	US 12,453,722 B2
	Maleate of nicotinyl alcohol ether derivative, crystal form thereof, and application thereof
Zhiqiang Feng, Beijing (CN); Xiaoguang Chen, Beijing (CN); Chen Ma, Beijing (CN); Yang Yang, Beijing (CN); Fangfang Lai, Beijing (CN); Yuchen Wang, Beijing (CN); Ming Ji, Beijing (CN); and Kaijing Guo, Beijing (CN)
Assigned to Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing (CN)
Appl. No. 17/641,265
Filed by INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES, Beijing (CN)
PCT Filed Sep. 9, 2020, PCT No. PCT/CN2020/114137 § 371(c)(1), (2) Date Aug. 4, 2022, PCT Pub. No. WO2021/047528, PCT Pub. Date Mar. 18, 2021.
Claims priority of application No. 201910864721.X (CN), filed on Sep. 9, 2019.
Prior Publication US 2025/0268874 A1, Aug. 28, 2025
Int. Cl. A61K 31/4406 (2006.01); A61P 35/00 (2006.01); C07D 213/30 (2006.01)

CPC A61K 31/4406 (2013.01) [A61P 35/00 (2018.01); C07D 213/30 (2013.01)]

12 Claims

1. A crystal form A solid substance of isopropyl (S)-N-(2-(pyridine-3-yl-methoxy)-4-(2-bromo-3-phenylbenzyloxy)-5-chlorobenzyl) serinate maleate, characterized in that, when powder X-ray diffraction analysis is used and Cu Target Radiation experimental conditions are adopted, the position of diffraction peak: 2-theta value (°) or d value (Å) and relative intensity (%) of diffraction peak have the following characteristics:


	2-Theta	d(Å)	intensity %
Peak	±0.2°	±0.2 Å	±5%

1	4.5	19.6	42.3
2	5.6	15.9	50.1
3	6.8	13.0	14.0
4	8.5	10.4	16.2
5	9.1	9.8	100
6	10.2	8.7	28.1
7	12.4	7.1	11.1
8	13.3	6.7	18.6
9	13.6	6.5	35.6
10	14.6	6.1	12.1
11	15.5	5.7	15
12	16.0	5.5	11
13	16.6	5.3	13.6
14	17.1	5.2	14.2
15	17.4	5.1	13.8
16	17.9	4.9	17.4
17	18.7	4.7	17.6
18	19.0	4.7	20.1
19	19.7	4.5	35.5
20	20.0	4.4	46.6
21	20.7	4.3	58.3
22	21.6	4.1	35.5
23	22.2	4.0	15
24	22.7	3.9	33.6
25	23.1	3.9	50.5
26	23.9	3.7	42
27	25.0	3.6	16.4
28	25.4	3.5	19.2
29	26.6	3.4	28
30	28.0	3.2	13.9
31	28.4	3.1	15.9
32	29.3	3.1	19.1
33	29.9	3.0	14.2
34	30.4	2.9	14.4
35	31.0	2.9	15.7
36	31.6	2.8	15.6
37	32.7	2.7	12.2
38	34.0	2.6	12.7
39	34.9	2.6	11.9
40	35.7	2.5	13.4
41	39.0	2.3	11.2