IP Library › Granted Patent US 12,583,869
Granted Patent B2
US 12,583,869 · App. 17/442,688 · Granted Mar 24, 2026

Salt form and crystal form of A2A receptor antagonist and preparation method therefor

Inventors: Kevin X Chen (Shanghai, CN); Kai Zhou (Shanghai, CN); Yanxin Yu (Shanghai, CN); Boyu Hu (Shanghai, CN); Li Zhang (Shanghai, CN); Zhaoguo Chen (Shanghai, CN)
Assignees: CSTONE PHARMACEUTICAL (SUZHOU) CO., LTD.; CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD.; CSTONE PHARMACEUTICALS
C07D519/00C07C57/145C07B2200/13
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Quick Facts
Patent No.
US 12,583,869
App. No.
17/442,688
Granted
Mar 24, 2026
Kind
B2
Abstract

Provided are a salt form and a crystal form of adenosine A 2A receptor antagonist, and preparation method therefor. Also provided is an application of the salt form or crystal form in the preparation of a medicine for A 2A receptor-related diseases, the maleate salt in the salt form has a structure of formula (I).

Claims (9)

1 . A crystal form of the compound of formula (I),

wherein an X-ray powder diffraction pattern thereof has characteristic diffraction peaks at the following 2θ angles: 7.16±0.2°, 9.66±0.2°, and 19.66±0.2°.

2 . The crystal form of the compound of formula (I) according to claim 1 , wherein the X-ray powder diffraction pattern thereof has additional characteristic diffraction peaks at the following 2θ angles: 13.59±0.2°, 14.30±0.2°, 15.87±0.2°, 17.73±0.2°, and 20.88±0.2°;

or, wherein a differential scanning calorimetry curve thereof has an onset of an endothermic peak at 205.67±3° C.;

or, wherein a thermogravimetric analysis curve thereof has a weight loss of 0.1846% at 120.00° C.±3° C.

3 . The crystal form of the compound of formula (I) according to claim 2 , wherein the X-ray powder diffraction pattern thereof has additional characteristic diffraction peaks at the following 2θ angles: 26.01±0.2°, 26.76±0.2°, and 27.21±0.2°.

4 . The crystal form of the compound of formula (I) according to claim 3 , wherein the XRPD pattern thereof is shown in FIG. 1 ;

or, a DSC pattern thereof is shown in FIG. 2 ;

or, a TGA pattern thereof is shown in FIG. 3 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 24, 2021
From: CHEN, KEVIN X; ZHOU, KAI; YU, YANXIN; HU, BOYU; ZHANG, LI; CHEN, ZHAOGUO
To: CSTONE PHARMACEUTICALS (SUZHOU) CO., LTD.; CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD.; CSTONE PHARMACEUTICALS
Reel/Frame 057601/0678 →
Priority Claims (1)
CN 201910244468.8 · Mar 28, 2019 · national
Continuity (1)
Related Publication 20220185825A1 · Jun 16, 2022
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