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1. 发明申请

WO2005068471A1 NEW CRYSTALLINE FORMS OF CLOPIDOGREL HYDROBROMIDE AND METHODS OF THEIR PREPARATION 审中-公开
标题翻译：氯碳酸氢盐的新型结晶形式及其制备方法
公开(公告)号：WO2005068471A1
公开(公告)日：2005-07-28
申请号：PCT/CZ2004/000089
申请日：2004-12-21
申请人： ZENTIVA, A.S. , HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
发明人： HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention concerns clopidogrel hydrobromide in the crystalline Form I characterized by an X-ray diffraction pattern with characteristic interplanar distances d of 4.01; 4.39 and 3.17 ú and which is further characterized by bands in the infrared spectra at 1743; 1421; 1237, 760 and 728 cm -1 . Clopidogrel hydrobromide in the crystalline Form II is characterized by an Xray diffraction pattern with characteristic interplanar distances d of 4.52; 3.83; 3.48 ú, as well as bands in the infrared spectra at 1754; 1436; 1317 and 1223 cm -1 . Crystalline form III is characterized by the following peaks ascertained by X-ray diffraction at 20 positions: 7.796 °; 15.380 °; 18.389 °; 19.369 ° and 23.895 °. The method of preparation of clopidogrel hydrobromide in the crystalline Form I consist in precipitating the clopidogrel base dissolved in toluene with a concentrated solution of hydrobromic acid. The method of preparation of clopidogrel hydrobromide in the crystalline Form II consist in dissolving the clopidogrel base in an organic solvent and precipitating it with a solution of hydrobromic acid in toluene or with gaseous hydrogen bromide. Form III can be used for the preparation of pharmaceutically applicable Form II.
摘要翻译：本发明涉及结晶形式I中的氯吡格雷氢溴酸盐，其特征在于具有4.01的特征性面间距离d的X射线衍射图谱; 4.39和3.17ú，其进一步特征在于1743年红外光谱中的谱带; 1421; 结晶形式II中的氯吡格雷氢溴酸盐的特征在于具有4.52的特征性面间距d的X射线衍射图; 3.83; 3.48ú，以及1754年的红外光谱带; 1436; 1317和1223厘米-1。结晶形式III的特征在于在20个位置通过X射线衍射确定的以下峰：7.796°; 15.380°; 18.389°; 19.369°和23.895°。结晶形式I中氯吡格雷氢溴酸盐的制备方法是用氢溴酸浓溶液沉淀溶解在甲苯中的氯吡格雷碱。在晶型II中制备氯吡格雷氢溴酸盐的方法包括将氯吡格雷碱溶解在有机溶剂中，并用氢溴酸在甲苯或与溴化氢气体的溶液中沉淀。 III型可用于制备药学上适用的II型。

2. 发明申请

WO2006042481A1 METHOD OF OBTAINING CLOPIDOGREL 审中-公开
标题翻译：获得胶质的方法
公开(公告)号：WO2006042481A1
公开(公告)日：2006-04-27
申请号：PCT/CZ2005/000077
申请日：2005-10-17
申请人： ZENTIVA A.S. , HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
发明人： HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Separation of the camphorsulfonic salts of the compounds of formula (I) and (II) by one or more crystallizations from a mixture of two solvents, both R(-)-10-camphorsulfonic acid and its salts with the compounds of formula (I) and (II) being well soluble in at least one of the components, the formula of which can be indicated as R a OH, wherein R a is a straight or branched C 1 to C 5 alkyl. In the other components, camphorsulfonic acid and its salts are less soluble; however, they dissolve compounds of formula (I) and (II) very well.
摘要翻译：通过一种或多种结晶从R（ - ） - 10-樟脑磺酸及其与式（I）化合物的盐的两种溶剂的混合物中分离式（I）和（II）化合物的樟脑磺酸盐，和（II）可溶于至少一种组分，其配方可以表示为R 1

3. 发明申请

WO2005121084A1 A METHOD OF PREPARATION OF RAMIPRIL 审中-公开
标题翻译：一种制备RAMIPRIL的方法
公开(公告)号：WO2005121084A1
公开(公告)日：2005-12-22
申请号：PCT/CZ2005/000048
申请日：2005-06-08
申请人： ZENTIVA, a. s. , STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
发明人： STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： A method of preparation of ramipril of formula (I), during which the benzyl ester hydrochloride of formula (III) is converted to the benzyl ester of formula (II), which in turn affords, by reaction with the carboxyanhydride of formula (V), the benzyl ester of ramipril of formula (IV), which is subsequently converted to ramipril of formula (I).
摘要翻译：制备式（I）的雷米普利的方法，其中式（III）的苄酯盐酸盐转化成式（II）的苄基酯，其又通过与式（V）的羧酸酐反应，，式（IV）的雷米普里的苄基酯，其随后转化成式（I）的雷米普利。

4. 发明申请

WO2006094468A1 METHOD OF RACEMIZATION OF THE R(-) ISOMER OF THE (2-CHLOROPHENYL)-6,7- DIHYDROTHIENO[3,2-c]PYRIDINE-5(4H)-ACETIC ACID METHYL ESTER 审中-公开
标题翻译：（2-氯苯基）-6,7-二氢苯并[3,2-c]吡啶-5（4H） - 甲酸甲酯的R（ - ）异构体的研究方法
公开(公告)号：WO2006094468A1
公开(公告)日：2006-09-14
申请号：PCT/CZ2006/000010
申请日：2006-03-03
申请人： ZENTIVA, A.S. , HAJICEK, Josef , STEPANKOVA, Hana , KALIDOVA, Jan
发明人： HAJICEK, Josef , STEPANKOVA, Hana , KALIDOVA, Jan
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Racemization of the R(-) isomer of the (2-chlorophenyl) -6, 7-dihydrothieno [3, 2-c]pyridine- 5 (4H) -acetic acid methyl ester (Formula II) (also called R clopidogrel) is performed via conversion of a portion thereof to the S (+) isomer and it takes place in an organic solvent selected from alcohols , esters, ketones or ethers, or in their mixtures, in the presence of a base selected from substances of formula R1R2R3R4N+OH" wherein R1, R2, R3 and R4 are identical or different substituents selected from C1-C5 alkyls or C5, C6 cycloalkyls or aryls, C7-C9 alkyl-cycloalkyls or alkyl-aryls, the molar ratio of the base to the starting substance being 1: 1 to 1: 10. ,OMe Cl I Cl
摘要翻译：（2-氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯（式II）（也称为氯吡格雷）的R（ - ）异构体的外消旋化为通过将其一部分转化成S（+）异构体而进行，并且其在选自醇，酯，酮或醚的有机溶剂或其混合物中，在选自式R 1 R 2 R 3 R 4 N + OH“，其中R 1，R 2，R 3和R 4是相同或不同的选自C 1 -C 5烷基或C 5，C 6环烷基或芳基的取代基，C 7 -C 9烷基 - 环烷基或烷基 - 芳基，碱与起始物质的摩尔比为1：1至1：10，OMe Cl I Cl

5. 发明申请

WO2009067960A2 A METHOD OF MANUFACTURING (3R,4S)-L-(4-FLUOROPHENYL)-3-[(3S)-3-(4-FLUOROPHENYL)-3- HYDROXYPROPYL)]-4-(4-HYDROXYPHENYL)-2-AZETIDINONE AND ITS INTERMEDIATES 审中-公开
标题翻译：制备（3R，4S）-L-（4-氟代苯基）-3 - [（3S）-3-（4-氟苯基）-3-羟基丙基）] -4-（4-羟基苯基）-2-氮杂环丁酮的方法及其中介
公开(公告)号：WO2009067960A2
公开(公告)日：2009-06-04
申请号：PCT/CZ2008/000136
申请日：2008-11-05
申请人： ZENTIVA, A.S. , STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
发明人： STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
IPC分类号： C07C251/24 , C07D205/08 , C07D407/06 , C07D413/06
CPC分类号： C07C251/24 , C07D205/08 , C07D405/06 , C07D413/06 , Y02P20/55
摘要： A method of manufacturing (3 R ,4 S )-l-(4-fluorophenyl)-3-[(3 S )-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) of formula I, in which a protected ketone of general formula II, wherein R stands for a protective group, such as benzyloxycarbonyl, tert -butoxycarbonyl, benzhydryl or trityl, is reduced with asymmetrical borane agents in an inert organic solvent in the temperature range of -30 to +40 °C, and finally the obtained protected alcohol of general formula III, wherein R has the same meaning as above, is deprotected by the action of hydro genolytic or acidic agents in an inert organic solvent.
摘要翻译：制备（3R，4S）-1-（4-氟苯基）-3 - [（3S）-3-（4-氟苯基）-3-羟丙基）] - 4-（4-羟基苯基）-2-氮杂环丁酮（ezetimibe）其中R代表保护基团的通式II的受保护酮如苄氧羰基，叔丁氧基羰基，二苯甲基或三苯甲基，在不饱和硼烷试剂中在惰性有机溶剂中还原 -30℃〜+ 40℃的温度范围内，最后得到的通式III的保护醇，其中R具有与上述相同的含义，在惰性有机溶剂中由氢解酸或酸性剂的作用脱保护。

6. 发明申请

WO2009006859A2 A METHOD OF MANUFACTURING 5-[2-CYCLOPROPYL-1-(2-FLUOROPHENYL)-2-OXOETHYL]-4,5,6,7- TETRAHYDROTHIENO[3,2-C]PYRIDIN-2-YL ACETATE (PRASUGREL) 审中-公开
标题翻译：制备5- [2-环丙基-1-（2-氟代苯基）-2-氧代乙基] -4,5,6,7-四氢OT并[3,2-C]吡啶-2-基乙酸乙酯（PRASUGREL）的方法
公开(公告)号：WO2009006859A2
公开(公告)日：2009-01-15
申请号：PCT/CZ2008/000079
申请日：2008-07-08
申请人： ZENTIVA A.S. , STEPANKOVA, Hana , HAJICEK, Josef
发明人： STEPANKOVA, Hana , HAJICEK, Josef
CPC分类号： C07D495/02
摘要： A method of manufacturing 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7- tetrahydrothieno[3,2-c]pyridin-2-yl acetate, known under the INN name prasugrel of formula (I), in which the substance of formula (VI) is reacted with a cyclopropyl magnesium halide to produce the substance of formula (V), which reacted with methanesulfonyl chloride to give the methanesulfonate of formula (IV), which is further reacted with the compound of formula (III) to be converted the substance of formula (II) and the latter is converted to the substance of formula (I) with an acetylation agent.
摘要翻译：制备5- [2-环丙基-1-（2-氟苯基）-2-氧代乙基] -4,5,6,7-四氢噻吩并[3,2-c]吡啶-3-酮的方法，（I）的INN名称普拉格雷已知其中式（VI）的物质与环丙基卤化镁反应以产生式（V）的物质，其与甲磺酰氯反应得到（IV）的甲磺酸盐，其进一步与式（III）的化合物反应以转化为式（II）的物质，并且后者用乙酰化剂转化为式（I）的物质。 p>

7. 发明申请

WO2004037771A1 A METHOD OF PRODUCTION OF (-)-(S)-3-[1-(DIMETHYLAMINO)ETHYL]PHENYL-N-ETHYL-N-METHYLCARBAMATE 审中-公开
标题翻译：（ - ） - （S）-3- [1-（二甲基氨基）乙基]苯基-N-乙基-N-甲基磺酸酯的生产方法
公开(公告)号：WO2004037771A1
公开(公告)日：2004-05-06
申请号：PCT/CZ2003/000058
申请日：2003-10-21
申请人： ZENTIVA, A.S. , STEPANKOVA, HANA , HAJICEK, Josef , SIMEK, Stanislav
发明人： STEPANKOVA, HANA , HAJICEK, Josef , SIMEK, Stanislav
IPC分类号： C07C269/00
CPC分类号： C07C271/44 , C07B2200/07 , C07C215/50
摘要： The compound of formula (III), optionally its alkaline salt, is reacted with a compound of formula VII, wherein X is a leaving group, resulting in (S)-rivastigmine of formula II, which is then optionally converted into (S)-rivastigmine hydrogentartrade of formula I.
摘要翻译：式（III）的化合物，任选其碱性盐与式VII化合物反应，其中X是离去基团，得到式II的（S） - 三卡的明，然后任选地转化为（S） - 式I的利凡斯的明。

8. 发明申请

WO2011120475A1 A METHOD OF MANUFACTURING (S)-5-METHOXY-2-[[(4-METHOXY-3,5-DIMETHYL-2- PYRIMIDINYL)METHYL]SULFINYL]-1H-BENZIMIDAZOLE USING A CHIRAL COMPLEX WITH MANDELIC ACID 审中-公开
标题翻译：制备（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]硫代] -1H-苯并咪唑的方法，其使用具有仲胺酸的主要复合物
公开(公告)号：WO2011120475A1
公开(公告)日：2011-10-06
申请号：PCT/CZ2010/000031
申请日：2010-03-17
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , ZEZULA, Josef , HAJICEK, Josef , KRAL, Vladimir
发明人： STEPANKOVA, Hana , ZEZULA, Josef , HAJICEK, Josef , KRAL, Vladimir
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention deals with a new manufacturing method of ( S )-5-methoxy-2-[[(4-methoxy- 3,5-dimethyl-2-pyridinyl)methyl]sulphinyl]-1 H -benzimidazole of formula (I) and its salts of general formula (II), wherein the sulfide of general formula (III) is oxidized by hydroperoxides on a catalyst consisting of a chiral metallic complex containing ligands constituted by chiral functional derivatives of mandelic acid.
摘要翻译：本发明涉及式（I）的（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑的新制备方法和其通式（II）的盐，其中通式（III）的硫化物被氢过氧化物氧化在由含有由扁桃酸的手性功能衍生物构成的配体的手性金属络合物组成的催化剂上。

9. 发明申请

WO2011069473A1 A METHOD FOR THE PREPARATION OF PRASUGREL HYDROCHLORIDE IN POLYMORPHOUS FORM B 审中-公开
标题翻译：在多形态B中制备前体氢氯化物的方法
公开(公告)号：WO2011069473A1
公开(公告)日：2011-06-16
申请号：PCT/CZ2010/000126
申请日：2010-12-09
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
发明人： STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a method for the manufacture of 5-[2-cyclopropyl-l-(2- fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate hydrochloride of formula I (prasugrel hydrochloride) in crystalline form B, wherein prasugrel base of formula II is dissolved or suspended in an organic solvent and reacted with hydrogen chloride dissolved in an organic solvent or in water at a temperature in the range of -20 °C to 75°C and crystallized, optionally after addition of a co-solvent.
摘要翻译：本发明涉及制备5- [2-环丙基-1-（2-氟苯基）-2-氧代乙基] -4,5,6,7-四氢噻吩并[3,2-c] 乙酸盐酸盐（结晶形式B的盐酸普拉格雷），其中式Ⅱ的普拉格雷碱溶解或悬浮在有机溶剂中，并与溶解在有机溶剂中或在水中的氯化氢反应，其温度范围为 - 20℃至75℃，任选地在加入共溶剂后结晶。

10. 发明申请

WO2011057592A1 METHOD OF PRODUCING HIGHLY PURE PRASUGREL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：生产高纯度原料的方法及其药学上可接受的盐
公开(公告)号：WO2011057592A1
公开(公告)日：2011-05-19
申请号：PCT/CZ2010/000115
申请日：2010-11-12
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
发明人： STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： A method for the production of 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]- 4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate of formula (I) or its salts, characterized in that the compound of formula (III) in the form of a salt with an arene sulfonic acid is reacted with the compound of formula (XV), wherein Y means: chlorine, bromine, or an OR 4 group, wherein R 4 means an alkane sulfonic group or arene sulfonic group, in an organic solvent in the presence of an inorganic base or organic base, to give, after addition of an acetylating reagent and organic base to the reaction mixture, the compound of formula (I), which, after addition of a co-solvent, is crystallized from the reaction mixture, and the compound of formula (I) is optionally purified by crystallization and optionally converted to a salt by reaction with an organic or inorganic acid in a suitable solvent. (Formulae (I), (III), (XV)
摘要翻译：制备式（I）的5- [2-环丙基-1-（2-氟苯基）-2-氧代乙基] -4,5,6,7-四氢噻吩并[3,2-c]吡啶-2-基乙酸酯的方法（I）化合物或其盐，其特征在于与式（ⅩⅤ）化合物反应呈与磺酰基磺酸盐形式的式（Ⅳ）化合物，其中Y表示：氯，溴或OR 4 基团，其中R 4表示烷基磺酸基或芳烃磺酸基，在有机溶剂中，在无机碱或有机碱的存在下，在反应混合物中加入乙酰化试剂和有机碱后，得到式（I），其在加入共溶剂之后从反应混合物中结晶，并且式（I）化合物任选地通过结晶进行纯化，并任选地通过与有机或无机酸反应形成盐合适的溶剂。（式（I），（III），（XV）

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