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Crystalline tripeptide epoxy ketone protease inhibitors
专利权人:
ONYX THERAPEUTICS INC.
发明人:
PHIASIVONGSA PASIT,SEHL LOUIS C
申请号:
NZ59584710
公开号:
NZ595847A
申请日:
2010.03.22
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
595847 Disclosed is a crystalline form of the compound (2S)-2-[{ (S)-2-[{ (2-methyl-thiazol-5-yl)carbonyl} amino]-3-methoxy-1-oxo-propyl} amino]-N-((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)-3-methoxy-propanamide having the structure as represented by formula (II) wherein the crystalline compound has 2theta values 8.94; 9.39; 9.76; 10.60; 11.09; 12.74; 15.27; 17.74; 18.96; 20.58; 20.88; 21.58; 21.78; 22.25; 22.80; 24.25; 24.66; 26.04; 26.44; 28.32; 28.96; 29.65; 30.22; 30.46; 30.78; 32.17; 33.65; 34.49; 35.08; 35.33; 37.85; and 38.48; and has a melting point of about 145 to about 150°C; said crystalline form can be obtained by (i) preparing a solution of a compound of Formula (II) in an organic solvent such as acetonitrile, ethyl acetate, heptanes, hexanes, isopropyl acetate, methanol, methylethyl ketone, tetrahydrofuran, toluene, water, or any combination thereof; (ii) bringing the solution to supersaturation to cause formation of crystals; and (iii) isolating the crystals.
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