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Crystalline peptide epoxyketone immunoproteasome inhibitor
专利权人:
ONYX THERAPEUTICS INC.
发明人:
PHIASIVONGSA PASIT
申请号:
NZ60287211
公开号:
NZ602872A
申请日:
2011.04.06
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
602872 Disclosed is crystalline (2S)-2-[{ (S)-2-(2-morpholinoacetamido)-1-oxo-propyl} amino]-3-(4-methoxyphenyl)-N-((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)propanamide having the structure of Formula (II) (and which is typically in the form of a toluene solvate), wherein the crystalline compound has 2&thetas values 3.62±0.20 6.52±0.20 7.20±0.20 8.66±0.20 0.04±0.20 10.82±0.20 12.98±0.20 14.42±0.20 16.46±0.20 17.32±0.20 17.98±0.20 18.02±0.20 18.88±0.20 19.06±0.20 19.56±0.20 19.88±0.20 20.40±0.20 21.36±0.20 22.16±0.20 23.20±0.20 25.40±0.20 and 28.82±0.20. Said crystalline compound is obtainable by a method comprising: (i) preparing a solution of a compound of Formula (II) in an organic solvent such as toluene (ii) bringing the solution to supersaturation to cause formation of crystals and (iii) isolating the crystals.
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