Patent application number | Description | Published |
20080299069 | Polymer Derivatives Comprising an Acetal or Ketal Branching Point - The invention provides a polymer comprising (i) a first water-soluble polymer segment that is covalently attached, either directly or through one or more atoms, to a first oxygen atom that is covalently attached to a linking carbon atom; (ii) a second water-soluble polymer segment is covalently attached, either directly or through one or more atoms, to a second oxygen atom that is covalently attached to the linking carbon atom; and (iii) a reactive group that is covalently attached, either directly or through one or more atoms, to the linking carbon atom. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like. | 12-04-2008 |
20080319091 | Polymer Derivatives Comprising an Imide Branching Point - The invention provides a water-soluble polymer comprising (i) an imide group comprising a linking nitrogen atom, a first carbonyl group covalently attached to the linking nitrogen atom, and a second carbonyl group covalently attached to the linking nitrogen atom; (ii) a first water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the first carbonyl group of the imide group and (iii) a second water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the second carbonyl group of the imide group. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like. | 12-25-2008 |
20090012241 | Hydrolytically stable maleimide-terminated polymers - The present invention is directed to hydrolytically stabilized maleimide-functionalized water soluble polymers and to methods for making and utilizing such polymers and their precursors. | 01-08-2009 |
20100004428 | Method of Preparing Propionic Acid-Terminated Polymers - The invention provides methods for preparing polymers bearing a terminal propionic acid. The method involves first reacting a water soluble and non-peptidic polymer comprising at least one hydroxyl group with a tertiary alkyl acrylate in the presence of a catalyst to form a propionic acid ester of the polymer, wherein the polymer has a weight average molecular weight of at least about 10,000 Da; and then treating the propionic acid ester of the polymer with a strong acid to form a propionic acid of the polymer. | 01-07-2010 |
20100010158 | 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. | 01-14-2010 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
20120238640 | Polymer Derivatives Comprising an Imide Branching Point - The invention provides a water-soluble polymer comprising (i) an imide group comprising a linking nitrogen atom, a first carbonyl group covalently attached to the linking nitrogen atom, and a second carbonyl group covalently attached to the linking nitrogen atom; (ii) a first water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the first carbonyl group of the imide group and (iii) a second water-soluble polymer segment covalently attached, either directly or through one or more atoms, to the second carbonyl group of the imide group. The invention also provides, among other things, methods for preparing polymers, conjugates, pharmaceutical compositions and the like. | 09-20-2012 |
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 |
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 |
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 |
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 |
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 |