# US 11,897,851 B2 · Heterocyclic GLP-1 agonists

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- Number: US 11,897,851 B2
- Document ID: US11897851B2
- Status: Granted
- Kind: B2
- Application number: 18/106,378
- Filed: 2023-02-06
- Published: 2023-06-22
- Granted: 2024-02-13
- Earliest claimed: 2021-08-06
- Assignees: Gasherbrum Bio, Inc.
- Applicants: Gasherbrum Bio, Inc.
- Inventors: Qinghua Meng; Hui Lei; Haizhen Zhang; Xichen Lin; Andrew Jennings
- Web page: https://patentgrep.com/patent/US11897851B2

## CPC

- C07D 273/01: having one nitrogen atom
- C07D 401/14: containing three or more hetero rings
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- C07D 405/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- 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

This disclosure relates to GLP-1 agonists of Formula I: including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.

## Claims

### Claim 1

A compound of Formula (I-A4-1), or a pharmaceutically acceptable salt thereof:
wherein:
is a single bond or a double bond;
R0-1 is selected from the group consisting of hydrogen and (C1-C3)alkyl;
X4 is selected from the group consisting of N and CRy;
Ry is selected from the group consisting of hydrogen, —OH, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, CN, and halogen;
T2 is (C1-C3)alkyl which is substituted with a substituent selected from the group consisting of (C1-C3)alkoxy, S(O)2(C1-C3 alkyl), (C3-C6)cycloalkyl, 3- to 6-membered heterocycloalkyl, phenyl, and 5- to 6-membered heteroaryl, wherein the phenyl or 5- to 6-membered heteroaryl are each optionally substituted with halogen or (C1-C3)alkyl;
Raa is selected from the group consisting of hydrogen and (C1-C3)alkyl;
Ring C is selected from the group consisting of phenyl and 6-membered heteroaryl;
b is 0, 1, or 2; and
each occurrence of Rb is independently selected from the group consisting of (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, halogen, and CN.

### Claim 2 (depends on 1)

The compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is selected from the group consisting of:

### Claim 3 (depends on 2)

A pharmaceutical composition comprising a compound of claim 2, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient.

### Claim 4 (depends on 2)

The compound of claim 2, or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is:

### Claim 5 (depends on 2)

The compound of claim 2, or a pharmaceutically acceptable salt or solvate thereof, wherein the compound is: