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1. 发明公开

KR1020090063817A 세펨 화합물의 결정형 산 부가염의 직접 제조방법 无效
标题翻译：制备CEPHEM衍生物的晶体酸添加盐的直接方法
公开(公告)号：KR1020090063817A
公开(公告)日：2009-06-18
申请号：KR1020070131322
申请日：2007-12-14
申请人： (주) 성운파마코피아 , 우진비엔지 주식회사
发明人： 정인화 , 박성진 , 이수철 , 최왕근 , 강석진
IPC分类号： C07D501/34
摘要： A method for manufacturing a crystalline acid-added salt of cephem compound which is used for antibiotics is provided to easily introduce nitrogen-containing heterocyclic group and directly obtain from the acid-added salt. A method for producing a crystalline acid-added salt of cephem compound comprises: a step of reacting a cepotaxim derivative of the chemical formula 2 or its salt and heterocycle compound of R1-H under the presence of base and halogenation silyl compound to obtain the acid-added salt of cephem compound of the chemical formula 1; and a step of crystallizing the acid-added salt of cephem compound using sulphuric acid(H2SO4). The cephem compound of the chemical formula 1 is cefepime, cefpirome, or cefquinome. The base is dimethylaniline or diethylaniline. The reaction solvent is acetonitrile, dichloromethane, dimethylformamide or dimethylacetamide.
摘要翻译：提供了用于抗生素的头孢烯化合物的结晶性酸加成盐的制造方法，容易地导入含氮杂环基，并直接从酸加成盐得到。一种头孢烯化合物的结晶性酸加成盐的制造方法，其特征在于，使化学式2的头孢噻肟衍生物或其盐与R1-H的杂环化合物在碱和卤化甲硅烷基化合物的存在下反应，得到酸化学式1的头孢烯化合物的添加盐; 和使用硫酸（H 2 SO 4）使头孢烯化合物的酸加成盐结晶的步骤。化学式1的头孢烯化合物是头孢吡肟，头孢匹罗或头孢喹肟。碱为二甲基苯胺或二乙基苯胺。反应溶剂为乙腈，二氯甲烷，二甲基甲酰胺或二甲基乙酰胺。

2. 发明授权

KR101016608B1 로큐로니움 브로마이드의 제조방법 有权
标题翻译：溴化溴化铵的制备方法
公开(公告)号：KR101016608B1
公开(公告)日：2011-02-22
申请号：KR1020080121867
申请日：2008-12-03
申请人： (주) 성운파마코피아
发明人： 정인화 , 박성진 , 이수철 , 최왕근
IPC分类号： C07J11/00 , C07J43/00
摘要： 본 발명에 따른 로큐로니움 브로마이드(Rocuronium Bromide)화합물의 제조방법은, 하기 화학식 IV의 화합물을 몰포린과 반응시키는 단계를 포함하는 제조방법으로서, 이를 통해 고순도 및 고품질의 로큐로니움 브로마이드 화합물을 제조할 수 있다.
(IV)
로큐로니움 브로마이드(Rocuronium Bromide)

3. 发明公开

KR1020100062929A 새로운 결정형의 아데포비어 디피복실, 그 조성물 및 이것의 제조방법 无效
标题翻译： ADEFOVIR DIPIVOXIL的新型水晶形态及其组合物及其制备方法
公开(公告)号：KR1020100062929A
公开(公告)日：2010-06-10
申请号：KR1020090115901
申请日：2009-11-27
申请人： (주) 성운파마코피아 , 박석용
发明人： 정인화 , 박성진 , 이수철 , 최왕근
IPC分类号： C07D473/16 , C07D473/02
摘要： PURPOSE: A novel crystal adefovir dipivoxil and a method for manufacturing the same are provided to ensure high solubility and dispersibility and to prepare adefovir dipivoxil of 98% or more of purity. CONSTITUTION: A crystal adefovir dipivoxil is a characteristic peak of 2θ at X-ray diffraction pattern. The adefovir dipivoxil has peak of about 6.4, 8.1, 8.6, 10.5, 12.8, 13.5, 14.5, 15.2, 15.6, 16.1, 16.5, 17.4, 17.8, 18.3, 18.7, 19.5, 20.1, 20.5, 20.9, 21.5, 22.2, 23.0, 23.6, 24.1, 24.4, 24.7, 26.9, 27.2, 30.1, or 33.4. The endoergic transition measured by differential scanning calorimetry(DSC) method is 67°C. A method for manufacturing the crystal adefovir dipivoxil comprises: a step of inputting amorphous adefovir dipivoxil in reactor; a step of adding isopropanol to form adefovir dipivoxil solution; a step of cooling the solution to crystallizing; and a step of filtering. A pharmaceutical composition contains the crystal adefovir dipivoxil and pharmaceutically acceptable carrier.
摘要翻译：目的：提供一种新颖的结晶阿德福韦酯及其制备方法，以确保高溶解性和分散性，并制备纯度达98％以上的阿德福韦酯。构成：阿德福韦酯是一种特征峰，为2＆amp; 在X射线衍射图。阿德福韦酯具有约6.4,8.1,8.6,10.5,12.8,13.5,14.5,15.2,15.6,16.1,16.5,17.4,17.8,18.3,18.7,19.5,20.1,20.5,20.9,21.5,22.2,23.0的峰。，23.6，24.1，24.4，24.7，26.9，27.2，30.1或33.4。通过差示扫描量热法（DSC）测定的消臭过渡是67℃。制备结晶阿德福韦酯的方法包括：在反应器中输入无定形阿德福韦酯的步骤; 加入异丙醇形成阿德福韦酯溶液的步骤; 将溶液冷却至结晶的步骤; 和过滤步骤。药物组合物含有阿德福韦酯和药学上可接受的载体。

4. 发明公开

KR1020100063370A 로큐로니움 브로마이드의 제조방법 有权
标题翻译：制备溴化硼的方法
公开(公告)号：KR1020100063370A
公开(公告)日：2010-06-11
申请号：KR1020080121867
申请日：2008-12-03
申请人： (주) 성운파마코피아
发明人： 정인화 , 박성진 , 이수철 , 최왕근
IPC分类号： C07J11/00 , C07J43/00
CPC分类号： C07J11/00 , C07J13/00 , C07J43/00
摘要： PURPOSE: A method for preparing high quality and high purity rocuronium bromide is provided, which is industrially useful. CONSTITUTION: A method for preparing rocuronium bromide comprises the steps of: obtaining the compound of the chemical formula V by reacting the compound of IV with morpholine; obtaining the compound of the chemical formula VI by reacting the compound of the chemical formula V with an acetate compound; obtaining a compound of the chemical formula VII by reacting the compound of the chemical formula VI with pyrrolidine; and obtaining the compound of the chemical formula VIII by reacting the compound of the chemical formula VII with acetyl chloride.
摘要翻译：目的：提供一种制备高品质，高纯度罗库溴铵的方法，在工业上有用。构成：制备罗库溴铵的方法包括以下步骤：通过使IV化合物与吗啉反应获得化学式V的化合物; 通过使化学式V的化合物与乙酸酯化合物反应获得化学式VI的化合物; 通过使化学式VI的化合物与吡咯烷反应获得化学式VII的化合物; 并通过化学式Ⅶ化合物与乙酰氯反应得到化学式Ⅷ化合物。

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