FIELD: chemistry.
SUBSTANCE: invention relates to polymorphic forms N-(cyanomethyl)-4-(2-((4-(2',2',6',6'-d4-morpholino)phenyl)amino)pyrimidin-4-yl)benzamide in form of dihydrochloride (form I), dihydrochloride monohydrate (form II) and monohydrochloride (forms III and IV, respectively). Polymorphic form I of dihydrochloride of compound I has 3 or more characteristic peaks on X-ray powder diffraction pattern, selected from a 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°. Polymorphic form II of dihydrochloride of compound I has 3 or more characteristic peaks on X-ray powder diffraction pattern, selected from group consisting of 17.249 ± 0.2°, 19.224±0.2°, 23.885 ± 0.2° and 29.488 ± 0.2°. Polymorphic form III of monohydrochloride of compound I has 3 or more characteristic peaks on X-ray powder diffraction pattern, selected from a group consisting of 15.178 ± 0.2°, 20.705 ± 0.2°, 26.390 ± 0.2° and 28,088 ± 0.2°. Polymorphic form IV monohydrochloride of compound I has 3 or more characteristic peaks on an X-ray powder diffraction pattern selected from a group consisting of 12.493 ± 0.2°, 14.447 ± 0.2°, 17.627 ± 0.2°, 19.59 ± 0.2°, 23.231 ± 0.2°, 23.805 ± 0.2° and 24.831 ± 0.2°. Also disclosed are methods of producing polymorphous forms according to the invention.
EFFECT: polymorphic form is suitable for preparing a pharmaceutical composition for suppressing activity of non-receptor tyrosine kinases (such as JAK-kinase).
21 cl, 19 dwg, 6 tbl, 34 ex
