# US 11,026,945 B2 · Protein kinase RNA-like endoplasmic reticulum kinase (PERK) inhibitors for prevention and/or treatment of lung injury and/or inflammation

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- Number: US 11,026,945 B2
- Document ID: US11026945B2
- Status: Granted
- Kind: B2
- Application number: 16/096,721
- Filed: 2017-04-27
- Published: 2020-02-20
- Granted: 2021-06-08
- Earliest claimed: 2016-04-29
- Assignees: The Trustees of the University of Pennsylvania
- Applicants: The Trustees of the University of Pennsylvania
- Inventors: Susan S. Margulies; Tamas Dolinay
- Web page: https://patentgrep.com/patent/US11026945B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/08: Bronchodilators
- C12N 15/1137: {against enzymes (viral enzymes C12N15/1131; receptors C12N15/1138)}
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- C12N 2310/14: interfering nucleic acids [NA]
- C12Y 207/11001: Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES

## Abstract

Disclosed herein are methods of preventing and/or treating lung injury and/or lung inflammation in a subject comprising administering to the subject a therapeutically effective dose of a PERK pathway inhibitor. Pharmaceutical compositions for the prevention and/or treatment of lung injury and/or lung inflammation comprising PERK pathway inhibitors are also provided. Also disclosed are uses of a PERK inhibitor in the manufacture of a medicament for the prevention and/or treatment of a lung injury and/or inflammation.

## Claims

### Claim 1

A method of treating lung injury and/or lung inflammation in a subject comprising administering to the subject a therapeutically effective dose of a PERK inhibitor to treat the lung injury and/or inflammation, wherein the PERK inhibitor is 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl]-2-(3-trifluoromethylphenyl)ethanone.

### Claim 2

A method of preventing lung injury and/or lung inflammation in a subject comprising administering to the subject a therapeutically effective dose of a PERK inhibitor to prevent the lung injury and/or inflammation, wherein the PERK inhibitor is 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl]-2-(3-trifluoromethylphenyl)ethanone.

### Claim 3 (depends on 1)

The method of claim 1, wherein the lung injury comprises acute respiratory distress syndrome.

### Claim 4 (depends on 1)

The method of claim 1, wherein the lung injury comprises ventilator-induced lung injury.

### Claim 5 (depends on 2)

The method of claim 2, wherein the lung injury comprises acute respiratory distress syndrome.

### Claim 6 (depends on 2)

The method of claim 2, wherein the lung injury comprises ventilator-induced lung injury.