IP Library Granted Patent US 12,729,210
Granted Patent B2
US 12,729,210 · App. 18/246,893 · Granted Sep 8, 2026

Crystal forms of pyridopyrazole compounds and preparation method therefor

Inventors: Jiansong Wang (Guangzhou, CN); Zhifei Fu (Shanghai, CN); Zhibo Luo (Guangzhou, CN); Miaorong Luo (Shanghai, CN); Yang Zhang (Shanghai, CN); Jian Li (Shanghai, CN); Shuhui Chen (Shanghai, CN); Yingxia Bao (Guangzhou, CN); Wei Wang (Guangzhou, CN); Zhoufan Xie (Guangzhou, CN)
Assignee: GUANGZHOU BAIYUNSHAN PHARMACEUTICAL HOLDINGS CO., LTD. BAIYUNSHAN PHARMACEUTICAL GENERAL FACTORY
C07D519/00A61P35/00C07B2200/13
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Quick Facts
Patent No.
US 12,729,210
App. No.
18/246,893
Granted
Sep 8, 2026
Kind
B2
Abstract

Provided are crystal forms of compounds represented by formula(II)-formula (VIII) and formula (I)-formula (VIII-1), a preparation method therefor and an application of the compounds and crystal forms in the preparation of a drug for treating a related disease.

Claims (79)

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

wherein the X-ray powder diffraction pattern of the crystal form A has characteristic diffraction peaks at the 2θ angles comprising: 15.51±0.20°, 16.30±0.20°, 19.16±0.20°, 21.69±0.20° and 24.63±0.20°.

2 . The crystal form A according to claim 1 , wherein the X-ray powder diffraction pattern of the crystal form A has characteristic diffraction peaks at the 20 angles of: 14.88 t 0.20°, 15.51±0.20°, 16.30±0.20°, 18.49±0.20°, 19.16±0.20°, 19.70±0.20°, 21.69±0.20° and 24.63±0.20°.

3 . The crystal form A according to claim 2 , wherein the X-ray powder diffraction pattern of the crystal form A has characteristic diffraction peaks at the 20 angles of: 7.79±0.20°, 9.58±0.20°, 12.61±0.20°, 14.88±0.20°, 15.51±0.20°, 16.30±0.20°, 18.49±0.20°, 19.16±0.20°, 19.70±0.20°, 21.69 t 0.20° and 24.63±0.20°.

4 . The crystal form A according to claim 1 , wherein the XRPD pattern of the crystal form A has characteristic diffraction peaks at the 2θ angles of:

No.

2θ angle (°)

1

3.29

2

6.19

3

7.79

4

9.21

5

9.58

6

10.32

7

12.61

8

14.88

9

15.10

10

15.51

11

16.30

12

16.60

13

17.65

14

18.49

15

19.16

16

19.70

17

20.03

18

20.45

19

21.69

20

22.24

21

22.83

22

23.38

23

24.63

24

25.29

25

25.76

26

26.58

27

27.70

28

28.34

29

29.06

30

31.71

31

32.97

32

33.49.

5 . The crystal form A according to claim 1 , wherein the differential scanning calorimetry curve of the crystal form A has a starting point of an endothermic peak at 188.7±2° C.

6 . The crystal form A according to claim 1 , wherein the thermogravimetric analysis curve of the crystal form A shows a weight loss of 1.20% at 180.0±3° C.

7 . The crystal form A according to claim 2 , wherein the differential scanning calorimetry curve of the crystal form A has a starting point of an endothermic peak at 188.7±2° C.

8 . The crystal form A according to claim 3 , wherein the differential scanning calorimetry curve of the crystal form A has a starting point of an endothermic peak at 188.7±2° C.

9 . The crystal form A according to claim 2 , wherein the thermogravimetric analysis curve of the crystal form A shows a weight loss of 1.20% at 180.0±3° C.

10 . The crystal form A according to claim 3 , wherein the thermogravimetric analysis curve of the crystal form A shows a weight loss of 1.20% at 180.0±3° C.

11 . A method of treating solid tumor in a subject in need thereof, comprising administering an effective amount of the crystal form A of the compound of Formula (I) according to claim 1 to the subject.

12 . The method according to claim 11 , wherein the solid tumor is an RET kinase-associated solid tumor.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2023
From: WANG, JIANSONG; FU, ZHIFEI; LUO, ZHIBO; LUO, MIAORONG; ZHANG, YANG; LI, JIAN; CHEN, SHUHUI; BAO, YINGXIA; WANG, WEI; XIE, ZHOUFAN
To: GUANGZHOU BAIYUNSHAN PHARMACEUTICAL HOLDINGS CO., LTD, BAIYUNSHAN PHARMACEUTICAL GENERAL FACTORY
Reel/Frame 063131/0309 →
Priority Claims (3)
CN 202011051252.9 · Sep 29, 2020 · national
CN 202011118921.X · Oct 19, 2020 · national
CN 202110051653.2 · Jan 13, 2021 · national
Continuity (1)
Related Publication 20230365596A1 · Nov 16, 2023
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