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    • 3. 发明专利
    • Crystal of sulfonyl amidine compound
    • 磺酰胺化合物的晶体
    • JP2014051470A
    • 2014-03-20
    • JP2012197913
    • 2012-09-07
    • Astellas Pharma Incアステラス製薬株式会社
    • YAMAMOTO HIROBUMIHIRANO SUKEAKIYAMAZAKI KOJI
    • C07D235/12
    • PROBLEM TO BE SOLVED: To provide a crystal of (2R)-N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzimidazole-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropanimidamide suitable for industrial production having sufficiently appropriate properties for a raw drug in the medicine development.SOLUTION: Inventors have completed this invention by successfully crystallizing (2R)-N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzimidazole-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropanimidamide, and by finding that a high melting point-type crystal and a low melting point-type crystal are suitable for industrial production having sufficiently appropriate properties for a raw drug in the medicine development. These crystals in this invention can be utilized as raw drugs of medicines for the treatment of sex hormone-dependent disorders.
    • 待解决的问题:为了提供(2R)-N - ({5- [3-(2,5-二氟苯基)-2-(1,3-二氢-2H-苯并咪唑-2-亚基)-3 - 异丙酰基] -2-氟苯基}磺酰基)-2-羟基丙酰亚胺酰胺,适用于工业生产,具有药物开发中原料药具有足够合适的性能。解决方案:发明人通过成功地结晶(2R)-N - ({5 - [3-(2,5-二氟苯基)-2-(1,3-二氢-2H-苯并咪唑-2-亚基)-3-氧代丙酰基] -2-氟苯基}磺酰基)-2-羟基丙酰亚胺酰胺, 高熔点型晶体和低熔点型晶体适用于药物开发中具有足够合适的原料药性的工业化生产。 本发明中的这些晶体可用作用于治疗性激素依赖性疾病的药物的原药。