FIELD: organic chemistry; pharmaceutics.
SUBSTANCE: present invention relates to the field of organic chemistry and pharmaceutics, namely to ERK2 inhibitors. (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide is disclosed, having the formula (1) in a crystal form. In addition, a method for the production of a crystal form of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide, amorphous salts of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide, and a method for the production of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide are disclosed. A pharmaceutical composition for prevention or treatment of diseases mediated with ERK1/2 is also described, containing effective amount of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide and a carrier. In addition, particles of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide are described, having an average-weight diameter from 1 mcm to 100 mcm. Among others, the use of the above-mentioned forms and salts of (2R)-2-(6-{5-chlor-2-[(oxane-4-yl)amino]pyrimidine-4-yl}-1-oxo-2,3-dihydro-1H-isoindole-2-yl)-N-[(1S)-1-(3-fluor-5-methoxyphenyl)-2-hydroxyethyl]propaneamide for the production of a drug for prevention or treatment of a disease or a condition mediated with ERK1/2 and a method for prevention or treatment of a disease or a condition mediated with ERK1/2, using these forms, are disclosed.
EFFECT: group of inventions provides effective inhibition of ERK2.
(1)
190 cl, 16 dwg, 11 tbl, 9 ex
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