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1. 发明公开

KR20070094230A PHARMACEUTICAL COMPOSITION CONTAINING CLOPIDOGREL CAMPHORSULFONATE OR POLYMORPHIC FORMS THEREOF 审中-公开
标题翻译：含有角叉菜酮或其多形态的药物组合物
公开(公告)号：KR20070094230A
公开(公告)日：2007-09-20
申请号：KR20060024610
申请日：2006-03-17
申请人： HANMI PHARM IND CO LTD
发明人： KIM WON JEOUNG , KIM HAN KYONG , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： A61K31/4743 , A61P7/02 , C07D495/04
CPC分类号： A61K31/47
摘要： A pharmaceutical composition comprising clopidogrel camphorsulfonate or a polymorphic form thereof is provided to maintain high purity at an initial state due to excellent moisture and heat stability of the clopidogrel camphorsulfonate or the polymorphic form thereof. A pharmaceutical composition for treating or preventing diseases caused by platelet aggregation comprises clopidogrel camphorsulfonate represented by the formula(1) or a polymorphic form thereof as an effective ingredient, wherein the diseases are stroke, cerebral arteriosclerosis, cardiomyopathy, angina pectoris, arrhythmia, peripheral arterial occlusive disease and Buerger`s disease.
摘要翻译：提供包含氯吡格雷樟脑磺酸盐或其多晶型形式的药物组合物，由于氯吡格雷樟脑磺酸盐或其多晶型物的优异的水分和热稳定性，在初始状态下保持高纯度。用于治疗或预防由血小板聚集引起的疾病的药物组合物包括由式（1）表示的氯吡格雷樟脑磺酸盐或其多晶型物作为有效成分，其中疾病为中风，脑动脉硬化，心肌病，心绞痛，心律失常，外周动脉闭塞性疾病和Buerger病。

2. 发明授权

KR100714197B1 PROCESS FOR THE PREPARATION OF VOGLIBOSE 无效
标题翻译：制备VOGLIBOSE的方法
公开(公告)号：KR100714197B1
公开(公告)日：2007-04-26
申请号：KR20060031066
申请日：2006-04-05
申请人： HANMI PHARM IND CO LTD
发明人： LEE JAE HEON , KIM DONG JUN , PARK EUN JU , YOO JAE HO , PARK GHA SEUNG , CHANG YOUNG KIL , LEE GWAN SUN
IPC分类号： C07C213/02 , C07C215/42 , C07C217/52
摘要： 본 발명은 보글리보스 (voglibose)의 신규한 제조방법에 관한 것으로, 1) 이노소스 (inosose) 유도체를 출발물질로 하여 환원성 아민화 (reductive amination) 반응을 통해 퍼벤질 보글리보스를 제조하는 단계; 2) 상기 퍼벤질 보글리보스에 벤젠설폰산을 가하여 이를 벤젠설폰산염의 상태로 분리하는 단계; 3) 상기 퍼벤질 보글리보스 벤젠설폰산염의 벤질기를 탈보호시켜 보글리보스 벤젠설폰산염을 수득하는 단계; 및 4) 상기 보글리보스 벤젠설폰산염을 강염기와 반응시켜 유리시키는 단계를 포함하는 본 발명의 제조방법에 의하면, 당뇨병 치료제인 보글리보스를 간단한 공정에 의해 고수율 및 고순도로 대량 생산할 수 있다.

3. 发明公开

KR20070095646A METHOD OF PREPARING CLOPIDOGREL 1,5-NAPHTHALENEDISULFONATE AND HYDRATE THEREOF 无效
标题翻译：氯萘酚1,5-萘硫代磺酸盐及其水合物的制备方法
公开(公告)号：KR20070095646A
公开(公告)日：2007-10-01
申请号：KR20060026110
申请日：2006-03-22
申请人： HANMI PHARM IND CO LTD
发明人： KIM EUN SOOK , YUN SANG MIN , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： A method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof is provided to conveniently mass-produce the desired product with excellent stability from a conventional acid-added salt of clopidogrel using a neutral disodium salt of 1,5-naphthalene disulfonic acid. A method for preparing clopidogrel 1,5-naphthalenedisulfonate represented by the formula(1) or a hydrate thereof comprises a step of performing a salt conversion reaction of an acid-added salt of clopidogrel represented by the formula(2) and a disodium salt of 1,5-naphthalene disulfonic acid represented by the formula(3) in the presence of water or a mixture of water and an organic solvent such as methanol, ethanol, isopropanol and acetone, wherein HX is an acid forming the acid-added salt with the clopidogrel(wherein the naphthalene disulfonic acid is excluded) and 0.45-0.7 mol of the disodium salt of 1,5-naphthalene disulfonic acid is used regarding 1 mol of the clopidogrel included in the acid-added salt.
摘要翻译：提供制备氯吡格雷1,5-萘二磺酸盐或其水合物的方法，以方便地使用1,5-萘二磺酸的中性二钠盐从常规的氯酸格酸加酸盐中大量生产具有优异稳定性的所需产物。由式（1）表示的氯吡格雷1,5-萘二磺酸盐或其水合物的制备方法包括以式（2）表示的氯吡格雷的酸加成盐和式（2）所示的二钠盐的盐转化反应由式（3）表示的1,5-萘二磺酸在水或水与有机溶剂如甲醇，乙醇，异丙醇和丙酮的混合物存在下，其中HX是形成酸加成盐的酸，对于1摩尔含酸盐中所含的氯吡格雷，使用氯吡格雷（其中不包括萘二磺酸）和0.45-0.7摩尔的1,5-萘二磺酸的二钠盐。

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