Aileron Therapeutics, Inc.

Noriyuki Kawahata

Huw M Nash

Vincent Guerlavais

Tomi K Sawyer

David Allen Annis

Rosana Kapeller-Libermann

Krzysztof Darlak

Sameer Ahmed Athamneh

Manoj Samant

Christopher Leitheiser

Matthew Iadanza

Eric Feyfant

Carl Elkin

Rosanna Kapeller-Libermann

Jiawen Han

Jia-Wen Han

Justin Noehre

Rosana Kapeller-Llbermann

The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

Peptidomimetic macrocycles

Provided are crystalline &#x3b1;, &#x3b1;-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 &#x3b1;, &#x3b1;-disubstituted amino acids and their salts; methods of making these, and methods of using these.

Disubstituted amino acids and methods of preparation and use thereof

The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.

Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an &#x3b1;,&#x3b1;-disubstituted amino acid, or may comprise a crosslinker linking the &#x3b1;-positions of at least two amino acids or at least one of said two amino acids may be an &#x3b1;,&#x3b1;-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.

The present invention provides peptidomimetic macrocycles capable of regulating HIF1&#x3b1; and methods of using such macrocycles for the treatment of diseases.

Peptidomimetic macrocycles and use thereof in regulating HIF1alpha

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.

Peptidomimetic macrocycles with improved properties

The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.

Methods for preparing purified polypeptide compositions

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.

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West Roxbury, MA, United States of America

Noriyuki Kawahata