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AssigneeAstellas Pharma Inc.
InventorsTakashi Nakamura, Takumi Okamoto, Yutaka Hirakura, Kouji Yamazaki, Akio Kakefuda, Hiroyuki Yamashita
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[Problem] A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide with excellent activity as an androgen receptor (AR) antagonistic compound, the salts thereof, or the solvate thereof, which is suitable for industrialization as a bulk drug of pharmaceutical products; a pharmaceutical composition comprising the crystal as an active ingredient; and the pharmaceutical composition which is the AR antagonistic drug are provided. [Solution] A01-type crystal of monohydrate, A01-type crystal of hydrochloride, A01-type crystal of hydrobromide, and A01-type crystal of methanesulfonate of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide, which have certain crystal forms, are provided.
(2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide monohydrate.
A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide monohydrate.
A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide hydrochloride.
A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide hydrobromide.
A crystal of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide methanesulfonate.
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Dependencies are inferred from the claim text.