# US 2026/0098031 A1 · Monocyclic compound having glp-1 receptor agonist activity

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2026/0098031 A1
- Document ID: US20260098031A1
- Status: Published application
- Kind: A1
- Application number: 19/112,482
- Filed: 2023-09-21
- Published: 2026-04-09
- Earliest claimed: 2022-09-22
- Assignees: Shionogi & Co., Ltd.
- Applicants: Shionogi & Co., Ltd.
- Inventors: Yuji NISHIURA
- Web page: https://patentgrep.com/patent/US20260098031A1

## CPC

- C07D 405/14: containing three or more hetero rings
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- 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 present invention relates to a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof. A compound represented by formula (I): wherein A1 is C(R5) or N, A2 is C(R6) or N, A3 is C(R7) or N, R5, R6, and R7 are each independently a hydrogen atom or the like, R2 is substituted or unsubstituted alkyl or the like, -L- is a group represented by: wherein R1 is a hydrogen atom or the like, R8 is a hydrogen atom or the like, R10s are each independently cyano or the like, m is an integer of 1 to 3, and R3 is phenyl optionally substituted with substituent group F, or the like, the substituent group F: halogen, cyano, alkyl, haloalkyl, alkyloxy, and haloalkyloxy.

## Claims

### Claim 1

A compound represented by formula (I):
wherein
A1 is C(R5) or N,
A2 is C(R6) or N,
A3 is C(R7) or N,
R5, R6, and R7 are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic carbocyclyl,
R2 is substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic heterocyclyl,
-L- is a group represented by:
wherein
R1 is a hydrogen atom, or substituted or unsubstituted alkyl,
R8 is a hydrogen atom, or substituted or unsubstituted alkyl,
R10s are each independently cyano, halogen, or substituted or unsubstituted alkyl, and
m is an integer of 1 to 3, and
R3 is phenyl optionally substituted with substituent group F, 5- or 6-membered aromatic heterocyclyl optionally substituted with substituent group F, bicyclic 9- or 10-membered aromatic heterocyclyl optionally substituted with substituent group F, or 5- to 12-membered non-aromatic heterocyclyl optionally substituted with substituent group F,
the substituent group F: halogen, cyano, alkyl, haloalkyl, alkyloxy, and haloalkyloxy,
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R2 is alkyl substituted with substituted or unsubstituted non-aromatic heterocyclyl, or alkyl substituted with substituted or unsubstituted aromatic heterocyclyl.

### Claim 3 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein -L- is represented by:
wherein R10a and R10b are each independently a hydrogen atom, cyano, halogen, or substituted or unsubstituted alkyl, and R1 has the same meaning as in claim 1.

### Claim 4 (depends on 3)

The compound according to claim 3 or a pharmaceutically acceptable salt thereof, wherein R10b is halogen, alkyl, or haloalkyl.

### Claim 5 (depends on 1)

The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R3 is a group below:
wherein
W is N, or CR15,
R11 is a hydrogen atom, halogen, cyano, alkyl, haloalkyl, alkyloxy, or haloalkyloxy,
R12 and R13 are each independently a hydrogen atom or halogen,
R14 and R15 are each independently a hydrogen atom, halogen, cyano, alkyl, haloalkyl, alkyloxy, or haloalkyloxy,
R11 and R12 may be taken together to form 5-membered aromatic heterocycle optionally substituted with substituent group F, or 5- to 7-membered non-aromatic heterocycle optionally substituted with substituent group F,
R11 and R13 may be taken together to form 5-membered aromatic heterocycle optionally substituted with substituent group F, or 5- to 7-membered non-aromatic heterocycle optionally substituted with substituent group F, and
R13 and R14 may be taken together to form 5-membered aromatic heterocycle optionally substituted with substituent group F, or 5- to 7-membered non-aromatic heterocycle optionally substituted with substituent group F.

### Claim 6 (depends on 5)

The compound according to claim 5 or a pharmaceutically acceptable salt thereof, wherein R3 is any one of groups below:
wherein R4s are each independently halogen, cyano, alkyl, haloalkyl, alkyloxy, or haloalkyloxy.

### Claim 7 (depends on 6)

The compound according to claim 6 or a pharmaceutically acceptable salt thereof, wherein R4s are each independently a fluorine atom, a chlorine atom, cyano, methyl, methyloxy, or difluoromethyloxy.

### Claim 8 (depends on 1)

The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein
(i) A1 is C(R5), A2 is C(R6), and A3 is C(R7),
(ii) A1 is N, A2 is C(R6), and A3 is C(R7),
(iii) A1 is C(R5), A2 is C(R6), and A3 is N, or
(iv) A1 is N, A2 is C(R6), and A3 is N.

### Claim 9 (depends on 8)

The compound according to claim 8 or a pharmaceutically acceptable salt thereof, wherein
(i) A1 is C(R5), A2 is C(R6), and A3 is C(R7), or
(ii) A1 is N, A2 is C(R6), and A3 is C(R7).

### Claim 10 (depends on 1)

The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R5, R6, and R7 are each independently a hydrogen atom, halogen, alkyl, alkyloxy, or 5- or 6-membered aromatic heterocyclyl optionally substituted with a substituent group E,
wherein the substituent group E is halogen, alkyl, haloalkyl, alkyloxy, haloalkyloxy.

### Claim 11 (depends on 1)

The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R2 is oxetanylmethyl.

### Claim 12 (depends on 1)

A pharmaceutical composition comprising the compound according to claim 1 or a pharmaceutically acceptable salt of thereof.

### Claim 13 (depends on 12)

The pharmaceutical composition according to claim 12, which is a GLP-1 receptor agonist.
