# US 2025/0205221 A1 · Muscle relaxant

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- Number: US 2025/0205221 A1
- Document ID: US20250205221A1
- Status: Published application
- Kind: A1
- Application number: 18/851,837
- Filed: 2023-03-30
- Published: 2025-06-26
- Earliest claimed: 2022-03-30
- Inventors: Hiroshi SUNAGA
- Web page: https://patentgrep.com/patent/US20250205221A1

## CPC

- A61K 31/472: Non-condensed isoquinolines, e.g. papaverine
- A61P 21/02: Muscle relaxants, e.g. for tetanus or cramps
- A61P 23/02: Local anaesthetics
- C07D 217/20: with oxygen atoms directly attached to the aromatic ring of said aralkyl radical, e.g. papaverine
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Provided is a novel compound that can be used as a neuromuscular blocking agent, and specifically is a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof, in which X1, X2, X3, and X4 each independently represent hydrogen or a C1-3 alkoxy group, and at least two of X1, X2, X3, and X4 are C1-3 alkoxy groups; Y1, Y2, Y3, Y4, and Y5 each independently represent hydrogen or a C1-3 alkoxy group, and at least two of Y1, Y2, Y3, Y4, and Y5 are C1-3 alkoxy groups; n is 0 or 1; and L represents a linker with a main chain of 5 to 20 atoms.

## Claims

### Claim 1

A compound represented by the general formula (I), or a pharmacologically acceptable salt thereof,
wherein, in the general formula (I),
X1, X2, X3, and X4 each independently represent hydrogen or a C1-3 alkoxy group, and at least two of X1, X2, X3, and X4 are C1-3 alkoxy groups,
Y1, Y2, Y3, Y4, and Y5 each independently represent hydrogen or a C1-3 alkoxy group, and at least two of Y1, Y2, Y3, Y4, and Y5 are C1-3 alkoxy groups,
n is 0 or 1, and
L represents a linker with a main chain of 5 to 20 atoms.

### Claim 2 (depends on 1)

The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein
X1 and X4 are hydrogen, and X2 and X3 are C1-3 alkoxy groups, and
Y3 and either Y2 or Y4 of Y1, Y2, Y3, Y4, and Y5 are C1-3 alkoxy groups, and the remaining groups are hydrogen.

### Claim 3 (depends on 1)

The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein
L is a divalent alkylene or alkenylene group with a main chain of 5 to 20 carbon atoms, wherein one or more —CH2— is replaced by —O— or —O—C(═O)— or —C(═O)—O—, and one or more hydrogen is optionally replaced by halogen.

### Claim 4 (depends on 1)

The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein
L is selected from the following general formulae (II) to (V),
wherein,
—(L′)n3— is a C1-6 alkylene or alkenylene group wherein one or more hydrogen is optionally replaced by halogen,
n1 is an integer of 1 to 5, and
n2 is an integer of 1 to 5.

### Claim 5 (depends on 1)

The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein
L is represented by the general formula (VI),
wherein,
—(L″)n4— is a C1-6 alkylene or alkenylene group wherein one or more hydrogen is optionally replaced by halogen,
n1 is an integer of 1 to 5, and
n2 is an integer of 1 to 5.

### Claim 6 (depends on 4)

The compound or a pharmacologically acceptable salt thereof according to claim 4, wherein
the compound represented by the general formula (I) is selected from the following compounds.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising the compound or a pharmacologically acceptable salt thereof according to claim 1, and a pharmacologically acceptable carrier.

### Claim 8 (depends on 7)

The pharmaceutical composition of claim 7, for use as a neuromuscular blocking agent.