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1. 发明授权

KR100596369B1 결정형의 암로디핀 유기산염 失效
标题翻译：氨氯地平的结晶有机酸盐
公开(公告)号：KR100596369B1
公开(公告)日：2006-07-03
申请号：KR1020030053072
申请日：2003-07-31
申请人： 씨제이 주식회사
发明人： 임동권 , 이혁구 , 서혜란 , 조성환 , 이광혁 , 김윤철 , 정성학 , 이성학 , 강현석 , 박경미 , 정윤택 , 천준희 , 박충실 , 윤용식 , 김영훈 , 연규정 , 채명윤 , 진해탁
IPC分类号： C07D211/90
摘要： 본 발명은 물리화학적 성질이 우수한 결정형의 암로디핀의 신규 유기산염, 그의 제조방법 및 그를 포함하는 약제학적 조성물에 관한 것이다.
암로디핀, 유기산염

2. 发明授权

KR100462304B1 암로디핀의 유기산염 失效
标题翻译： 암로디핀의유기산염
公开(公告)号：KR100462304B1
公开(公告)日：2004-12-17
申请号：KR1020020044857
申请日：2002-07-30
申请人： 씨제이 주식회사
发明人： 조성환 , 윤용식 , 정윤택 , 박충실 , 이혁구 , 이광혁 , 정은주 , 김영훈 , 진해탁 , 천준희 , 이성학 , 정성학 , 임동권 , 연규정 , 김윤철 , 박경미 , 강현석
IPC分类号： C07D211/86
CPC分类号： C07D211/90
摘要： Disclosed are a novel organic acid salt of amlodipine with superb physicochemical properties, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient.
摘要翻译：公开了一种具有极好物理化学性质的新型氨氯地平有机酸盐，其制备方法和含有它作为治疗活性成分的药物组合物。

3. 发明授权

KR100454890B1 4,5-디아미노 피리미딘 유도체 失效
公开(公告)号：KR100454890B1
公开(公告)日：2004-11-06
申请号：KR1019990011071
申请日：1999-03-22
申请人： 씨제이 주식회사
发明人： 장명식 , 서병철 , 이정근 , 이광혁 , 이윤하 , 김영지
IPC分类号： C07D403/04
摘要： PURPOSE: Provided are 4,5-diamino pyrimidine derivatives, which have improved solubility and bio-absorption rate, and inhibit both of cyclic guanosine 3', 5'-monophosphate phosphodiesterase and cyclic adenosine 3', 5'-monophosphate phosphodiesterase, so that they are useful for treatment of asthma. CONSTITUTION: The 4,5-diamino pyrimidine derivatives represented by formula (I) and physiologically acceptable salts thereof are provided, wherein X is C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl(C1-4)alkylene; Y is C1-2 alkyl; R1 is (i) phenyl optionally substituted with one or two groups selected from halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, or (ii) 1,3-dioxaindane substituted with one or two groups selected from halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R2 is tetrazol optionally substituted with one or two groups selected from halogen, hydroxy(C1-5)alkyl, C1-6 alkyl, C3-6 alkenyl, carboxy and halogen C1-4 alkoxy; R3 is COR4 or SOOR5; R4 and R5 are independently (i) a group selected from hydroxy, C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen C2-6 alkenyl and C1-4 alkoxy, or (ii) R6-benzene ring; and R6 is selected from hydrogen, hydroxy, C1-6 alkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen, nitro and C1-4 alkoxy.

4. 发明公开

KR1020040025549A 결정형의 암로디핀 유기산염 失效
标题翻译：水溶性有机酸盐
公开(公告)号：KR1020040025549A
公开(公告)日：2004-03-24
申请号：KR1020030053072
申请日：2003-07-31
申请人： 씨제이 주식회사
发明人： 임동권 , 이혁구 , 서혜란 , 조성환 , 이광혁 , 김윤철 , 정성학 , 이성학 , 강현석 , 박경미 , 정윤택 , 천준희 , 박충실 , 윤용식 , 김영훈 , 연규정 , 채명윤 , 진해탁
IPC分类号： C07D211/90
摘要： PURPOSE: A crystalline organic acid salt of amlodipine is provided, which has improved physicochemical properties such as water-resistance, stability, solubility and processing easiness, especially improved photostability. Therefore, it can be easily moved within the body of a patient and be stored for a long time. CONSTITUTION: A photostable crystalline form adipic acid salt of amlodipine has diffraction X-ray peaks at diffraction angle of 10.85 degree, 13.02 degree, 15.10 degree, 16.31 degree, 18.21 degree, 21.69 degree, 23.70 degree, 26.18 degree and 28.74 degree measured by X-ray powder diffraction method, and has X-ray powder diffraction pattern shown in figure 1 and melting point of 164 to 168 deg. C. A method for preparing the crystalline form adipic acid salt of amlodipine comprises reacting amlodipine with adipic acid in an inert solvent such as methanol. A pharmaceutical composition for treating ischemic heart disease or hypertension contains the crystalline form adipic acid salt of amlodipine, and pharmaceutically acceptable diluents or carriers.
摘要翻译：目的：提供氨氯地平的结晶有机酸盐，其具有改善的物理化学性质如耐水性，稳定性，溶解性和加工容易性，特别是改善的光稳定性。因此，可以容易地在患者体内移动并长时间储存。构成：氨氯地平己二酸盐的光稳定结晶形式衍射X射线衍射峰为X射线衍射峰，分别为X射线衍射峰，X射线衍射峰，射线粉末衍射法，并且具有图1所示的X射线粉末衍射图案，并且熔点为164至168度。 C.制备氨氯地平的结晶形式己二酸盐的方法包括在惰性溶剂如甲醇中使氨氯地平与己二酸反应。用于治疗缺血性心脏病或高血压的药物组合物含有氨氯地平的结晶形式己二酸盐和药学上可接受的稀释剂或载体。

5. 发明公开

KR1020040011754A 암로디핀의 유기산염 失效
标题翻译：有机酸亚麻酸盐
公开(公告)号：KR1020040011754A
公开(公告)日：2004-02-11
申请号：KR1020020044859
申请日：2002-07-30
申请人： 씨제이 주식회사
发明人： 조성환 , 윤용식 , 정윤택 , 박충실 , 이혁구 , 이광혁 , 정은주 , 김영훈 , 진해탁 , 천준희 , 이성학 , 정성학 , 임동권 , 연규정 , 김윤철 , 박경미 , 강현석
IPC分类号： C07D211/86
CPC分类号： C07D211/90
摘要： PURPOSE: Organic acid salt of amlodipine with excellent physico-chemical properties, its manufacture method and a pharmaceutical composition containing it are provided. CONSTITUTION: Amlodipine p-hydroxyphenylacetic acid salt represented by the formula(2) has crystallized form and is manufactured by reacting amlodipine and p-hydroxyphenylacetic acid. A pharmaceutical composition for the treatment of hypertension and cardiac diseases contains amlodipine p-hydroxyphenylacetic acid salt and a pharmaceutically acceptable diluent or carrier.
摘要翻译：目的：提供具有优异物理化学性质的氨氯地平的有机酸盐，其制备方法和含有它的药物组合物。构成：由式（2）表示的氨氯地平对羟基苯基乙酸盐具有结晶形式，并通过氨氯地平和对羟基苯基乙酸反应来制备。用于治疗高血压和心脏病的药物组合物含有氨氯地平对羟基苯基乙酸盐和药学上可接受的稀释剂或载体。

6. 发明公开

KR1020040011751A 암로디핀의 유기산염 无效
标题翻译：有机酸亚麻酸盐
公开(公告)号：KR1020040011751A
公开(公告)日：2004-02-11
申请号：KR1020020044856
申请日：2002-07-30
申请人： 씨제이 주식회사
发明人： 조성환 , 윤용식 , 정윤택 , 박충실 , 이혁구 , 이광혁 , 정은주 , 김영훈 , 진해탁 , 천준희 , 이성학 , 정성학 , 임동권 , 연규정 , 김윤철 , 박경미 , 강현석
IPC分类号： C07D211/86
CPC分类号： C07D211/90
摘要： PURPOSE: Provided is novel organic acid salt of amlodipine which has excellent physico-chemical properties. Also, provided are its manufacturing method and a pharmaceutical composition containing it as an active ingredient. CONSTITUTION: Amlodipine camphorsulfonic acid salt is represented by the formula(2). It has photostability and the crystallized form. Its manufacturing method is characterized by reacting amlodipine and camphorsulfonic acid in an inert solvent. A pharmaceutical composition for the treatment of hypertension or cardiac diseases contains amlodipine camphorsulfonic acid salt and a pharmaceutically acceptable diluent or carrier.
摘要翻译：目的：提供氨氯地平的新型有机酸盐，具有优异的物理化学性质。此外，其制造方法和含有它作为活性成分的药物组合物。构成：氨氯地平樟脑磺酸盐由式（2）表示。它具有光稳定性和结晶形式。其制备方法的特征在于使氨氯地平和樟脑磺酸在惰性溶剂中反应。用于治疗高血压或心脏病的药物组合物含有氨氯地平樟脑磺酸盐和药学上可接受的稀释剂或载体。

7. 发明公开

KR1020030066204A 세프디토렌 중간체의 제조방법 无效
标题翻译：制备中间体有用的合成CEFDITOREN的方法
公开(公告)号：KR1020030066204A
公开(公告)日：2003-08-09
申请号：KR1020020006540
申请日：2002-02-05
申请人： 씨제이 주식회사
发明人： 이광혁 , 조성환 , 윤용식 , 박충실 , 임동권
IPC分类号： C07D501/16
摘要： PURPOSE: A process for the preparation of an intermediate useful in the synthesis of cefditoren is provided, thereby preparing the high quality cefditoren intermediate without using any organic solvent at room temperature. CONSTITUTION: A process for the preparation of 7 - amino - 3 - £2 - (4 - methylthiazol - 5 - yl) vinyl| - 3 - cephem carboxylic acid of the formula (I) as an intermediate useful in the synthesis of cefditoren comprises reacting 7 - phenylacetamido - 3 - £2 - (4 - methylthiazol - 5 - yl) vinyl| - 3 - cephem carboxylic acid of the formula (II) with penicillin G amidase to remove a phenylacet group at 7-site, wherein the reaction temperature is 5 to 40 deg. C and the reaction pH is 8 to 8.5; a filtration process of the immobilized penicillin G amidase is optionally added after the completion of the reaction; and a crystallization process by adding an organic solvent into the filtered solution to control pH of the solution is optionally added.
摘要翻译：目的：提供一种制备可用于合成头孢托仑的中间体的方法，从而在室温下不使用任何有机溶剂制备高品质的头孢托仑中间体。构成：制备7-氨基-3-（2-（4-甲基噻唑-5-基）乙烯基）的方法作为可用于合成头孢托伦的中间体的式（I）的头孢烯羧酸，包括使7-苯基乙酰氨基-3-（2-甲基噻唑-5-基）乙烯基| （II）的头孢烯羧酸与青霉素G酰胺酶在7-位上除去苯乙酸基，其中反应温度为5〜40℃。 C，反应pH为8〜8.5; 任选地在反应完成后加入固定的青霉素G酰胺酶的过滤方法; 并且任选地加入通过向过滤的溶液中加入有机溶剂以控制溶液的pH的结晶方法。

8. 发明授权

KR100383136B1 7-아미노세팔로스포라닌산의 결정화 방법 失效
标题翻译： 7-아미노세팔로스포라닌산의결정화방법
公开(公告)号：KR100383136B1
公开(公告)日：2003-05-12
申请号：KR1020000078894
申请日：2000-12-20
申请人： 씨제이 주식회사
发明人： 이광혁 , 김진완 , 고동현 , 최광도
IPC分类号： C07D501/12
摘要： PURPOSE: Provided is a method for crystallizing 7-aminocephalosporanic acid(7-ACA) by adding acid having the mean value of each pKa of amino groups and carboxyl group to increase dissolving rate and filtration time. CONSTITUTION: The crystallizing method of 7-ACA is characterized by adding acid having 4-5 pKa, wherein in the acid is selected from the group consisting of acetic acid or formic acid. Therefore, 7-ACA having regular crystal size is manufactured in high yield.
摘要翻译：目的：提供一种通过加入具有每个氨基pKa和羧基的平均值的酸来结晶7-氨基头孢菌酸（7-ACA）以增加溶解速率和过滤时间的方法。构成：7-ACA的结晶方法的特征在于加入具有4-5pKa的酸，其中酸选自乙酸或甲酸。因此，具有规则晶体尺寸的7-ACA以高收率制造。

9. 发明授权

KR100337037B1 피리돈카르복실산유도체의중간체제조방법 失效
标题翻译：制备吡啶酮羧酸衍生物中间体的方法
公开(公告)号：KR100337037B1
公开(公告)日：2002-10-31
申请号：KR1019950016825
申请日：1995-06-22
申请人： 씨제이 주식회사
发明人： 송석범 , 황호성 , 이기호 , 이재목 , 김진완 , 이광혁
IPC分类号： C07D209/52
摘要： PURPOSE: A process for preparing intermediates of pyridone carboxylic acid derivatives is provided, thereby cheaply preparing the intermediates of pyridone carboxylic acid derivatives in higher yield. CONSTITUTION: A process for preparing intermediates of pyridone carboxylic acid derivatives represented by the formula(I) comprises halogen reaction of a compound of the formula(II), followed by the reaction with base in an organic solvent, wherein R1 and R2 are independently hydrogen or C1 to C5 lower alkyl, provided that one of two is hydrogen; R3 and R4 are independently hydrogen or C1 to C5 lower alkyl, provided that one of two is hydrogen; R5 is hydrogen or C1 to C5 lower alkyl; P is an amine protecting group; the organic solvent is selected from the group consisting of chloroform, acetone, acetonitrile, diethylether, benzene, xylene, carbon tetrachloride, toluene and dichloromethane; the base is selected from the group consisting of triethylamine, pyridine, N,N'-dimethylaniline, N,N'-diethylaniline, trimethylamine and 1,8-diazabicyclo£5,4,0|-7-undecane; and the reaction is carried out at 30 to 200 deg. C for 1 to 10 hours.

10. 发明公开

KR1020020047858A 세푸록심의 나트륨염을 함유하는 약학적 조성물의 안정화방법 失效
标题翻译：含有蛋白质钠盐的药物组合物稳定化方法
公开(公告)号：KR1020020047858A
公开(公告)日：2002-06-22
申请号：KR1020000076485
申请日：2000-12-14
申请人： 씨제이 주식회사
发明人： 이광혁 , 조성환 , 윤명식 , 류동수
IPC分类号： A61K31/546
摘要： PURPOSE: A method for the stabilization of a pharmaceutical composition containing sodium salt of cefuroxime is provided, thereby long-lasting the quality of the sodium salt of cefuroxime. CONSTITUTION: The method for the stabilization of a pharmaceutical composition containing sodium salt of cefuroxime comprises formulating the sodium salt of cefuroxime under 90% by volume, preferably 94% by volume of nitrogen-containing atmosphere with little water. The composition containing sodium salt of cefuroxime may be filled in a sealing vessel such as ample or vial with pyrogenetic free materials such as water, or in a big storing vessel with nitrogen liquid.
摘要翻译：目的：提供一种稳定含有头孢呋辛钠钠盐的药物组合物的方法，从而持续头孢呋辛钠钠的质量。构成：含有头孢呋辛钠钠盐的药物组合物的稳定化方法包括以少量的水配制90％（体积），优选94体积％的含氮气氛的头孢呋辛钠盐。包含头孢呋肟钠盐的组合物可以填充在诸如大量或小瓶的密封容器中，其中不含热原性物质如水，或者在具有氮气液体的大储存容器中。

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