| 摘要 |
PURPOSE: A 1-{(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-yl]-4-oxobutyl}-5,5-difluoropiperidine-2-one tartrate 1.5 hydrate is provided to ensure excellent storage stability. CONSTITUTION: A method for preparing 1.5 hydrate of 1-{(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-yl]-4-oxobutyl}-5,5-difluoropiperidine-2-one tartrate comprise a step of recrystallizing 1-{(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-yl]-4-oxobutyl}-5,5-difluoropiperidine-2-one tartrate with water, acetonitrile/water, ethanol/water, ethanol/hexane or ethyl acetate/hexane solvent. A pharmaceutical composition for suppressing DPP-IV contains the 1.5 hydrate and pharmaceutically acceptable carrier. The composition is used for treating or preventing diabetes or obesity.
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