Phenyl amino pyrimidine compound or polymorph of salt thereof
AssigneeSuzhou Zelgen Biopharmaceuticals Co., Ltd.
InventorsBinhua Lv, Chengwei Li, Dan Xiao
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Abstract
The present invention relates to a phenyl amino pyrimidine compound or a polymorph of a salt thereof, specifically, to N-(cyanomethyl)-4-(2-((4-(2′,2′,6′,6′-d4-morpholino)phenyl)amino)pyrimidin-4-yl)benzamide, or a pharmaceutically acceptable salt thereof, or a polymorph of a solvate thereof, that is, a compound shown in formula I or salt thereof, or a polymorph of a solvate thereof. The polymorph is suitable for preparing a pharmaceutical composition for suppressing non-receptor tyrosine kinases (such as JAK kinase).
Claims15
A polymorph, wherein the polymorph is a polymorph of compound I or a pharmaceutically acceptable salt thereof or a solvate thereof:
- wherein the polymorph is selected from the group consisting of:
- polymorph I of the hydrochloride of compound I, wherein the polymorph I has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 5.426±0.2°, 9.985±0.2°, 13.424±0.2°, 14.765±0.2°, 25.148±0.2° and 26.566±0.2°;
- polymorph II of the solvate of the hydrochloride of compound I, wherein the polymorph II has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 17.249±0.2°, 19.224±0.2°, 23.885±0.2° and 29.488±0.2°,
- polymorph III of the hydrochloride of compound I, wherein the polymorph III has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 15.178±0.2°, 20.705±0.2°, 26.390±0.2° and 28.088±0.2°,
- polymorph IV of the hydrochloride of compound I, wherein the polymorph IV has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 12.493±0.2°, 14.447±0.2°, 17.627±0.2°, 19.519±0.2°, 23.231±0.2°, 23.805±0.2° and 24.831±0.2°,
- polymorph V of the compound I, wherein the polymorph V has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 13.621±0.2°, 18.634±0.2°, 20.331±0.2°, 21.675±0.2°, 22.621±0.2° and 28.048±0.2°, and
- polymorph VI of the compound I, wherein the polymorph VI has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 4.084±0.2°, 18.832±0.2°, 19.542±0.2°, 20.529±0.2°, and 26.468±0.2°.
A method for preparing a polymorph, wherein the polymorph is polymorph II of the solvate of the hydrochloride of compound I, wherein the polymorph II has a characteristic X-ray powder diffraction spectrum comprising diffraction peaks at at least three diffraction angles (2θ) selected from the group consisting of 17.249±0.2°, 19.224±0.2°, 23.885±0.2° and 29.488±0.2°, the method comprising steps of:
- (1) mixing compound I and a first solvent to form a first solvent containing compound I:
- (2) adding hydrochloric acid and acetone to the first solvent to form a first mixture;
- (3) stirring the first mixture, thereby precipitating a solid;
- (4) separating and obtaining the solid precipitated from step (3);
- (5) mixing the separated solid and the mixed solvent of acetone/water to form a second mixture;
- and
- (6) separating crystallized polymorph II from the second mixture.
Dependencies are inferred from the claim text.