Patents by Inventor Antoni Kozlowski

Antoni Kozlowski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Method for Preparing Branched Functionalized Polymers Using Branched Polyol Cores
    Publication number: 20140039205
    Abstract: 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.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski
  • Multi-arm polymeric alkanoate conjugates
    Patent number: 8637466
    Abstract: 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.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: January 28, 2014
    Assignee: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Samuel P. McManus, Jennifer Riggs-Sauthier, Xiaoming Shen, Wen Zhang
  • Non-Ring Hydroxy Substituted Taxanes and Methods for Synthesizing the Same
    Publication number: 20140024845
    Abstract: 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.
    Type: Application
    Filed: December 22, 2011
    Publication date: January 23, 2014
    Applicant: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Samuel P. McManus
  • Methods for forming polymer-drug conjugates
    Patent number: 8633277
    Abstract: 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.
    Type: Grant
    Filed: March 8, 2011
    Date of Patent: January 21, 2014
    Assignee: Nektar Therapeutics
    Inventors: J. Milton Harris, Antoni Kozlowski, Samuel P. McManus, Michael D. Bentley, Stephen A. Charles
  • Multi-Arm Polymeric Prodrug Conjugates of Cabazitaxel-Based Compounds
    Publication number: 20130345298
    Abstract: 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.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 26, 2013
    Applicant: Nektar Therapeutics
    Inventor: Antoni Kozlowski
  • DEUTERATED AND/OR FLUORINATED TAXANE DERIVATIVES
    Publication number: 20130338216
    Abstract: 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.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 19, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Antoni Kozlowski, Timothy A. Riley, Samuel P. Mcmanus
  • MULTI-ARM POLYMERIC PRODRUG CONJUGATES OF TAXANE-BASED COMPOUNDS
    Publication number: 20130331443
    Abstract: 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.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 12, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Antoni Kozlowski, Timothy A. Riley, Samuel P. McManus
  • POLYMER-SUNITINIB CONJUGATES
    Publication number: 20130331425
    Abstract: 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.
    Type: Application
    Filed: December 23, 2011
    Publication date: December 12, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Sean M. Culbertson, Antoni Kozlowski, Tony Drew Vinson
  • Method for preparing functionalized polymers from polymer alcohols
    Patent number: 8604159
    Abstract: The present invention provides, among other things, methods for preparing functionalized and other polymers from polymer from polymer alcohols such as poly(ethylene glycol)s. In addition, polymer compositions, conjugates, polymeric reagents, are also provided.
    Type: Grant
    Filed: July 22, 2004
    Date of Patent: December 10, 2013
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, J. Milton Harris
  • Method for preparing branched functionalized polymers using branched polyol cores
    Patent number: 8568705
    Abstract: 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.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: October 29, 2013
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski
  • POLYMERIC ALPHA-HYDROXY ALDEHYDE AND KETONE REAGENTS AND CONJUGATION METHOD
    Publication number: 20130280783
    Abstract: Provided herein are polymeric ?-hydroxy aldehyde or ?-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 ?-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.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 24, 2013
    Inventors: Sean M. CULBERTSON, Xiaoming Shen, Antoni Kozlowski, Samuel P. McManus
  • STABILIZED POLYMERIC THIOL REAGENTS
    Publication number: 20130280206
    Abstract: Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 2, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Inventors: Antoni Kozlowski, Samuel P. Mcmanus
  • Method of Preparing Carboxylic Acid Functionalized Polymers
    Publication number: 20130281634
    Abstract: 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.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: J. Milton Harris, Antoni Kozlowski, Lihong Guo
  • Polymer derivatives comprising an acetal or ketal branching point
    Patent number: 8562965
    Abstract: 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.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: October 22, 2013
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski
  • Method involving 1-benzotriazolyl carbonate esters of poly(ethylene glycol)
    Patent number: 8563651
    Abstract: 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.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: October 22, 2013
    Assignee: Nektar Therapeutics
    Inventor: Antoni Kozlowski
  • Methods for Preparing Polymeric Reagents and Compositions of Polymeric Reagents
    Publication number: 20130253203
    Abstract: 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.
    Type: Application
    Filed: May 15, 2013
    Publication date: September 26, 2013
    Applicant: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Jon McKannan, Samuel P. McManus
  • Salt Form of a Multi-Arm Polymer-Drug Conjugate
    Publication number: 20130231359
    Abstract: 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.
    Type: Application
    Filed: November 18, 2010
    Publication date: September 5, 2013
    Applicant: Nektar Therapeutics
    Inventors: Anthony O. Chong, Seoju Lee, Bhalchandra V. Joshi, Brian Bray, Shaoyong Nie, Patrick L. Spence, Antoni Kozlowski, Samuel P. McManus, Sachin Tipnis, Greg Lavaty, David Swallow, John R. Handley, Anthony G. Schaefer
  • METHOD FOR PREPARING WATER-SOLUBLE POLYMER DERIVATIVES BEARING AN N-SUCCINIMIDYL ESTER
    Publication number: 20130231490
    Abstract: 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.
    Type: Application
    Filed: April 4, 2013
    Publication date: September 5, 2013
    Applicant: Nektar Therapeutics
    Inventor: Antoni Kozlowski
  • Polymeric alpha-hydroxy aldehyde and ketone reagents and conjugation method
    Patent number: 8492503
    Abstract: Provided herein are polymeric ?-hydroxy aldehyde or ?-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 ?-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.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: July 23, 2013
    Assignee: Nektar Therapeutics
    Inventors: Sean M. Culbertson, Xiaoming Shen, Antoni Kozlowski, Samuel P. McManus
  • Stabilized polymeric thiol reagents
    Patent number: 8492488
    Abstract: Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: July 23, 2013
    Assignee: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Samuel P. McManus