HYDROCHLORIDE OF DERIVATIVE PURINONA Russian patent published in 2017 - IPC C07D473/18 A61K31/522 A61P29/00 A61P7/02 A61P19/00 A61P35/00 A61P37/08 A61P37/02 

Abstract RU 2615999 C2

FIELD: chemistry.

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.

EFFECT: said compound has a higher solubility and activity.

10 cl, 4 dwg, 6 tbl, 13 ex

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RU 2 615 999 C2

Authors

Yamamoto Singo

Esidzava Tosio

Dates

2017-04-12Published

2012-11-28Filed