FIELD: medicine.
SUBSTANCE: invention relates to a crystal form of N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridine-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5-amine hydrochloride characterized by a powder X-ray diffraction pattern containing peaks at following values 2θ (CuKα λ=1.5418 Å), equal to 12.5±0.1, 13.0±0.1, 14.2±0.1, 18.7±0.1, 25.2±0.1 and 30.8±0.1. The invention also relates to a method for obtaining the specified crystal form of N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridine-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5-amine hydrochloride, which includes following stages: 1) slurrying of N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridine-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5-amine (Compound A) in a mixture of water and an organic solvent mixed with water selected from a group consisting of ethanol and acetone; 2) heating the resulting suspension to a temperature of approximately 50°C to 75°C; 3) acidification of the resulting suspension with hydrochloric acid to form a transparent solution, while maintaining the temperature of about 50°C to 75°C; and 4) lowering the temperature of the resulting solution to obtain the crystal form of N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridine-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5-amine, where the mass fraction of the residual organic solvent contained in the specified crystal form is less than 0.5%.
EFFECT: crystal form of N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridine-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidine-5-amine hydrochloride is obtained, which can be used in medicine in the treatment of a disease or disorder mediated by PRC2.
7 cl, 11 dwg, 3 tbl, 4 ex
| Title | Year | Author | Number |
|---|---|---|---|
| PYRIDINONE PYRIDAZINONE DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) | 2007 |
|
RU2472782C2 |
| mTOR KINASE INHIBITORS FOR ONCOLOGICAL INDICATIONS AND DISEASES METABOLICALLY BOUND TO mTOR/PI3K/AKT | 2009 |
|
RU2546658C2 |
| MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM | 2009 |
|
RU2692796C2 |
| TRIAZOLO-PYRIMIDINE COMPOUNDS AND THEIR USE | 2019 |
|
RU2802866C2 |
| COMPOUNDS APPLICABLE AS ATR KINASE INHIBITORS | 2020 |
|
RU2750148C1 |
| COMPOUNDS SUITABLE FOR USE AS ATR KINASE INHIBITORS | 2014 |
|
RU2687276C2 |
| METHOD OF PRODUCING ATR KINASE INHIBITORS (EMBODIMENTS) | 2014 |
|
RU2720408C2 |
| TRICYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM AND USING THEM FOR TREATING IMMUNOLOGICAL AND ONCOLOGICAL COMPOUNDS | 2009 |
|
RU2545023C9 |
| HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES | 2013 |
|
RU2671628C2 |
| COMPOUNDS BASED ON PYRAZOLOPYRIDINONE | 2018 |
|
RU2806751C2 |
