6--3-4-[2--1-]--2-4-[] A Novel Crystalline Form of 6-Hydroxy-3-4-[2-Piperidin-1-YlEthoxy]-Phenoxy-2-4-MethoxyphenylBenzo[b] Thiophene Hydrochloride

• Main Authors: CONRAD PRESTON CHARLES, FLOM MERLYN GERARD, BUSH JULIE KAY
• Format: Patent
• Language: English; Korean
• Published: 15.06.2001
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PURPOSE: 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. CONSTITUTION: A 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 2 =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. 본 발명은 6-히드록시-3-(4-[2-(피페리딘-1-일)에톡시]-페녹시)-2-(4-메톡시페닐)벤조[b]티오펜 히드로클로라이드의 신규한 결정수화물 및 이의 용도에 관한 것이다. 이의 용도는 심혈관성 질병, 고지질혈증 및 골다공증을 포함하는 에스트로겐 결핍과 관련된 질환의 억제; 그리고, 자궁내막증, 자궁 섬유증, 에스트로겐-의존성 암(유방암과 자궁암), 전립선 암, 양성 전립선 과형성, 알츠하이머 병을 포함하는 중추 신경계 장애와 같은 다른 병리학적 상태의 억제, 유방암의 예방 및 ChAT를 증가시키는 것(up-regulating ChAT)이다.