FIELD: pharmaceutics.
SUBSTANCE: invention relates to polymorphous solid crystalline forms 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)piperidine-2,6-dione of following structural formula. Solid crystalline forms of compound corresponding to structural formula
,
represent crystalline form A1 of hydrochloride salt of said compound with indications of powder x-ray peak at approximately 8.6, 13.1, 20.5 and 26.3 degrees 2θ; either crystalline form of A monohydrate of said compound, having powder x-ray, including peaks at approximately 14.6, 15.6, 16.7, 21.9 and 30.0 degrees 2θ; crystalline form B, having powder x-ray, including peaks at approximately 10.6, 14.7, 19.1 and 25.9 degrees 2θ; crystalline form C with powder x-ray, including peaks at approximately 10.8, 15.1, 25.1 and 26.6 degrees 2θ; crystalline form E hydrate with powder x-ray, including peaks at approximately 7.3, 14.6, 22.0, 30.0 and 37.0 degrees 2θ; crystalline form F, having powder x-ray, including peaks at approximately 14.5, 15.7, 22.7 and 29.9 degrees 2θ. Invention covers also data of differential scanning calorimetry, thermogravimetric analysis data, indices of hygroscopicity and stability of obtained solid crystalline forms. Invention also relates to pharmaceutical composition containing therapeutically effective amount of solid shape and pharmaceutically acceptable carrier, thinner or excipient.
EFFECT: compound possesses properties of TNF-α and can be used for treating various forms of cancer, angiogenesis, macular degeneration and associated syndrome, pain and other disorders and diseases associated with TNF-α.
42 cl, 23 dwg, 10 tbl, 4 ex
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