# US 10,246,491 B2 · Peptidomimetic macrocycles and use thereof in regulating HIF1alpha

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- Number: US 10,246,491 B2
- Document ID: US10246491B2
- Status: Granted
- Kind: B2
- Application number: 14/843,079
- Filed: 2015-09-02
- Published: 2016-02-25
- Granted: 2019-04-02
- Earliest claimed: 2013-03-06
- Assignees: Aileron Therapeutics, Inc.
- Applicants: Aileron Therapeutics, Inc.
- Inventors: Vincent Guerlavais; Noriyuki Kawahata; Huw M. Nash; Carl Elkin; Eric Feyfant
- Web page: https://patentgrep.com/patent/US10246491B2

## CPC

- C07K 7/56: the cyclisation not occurring through 2,4-diamino-butanoic acid
- A61K 47/54: the modifying agent being an organic compound
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present invention provides peptidomimetic macrocycles capable of regulating HIF1α and methods of using such macrocycles for the treatment of diseases.

## Claims

### Claim 1

A peptidomimetic macrocycle having the formula
or a pharmaceutically acceptable salt thereof.

### Claim 2

A peptidomimetic macrocycle having the formula
or a pharmaceutically acceptable salt thereof.

### Claim 3

A peptidomimetic macrocycle having the formula
or a pharmaceutically acceptable salt thereof.