Crystal form a of (5-amino-8-(2-methyl-6-(trifluoromethyl)pyridin-4-yl)-7-phenyl-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)methanol (compound 1)
Disclosed in the present invention are a crystal form of a [1,2,4]triazolo[1,5-c]pyrimidine compound and a preparation method thereof. Further disclosed is a use of the crystal form in the preparation of a medicament for treating A 2A receptor related diseases.
1. A crystal form A of (5-amino-8-(2-methyl-6-(trifluoromethyl)pyridin-4-yl)-7-phenyl-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)methanol (Compound 1) of the following formula:
wherein the crystal form A is characterized by an X-ray powder diffraction pattern comprising characteristic diffraction peaks (° 2θ) at the following angles of 11.30°±0.2° 2θ, 16.90°±0.2° 2θ, and 22.52°±0.2° 2θ.
2. The crystal form A according to claim 1 , wherein the crystal form A is further characterized by an X-ray powder diffraction pattern further comprising additional characteristic diffraction peaks (° 2θ) at the following angles of 8.08°±0.2° 2θ, 14.00°±0.2° 2θ, 18.30°±0.2° 2θ, 23.15°±0.2° 2θ, and 25.26°±0.2° 2θ.
3. The crystal form A according to claim 2 , wherein the crystal form A is further characterized by an X-ray powder diffraction pattern as shown in FIG. 1 .
4. The crystal form A according to claim 1 , wherein the crystal form A is further characterized by a differential scanning calorimetry curve having a starting point of the endothermic peak at 198.61° C.±2° C.
5. The crystal form A according to claim 4 , wherein the crystal form A is further characterized by a differential scanning calorimetry curve as shown in FIG. 2 .
6. The crystal form A according to claim 1 , wherein the crystal form A is further characterized by a thermogravimetric analysis curve having a weight loss in the range of 0.0% to 0.4423% at 199.80° C.±3° C.
7. The crystal form A according to claim 4 , wherein the crystal form A is further characterized by a thermogravimetric analysis curve having a weight loss in the range of 0.0% to 0.4423% at 199.80° C.±3° C.
8. The crystal form A according to claim 6 , wherein the crystal form A is further characterized by a thermogravimetric analysis curve as shown in FIG. 3 .
9. The crystal form A according to claim 7 , wherein the crystal form A is further characterized by a thermogravimetric analysis curve as shown in FIG. 3 .
10. A method for inhibiting the activity of an adenosine A 2A receptor in a subject in need thereof, wherein the method comprises administering to the subject the crystal form A according to claim 1 .
11. The method according to claim 10 , wherein the subject has a disease related to the adenosine A 2A receptor, and wherein the disease related to the adenosine A 2A receptor is colon cancer or rectal cancer.
12. The method according to claim 11 , wherein the disease related to the adenosine A 2A receptor is colorectal cancer.