output waveform signal at least partially based on the phase shift. Further, embodiments may involve adjusting the voltage of the output waveform signal at least partially based on the frequency of the output waveform signal.05-10-2012
20120108785Hydrolytically Degradable Polymers and Hydrogels Made Therefrom - Methods for preparing a poly(ether carbonates) of the formula HO—[(CH05-03-2012
20120108501Protease Inhibitors - The invention relates to (among other things) protease inhibitors containing both a water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over protease inhibitor compounds lacking the water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue.05-03-2012
20120101145Oligomer-Containing Pyrrolidine Compounds - The invention relates to (among other things) oligomer-containing pyrrolidine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.04-26-2012
20120100096CONJUGATES PF SMALL-INTERFERING NUCLEIC ACIDS - The present invention relates to conjugates of small-interfering nucleic acids (siNA). Compositions of siNA suited for administration to a patient are described. Methods for delivering the compositions are also described.04-26-2012
20120094998Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.04-19-2012
20120088927Methods for the Formation of Hydrogels Using Thiosulfonate Compositions and Uses Thereof - The present invention provides both crosslinked polymer compositions capable of forming hydrogels upon exposure to an aqueous environment and thiosulfonate hydrogel-forming components. The thiosulfonate hydrogel-forming components of the invention are preferably multi-arm thiosulfonate polymer derivatives that form a crosslinked polymer composition when exposed to a base without requiring the presence of a second cross-linking reagent, redox catalyst, or radiation. Methods for forming hydrogel compositions, as well as methods for using the hydrogels, are also provided.04-12-2012
20120071627Soluble, Degradable Poly(ethylene glycol) Derivatives for Controllable Release of Bound Molecules into Solution - 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.03-22-2012
20120071492Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.03-22-2012
20120071491Oligomer-Protein Tyrosine Kinase Inhibitor Conjugates - The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.03-22-2012
20120065429WATER-SOLUBLE POLYMER ALKANALS - 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.03-15-2012
20120065330Thioester-Terminated Water Soluble Polymers and Method of Modifying the N-Terminus of a Polypeptide Therewith - The invention provides reagents and methods for conjugating a polymer specifically to the α-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 α-amine of a polypeptide having a cysteine 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.03-15-2012
20120046422Multi-Arm Block Copolymers as Drug Delivery Vehicles - 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.02-23-2012
20120046279Oligomer-Phenothiazine Conjugates - The invention relates to (among other things) oligomer-phenothiazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated phenothiazine compounds.02-23-2012
20120041155Method of Preparing Carboxylic Acid Functionalized Polymers - Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═O)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.02-16-2012
20120027714Segmented Polymers and Their Conjugates - Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.02-02-2012
20120022220Method for Preparing Polymer Maleimides - Methods for preparing polymeric reagents bearing a maleimide are provided. Also provided are related compositions.01-26-2012
20120022063Oligomer-Cannabinoid Conjugates - The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.01-26-2012
20120004422Intermediates Useful in the Preparation of Maleimide Functionalized Polymers - Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.01-05-2012
20120004242Oligomer-Diarylpiperazine Conjugates - The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.01-05-2012
20110318322Conjugates of a Lysosomal Enzyme Moiety and a Water Soluble Polymer - Conjugates of a lysosomal enzyme moiety and one or more non-peptidic water soluble polymers are provided. Typically, the non-peptidic water soluble polymer is a poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising such conjugates, methods of making the conjugates, and methods of administering the compositions to a patient, e.g., for treatment of a lysosomal storage disease.12-29-2011
20110269789Compositions and Methods for Achieving Sustained Therapeutic Drug Concentrations in a Subject - Provided herein are compounds and methods for achieving a sustained therapeutic effect of small molecule anti-cancer agents when administered in vivo.11-03-2011
20110269677Oligomer-Protease Inhibitor Conjugates - The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.11-03-2011
20110262379Maleamic Acid Polymer Derivatives and Their Bioconjugates - The present invention is directed a method comprising administering a composition to an individual, wherein the composition comprises a plurality of conjugates, each conjugate in the plurality a protein derivatized with a water-soluble polymer, wherein the polymer is coupled to the protein via succinimide groups covalently attached to either cysteine sulfhydryl groups or lysine amino groups, and substantially all of the succinimide groups present in the composition are present in a ring-opened form.10-27-2011
20110257106Polymer Stabilized Neuropeptides - A substantially hydrophilic conjugate is provided having a peptide that is capable of passing the blood-brain barrier covalently linked to a water-soluble nonpeptidic polymer such as polyethylene glycol. The conjugate exhibits improved solubility and in vivo stability and is capable of passing the blood-brain barrier of an animal.10-20-2011
20110237747Multi-Arm Polypeptide-Poly(ethylene glycol) Block Copolymers as Drug Delivery Vehicles - The invention provides a multi-arm block copolymer for use in delivering a variety of bioactive agents. The copolymer of the invention contains a central core from which extend multiple (3 or more) copolymer arms. Each copolymer arm possesses an inner polypeptide segment and an outer hydrophilic polymer segment. Thus, the overall structure of the copolymer comprises an inner core region that includes the central core and the inner polypeptide segment, while the outer core region is hydrophilic in nature. The multi-arm copolymer of the invention is particularly useful for delivery of biologically active agents that can be entrapped within the inner core region.09-29-2011
20110237746Method Involving 1-Benzotriazolyl Carbonate Esters of Polymers - The invention provides a method comprising the steps of (i) reacting a water-soluble and non-peptidic polymer having two or more terminal hydroxyl groups with di(1-benzotriazolyl)carbonate to form a water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups; and (ii) reacting the water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups with a water-soluble and non-peptidic polymer having three or more primary amino groups under conditions effective to form a cross-linked polymer composition.09-29-2011
20110237614Pegylated Opioids with Low Potential for Abuse - The invention provides opioid agonists covalently bound to a water-soluble oligomer having reduced potential for substance abuse and uses thereof. The compounds of the invention possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.09-29-2011
20110237524POLYMER CONJUGATES OF AOD-LIKE PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.09-29-2011
20110230618Polymeric Alpha-Hydroxy Aldehyde and Ketone Reagents and Conjugation Method - Provided herein are polymeric α-hydroxy aldehyde or α-hydroxy ketone reagents which can be conjugated to amine-containing compounds to form stable conjugates in a single-step reaction. In selected embodiments, the polymeric reagent itself incorporates an internal proton-abstracting (basic) functional group, to promote more efficient reaction. The substituent is appropriately situated, via a linker if necessary, to position the group for proton abstraction, preferably providing a 4- or 5-bond spacing between the abstracting atom and the hydrogen atom on the α-carbon. Also provided are methods of using the reagents and stable, solubilized conjugates of the reagents with biologically active compounds. In preferred embodiments, the polymeric component of the reagent or conjugate is a polyethylene glycol.09-22-2011
20110213013Complexes of Small-Interfering Nucleic Acids - The present invention relates to complexes of small-interfering nucleic acids (siNA). Compositions of siNA suited for administration to a patient are described. Methods for delivering the compositions are also described.09-01-2011
20110207896Sterically Hindered Poly(ethylene glycol) Alkanoic Acids and Derivatives Thereof - The invention provides a sterically hindered polymers and conjugates formed therefrom that comprise a water-soluble and non-peptidic polymer backbone having at least one terminus covalently bonded to an alkanoic acid or alkanoic acid derivative prior to conjugation, wherein the carbon adjacent to the carbonyl group of the acid or acid derivative group has an alkyl or aryl group pendent thereto. The steric effects of the alkyl or aryl group allow greater control of the hydrolytic stability of polymer derivatives. The polymer backbone may be poly(ethylene glycol).08-25-2011
20110200550Multi-Arm Polymeric Alkanoate Conjugates - Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.08-18-2011
20110195940Protease Inhibitors Having Enhanced Features - Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. Exemplary potent HIV protease inhibitors are mono-m-PEG3-atazanavir, mPEGn-N-darunavir (wherein n is 3 or 5), mPEGn-NHCO-saquinavir (wherein n is 5 or 7), and di-mPEG3-atazanavir.08-11-2011
20110195912Oligomer-Protease Inhibitor Conjugates - Provided are small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water soluble oligomer.08-11-2011
20110190209CONJUGATES HAVING A RELEASABLE LINKAGE - The present invention provides conjugates having a releasable linkage. Methods of making conjugates, and methods for administering conjugates, are also provided.08-04-2011
20110178242Methods for Forming Polymer-Drug Conjugates - Methods for preparing polymer-drug conjugates are provided. The disclosed methods involve polymeric reagents comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble polymer and a reactive group. Related methods, compositions, preparations, and so forth are also provided.07-21-2011
20110171716CARBOHYDRATE-BASED DRUG DELIVERY POLYMERS AND CONJUGATES THEREOF - Provided herein are water-soluble carbohydrate polymers which are monoderivatized at their reducing terminus, such that the carbohydrate polymers can be selectively conjugated at a single location. Also provided are methods of preparation and conjugation of the monoderivatized carbohydrate polymers.07-14-2011
20110171312MODIFIED THERAPEUTIC PEPTIDES, METHODS OF THEIR PREPARATION AND USE - Modified therapeutic peptide compositions comprising conjugates of therapeutic peptides covalently coupled to one or more hydrophilic polymers. Optionally, the therapeutic peptide is also covalently coupled to one or more moieties having one to ten carbon atoms. Methods of making and use are also provided. The conjugates, when administered by any of a number of administration routes, exhibit characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer and/or one or moiety having one to ten carbon atoms.07-14-2011
20110171164POLYMER CONJUGATES OF GLP-2-LIKE PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.07-14-2011
20110171163POLYMER CONJUGATES OF ZICONOTIDE PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.07-14-2011
20110171162POLYMER CONJUGATES OF THYMOSIN ALPHA 1 PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.07-14-2011
20110171161POLYMER CONJUGATES OF PROTEGRIN PEPTIDES - The invention provides protegrin that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention has enhanced half-life and/or reduced clearance.07-14-2011
20110171160POLYMER CONJUGATES OF KISS1 PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.07-14-2011
20110166063POLYMER CONJUGATES OF THERAPEUTIC PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water-soluble oligomer.07-07-2011
20110165113POLYMER CONJUGATES OF V681-LIKE PEPTIDES - The invention provides peptides that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water-soluble oligomer.07-07-2011
20110165112POLYMER CONJUGATES OF C-PEPTIDES - The invention provides pro insulin c-peptides that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water soluble oligomer.07-07-2011
20110165111POLYMER CONJUGATES OF NESIRITIDE PEPTIDES - The invention provides nesiritide that is chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of nesiritide not attached to the water-soluble oligomer.07-07-2011
20110160186Methods of Treating CYP2D6 Alternative Metabolizers - The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.06-30-2011
20110135623Conjugates of a Cholinesterase Moiety and a Polymer - Conjugates of a cholinesterase moiety and one or more nonpeptidic, water soluble polymers are provided. Typically, the nonpeptidic, water soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising conjugates, methods of making conjugates, and methods of administering compositions to a patient.06-09-2011
20110135592Hydrolytically Degradable Polymers and Hydrogels Made Therefrom - Methods for delivering a biologically active agent into the body of a mammal are provided, the method comprising administering a carbamate-containing conjugate to the mammal.06-09-2011
20110130539Method of Preparing Carboxylic Acid Functionalized Polymers - Methods for preparing water soluble, non-peptidic polymers carrying carboxyl functional groups, particularly carboxylic acid functionalized poly(ethylene glycol) (PEG) polymers are disclosed, as are the products of these methods. In general, an ester reagent R(C═0)OR′, wherein R′ is a tertiary group and R comprises a functional group X, is reacted with a water soluble, non-peptidic polymer POLY-Y, where Y is a functional group which reacts with X to form a covalent bond, to form a tertiary ester of the polymer, which is then treated with a strong base in aqueous solution, to form a carboxylate salt of the polymer. Typically, this carboxylate salt is then treated with an inorganic acid in aqueous solution, to convert the carboxylate salt to a carboxylic acid, thereby forming a carboxylic acid functionalized polymer.06-02-2011
20110112277Stabilized Polymeric Thiol Reagents - Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y—S—W]05-12-2011
20110108025AEROSOLIZATION DEVICE - An aerosol transfer device (05-12-2011
20110105438Oligomer-Foscarnet Conjugates - The invention relates to (among other things) oligomer-foscarnet conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated foscarnet compounds.05-05-2011
20110098273Oligomer-Calcium Channel Blocker Conjugates - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.04-28-2011
20110077362Branched Polymers - The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through ether linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)03-31-2011
20110071207Oligomer-Aryloxy-Substituted Propanamine Conjugates - The invention relates to (among other things) oligomer-aryloxy-substituted propanamine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated aryloxy-substituted propanamine compounds.03-24-2011
20110071093Novel Reagents - Oligomeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble, non-peptidic oligomer and a pharmaceutically active agent. The oligomeric reagents are useful for, among other things, forming oligomer active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.03-24-2011
20110065862Thioester-Terminated Water Soluble Polymers and Method of Modifying the N-Terminus of a Polypeptide Therewith - The invention provides reagents and methods for conjugating a polymer specifically to the α-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 α-amine of a polypeptide having a cysteine 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.03-17-2011
20110046315Method for Preparing Conjugates Using Polymer Maleimides - Methods for preparing conjugates using polymeric reagents bearing a maleimide are provided. Also provided are compositions comprising the conjugates.02-24-2011
20110034737Water-Soluble Polymer Alkanals - 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.02-10-2011
20110034643Thiol-Selective Water-Soluble Polymer Derivatives - The present invention provides water-soluble, polymer derivatives having a thiol-selective terminus suitable for selective coupling to thiol groups, such as those contained in the cysteine residues of proteins, as well as methods for preparing the water-soluble, polymer derivatives having a thiol-selective terminus.02-10-2011
20110021761Segmented Polymers and Their Conjugates - Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.01-27-2011
20110020422Hydroxyapatite-Targeting Poly(ethylene glycol) and Related Polymers - Isolatable, hydroxyapatite-targeting polymeric structures, and biologically active conjugates thereof, are provided. The polymeric structure includes a linear or branched water-soluble and non-peptidic polymer backbone, such as a PEG backbone, having at least two termini, a first terminus being covalently bonded to a hydroxyapatite-targeting moiety, such as a bisphosphonate, and a second terminus covalently bonded to a chemically reactive group, wherein said chemically reactive group is protected or unprotected. Methods of preparing and using hydroxyapatite-targeting polymeric structures, and biologically active conjugates thereof, are also provided.01-27-2011
20110018181ELASTOMER COMPONENTS THAT CAN BE PRESTRESSED BY PRESSURE MEANS AND METHOD FOR THE PRODUCTION THEREOF - Elastomer components (01-27-2011
20110009446OLIGOMER-GUANIDINE CLASS CONJUGATES - The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.01-13-2011
20100317707Oligomer-Nitroimidazole Anti-Infective Conjugates - The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer.12-16-2010
20100317705Oligomer-Dantrolene Conjugates and Related Compounds - The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.12-16-2010
20100303753Oligomer Conjugates of Lidocaine and Its Derivatives - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.12-02-2010
20100298496MULTI-ARMED, MONOFUNCTIONAL, AND HYDROLYTICALLY STABLE DERIVATIVES OF POLY(ETHYLENE GLYCOL) AND RELATED POLYMERS FOR MODIFICATION OF SURFACES AND MOLECULES - Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure11-25-2010
20100298296Oligomer-Tricyclic Conjugates - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.11-25-2010
20100286355Hydroxyapatite-Targeting Multiarm Polymers and Conjugates Made Therefrom - The present invention provides hydmoxyapatite-targeting, multiarm polymer reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatile-targeting moieties located at the terminus of one or more of the polymer chains. The multiarm polymers are optionally divided or separated by one or more degradable linkages into polymer segments having a molecular weight suitable for renal clearance. The polymeric reagents of the invention can have a substantially linear structure, although branched or multiarm structures are contemplated as well. The invention is suited for applications in which use of a high molecular weight polymer is desired, such as a total polymer number average molecular weight of at least about 30,000 Da for linear polymers and 20,000 Da for multiarm polymers. Each structure includes one or more linkages capable of degradation in vivo. The use of multiple hydroxyapatite-targeting moieties on each polymer molecule enhances the ability of the polymer reagent to selectively target and bind to hydroxyapatite surfaces, which in turn, can increase the concencentration of biologically active moiety delivered to the bone site.11-11-2010
20100286107Oligomer-Corticosteroid Conjugates - The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.11-11-2010
20100286084Oligomer-Nucleoside Phosphate Conjugates - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.11-11-2010
20100267895Hydrolytically Degradable Polymers and Hydrogels Made Therefrom - Conjugates between a protein and a water soluble polymer comprising multiple degradable carbonate linkages are provided.10-21-2010
20100261841Intermediates Useful in the Preparation of Maleimide Functionalized Polymers - Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.10-14-2010
20100249033POLYMER FACTOR IX MOIETY CONJUGATES - 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.09-30-2010
20100210505POLYMER CONJUGATES OF GLP-1 - 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.08-19-2010
20100197806Method Involving 1-Benzotriazolyl Carbonate Esters of Polymers - The invention provides a method comprising the steps of (i) reacting a water-soluble and non-peptidic polymer having two or more terminal hydroxyl groups with di(1-benzotriazolyl)carbonate to form a water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups; and (ii) reacting the water-soluble and non-peptidic polymer having two or more 1-benzotriazolylcarbonate ester groups with a water-soluble and non-peptidic polymer having three or more primary amino groups under conditions effective to form a cross-linked polymer composition.08-05-2010
20100190933MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.07-29-2010
20100184989De Novo Synthesis of Conjugates - The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.07-22-2010
20100184937Polymer Derivatives with Proximal Reactive Groups - An activated, substantially water-soluble polyoxazoline is provided having 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 polyoxazoline and the biologically active agent.07-22-2010
20100168232Oligomer-Anticholinergic Agent Conjugates - The invention provides anticholinergic agents that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the anticholinergic agent not attached to the water-soluble oligomer.07-01-2010
20100160610Conjugates of an EPO Moiety and a Polymer - Conjugates of an EPO moiety and one or more non-peptidic water-soluble polymers are provided. Typically, the non-peptidic water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising such conjugates, methods of making conjugates, and methods of administering compositions comprising such conjugates to a patient.06-24-2010
20100152414MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.06-17-2010
20100152201Oligomer-Antihistamine Conjugates - The invention provides antihistamine drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the antihistamine drug not attached to the water-soluble oligomer.06-17-2010
20100137511POLYMER FACTOR IX MOIETY CONJUGATES - 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.06-03-2010
20100130684POLYMER FACTOR IX MOIETY CONJUGATES - 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.05-27-2010
20100130428POLYMER FACTOR IX MOIETY CONJUGATES - 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.05-27-2010
20100130427POLYMER-FACTOR VIII MOIETY CONJUGATES - Conjugates of a Factor VIII 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 are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.05-27-2010
20100125049POLYMER FACTOR VIII MOIETY CONJUGATES - Conjugates of a Factor VIII 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 are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.05-20-2010
20100121019Sterically Hindered Poly(ethylene glycol) Alkanoic Acids and Derivatives Thereof - The invention provides a sterically hindered polymer that comprises a water-soluble and non-peptidic polymer backbone having at least one terminus covalently bonded to an alkanoic acid or alkanoic acid derivative, wherein the carbon adjacent to the carbonyl group of the acid or acid derivative group has an alkyl or aryl group pendent thereto. The steric effects of the alkyl or aryl group allow greater control of the hydrolytic stability of polymer derivatives. The polymer backbone may be poly(ethylene glycol).05-13-2010
20100120982POLYMER-FACTOR IX MOIETY CONJUGATES - 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.05-13-2010
20100120689POLYMER FACTOR VIII MOIETY CONJUGATES - Conjugates of a Factor VIII 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 are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.05-13-2010
20100113329Maleamic Acid Polymer Derivatives and Their Bioconjugates - The present invention is directed to maleamic acid derivatives of water soluble polymers, to chemically stable water-soluble polymer succinamic acid-active agent conjugates, and to methods for reproducibly preparing, characterizing and using such polymer reagents and their conjugates.05-06-2010
20100112607METHODS FOR DETERMINING ACTIVE INGREDIENTS IN PRO-DRUG PEG PROTEIN CONJUGATES WITH RELEASABLE PEG REAGENTS (IN VITRO DE-PEGYLATION) - The invention relates to the development of in vitro assay systems that force the release of a water-soluble polymer, such as polyethylene glycol (PEG) and polysialic acid (PSA), from proteins modified with a reversibly-linked water-soluble polymer. The invention includes methods for analyzing the release of the water-soluble polymer and measuring regained protein activity. The invention further includes methods appropriate for the quality control of proteins modified with releasable water-soluble polymers, including polymers like PEG and PSA.05-06-2010
20100105946Hydrolytically Degradable Carbamate Derivatives of Poly(Ethylene Glycol) - Poly(ethylene glycol) carbamate derivatives useful as water-soluble pro-drugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be either trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the amine drug at a controllable rate as the gel degrades.04-29-2010
20100069571Thioester-Terminated Water Soluble Polymers and Method of Modifying the N-Terminus of a Polypeptide Therewith - The invention provides reagents and methods for conjugating a polymer specifically to the α-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 α-amine of a polypeptide having a cysteine 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.03-18-2010
20100063328HETEROBIFUNCTIONAL POLY(ETHYLENE GLYCOL) DERIVATIVES AND METHODS FOR THEIR PREPARATION - This invention provides a method related to the preparation of derivatives of poly(ethylene glycol).03-11-2010
20100048707Polymeric Reagents Comprising a Terminal Vinylic Group and Conjugates Formed Therefrom - The present invention provides conjugates having a degradable linkage and polymeric reagents useful in preparing such conjugates. Methods of making polymeric reagents and conjugates, as well as methods for administering conjugates and compositions, are also provided.02-25-2010
20100048602Oligomer-Opioid Agonist Conjugates - The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.02-25-2010
20100021481CONJUGATES OF AN ANTI-TNF-ALPHA ANTIBODY - Conjugates of an anti-TNF antibody and one or more nonpeptidic water soluble polymers are provided. Typically, the nonpeptidic water soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising conjugates, methods of making conjugates, and methods of administering compositions to a patient.01-28-2010
20100004428Method of Preparing Propionic Acid-Terminated Polymers - The invention provides methods for preparing polymers bearing a terminal propionic acid. The method involves first reacting a water soluble and non-peptidic polymer comprising at least one hydroxyl group with a tertiary alkyl acrylate in the presence of a catalyst to form a propionic acid ester of the polymer, wherein the polymer has a weight average molecular weight of at least about 10,000 Da; and then treating the propionic acid ester of the polymer with a strong acid to form a propionic acid of the polymer.01-07-2010
20100004424Methods for the Formation of Hydrogels Using Thiosulfonate Compositions and Uses Thereof - The present invention provides both crosslinked polymer compositions capable of forming hydrogels upon exposure to an aqueous environment and thiosulfonate hydrogel-forming components. The thiosulfonate hydrogel-forming components of the invention are preferably multi-arm thiosulfonate polymer derivatives that form a crosslinked polymer composition when exposed to a base without requiring the presence of a second cross-linking reagent, redox catalyst, or radiation. Methods for forming hydrogel compositions, as well as methods for using the hydrogels, are also provided.01-07-2010
20100004392Hydrolytically Degradable Polymers and Hydrogels Made Therefrom - A water soluble polymer comprising multiple degradable carbonate linkages in a backbone and, for each carbonate linkage in the backbone, an oligomer linked thereto by the carbonate linkage, wherein the oligomer is branched.01-07-2010
20090288658Antibiotic Formulations, Unit Doses, Kits, and Methods - An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.11-26-2009
20090117193Compositions Comprising an Active Agent - The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention possesses superior aerosol properties and is thus preferred for aerosolized administration to the lung. Also provided are a method for (i) increasing the dispersibility of an active-agent containing formulation for administration to the lung, and (ii) delivery of the composition to the lungs of a subject.05-07-2009
20090095289Increased Dosage Metered Dose Inhaler - An aerosolization apparatus comprises a container containing a pharmaceutical formulation, the pharmaceutical formulation comprising an active agent and a propellant. The aerosolization apparatus further comprises a metering chamber in communication with the container, the metering chamber adapted to hold a metered amount of the pharmaceutical formulation, a valve to allow the metered amount of the pharmaceutical formulation to be released from the metering chamber when the valve is actuated, and a pressurizer that applies pressure to the pharmaceutical formulation in the metering chamber while the pharmaceutical formulation is being released from the metering chamber. In one version, the metering chamber is sized so that at least 2 mg, and preferably at least 5 mg, of the active agent is be aerosolized for delivery to a user during inhalation.04-16-2009
20090081302PULMONARY DELIVERY OF POLYENE ANTIFUNGAL AGENTS - The present invention provides spray-dried polyene compositions for oral inhalation to the lung. The polyene antifungal compositions demonstrate superior aerosol properties, do not exhibit appreciable degradation of the polyene upon spray-drying, and are useful in the treatment and prophylaxis of both pulmonary and systemic fungal infections.03-26-2009
20090035264STORAGE STABLE POWDER COMPOSITIONS OF INTERLEUKIN-4 RECEPTOR - The present invention provides storage stable dry powder compositions of IL-4R. The powder compositions demonstrate superior chemical and physical stability over their solution counterparts, particularly upon storage under varying conditions of temperature and humidity. Moreover, the powders, as prepared, possess good aerosol properties, which are maintained upon storage.02-05-2009
20090032427Receptacles and Kits, Such as for Dry Powder Packaging - A receptacle (02-05-2009
20080233194Dispersion for pulmonary delivery of a bioactive agent - Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.09-25-2008
20080230058Dry powder dispersing apparatus and methods for their use - The invention provides various apparatus and methods for aerosolizing a powdered medicament. In one exemplary embodiment, an apparatus includes a pressurization cylinder, and a piston which is slidable within the cylinder to pressurize a gas. A handle is coupled to the piston and is movable between an extended position and a home position to pressurize the gas. An aerosolizing mechanism is included and is configured to aerosolize a powdered medicament that is held within a receptacle with pressurized gas from the cylinder. A carriage assembly is included to receive the receptacle and to couple the receptacle to the aerosolizing mechanism. A first and a second interlock are operably engageable with the carriage assembly to prevent coupling of the receptacle with the aerosolization mechanism. The first interlock is released to allow movement of the carriage upon movement of the handle to the extended position. The second interlock remains engaged if the receptacle is only partially inserted into the carriage assembly.09-25-2008
20080214481Methods of Treatment of Endobronchial Infections - The present invention provides methods for the treatment of an endobronchial infection in a patient by administering to the endobronchial system of the patient a dry powder aerosol composition comprising from 90 to 130 mg of an aminoglycoside antibiotic one to three times a day for a first treatment period of 20 to 36 days.09-04-2008

Patent applications by Nektar Therapeutics