# US 12,760,027 B2 · Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators

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- Number: US 12,760,027 B2
- Document ID: US12760027B2
- Status: Granted
- Kind: B2
- Application number: 18/775,532
- Filed: 2024-07-17
- Published: 2024-11-28
- Granted: 2026-10-13
- Earliest claimed: 2017-03-20
- Assignees: Novo Nordisk Healthcare AG
- Applicants: Novo Nordisk Healthcare AG
- Inventors: Anna Ericsson; Neal Green; Gary Gustafson; Bingsong Han; David R. Lancia, Jr.; Lorna Mitchell; David Richard; Tatiana Shelekhin; Chase C. Smith; Zhongguo Wang; Xiaozhang Zheng
- Web page: https://patentgrep.com/patent/US12760027B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.

## Claims

### Claim 1

A compound of formula
or a pharmaceutically acceptable salt thereof.

### Claim 2

A compound of formula

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 4 (depends on 2)

A pharmaceutical composition comprising the compound of claim 2, and a pharmaceutically acceptable carrier.