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PROBLEM TO BE SOLVED: To provide a p-toluenesulfonic acid salt (PTSA) of a selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H- chromen-4-one (TGR-1202) that exhibits enhanced solubility and pharmacokinetics upon oral administration.
SOLUTION: The present invention relates to a PTSA salt of TGR-1202 having a d(0.9) of from about 5 to about 50 μm, such as from about 5 to about 25 μm or from about 5 to about 15 μm.
SELECTED DRAWING: None
COPYRIGHT: (C)2020,JPO&INPIT
【課題】本発明が解決しようとする課題は、経口投与において高められた溶解性及び薬物動態を示す、選択的PI3Kデルタ抑制剤(S)−2−(1−(4−アミノ−3−(3−フルオロ−4−イソプロポキシフェニル)−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−6−フルオロ−3−(3−フルオロフェニル)−4H−クロメン−4−オン(TGR−1202)のp−トルエンスルホン酸塩(PTSA)を提供することである。【解決手段】本発明は、約5〜約50μm、例えば、約5〜約25μmまたは約5〜約15μmのd(0.9)を有する、TGR−1202のPTSA塩に関する。【選択図】なし