abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to the unknown hydrochloride of 6-amino-9-[(3R)-1-(2-butinoil)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8 and its crystalline form. The compound has the properties of a selective inhibitor of Bruton's tyrosine kinase (Btk) and can be used as an agent for the prophylaxis and / or treatment of diseases associated with Btk involving B-cells and mast cells. Such diseases are allergic, autoimmune, inflammatory, embolic, bone disease or malignancy. The latter may be a non-Hodgkin's lymphoma. Crystals of hydrochloride of 6-amino-9-[(3R)-1-(2-butinoil)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8 have in the powder X-ray diffraction, at least, 2 or more peaks at angles 2θ selected from about 8.11, 8.43, 11.57, 12.73, 13.85, 14.20, 14.67, 14.91, 15.94, 16.64, 18.06, 19.74, 20.42, 21.05, 22.57, 23.21, 23.85 and 24.70 degrees. The hydrochloride crystalline form has an endothermic peak at the temperature of 216°C. n EFFECT: said compound has a higher solubility and activity. n 10 cl, 4 dwg, 6 tbl, 13 ex |