发明名称 NEW CRYSTAL FORM OF 6-HYDROXY-3-(4-[2-(PIPERIDIN-1-YL) ETHOXY] PHENOXY)-2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE
摘要 PROBLEM TO BE SOLVED: To obtain the subject crystal form having an X-ray diffraction pattern including specific peaks, being a nonsteroidal mixed estrogen antagonist/agonist useful for reducing serum cholesterol and preventing hyperadiposis, osteoporosis, an estrogen-dependent cancer such as breast cancer, etc. SOLUTION: This crystalline 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride(arzoxifene) has an X-ray diffraction pattern including peaks at 2θ=4.6±0.2, 7.8±0.2, 9.3±0.2, 14.0±0.2, 17.6±0.2, 20.8±0.2 and 24.3±0.2 (in the case of obtaining these data from a copper radiation source at 25±2 deg.C at 35±10%; relative humidity). The compound can be produced and isolated at a room temperature, for example, by crystallizing arzoxifene from a mixed solution of isopropyl alcohol and water.
申请公布号 JP2001048880(A) 申请公布日期 2001.02.20
申请号 JP20000228949 申请日期 2000.07.28
申请人 ELI LILLY & CO 发明人 BUSH JULIE KAY;CONRAD PRESTON CHARLES;FLOM MERLYN GERARD
分类号 C07D409/12;A61K31/4433;A61K31/445;A61K31/4535;A61K31/565;A61K35/22;A61K38/09;A61P3/06;A61P5/32;A61P9/00;A61P13/08;A61P15/00;A61P19/00;A61P19/10;A61P25/00;A61P25/28;A61P35/00;C07D333/64;(IPC1-7):C07D409/12;A61K31/453 主分类号 C07D409/12
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