# US 12,180,223 B2 · 3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives as TRPA1 inhibitors

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- Number: US 12,180,223 B2
- Document ID: US12180223B2
- Status: Granted
- Kind: B2
- Application number: 17/719,432
- Filed: 2022-04-13
- Published: 2022-10-27
- Granted: 2024-12-31
- Earliest claimed: 2021-04-14
- Assignees: Boehringer Ingelheim International GmbH
- Applicants: Boehringer Ingelheim International GmbH
- Inventors: Florian Paul Christian Binder; Jens Willwacher; Martin Thomas Fleck
- Web page: https://patentgrep.com/patent/US12180223B2

## CPC

- C07D 495/04: Ortho-condensed systems
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/14: Antitussive agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure provides certain 3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

## Claims

### Claim 1

A compound according to formula (I)
wherein
A is selected from the group consisting of phenyl, thiophenyl, benzofuranyl and benzothiophenyl, and wherein A is unsubstituted or substituted with one or two members of the group R1 selected from the group consisting of halogen, C1-4-alkyl and O—C1-4-alkyl;
or a salt thereof.

### Claim 2 (depends on 1)

The compound of formula (I) according to claim 1, wherein R1 is selected from the group consisting of F, CI, I, CH3 and OCH3.

### Claim 3 (depends on 1)

The compound of formula (I) according to claim 1, wherein A is selected from the group consisting of

### Claim 4 (depends on 1)

The compound of formula (I) according to claim 1, selected from the group consisting of

### Claim 5 (depends on 1)

A salt of a compound according to claim 1.

### Claim 6 (depends on 1)

A pharmaceutically acceptable salt of a compound according to claim 1.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising at least one compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

### Claim 8 (depends on 1)

A method for the treatment of inflammatory airway diseases or fibrotic diseases in a patient, comprising administering to the patient an effective amount of a compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof.

### Claim 9 (depends on 8)

The method according to claim 8 for the treatment of idiopathic pulmonary fibrosis (IPF).