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1. 发明授权

KR100408431B1 1,2,3,9-테트라히드로-9-메틸-3-[(2-메틸-1Ｈ-이미다졸-1-일)메틸]-4Ｈ-카바졸-4-온 또는 그의 약제학적으로허용가능한 염의 제조 방법 失效
标题翻译： 1,2,3,9-테트라히드로-9-메틸-3 - [（2-메틸1H이미다졸）메틸] -4H-카바졸-4-또또또또또는그의약제학적으로허용가능한 염의제조방법
公开(公告)号：KR100408431B1
公开(公告)日：2003-12-06
申请号：KR1020010041524
申请日：2001-07-11
申请人： 한미사이언스 주식회사
发明人： 이광옥 , 김희석 , 함영진 , 김맹섭 , 김한경 , 김철경 , 정금신 , 이회철 , 김기은 , 이관순
IPC分类号： C07D403/06
摘要： PURPOSE: Provided is a novel manufacturing method of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on or its pharmaceutically acceptable salt in higher yield and purity than conventional methods. CONSTITUTION: The manufacturing method is characterized by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-on of the formula(2) with 2-methylimidazole derivative of the formula(3) in a mixed solvent of organic solvent and water at room temperature to 150 deg.C fro 2-12 hours to manufacture 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on of the formula(1) or its pharmaceutically acceptable salt.
摘要翻译：用途：提供了1,2,3,9-四氢-9-甲基-3 - （（2-甲基-1H-咪唑-1-基））-4H-咔唑-4-酮或其新的制备方法药学上可接受的盐比常规方法具有更高的收率和纯度。构成：制造方法的特征在于使式（2）的1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮与式（3）的2-甲基咪唑衍生物在混合物有机溶剂和水的溶剂在室温至150℃反应2-12小时，制得1,2,3,9-四氢-9-甲基-3 - （（2-甲基-1H-咪唑-1-基））） - 4H-咔唑-4-酮的式（1）或其药学上可接受的盐。

2. 发明授权

KR100342944B1 고순도 세프포독심 프록세틸의 제조방법 失效
标题翻译：制备高纯度CEFPODOXIME PROXETIL的方法
公开(公告)号：KR100342944B1
公开(公告)日：2002-07-02
申请号：KR1019990049174
申请日：1999-11-08
申请人： 한미사이언스 주식회사
发明人： 이관순 , 장영길 , 이재헌 , 박철현 , 박가승 , 정금신
IPC分类号： C07D501/36
CPC分类号： C07D501/00
摘要： 본발명은경구용세팔로스포린계항생제인세프포독심프록세틸을제조하는방법에관한것으로서, 유기용매중에서크라운에테르촉매존재하에세프포독심염을 1-아이오도에틸이소프로필카보네이트와반응시키는본 발명의방법에따르면, 하기화학식 1의세프포독심프록세틸을고순도로간편하게제조할수 있다:

3. 发明公开

KR1020040008377A 신규한 ｐ-당단백질 저해제, 그의 제조방법 및 이를유효성분으로 하는 경구투여용 조성물 失效
标题翻译： P-糖蛋白抑制剂，其制备方法和含有该组合物的口服组合物作为有效成分
公开(公告)号：KR1020040008377A
公开(公告)日：2004-01-31
申请号：KR1020020042005
申请日：2002-07-18
申请人： 한미사이언스 주식회사
发明人： 김희석 , 함영진 , 이광옥 , 방극찬 , 안영길 , 김한경 , 정금신 , 이회철 , 김기은 , 김맹섭
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D215/20 , C07D401/12
摘要： PURPOSE: A p-glycoprotein inhibitor, a preparation method thereof and an oral composition containing the same as an effective component are provided, thereby increasing the oral adsorption rate of an anti-cancer agent having low bioavailability. CONSTITUTION: A compound as a p-glycoprotein inhibitor is represented by the formula 1, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently hydrogen, hydroxyl, C1-3 alkyl or alkoxy; R5 and R6 may form 4 to 8-membered ring together; l, m and n are independently an integer of 0 to 4; X is R11, OR12 or NR13R14; and R11, R12, R13 and R14 are independently optionally substituted phenyl, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, quinazoline, quinoxaline, pyrrole, pyrazol, imidazol, triazol, tetrazol, oxazole, thiazole, oxadiazole, thiadiazol, benzimidazol, benzthiazol, isoxazole, isothiazole, benzoxazole, pyridazine or triazine. A method for preparing the compound of the formula 1 comprises reacting a compound of the formula 2 with a compound of the formula 3, wherein E is a leaving group such as halogen, methanesulfonyloxy or toluenesulfonyloxy.
摘要翻译：目的：提供p型糖蛋白抑制剂及其制备方法和含有该组合物的有效成分的口服组合物，从而提高生物利用度低的抗癌剂的口服吸附率。构成：作为p-糖蛋白抑制剂的化合物由式1表示，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地为氢，羟基，C 1-3烷基或烷氧基; R5和R6可以一起形成4至8元环; l，m和n分别为0〜4的整数。 X为R11，OR12或NR13R14; 吡唑，喹唑啉，喹喔啉，吡咯，吡唑，咪唑，三唑，四唑，恶唑，噻唑，恶二唑，噻二唑，苯并咪唑，苯并噻唑，苯并噻唑等。其中R 11，R 12，R 13和R 14独立地为任选取代的苯基，吡啶，嘧啶，吡嗪，异恶唑，异噻唑，苯并恶唑，哒嗪或三嗪。制备式1化合物的方法包括使式2化合物与式3化合物反应，其中E为离去基团如卤素，甲磺酰氧基或甲苯磺酰氧基。

4. 发明公开

KR1020030015655A 항암제의 경구흡수율을 증가시키는 인단계 화합물의결정성 산부가염, 이의 제조방법 및 이를 함유하는 약학적조성물 无效
标题翻译：增加基于反应物的化合物的盐酸添加盐，其增加了抗癌剂的口服吸收，其制备方法和含有其的药物组合物
公开(公告)号：KR1020030015655A
公开(公告)日：2003-02-25
申请号：KR1020010049522
申请日：2001-08-17
申请人： 한미사이언스 주식회사
发明人： 이관순 , 김맹섭 , 함영진 , 이광옥 , 김희석 , 김한경 , 김철경 , 정금신
IPC分类号： C07C255/47
摘要： PURPOSE: Provided are a crystalline acid addition salt having excellent stability, which increases the oral absorbance of anticancer agent having extremely low bioavailability when orally administered, a method for preparing the same, and a pharmaceutical composition containing the same. CONSTITUTION: The crystalline acid addition salt of indane-based compound is represented by formula 1(wherein HX is pharmaceutically acceptable inorganic or organic acid). The HX is selected from the group consisting of sulfuric acid, hydrochloric acid, phosphoric acid, nitric acid, acetic acid, hemisuccinic acid(1/2 succinic acid), malonic acid, maleic acid, citric acid, tartaric acid, lactic acid, fumaric acid, methanesulfonic acid, benzenesulfonic acid, toluylsulfonic acid, and trifluoroacetic acid. The method comprises adding an acid to the indane-based compound of formula 2 in water or organic solvent, or adding an acid to reactant solution for forming the indane-based compound of formula 2.
摘要翻译：目的：提供具有优异的稳定性的结晶酸加成盐，其口服给药时生物利用度极低的抗癌剂的口服吸光度，其制备方法和含有该药物的药物组合物。构成：茚满基化合物的结晶酸加成盐由式1表示（其中HX是药学上可接受的无机酸或有机酸）。 HX选自硫酸，盐酸，磷酸，硝酸，乙酸，半琥珀酸（1/2琥珀酸），丙二酸，马来酸，柠檬酸，酒石酸，乳酸，富马酸酸，甲磺酸，苯磺酸，甲苯磺酸和三氟乙酸。该方法包括在水或有机溶剂中向式2的茚满基化合物中加入酸，或向反应物溶液中加入酸以形成式2的茚满基化合物。

5. 发明授权

KR100503161B1 신규한 ｐ-당단백질 저해제, 그의 제조방법 및 이를유효성분으로 하는 경구투여용 조성물 失效
标题翻译：新型P-糖蛋白抑制剂，其制备方法和包含其的口服组合物
公开(公告)号：KR100503161B1
公开(公告)日：2005-07-25
申请号：KR1020020042005
申请日：2002-07-18
申请人： 한미사이언스 주식회사
发明人： 김희석 , 함영진 , 이광옥 , 방극찬 , 안영길 , 김한경 , 정금신 , 이회철 , 김기은 , 김맹섭
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D215/20 , C07D401/12
摘要： 본 발명은
화학식 1 의 구조를 갖는 p-당단백질 저해제 또는 약학적으로 허용가능한 그의 염, 그의 제조방법 및 이를 유효성분으로 함유하는 경구투여용 약학 조성물에 관한 것으로, 본 발명의 p-당단백질 저해제는 생체이용률이 극히 저조한 항암제와 동시에 경구투여하는 경우 약물의 경구흡수율을 월등히 증가시키므로 항암제의 경구투여용 제제의 제조에 유용하게 사용될 수 있다.

상기 식에서,
R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , R
8 , R
9 및 R
10 은 각각 독립적으로 수소, 히드록실, C
1-3 알킬 또는 알콕시이고;
R
5 와 R
6 은 함께 연결되어 4 내지 8-원 고리를 형성할 수 있고;
l, m, n은 각각 독립적으로 0 내지 4의 정수이고;
X는 R
11 , OR
12 또는 NR
13 R
14 이고;
R
11 , R
12 , R
13 및 R
14 는 각각 독립적으로 치환되거나 치환되지 않은 페닐, 피리딘, 피리미딘, 피라진, 퀴놀린, 이소퀴놀린, 퀴나졸린, 퀴녹살린, 피롤, 파라졸, 이미다졸, 트리아졸, 테트라졸, 옥사졸, 티아졸, 옥사디아졸, 티아디아졸, 벤즈이미다졸, 벤즈티아졸, 이소옥사졸, 이소티아졸, 벤즈옥사졸, 피리다진 또는 트리아진이다.

6. 发明公开

KR1020020039223A 1,2,3,9-테트라히드로-9-메틸-3-[(2-메틸-1Ｈ-이미다졸-1-일)메틸]-4Ｈ-카바졸-4-온 또는 그의 약제학적으로허용가능한 염의 제조 방법 失效
标题翻译： 1,2,3,9-四氢-9-甲基-3 - （（2-甲基-1H-咪唑-1-基））-4H-卡巴唑-4-酮或其药学上可接受的盐的制备方法
公开(公告)号：KR1020020039223A
公开(公告)日：2002-05-25
申请号：KR1020010041524
申请日：2001-07-11
申请人： 한미사이언스 주식회사
发明人： 이광옥 , 김희석 , 함영진 , 김맹섭 , 김한경 , 김철경 , 정금신 , 이회철 , 김기은 , 이관순
IPC分类号： C07D403/06
摘要： PURPOSE: Provided is a novel manufacturing method of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on or its pharmaceutically acceptable salt in higher yield and purity than conventional methods. CONSTITUTION: The manufacturing method is characterized by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-on of the formula(2) with 2-methylimidazole derivative of the formula(3) in a mixed solvent of organic solvent and water at room temperature to 150 deg.C fro 2-12 hours to manufacture 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on of the formula(1) or its pharmaceutically acceptable salt.
摘要翻译：目的：提供1,2,3,9-四氢-9-甲基-3 - （（2-甲基-1H-咪唑-1-基））-4H-咔唑-4-酮或其制备方法的新颖制备方法药学上可接受的盐，其产率和纯度高于常规方法。构成：制备方法的特征在于使式（2）的1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮与式（3）的2-甲基咪唑衍生物在混合溶剂的有机溶剂和水在室温至150℃下反应2-12小时，制备1,2,3,9-四氢-9-甲基-3 - （（2-甲基-1H-咪唑-1-基）））-4H-咔唑-4-酮或其药学上可接受的盐。

7. 发明公开

KR1020010045748A 고순도 세프포독심 프록세틸의 제조방법 失效
标题翻译：制备高纯度CEFPODOXIME PROXETIL的方法
公开(公告)号：KR1020010045748A
公开(公告)日：2001-06-05
申请号：KR1019990049174
申请日：1999-11-08
申请人： 한미사이언스 주식회사
发明人： 이관순 , 장영길 , 이재헌 , 박철현 , 박가승 , 정금신
IPC分类号： C07D501/36
CPC分类号： C07D501/00
摘要： PURPOSE: Provided is a method for simply and economically manufacturing high-purity cefpodoxime proxetil which is useful as antibiotics without generating byproducts. CONSTITUTION: The method for manufacturing high-purity cefpodoxime proxetil of the formula (1) is characterized by reacting cefpodoxime salt of the formula (3) with 1-iodoethylisopropylcarbonate of the formula (4) at minus10-40 deg.C, preferably 0-30 deg.C, for 0.5-3.0 hours, preferably 0.5-1.5 hours, in the presence of catalyst like crown ether and organic solvent. And cefpodoxime salt and 1-iodoethylisopropylcarbonate are added in a ratio of 1:1-3, preferably 1.2-1.5. The organic solvent is selected from acetonitrile, tetrahydrofuran, N,N-dimethylformamide, N,N-dimethylsulfoxide, and N,N-dimethylacetamide.
摘要翻译：目的：提供简单经济地制造高纯度头孢泊肟酯的方法，它可用作抗生素而不产生副产物。构成：式（1）的高纯度头孢泊肟酯的制备方法的特征在于使式（3）的头孢泊肟盐与式（4）的1-碘代乙基异丙基碳酸酯在-10-40℃下反应， 30℃，0.5-3.0小时，优选0.5-1.5小时，在催化剂如冠醚和有机溶剂存在下进行。并且加入头孢泊肟盐和1-碘乙基异丙基碳酸酯的比例为1:1.3，优选1.2-1.5。有机溶剂选自乙腈，四氢呋喃，N，N-二甲基甲酰胺，N，N-二甲基亚砜和N，N-二甲基乙酰胺。

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