Aileron Therapeutics, Inc.

Merck + Co., Inc.

Alleron Therapeutics, Inc.

David Allen Annis

Huw M Nash

Tomi K Sawyer

Noriyuki Kawahata

Rosana Kapeller-Libermann

Karen Olson

Manuel Aivado

Vincent Guerlavais

Hubert Chen

Yong Chang

Chris J Viau

Joseph P Vacca

Craig Alan Coburn

Thomas G Steele

Tong Wang

Praveen K Tadikonda

Jiawen Han

Rosanna Kapeller-Libermann

Krzysztof Darlak

Chris Rhodes

Sonoko Kanai

Rosana Kapeller-Llbermann

Joerg Hoernschemeyer

Gergely M Makara

Michaela Grass

The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

Peptidomimetic macrocycles and uses thereof

Aqueous pharmaceutical formulations, for parenteral administration, comprising peptidomimetic macrocycle or a pharmaceutically acceptable salt thereof wherein the peptidomimetic macrocycle binds to MDM2 and/or MDMX proteins are disclosed. Also disclosed are methods of treating diseases and disorders using the aqueous pharmaceutical formulations disclosed herein.

Peptidomimetic macrocycles and formulations thereof

Methods for treating solid tumor, determined to lack a p53 deactivation mutation, in a subject are provided. Also provided are peptidomimetic macrocycles for use in treatment of a solid tumor, determined to lack a p53 deactivation mutation, in a subject.

Methods for treating liquid cancer, determined to lack a p53 deactivation mutation, in a subject are provided. Also provided are peptidomimetic macrocycles for use in treatment of a liquid cancer, determined to lack a p53 deactivation mutation, in a subject.

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

Peptidomimetic macrocycles

Novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of viral diseases are described.

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

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.

Peptidomimetic macrocycles and methods of using such macrocycles for the treatment of viral disease are described.

The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.

Therapeutic peptidomimetic macrocycles

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.

Biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides; and methods of making and identifying such improved polypeptides.

The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

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Cambridge, MA, United States of America

David Allen Annis