Patents by Inventor Stephen B. H. Kent

Stephen B. H. Kent 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).

  • Publication number: 20160223560
    Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.
    Type: Application
    Filed: February 1, 2016
    Publication date: August 4, 2016
    Inventors: Dana Ault-Riche, Stephen B.H. Kent, Sachdev S. Sidhu, Maruti Uppalapati
  • Patent number: 9285372
    Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: March 15, 2016
    Assignees: Reflexion Pharmaceuticals, Inc., The Governing Council of the University of Toronto
    Inventors: Dana Ault-Riche, Stephen B. H. Kent, Sachdev S. Sidhu, Maruti Uppalapati
  • Patent number: 8618049
    Abstract: Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include GluA4-ThrB30 ester insulin, in which side chains of GluA4 and ThrB30 of native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The ThrB30-GluA4 ester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: December 31, 2013
    Inventors: Stephen B. H. Kent, Youhei Soma
  • Publication number: 20120220522
    Abstract: Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include GluA4-ThrB30 ester insulin, in which side chains of GluA4 and ThrB30 of native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The ThrB30-GluA4 ester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.
    Type: Application
    Filed: September 7, 2010
    Publication date: August 30, 2012
    Inventors: Stephen B.H. Kent, Yohei Soma
  • Publication number: 20120178643
    Abstract: Methods and compositions for identifying D-peptidic compounds that specifically bind target proteins are provided. Aspects of the methods include screening libraries of 20 residue or more L-peptidic compounds for specific binding to 40 residue or more D-target proteins. Once a L-peptidic compound has been identified that specifically binds to the D-target protein, the D-enantiomer of that compound may be produced.
    Type: Application
    Filed: November 10, 2011
    Publication date: July 12, 2012
    Inventors: DANA AULT-RICHE, STEPHEN B. H. KENT, SACHDEV S. SIDHU, MARUTI UPPALAPATI
  • Patent number: 8034900
    Abstract: Water-soluble thioester and selenoester compounds, their generators, as well as methods for making and using the same, are provided. The subject thioester and selenoester compounds are characterized by including an amino acid synthon having a C-terminal group bonded to a water-soluble polymer through a thioester or selenoester linkage. Solid phase resins and protocols for generating the subject compounds are also provided. The subject water soluble thioester and selenoester compounds and generators find use in a variety of different applications, including thioester or selenoester mediated chemical ligation reactions.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: October 11, 2011
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Leslie Philip Miranda, Stephen B. H. Kent
  • Patent number: 7482425
    Abstract: The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: January 27, 2009
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Gerd. G. Kochendoerfer, Christie L. Hunter, Stephen B. H. Kent, Paolo Botti
  • Patent number: 7408026
    Abstract: Proteins of moderate size having native peptide backbones are produced by a method of native chemical ligation. Native chemical ligation employs a chemoselective reaction of two unprotected peptide segments to produce a transient thioester-linked intermediate. The transient thioester-linked intermediate then spontaneously undergoes a rearrangement to provide the full length ligation product having a native peptide bond at the ligation site. Full length ligation products are chemically identical to proteins produced by cell free synthesis. Full length ligation products may be refolded and/or oxidized, as allowed, to form native disulfide-containing protein molecules. The technique of native chemical ligation is employable for chemically synthesizing full length proteins.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: August 5, 2008
    Assignee: The Scripps Research Institute
    Inventors: Stephen B. H. Kent, Tom W. Muir, Philip E. Dawson
  • Patent number: 7341874
    Abstract: This invention provides for novel methods of identifying covalent modifications of an amino acid residue in a polypeptide chain by detecting mass differences.
    Type: Grant
    Filed: March 2, 2004
    Date of Patent: March 11, 2008
    Assignees: The Rockefeller University, The Scripps Research Institute
    Inventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
  • Patent number: 7118737
    Abstract: The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: October 10, 2006
    Assignee: Amylin Pharmaceuticals, Inc.
    Inventors: Gerd G. Kochendoerfer, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Christie L. Hunter, Stephen B. H. Kent, Donald W. Low, Jill G. Wilken
  • Patent number: 7094871
    Abstract: The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: August 22, 2006
    Assignee: Gryphon Therapeutics
    Inventors: Lynne Canne, Stephen B. H. Kent, Reyna Simon
  • Patent number: 7030217
    Abstract: The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: April 18, 2006
    Assignee: Gryphon Therapeutics, Inc.
    Inventors: Lynne Canne, Stephen B. H. Kent, Reyna Simon
  • Patent number: 7030218
    Abstract: The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: April 18, 2006
    Assignee: Gryphon Therapeutics
    Inventors: Christie L. Hunter, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Stephen B. H. Kent, Gerd G. Kochendoerfer, Donald W. Low
  • Patent number: 6977292
    Abstract: The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 20, 2005
    Assignee: Gryphon Therapeutics
    Inventors: Paolo Botti, James A. Bradburne, Stephen B. H. Kent
  • Patent number: 6844161
    Abstract: Novel proteins and protein libraries are disclosed. The proteins possess one or more functional protein modules from different parent protein molecules. The proteins and protein libraries are exemplified by the preparation of cross-over chemokines that contain various combinations of peptide segments derived from RANTES, SDS-1 and vMIP-I and to vMIP-II. The proteins and libraries are extremely pure and can be provided in non-limiting high yields suitable for diagnostic and high-throughput screening assays.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: January 18, 2005
    Assignee: Gryphon Therapeutics, Inc.
    Inventors: Michael A. Siani, Jill Wilken, Reyna Simon, Stephen B. H. Kent
  • Publication number: 20040265944
    Abstract: Method is described for sequencing polypeptides by forming peptide ladders comprising a series of polypeptides in which adjacent members of the series vary by one amino acid residue and determining the identity and position of each amino acid in the polypeptide by mass spectroscopy.
    Type: Application
    Filed: March 2, 2004
    Publication date: December 30, 2004
    Applicants: The Rockefeller University, The Scripps Research Institute
    Inventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
  • Publication number: 20040138412
    Abstract: The invention is directed to methods and compositions for chemical ligation of components comprising a first component having a carboxythioester, and preferable an &agr;-carboxythioester, moiety and a second component having an N-substituted, and preferably an N&agr;-substituted, 2 or 3 carbon chain alkyl or aryl thiol to give a ligation product having an N-substituted amide bond at the ligation site. The reactants of the invention are chemoselective, and the alkyl or aryl thiol moiety is removable from the ligation product. Removal of the alkyl or aryl thiol gives a native amide bond at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers having a native amide bond at the ligation site.
    Type: Application
    Filed: January 15, 2003
    Publication date: July 15, 2004
    Inventors: Paolo Botti, James A Bradburne, Stephen B H Kent, Donald W Low
  • Publication number: 20040115774
    Abstract: The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.
    Type: Application
    Filed: January 8, 2003
    Publication date: June 17, 2004
    Inventors: Gerd G Kochendoerfer, Paolo Botti, James A Bradburne, Shiah-yun Chen, Sonya Cressman, Christie L Hunter, Stephen B H Kent, Donald W Low, Jill G Wilken
  • Patent number: 6750061
    Abstract: Method is described for sequencing polypeptides by forming peptide ladders comprising a series of polypeptides in which adjacent members of the series vary by one amino acid residue and determining the identity and position of each amino acid in the polypeptide by mass spectroscopy.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: June 15, 2004
    Assignees: The Rockefeller University, The Scripps Research Institute
    Inventors: Brian T. Chait, Ronald Beavis, Rong Wang, Stephen B. H. Kent
  • Publication number: 20030208046
    Abstract: The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
    Type: Application
    Filed: January 8, 2003
    Publication date: November 6, 2003
    Inventors: Christie L. Hunter, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Stephen B.H. Kent, Gerd G. Kochendoerfer, Donald W. Low