[1,2,4] TRIAZOLO [1,5-a] PYRIDINE DERIVATIVE AND CRYSTALLINE FORM THEREOF
AssigneeWest China Hospital, Sichuan University
InventorsWeimin LI, Yang HE, Li ZHANG, Bojiang CHEN, Zhixin QIU
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Abstract
The present invention discloses [1,2,4]triazolo[1,5-a]pyridine derivatives, as well as the crystalline form thereof. Compounds provided in the present invention have significant inhibitory effects on tumor cells, can be used for the prevention and/or treatment of tumor-related diseases, especially lung cancer, and have wide application prospects.
Claims20
Compounds of formula (I), or the pharmaceutically acceptable salts thereof, or the solvates thereof:
- In which,
- R1 represents halogens, —CN, —OH, —NH2, —NH(C1-C4 alkyl) or —N(C1-C4 alkyl)2;
- R2 and R3 independently represent none, or one or more halogens, or one or more C1-C4 alkyls in the ring of their linkage, respectively;
- R4 and R5 independently represent hydrogen, halogen or C1-C4 alkyl, respectively;
- or, R4 and R5, together with the nitrogen linked with them, form 5-7 members heterocyclic ring containing 0-1 oxygen or sulfur atom, in which the carbons can be optionally further substituted by C1-C4 alkyl;
- n represents 1, 2, or 3.
Crystal form A of compound of formula (III), characterized in that:
- In the X-ray powder diffraction of this crystal form, the typical peaks are observed at 2θ diffraction angles of 9.85±0.20, 10.13±0.20, 17.19±0.20, 17.48±0.20, 17.56±0.20, 17.64±0.20, 17.72±0.20, 19.36±0.20, 19.80±0.20, 19.97±0.20, 20.16±0.20, 20.22±0.20, 20.86±0.20, 21.01±0.20, 21.26±0.20, 23.84±0.20, 23.92±0.20, 24.43±0.20, 26.23±0.20, 27.55±0.20, and 27.64±0.20.
Crystal form B of compound of formula (IV), characterized in that:
- In the X-ray powder diffraction of this crystal form, the typical peaks are observed at 2θ diffraction angles of 9.80±0.20, 14.93±0.20, 19.39±0.20, 19.78±0.20, 22.95±0.20, 29.90±0.20, 30.20±0.20, 30.29±0.20, 38.03±0.20, 38.14±0.20, 46.06±0.20, 46.19±0.20, 54.34±0.20, and 54.48±0.20.
Dependencies are inferred from the claim text.