# US 2026/0085071 A1 · Novel crystalline form of 1-(8-bromopyrido[2,3- e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-nmethylazetidin- 3-amine

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- Number: US 2026/0085071 A1
- Document ID: US20260085071A1
- Status: Published application
- Kind: A1
- Application number: 19/110,267
- Filed: 2023-09-29
- Published: 2026-03-26
- Earliest claimed: 2022-09-29
- Assignees: Jw Pharmaceutical Corporation
- Applicants: Jw Pharmaceutical Corporation
- Inventors: Suha PARK; Seiho CHIN; Sumin LEE
- Web page: https://patentgrep.com/patent/US20260085071A1

## CPC

- A61P 17/00: Drugs for dermatological disorders
- C07D 471/14: Ortho-condensed systems
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61P 17/04: Antipruritics
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

Novel crystalline forms of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-N-methylazetidin-3-amine is provided along with pharmaceutical compositions comprising the same. Also disclosed is the use of the novel polymorph for the treatment of diseases, such as atopic dermatitis (AD), itch, pruritus and various forms of urticaria for example chronic idiopathic urticaria subtypes.

## Claims

### Claim 1

Crystalline 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-N-methylazetidin-3-amine form A characterized by one or more XRPD reflections at approximately (°2θ) 7.0, 22.6 and/or 26.3 (±0.2 degrees).

### Claim 2 (depends on 1)

The crystalline compound according to claim 1, characterized by one or more XRPD reflections at approximately (°2θ) 7.0, 14.3, 15.8, 22.6, 23.4 and/or 26.3 (±0.2 degrees).

### Claim 3 (depends on 1)

The crystalline compound according to claim 1, characterized by one or more XRPD reflections at approximately 7.0, 22.6 and 26.3 (±0.2 degrees).

### Claim 4 (depends on 1)

The crystalline compound according to claim 1, characterized by one or more XRPD reflections at approximately (°2θ) 7.0, 14.3, 15.8, 22.6, 23.4 and 26.3 (±0.2 degrees).

### Claim 5 (depends on 1)

The crystalline compound according to claim 1, wherein the crystalline compound has an XRPD pattern essentially similar to the XRPD pattern in FIG. 1A or 1B.

### Claim 6 (depends on 1)

The crystalline compound according to claim 1, wherein the crystalline compound has an XRPD pattern according to the XRPD pattern in FIG. 1A or 1B.

### Claim 7 (depends on 1)

The crystalline compound according to claim 1, wherein the crystalline compound is characterized by a solid state 13C CP/MAS NMR spectrum with peaks at one or more of 149.1, 148.1, 139.9, 128.0, 119.9, 112.7, 64.6, 63.1, 61.1, 53.6, 51.7, 37.7 and/or 35.4 ppm±0.2 ppm.

### Claim 8 (depends on 7)

The crystalline compound according to claim 7 characterized by having a 13C CP/MAS NMR spectrum essentially similar to the 13C CP/MAS NMR spectrum in FIG. 4.

### Claim 9 (depends on 7)

The crystalline compound according to claim 7 characterized by having a 13C CP/MAS NMR spectrum according to the 13C CP/MAS NMR spectrum in FIG. 4.

### Claim 10 (depends on 7)

The crystalline compound according to claim 7, further characterized by one or more XRPD reflections at approximately (°2θ) 7.0, 22.6 and 26.3 (±0.2 degrees).

### Claim 11 (depends on 1)

The crystalline compound according to claim 1 wherein the crystalline compound is characterized by having the single-crystal X-Ray crystallography (SXRC) parameters as shown in table 1.

### Claim 12 (depends on 1)

The crystalline compound according to claim 1 wherein the crystalline compound is characterized by having the single-crystal X-Ray crystallography (SXRC) parameters which are substantially the same as those provided in Table 1.

### Claim 13 (depends on 1)

The crystalline compound according to claim 1 wherein the crystalline has an DSC and TGA curve essentially similar as shown in FIG. 2 consisting of a not separated endothermic-exothermic event with an onset at 273.6±2° C. and a corresponding weight loss in the TGA curve.

### Claim 14 (depends on 1)

A pharmaceutical composition comprising a crystalline salt according to claim 1 and a pharmaceutically acceptable carrier.

### Claim 15 (depends on 1)

A method for the treatment of disease selected from atopic dermatitis, itch, pruritus, and various forms of urticaria, the method comprising:
administering to a subject in need thereof the crystalline compound of claim 1.

### Claim 16 (depends on 15)

The method according to claim 15, wherein the disease is atopic dermatitis.