Abstract: The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. 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.
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:
January 17, 2017
Date of Patent:
March 6, 2018
Assignee:
Nektar Therapeutics
Inventors:
Sean M. Culbertson, Xiaoming Shen, Antoni Kozlowski, Samuel P. McManus
Abstract: Conjugates of an interleukin-2 (“IL-2”) 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, methods of administering compositions to an individual, nucleic acid sequences, expression systems, host cells, and methods for preparing IL-moieties.
Type:
Grant
Filed:
November 11, 2011
Date of Patent:
January 9, 2018
Assignee:
Nektar Therapeutics
Inventors:
Mary J. Bossard, Cherie F. Ali, Xiaofeng Liu, Deborah H. Charych, Yujun Wang
Abstract: 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.
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:
Grant
Filed:
December 23, 2011
Date of Patent:
November 28, 2017
Assignee:
Nektar Therapeutics
Inventors:
Sean M. Culbertson, Antoni Kozlowski, Tony Drew Vinson
Abstract: 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.
Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water—soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water—soluble oligomer.
Type:
Grant
Filed:
November 2, 2016
Date of Patent:
November 28, 2017
Assignee:
Nektar Therapeutics
Inventors:
Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
Abstract: Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.
Type:
Grant
Filed:
June 27, 2014
Date of Patent:
November 14, 2017
Assignee:
Nektar Therapeutics
Inventors:
Neel K. Anand, Franco J. Duarte, Wen Zhang, Zhongxu Ren
Abstract: 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.
Type:
Grant
Filed:
May 2, 2016
Date of Patent:
November 7, 2017
Assignee:
Nektar Therapeutics
Inventors:
Xuan Zhao, Michael David Bentley, Zhongxu Ren, Tacey X. Viegas
Abstract: 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.
Type:
Grant
Filed:
November 26, 2014
Date of Patent:
October 31, 2017
Assignee:
Nektar Therapeutics
Inventors:
Michael A. Eldon, Shibani S. Harite, Tamra L. Barker
Abstract: The invention provides water-soluble oligomer-beta blocker drug conjugates. A drug conjugate of the invention can be administered by any of a number of administration routes and exhibits properties that are different from the corresponding beta blocker not attached to the water-soluble oligomer.
Type:
Grant
Filed:
March 12, 2008
Date of Patent:
October 10, 2017
Assignee:
Nektar Therapeutics
Inventors:
Jennifer Riggs-Sauthier, Franco J. Duarte
Abstract: The present invention provides among other things a composition of a polymeric reagent and an antioxidant, such as butylated hydroxyl toluene.
Type:
Grant
Filed:
June 1, 2016
Date of Patent:
October 3, 2017
Assignee:
Nektar Therapeutics
Inventors:
Michael D. Bentley, Sean M. Culbertson, Samuel P. McManus
Abstract: 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.
Type:
Grant
Filed:
August 7, 2015
Date of Patent:
September 19, 2017
Assignee:
Nektar Therapeutics
Inventors:
Yujun Wang, Haim Moskowitz, Xiaofeng Liu, Steven O. Roczniak, Mary J. Bossard
Abstract: Methods, systems, and devices are described for sealing a nebulizer's liquid reservoir. A nebulizer liquid reservoir may be provided that is in fluid communication with an aerosol generator. The nebulizer liquid reservoir may have an open end and a headspace. A cap may be placed on the open end of the nebulizer liquid reservoir, wherein the cap partially fills the headspace of the nebulizer liquid reservoir. The cap can include a plunger that passes through the cap and allows for air to escape from the headspace of the nebulizer liquid reservoir through the cap. The cap can seal the nebulizer liquid reservoir by actuating the plunger to a locked position. The plunger may create an airtight seal with the cap when in the locked position. An ambient pressure may be maintained in the sealed nebulizer liquid reservoir until a portion of the liquid is dispensed.
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:
Grant
Filed:
April 12, 2016
Date of Patent:
August 15, 2017
Assignee:
Nektar Therapeutics
Inventors:
Antoni Kozlowski, Jon McKannan, Samuel P. McManus
Abstract: 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.
Type:
Grant
Filed:
September 6, 2013
Date of Patent:
August 8, 2017
Assignee:
Nektar Therapeutics
Inventors:
Wen Zhang, Xuyuan Gu, Stephanie Allums-Donald, Jennifer Riggs-Sauthier
Abstract: 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.
Type:
Grant
Filed:
April 13, 2016
Date of Patent:
July 11, 2017
Assignee:
Nektar Therapeutics
Inventors:
Peter York, Boris Yu Shekunov, Mahboob Ur Rehman, Jane Catherine Feeley
Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Type:
Grant
Filed:
November 27, 2014
Date of Patent:
June 27, 2017
Assignee:
Nektar Therapeutics
Inventors:
Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
Abstract: 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.
Abstract: Solid forms of certain opioid agonists are provided herein. Methods of preparing the solid forms, methods of using the solid forms, and pharmaceutical compositions comprising the solid forms are also provided herein.
Type:
Grant
Filed:
October 29, 2013
Date of Patent:
June 20, 2017
Assignee:
Nektar Therapeutics
Inventors:
Patricia Andres, Yogesh Datar, Ramakrishna Gadiraju, Bruce Andrew Kowalczyk, Gabriel Christian Kuklis, Mahmoud Mirmehrabi, Nicholas Paschalides