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:
Grant
Filed:
September 28, 2016
Date of Patent:
December 19, 2017
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Krzysztof Darlak, Noriyuki Kawahata, Sameer Ahmed Athamneh
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 described.
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:
Grant
Filed:
November 1, 2013
Date of Patent:
March 28, 2017
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Krzysztof Darlak, Noriyuki Kawahata, Sameer Ahmed Athamneh
Abstract: The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.
Type:
Grant
Filed:
June 25, 2015
Date of Patent:
December 20, 2016
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Noriyuki Kawahata, Vincent Guerlavais, Manoj Samant
Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.
Type:
Grant
Filed:
September 26, 2014
Date of Patent:
November 29, 2016
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
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. Macrocycles of the invention include triazole moieties that crosslink amino acid side chains. The cross links can stabilize a secondary structure of a peptidomimetic macrocycle, such as an ?-helix.
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:
Grant
Filed:
November 24, 2009
Date of Patent:
October 4, 2016
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata
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:
Grant
Filed:
January 13, 2012
Date of Patent:
July 19, 2016
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Huw M. Nash, Matthew Iadanza, Christopher Leitheiser, Noriyuki Kawahata
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:
Grant
Filed:
September 22, 2009
Date of Patent:
December 8, 2015
Assignee:
AILERON THERAPEUTICS, INC.
Inventors:
Huw M. Nash, Matthew Iadanza, Christopher Leitheiser, Noriyuki Kawahata
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.
Type:
Grant
Filed:
August 2, 2013
Date of Patent:
November 3, 2015
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosanna Kapeller-Libermann, 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.
Type:
Grant
Filed:
October 18, 2012
Date of Patent:
August 4, 2015
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Noriyuki Kawahata, Vincent Guerlavais, Manoj Samant
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. Macrocycles of the invention include triazole moieties that crosslink amino acid side chains. The cross links can stabilize a secondary structure of a peptidomimetic macrocycle, such as an ?-helix.
Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.
Type:
Grant
Filed:
February 14, 2013
Date of Patent:
January 6, 2015
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
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:
January 15, 2014
Publication date:
October 30, 2014
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, Rosanna Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata, Vincent Guerlavais, Matthew Iadanza
Abstract: The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
Type:
Grant
Filed:
January 17, 2012
Date of Patent:
August 19, 2014
Assignee:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata, Jiawen Han
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:
August 2, 2013
Publication date:
May 15, 2014
Applicant:
Aileron Therapeutics, Inc.
Inventors:
Huw M. Nash, David Allen Annis, Rosanna Kapeller-Libermann, Tomi K. Sawyer, 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.