Abstract: Provided are crystalline ?, ?-disubstituted amino acids and their crystalline salts containing a terminal alkene on one of their side chains, as well as optionally crystalline halogenated and deuterated analogs of the ?, ?-disubstituted amino acids and their salts; methods of making these, and methods of using these.
Type:
Application
Filed:
November 1, 2013
Publication date:
May 8, 2014
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Krzysztof Darlak, Noriyuki Kawahata, Sameer Ahmed Athamneh
Abstract: Provided herein are novel alkynyl and azide containing amino acids; kits containing these amino acids; peptides containing these amino acids; peptide macrocycles whose secondary structures are stabilized with linkers containing triazoles synthesized by reacting the side chains of the alkynyl and azide containing amino acids; and methods of making and using the alkynyl and azide containing amino acids, kits, peptides, triazole containing linkers, and peptide macrocycles.
Abstract: Biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins, and methods of identifying and making such improved polypeptides are described.
Type:
Grant
Filed:
September 22, 2009
Date of Patent:
September 3, 2013
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Llbermann, Tomi K. Sawyer, Noriyuki Kawahata
Abstract: The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.
Abstract: Biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides; and methods of making and identifying such improved polypeptides.
Type:
Grant
Filed:
February 3, 2012
Date of Patent:
March 19, 2013
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata
Abstract: The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Type:
Application
Filed:
August 8, 2012
Publication date:
January 24, 2013
Applicant:
AILERON THERAPEUTICS, INC.
Inventors:
Huw M. NASH, Rosana KAPELLER-LIBERMANN, Tomi K. SAWYER, Noriyuki KAWAHATA, Vincent GUERLAVAIS, Matthew IADANZA
Abstract: The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Type:
Application
Filed:
January 13, 2012
Publication date:
October 18, 2012
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, Matthew Iadanza, Christopher Leitheiser, Noriyuki Kawahata
Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
Abstract: The present invention provides biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins. The invention additionally provides methods of identifying and making such improved polypeptides.
Type:
Application
Filed:
February 3, 2012
Publication date:
July 5, 2012
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata
Abstract: The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
Type:
Application
Filed:
January 17, 2012
Publication date:
June 14, 2012
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata, Jiawen Han
Abstract: The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.
Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
Type:
Application
Filed:
April 29, 2011
Publication date:
October 27, 2011
Applicant:
Aileron Therapeutics, Inc., a Delaware Corporation
Abstract: The present invention provides biologically active peptidomimetic macrocycles with improved properties, such as protease resistance, relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Type:
Application
Filed:
October 14, 2010
Publication date:
September 15, 2011
Applicant:
AILERON THERAPEUTICS, INC.
Inventors:
Huw M. NASH, David Allen ANNIS, Vincent GUERLAVAIS, Lawrence LICKLIDER
Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. In various embodiments, the peptidomimetic macrocycles are of Formula I: The linker L includes a triazole moiety. Peptidomimetic macrocycles according to the invention may exhibit increased ?-helical or beta sheet structure in aqueous solution compared to a corresponding non-macrocyclic polypeptide.
Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production, are provided.
Abstract: The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
Type:
Application
Filed:
October 13, 2009
Publication date:
June 16, 2011
Applicant:
AILERON Therapeutics, Inc.
Inventors:
Huw M. Nash, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata, Vincent Guerlavais, Matthew Iadanza
Abstract: Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production, are provided.