Nektar Therapeutics Patent applications |
Patent application number | Title | Published |
20160058958 | SYSTEMS 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. | 03-03-2016 |
20150340590 | VIBRATION SYSTEMS AND METHODS - In one arrangement, a vibration system includes a vibratable plate, a support member surrounding the vibratable plate, and a vibration-inducing member surrounding the support member. The vibration-inducing member is configured to radially expand and contract against the support member so as to produce axial vibration of the vibratable plate. In another arrangement, the vibratable plate has an outer circumference; a tubular member is concentrically disposed about the outer circumference of the plate, and an annular vibration-inducing member is concentrically disposed about the outer circumference of the tubular member. The vibration-inducing member is preferably a piezoelectric ring that is radially expandable and contractable against the wall of the tubular member to cause the plate to vibrate in the axial direction. | 11-26-2015 |
20150328331 | Compositions Comprising a Polymeric Reagent and a Pharmacologically Active Agent - Pharmaceutical compositions of conjugates are provided. The conjugates can be prepared by (among other ways) conjugating a pharmacologically active agent with a polymeric reagent that has a particular arrangement of atoms. Related methods, preparations, and so forth are also provided. | 11-19-2015 |
20150309032 | Method for Assessing and Predicting Efficacy of Breast Cancer Treatment with a Long-Acting Topoisomerase I Inhibitor - Provided is a method of treating an individual suffering from a cancer such as breast cancer by administering to the individual a long-acting topoisomerase I inhibitor such as SN-38 or irinotecan, and correlating the level of at least one tumor marker such as CA27.29 in the individual with response of the cancer to treatment with the long-acting topoisomerase I inhibitor, to thereby provide a method for predicting and assessing the therapeutic efficacy of the treatment. | 10-29-2015 |
20150283336 | NEGATIVELY BIASED SEALED NEBULIZER 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. | 10-08-2015 |
20150250894 | Oligomer-Containing Benzamide-Based Compounds - The invention relates to (among other things) oligomer-containing benzamide-based compounds. A compound of the invention exhibits one or more advantages over corresponding compounds lacking the oligomer. | 09-10-2015 |
20150197470 | CHEMICALLY MODIFIED SMALL MOLECULES - Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material. | 07-16-2015 |
20150174264 | Oligomer-Antihistamine 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. | 06-25-2015 |
20150141665 | METHODS FOR PREPARING POLYMERIC REAGENTS - The present invention provides among other things methods for preparing polymeric reagents, wherein the method comprises (a) providing an aromatic moiety bearing a hydroxy group, a first amino group and a second amino group; (b) reacting a functional group reagent with the hydroxy group to result in a hydroxy group bearing a functional group capable of reacting with an amino group of an active agent and resulting in a hydolyzable carbamate; and (c) reacting a plurality of poly(alkylene glycol) water-soluble polymers bearing a reactive group with the first amino group and second amino group to result in (i) a first amino group bearing a water-soluble polymer through a spacer moiety, and (ii) a second amino group bearing a second water-soluble polymer through a spacer moiety. | 05-21-2015 |
20150107489 | Heterobifunctional Poly(ethylene glycol) Derivatives and Methods for Their Preparation - This invention provides a method related to the preparation of derivatives of poly(ethylene glycol). | 04-23-2015 |
20150105519 | ACID SALT FORMS OF POLYMER-DRUG CONJUGATES AND ALKOXYLATION METHODS - Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate. | 04-16-2015 |
20150087668 | Methods for Treating Humans Having Brain Cancer - Among other things, a method of treating a human having brain cancer is, the method comprising administering via a non-continuous dosing regimen to the human having brain cancer, a therapeutically effective amount of a pharmaceutical composition comprising a prodrug or a pharmaceutically acceptable salt thereof, wherein the non-continuous dosing regimen comprises administering the pharmaceutical composition no more frequently than once every seven days for at least two dosings. | 03-26-2015 |
20150051371 | CARBOHYDRATE-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. | 02-19-2015 |
20140378404 | Treatment of Patients Suffering from Cancer - The invention relates to (among other things) a method comprising the steps of (a) administering to a patient a topoisomerase II-inhibiting amount of a long-acting topoisomerase II inhibitor; and (b) administering to the patient a topoisomerase I-inhibiting amount of a long-acting topoisomerase I inhibitor. | 12-25-2014 |
20140371258 | Water-Soluble Polymer Conjugates of Topotecan - Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same. | 12-18-2014 |
20140371168 | OLIGOMER-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 administration routes, exhibits advantages over previously administered compounds. | 12-18-2014 |
20140357659 | METHOD FOR PREDICTING AND EVALUATING RESPONSIVENESS TO CANCER TREATMENT WITH DNA-DAMAGING CHEMOTHERAPEUTIC AGENTS - Provided herein are methods directed to the prediction and early assessment of the efficacy of cancer treatment regimens, in particular in patients undergoing therapy with a DNA-damaging chemotherapeutic agent, by determining expression levels of certain proteins found to be useful as biomarkers in circulating tumor cells obtained from the patient both prior to and post-treatment. | 12-04-2014 |
20140330041 | THIOL-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. | 11-06-2014 |
20140329990 | Hydroxyapatite-Targeting Multiarm Polymers and Conjugates Made Therefrom - The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance. | 11-06-2014 |
20140329828 | Oligomer-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. | 11-06-2014 |
20140323565 | Oligomer-Calcimimetic Conjugates and Related Compunds - The invention relates to (among other things) oligomer-calcimimetic 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. | 10-30-2014 |
20140323529 | OLIGOMER-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. | 10-30-2014 |
20140303403 | CHEMICALLY MODIFIED SMALL MOLECULES - Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material. | 10-09-2014 |
20140256957 | N-Maleimidyl Polymer Derivatives - The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives. | 09-11-2014 |
20140256951 | STABILIZED POLYMERIC THIOL REAGENTS - Disclosed are water soluble polymeric thiol reagents. Also disclosed are uses for the polymeric thiol reagents and methods for preparing the polymeric thiol reagents. | 09-11-2014 |
20140256732 | OLIGOMER-CONTAINING SUBSTITUTED AROMATIC TRIAZINE COMPOUNDS - The invention relates to (among other things) methods for treatment comprising administering 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. | 09-11-2014 |
20140155412 | OLIGOMER-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. | 06-05-2014 |
20140141483 | POLYMER 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 polyethylene 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. | 05-22-2014 |
20140128619 | Intermediates 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. | 05-08-2014 |
20140113961 | MULTI-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. | 04-24-2014 |
20140107349 | Methods for Preparing Polymeric Reagents - The present invention provides among other things methods for preparing polymeric reagents, wherein the method comprises (a) providing an aromatic moiety bearing a hydroxy group, a first amino group and a second amino group; (b) reacting a functional group reagent with the hydroxy group to result in a hydroxy group bearing a functional group capable of reacting with an amino group of an active agent and resulting in a hydrolyzable carbamate; and (c) reacting a plurality of poly(alkylene glycol) water-soluble polymers bearing a reactive group with the first amino group and second amino group to result in (i) a first amino group bearing a water-soluble polymer through a spacer moiety, and (ii) a second amino group bearing a second water-soluble polymer through a spacer moiety. | 04-17-2014 |
20140100268 | OLIGOMER-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. | 04-10-2014 |
20140088021 | Water-Soluble Polymer-Linked Binding Moiety and Drug Compounds - Compounds comprising a binding moiety, water-soluble, non-peptidic polymer, and drug are provided. Also provided are methods preparing such compounds, compositions comprising such compounds and methods for administering and using such compounds and compositions. | 03-27-2014 |
20140080839 | OLIGOMER-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. | 03-20-2014 |
20140079782 | PARTICULATE MATERIALS - The present invention relates to active substances in particulate form, to methods for preparing them and to their uses. The present invention provides particulate powders, such as might be of use for delivery using a dry powder inhaler (DPI) or similar delivery device, having properties which may be beneficial to the DPI delivery process. | 03-20-2014 |
20140073802 | MALEIMIDYL POLYMER DERIVATIVES - The present invention provides, among other things, compounds that include a water-soluble and non-peptidic polymer as well as a maleimidyl group. The compounds are useful as, among other things, polymeric reagents. | 03-13-2014 |
20140051845 | Method Involving 1-Benzotriazolyl Carbonate Esters of Poly(ethylene glycol) - The invention provides for preparing a polymer-active agent conjugate, the method comprising the steps of reacting an amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate. | 02-20-2014 |
20140045770 | OLIGOMER-PROTEASE INHIBITOR 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 small molecule drug not attached to the water-soluble oligomer. | 02-13-2014 |
20140044672 | CONJUGATES OF A GM-CSF MOIETY AND A POLYMER - Conjugates of a GM-CSF 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 conjugates, methods of making conjugates, and methods of administering compositions comprising conjugates to a patient. | 02-13-2014 |
20140039205 | Method for Preparing Branched Functionalized Polymers Using Branched Polyol Cores - A method of preparing a multiarm polymer includes reacting a branched polyol with one or more functionalizing reagents to effect substitution of an ionizable functional group or a protected ionizable functional group, Y, to form a mixture comprising (i) unsubstituted branched polyol containing no Y groups; (ii) a monosubstituted polyol comprising one Y group, and (iii) a multisubstituted polyol (e.g., a disubstituted polyol comprising two Y groups); followed by purifying the mixture to separate the monosubstituted polyol from other species Thereafter, a water-soluble and non-peptidic polymer segment is attached to the monosubstituted branched polyol at the site of at least one of the hydroxyl groups. The invention also provides purified monosubstituted branched polyols and multiarm polymers prepared by the method and polyol precursors for use in the method. | 02-06-2014 |
20140039030 | POLYMER-DES-ETHYL SUNITINIB CONJUGATES - The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form. | 02-06-2014 |
20140039020 | Oligomer-Containing Hydantoin Compounds - The invention relates to (among other things) oligomer-containing hydantoin 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. | 02-06-2014 |
20140037697 | PARTICULATE MATERIALS - Embodiments of the invention relate to particles of active substances, methods for preparing the particles, formulations containing the particles, and metered dose inhalers containing such particles or formulations. In one embodiment, a composition of an aerosol formulation is provided and contains a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μm suspended in a hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v. The aerosol formulation exhibits a flocculation volume of about 85% or greater about 1 minute after mixing the particulate active substance and the hydrofluorocarbon fluid vehicle. The particulate active substance contains an alkaloid ergotamine, pharmaceutically acceptable salts thereof, analogues thereof, or derivatives thereof. In some examples, the alkaloid ergotamine contains dihydroergotamine, such as dihydroergotamine mesylate and the hydrofluorocarbon fluid vehicle contains HFA 134a, HFA 227ea, or mixtures thereof. | 02-06-2014 |
20140024845 | Non-Ring Hydroxy Substituted Taxanes and Methods for Synthesizing the Same - The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer. | 01-23-2014 |
20140020680 | Aerosolization Device - An aerosol transfer device for medical aerosol generators comprises a body, fluidically coupled to a nebulizer and to a patient interface. An ambient air intake is formed into a lower body. The body is shaped and configured to optimize mixing of ambient air from the ambient air intake and the aerosol generated by the nebulizer, resulting in the formation of an aerosol plume having optimum characteristics for delivery of the aerosol to the patient's pulmonary system, such as the central or deep lung regions. The shape and dimensions of the body are further designed to minimize aerosol deposition, thus improving delivery efficiency. | 01-23-2014 |
20140011855 | POLYMER-SEMAXANIB MOIETY CONJUGATES - The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form. | 01-09-2014 |
20140007864 | SYSTEMS AND METHODS FOR DRIVING NEBULIZERS - In various arrangements, a nebulizer element of a nebulizer may be energized with a drive signal. A phase offset of the drive signal may be measured. A phase delta may be determined. The phase delta may indicate a difference between a target phase offset and the measured phase offset. The target phase offset may indicate a non-zero target phase difference between the voltage of the drive signal and the current of the drive signal. A frequency of the drive signal may be changed to decrease the phase delta. | 01-09-2014 |
20140005419 | Method for Preparing a Polymer Conjugate | 01-02-2014 |
20130345298 | Multi-Arm Polymeric Prodrug Conjugates of Cabazitaxel-Based Compounds - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the cabazitaxel-based compound is achieved. | 12-26-2013 |
20130338216 | DEUTERATED AND/OR FLUORINATED TAXANE DERIVATIVES - The invention relates to (among other things) deuterated and/or fluorinated docetaxel and cabazitaxel and derivatives thereof, as well as compositions comprising each of the foregoing. | 12-19-2013 |
20130338204 | Oligomer-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. | 12-19-2013 |
20130338175 | Multi-Arm Polymeric Prodrug Conjugates of Pemetrexed-Based Compounds - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved. | 12-19-2013 |
20130331549 | Hydroxyapatite-Targeting Multiarm Polymers and Conjugates Made Therefrom - The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance. | 12-12-2013 |
20130331443 | MULTI-ARM POLYMERIC PRODRUG CONJUGATES OF TAXANE-BASED COMPOUNDS - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved. | 12-12-2013 |
20130331425 | POLYMER-SUNITINIB CONJUGATES - The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form. | 12-12-2013 |
20130317114 | Hydroxylated Tricyclic Compounds - The invention provides small molecule drugs 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 the characteristics of the small molecule drug not attached to the water-soluble oligomer. | 11-28-2013 |
20130281634 | Method 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. | 10-24-2013 |
20130261072 | OLIGOMER CONJUGATES OF HETEROPENTACYCLIC NUCLEOSIDES - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer | 10-03-2013 |
20130253207 | N-MALEIMIDYL POLYMER DERIVATIVES - The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives. | 09-26-2013 |
20130253203 | Methods for Preparing Polymeric Reagents and Compositions of Polymeric Reagents - Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions. | 09-26-2013 |
20130231490 | METHOD FOR PREPARING WATER-SOLUBLE POLYMER DERIVATIVES BEARING AN N-SUCCINIMIDYL ESTER - A method is provided for preparing water-soluble polymer derivatives bearing a terminal N-succinimidyl ester. The method involves the hydrolyzing an ortho ester of a water-soluble polymer so as provide the corresponding acid and subsequently esterifying the acid. | 09-05-2013 |
20130231359 | Salt Form of a Multi-Arm Polymer-Drug Conjugate - Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate. | 09-05-2013 |
20130184443 | Methods for Preparing Conjugates - The present invention provides pharmaceutical compositions comprising a pharmaceutically acceptable excipient and a conjugate having a degradable linkage. The conjugates include at least one of each the following: an aromatic moiety comprising an ionizable hydrogen atom, a spacer moiety, and a water-soluble polymer. Methods for delivering such compositions are also provided. | 07-18-2013 |
20130177961 | MULTI-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 structure | 07-11-2013 |
20130158062 | MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically 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. | 06-20-2013 |
20130150441 | Oligomer-Anticholinergic Agent 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 as compared to the characteristics of the small molecule drug not attached to the water-soluble oligomer. | 06-13-2013 |
20130149355 | HYDROXYAPATITE-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. | 06-13-2013 |
20130144014 | MULTI-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. | 06-06-2013 |
20130143909 | Acid Salt Forms of Polymer-Drug Conjugates and Alkoxylation Methods - Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate. | 06-06-2013 |
20130096258 | POLYMER CONJUGATES OF GLP-1 - Conjugates of a GLP-1 moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-1 polymer conjugate may include a GLP-1 moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-1 polymer conjugate may include a GLP-1 moiety covalently attached to a water-soluble polymer, wherein the GLP-1 moiety possesses an N-methyl substituent. | 04-18-2013 |
20130079555 | Thiol-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. | 03-28-2013 |
20130079533 | Method for Preparing a Polymer Conjugate - Provided herein is a straightforward and efficient method for covalently attaching a polyethylene glycol polymer to a taxane. The method involves, among other things, a step of reacting a taxame with a polyethylene glycol polymer comprising a functional group reactive with a functional group within said taxane in the presence of a coupling reagent and DPTS. The result of the reacting step is the formation of a polyethylene glycol-taxane conjugate. | 03-28-2013 |
20130072709 | Segmented Degradable Polymers and Conjugates Made Therefrom - The present invention provides, among other things, segmented, degradable polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains divided or separated by one or more degradable linkages into polymer segments having a molecular weight suitable for renal clearance. The polymeric reagents can have a substantially linear structure, a branched structure, or a multiarm structure. Each structure includes one or more linkages capable of degradation in vivo. | 03-21-2013 |
20130059360 | POLYMER-BASED COMPOSITIONS AND CONJUGATES OF ANTIMICROBIAL AGENTS - Provided herein are water-soluble polymer conjugates and polymer-based compositions of antimicrobial agents. Also provided are methods for synthesizing and administering such conjugates and compositions. | 03-07-2013 |
20130053514 | Method Involving 1-Benzotriazolyl Carbonate Esters of Poly(ethylene glycol) - The invention provides a method comprising the steps of providing a poly(ethylene glycol) having one terminal hydroxyl group; reacting the terminal hydroxyl group of the poly(ethylene glycol) with di(1-benzotriazolyl)carbonate to form a 1-benzotriazolylcarbonate ester of the poly(ethylene glycol); reacting the 1-benzotriazolylcarbonate ester of the poly(ethylene glycol) with an amino acid to form an amino acid derivative; and reacting the amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate. | 02-28-2013 |
20130053400 | OLIGOMER-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. | 02-28-2013 |
20130040961 | OLIGOMER MODIFIED DIAROMATIC SUBSTITUTED COMPOUNDS - Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) PEG) oligomers. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds. | 02-14-2013 |
20130018190 | STEREOSELECTIVE REDUCTION OF A MORPHINONE - 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. | 01-17-2013 |
20130012442 | VON WILLEBRAND FACTOR- AND FACTOR VIII-POLYMER CONJUGATES HAVING A RELEASABLE LINKAGE - The present invention provides von Willebrand Factor-polymer conjugates and Factor VIII-polymer conjugates, each having a releasable linkage. Methods of making conjugates, methods for administering conjugates, are also provided. | 01-10-2013 |
20120322134 | BRANCHED 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-) | 12-20-2012 |
20120318701 | POLYMERIC 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. | 12-20-2012 |
20120302761 | INTERMEDIATES 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. | 11-29-2012 |
20120291777 | IDENTIFYING DRY NEBULIZER ELEMENTS - Various arrangements for determining whether a liquid is in contact with a nebulizer element are disclosed. A nebulizer element may be energized with an electrical signal at a measurement frequency. An impedance of the nebulizer element may be measured, thereby obtaining a measured impedance value. The impedance value may be compared to a stored impedance value. Based on the comparison, it may be determined whether the liquid contacts the nebulizer element. | 11-22-2012 |
20120289609 | METHODS 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. | 11-15-2012 |
20120271000 | COMPOSITIONS COMPRISING CONJUGATES AND MALEAMIC ACID-TERMINATED, WATER-SOLUBLE POLYMERS - Methods for preparing conjugates using polymeric reagents bearing a maleimide are provided. Also provided are compositions comprising the conjugates. | 10-25-2012 |
20120258985 | STABILIZED POLYMERIC THIOL REAGENTS - Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A] | 10-11-2012 |
20120258912 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR DELIVERING SUCH COMPOSITIONS - The present invention provides pharmaceutical compositions comprising a pharmaceutically acceptable excipient and a conjugate having a degradable linkage. The conjugates include at least one of each the following: an aromatic moiety comprising an ionizable hydrogen atom, a spacer moiety, and a water-soluble polymer. Methods for delivering such compositions are also provided. | 10-11-2012 |
20120245289 | POLYMER-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. | 09-27-2012 |
20120244597 | POLYMER 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. | 09-27-2012 |
20120238735 | Monoconjugated Chitosans as Delivery Agents for Small Interfering Nucleic Acids - Conjugates are provided, an exemplary conjugating having a single water-soluble, non-peptidic polymer, such as a poly(ethylene oxide), attached to a chitosan. Complexes of small interfering nucleic acids formed with such conjugates as well as small interfering nucleic acids attached to such conjugates are also provided. Related methods, intermediates, and compositions are also provided. | 09-20-2012 |
20120238621 | Oligomer-Calcimimetic Conjugates and Related Compounds - The invention relates to (among other things) oligomer-calcimimetic 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. | 09-20-2012 |
20120226022 | HYDROLYTICALLY 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. | 09-06-2012 |
20120214952 | Methods for Preparing Polymeric Reagents and Compositions of Polymeric Reagents - Methods for preparing active carbonate esters of water-soluble polymers are provided. Also provided are other methods related to the active carbonate esters of water-soluble polymers, as well as corresponding compositions. | 08-23-2012 |
20120209027 | Method for Preparing Water-Soluble Polymer Derivatives Bearing a Terminal Carboxylic Acid - 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. | 08-16-2012 |
20120195847 | POLYMER CONJUGATES OF BIPHALIN 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. | 08-02-2012 |
20120178692 | DOSAGE FORMS OF POLYMER-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. | 07-12-2012 |
20120142594 | Von Willebrand Factor- and Factor VIII-Polymer Conjugates Having a Releasable Linkage - The present invention provides von Willebrand Factor-polymer conjugates and Factor VIII-polymer conjugates, each having a releasable linkage. Methods of making conjugates, methods for administering conjugates, are also provided. | 06-07-2012 |
20120123065 | Hydrolytically 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 |
20120122871 | Oligomer-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 |
20120118284 | NEGATIVELY 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 |
20120111963 | SYSTEMS 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 |
20120108785 | Hydrolytically Degradable Polymers and Hydrogels Made Therefrom - Methods for preparing a poly(ether carbonates) of the formula HO—[(CH | 05-03-2012 |
20120108501 | Protease 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 |
20120101145 | Oligomer-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 |
20120100096 | CONJUGATES 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 |
20120094998 | Oligomer-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 |
20120088927 | Methods 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 |
20120071627 | Soluble, 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 |
20120071492 | Oligomer-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 |
20120071491 | Oligomer-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 |
20120065429 | WATER-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 |
20120065330 | Thioester-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 |
20120046422 | Multi-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 |
20120046279 | Oligomer-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 |
20120041155 | Method 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 |
20120027714 | Segmented 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 |
20120022220 | Method for Preparing Polymer Maleimides - Methods for preparing polymeric reagents bearing a maleimide are provided. Also provided are related compositions. | 01-26-2012 |
20120022063 | Oligomer-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 |
20120004422 | Intermediates 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 |
20120004242 | Oligomer-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 |
20110318322 | Conjugates 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 |
20110269789 | Compositions 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 |
20110269677 | Oligomer-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 |
20110262379 | Maleamic 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 |
20110257106 | Polymer 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 |
20110237747 | Multi-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 |
20110237746 | Method 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 |
20110237524 | POLYMER 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 |
20110230618 | Polymeric 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 |
20110213013 | Complexes 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 |
20110207896 | Sterically 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 |
20110200550 | Multi-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 |
20110195940 | Protease 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 |
20110195912 | Oligomer-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 |
20110190209 | CONJUGATES 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 |
20110178242 | Methods 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 |
20110171716 | CARBOHYDRATE-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 |
20110171312 | MODIFIED 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 |
20110171164 | POLYMER 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 |
20110171163 | POLYMER 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 |
20110171162 | POLYMER 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 |
20110171161 | POLYMER 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 |
20110171160 | POLYMER 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 |
20110166063 | POLYMER 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 |
20110165113 | POLYMER 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 |
20110165112 | POLYMER 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 |
20110165111 | POLYMER 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 |
20110160186 | Methods 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 |
20110135623 | Conjugates 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 |
20110135592 | Hydrolytically 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 |
20110130539 | Method 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 |
20110112277 | Stabilized Polymeric Thiol Reagents - Disclosed are water soluble polymeric reagents comprising the structure POLY-[Y—S—W] | 05-12-2011 |
20110108025 | AEROSOLIZATION DEVICE - An aerosol transfer device ( | 05-12-2011 |
20110105438 | Oligomer-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 |
20110098273 | Oligomer-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 |
20110077362 | Branched 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 |
20110071207 | Oligomer-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 |
20110071093 | Novel 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 |
20110065862 | Thioester-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 |
20110046315 | Method 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 |
20110034737 | Water-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 |
20110034643 | Thiol-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 |
20110021761 | Segmented 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 |
20110020422 | Hydroxyapatite-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 |
20110018181 | ELASTOMER COMPONENTS THAT CAN BE PRESTRESSED BY PRESSURE MEANS AND METHOD FOR THE PRODUCTION THEREOF - Elastomer components ( | 01-27-2011 |
20110009446 | OLIGOMER-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 |
20100317707 | Oligomer-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 |
20100317705 | Oligomer-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 |
20100303753 | Oligomer 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 |
20100298496 | MULTI-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 structure | 11-25-2010 |
20100298296 | Oligomer-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 |
20100286355 | Hydroxyapatite-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 |
20100286107 | Oligomer-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 |
20100286084 | Oligomer-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 |
20100267895 | Hydrolytically 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 |
20100261841 | Intermediates 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 |
20100249033 | POLYMER 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 |
20100210505 | POLYMER 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 |
20100197806 | Method 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 |
20100190933 | MULTI-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 |
20100184989 | De 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 |
20100184937 | Polymer 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 |
20100168232 | Oligomer-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 |
20100160610 | Conjugates 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 |
20100152414 | MULTI-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 |
20100152201 | Oligomer-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 |
20100137511 | POLYMER 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 |
20100130684 | POLYMER 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 |
20100130428 | POLYMER 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 |
20100130427 | POLYMER-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 |
20100125049 | POLYMER 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 |
20100121019 | Sterically 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 |
20100120982 | POLYMER-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 |
20100120689 | POLYMER 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 |
20100113329 | Maleamic 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 |
20100112607 | METHODS 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 |
20100105946 | Hydrolytically 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 |
20100069571 | Thioester-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 |
20100063328 | HETEROBIFUNCTIONAL 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 |
20100048707 | Polymeric 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 |