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1. 发明申请

WO2009006861A2 A METHOD FOR ISOLATION AND PURIFICATION OF MONTELUKAST 审中-公开
标题翻译： MONTELUKAST的分离和纯化方法
公开(公告)号：WO2009006861A2
公开(公告)日：2009-01-15
申请号：PCT/CZ2008000081
申请日：2008-07-08
申请人： ZENTIVA AS , HALAMA ALES , JIRMAN JOSEF , PETRICKOVA HANA
发明人： HALAMA ALES , JIRMAN JOSEF , PETRICKOVA HANA
CPC分类号： C07D215/18
摘要： A method of isolation of Montelukast of formula I from reaction mixtures, comprising conversion of the crude substance to well-crystallizing salts with primary amines in the environment of at least one organic solvent and acetonitrile, followed by re-crystallization of these salts with simultaneous removal of chemical impurities and use of the chemically pure salts of Montelukast with primary amines for direct transformation to the pharmaceutically useful amorphous form of Montelukast sodium of formula II.
摘要翻译：一种从反应混合物中分离式I的孟鲁司他的方法，包括在至少一种有机溶剂和乙腈的环境中将粗物质与伯胺转化为结晶良好的盐，随后重新结晶这些盐同时除去的化学杂质，并使用Montelukast的化学纯盐与伯胺直接转化成药学上可用的无定形形式的式II的蒙特鲁卡斯钠。

2. 发明申请

WO2009111998A2 SPECIFIC IMPURITIES OF MONTELUKAST 审中-公开
标题翻译： MONTELUKAST的具体特点
公开(公告)号：WO2009111998A2
公开(公告)日：2009-09-17
申请号：PCT/CZ2009/000038
申请日：2009-03-11
申请人： ZENTIVA, K.S. , HALAMA, Ales , BOUSKOVA, Olga , GIBALA, Petr , JIRMAN, Josef
发明人： HALAMA, Ales , BOUSKOVA, Olga , GIBALA, Petr , JIRMAN, Josef
IPC分类号： C07D215/18 , C07D405/10 , A61K31/47 , A61P37/00
CPC分类号： C07D215/18 , C07D405/10
摘要： The subject-matter of the invention consists in a method of removing specific impurities of montelukast of formula (I), which occur due to chemical instability of the target substance and also contaminate the substance in the preparation process. Further, methods of isolation of specific impurities of montelukast defined by formulae (V-A), (IV-A), (XIIIa-A), (XIIIb-A) and analytic methods used for the control of the production of montelukast in the pharmaceutical quality.
摘要翻译：本发明的主题是一种除去由于目标物质的化学不稳定性而发生的式（I）的孟鲁司特的特定杂质的方法，并且在制备过程中污染该物质。此外，分离由式（VA），（IV-A），（XIIIa-A），（XIIIb-A）定义的孟鲁司特的特定杂质和用于控制药物质量中孟鲁司特的生产的分析方法。

3. 发明申请

WO2008083635A1 A METHOD FOR THE PREPARATION OF MONTELUKAST 审中-公开
标题翻译：一种制备蒙脱石的方法
公开(公告)号：WO2008083635A1
公开(公告)日：2008-07-17
申请号：PCT/CZ2008/000002
申请日：2008-01-08
申请人： ZENTIVA, A.S. , HALAMA, Ales , JIRMAN, Josef
发明人： HALAMA, Ales , JIRMAN, Josef
IPC分类号： C07D215/18 , C07D323/00
CPC分类号： C07D215/18 , C07D323/00
摘要： A method of preparation of Montelukast of formula (I) by reaction of the compound of formula (III) and a compound of formula (IX), characterized in that the reaction is carried out in the presence of a base, an inert solvent and a component increasing selectivity of the process, especially of a polyether of general formula (XIII), wherein R stands for hydrogen or an alkyl and the value of n varies from 1 to 40, polyethyleneglycol of general formula (XIV), wherein n=l to 40 or a crown-ether of formulae (XV), (XVI) or (XVII).
摘要翻译：通过式（III）化合物和式（IX）化合物的反应制备式（I）孟鲁司特的方法，其特征在于该反应在（其中R代表氢或烷基并且n的数值在1至40之间变化），通式（XIII）的聚乙二醇，通式（XIII）的聚乙二醇， XIV），其中n = 1至40或式（XV），（XVI）或（XVII）的冠醚。

4. 发明申请

WO2002088120A1 METHOD FOR OBTAINING PIOGLITAZONE AS AN ANTIDIABETIC AGENT 审中-公开
标题翻译：获得PIOGLITAZONE作为抗菌剂的方法
公开(公告)号：WO2002088120A1
公开(公告)日：2002-11-07
申请号：PCT/CZ2002/000024
申请日：2002-04-25
申请人： LÉCIVA, A.S. , HALAMA, Ales , HEJTMÁNKOVÁ, Ludmila , LUSTIG, Petr , RICHTER, Jindrich , SRSNOVÁ, Lucie , JIRMAN, Josef
发明人： HALAMA, Ales , HEJTMÁNKOVÁ, Ludmila , LUSTIG, Petr , RICHTER, Jindrich , SRSNOVÁ, Lucie , JIRMAN, Josef
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , Y02P20/55
摘要： A method for obtaining antidiabetic of formula (I), wherein the method comprises condensing of a 4-derivatized phenol or phenolate of general formula (II), wherein R is an amino group-containing organic residue, selected from the group comprising a residue of the following formula -NHR 3 , wherein R 3 is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein R b represents a carboxy group either in the free acid form or in the form of a salt or ester or another functional derivative or the nitrile group CN, and M represents a hydrogen or alkali metal atom, with a pyridine base of general formula (III), wherein Z is a leaving group other than a halogen, wherein, before or after carrying out the condensation, the following operations are carried out: (a) diazotizing the amino group present in organic residue R; (b) converting the diazotised residue R into a derivative of 2-halopropionate or 2-halopropionitrile of formula (B), wherein R b is as defined above and X is a halogen; (c) cyclizing the derivative of 2-halopropionate or 2-halopropionitrile with thiourea; (d) hydrolysing the resulting imine thus giving pioglitazone of formula (I).
摘要翻译：一种获得式（I）抗糖尿病的方法，其中所述方法包括将通式（II）的4-衍生化苯酚或酚盐缩合，其中R是含氨基的有机残基，其选自包含下述式-NHR 3其中R 3为氢或保护基，其在进一步处理前除去，和通式（A）的残基，其中R b表示羧基，游离酸形式或盐或酯或其它官能衍生物或腈基CN形式，M表示氢或碱金属原子与通式（III）的吡啶碱形成，其中Z为离去基团其它其中，在进行缩合之前或之后进行以下操作：（a）重氮化存在于有机残基R中的氨基; （b）将重氮化残基R转化为式（B）的2-卤代丙酸酯或2-卤代丙腈的衍生物，其中R b如上所定义，X是卤素; （c）用硫脲使2-卤代丙酸酯或2-卤代丙腈的衍生物环化; （d）水解所得的亚胺，从而得到式（I）的吡格列酮。

5. 发明申请

WO2010022690A2 A METHOD OF PREPARATION OF HIGHLY PURE VILDAGLIPTIN 审中-公开
标题翻译：一种制备高纯度维拉胶的方法
公开(公告)号：WO2010022690A2
公开(公告)日：2010-03-04
申请号：PCT/CZ2009/000105
申请日：2009-08-25
申请人： ZENTIVA, K.S. , HALAMA, Ales , KAFKOVA Bozena , CHVOJKA, Tomas
发明人： HALAMA, Ales , KAFKOVA Bozena , CHVOJKA, Tomas
CPC分类号： C07D207/16
摘要： The present invention deals with a new method of preparation of chemically highly pure and pharmaceutically usable vildagliptin (I), including analytic control of the production process and quality of the target substance. The newly found process is based on the preparation and isolation of a mixture of l-haloacetyl-2-(S)-pyrrolidine carboxamide of chemical formula (VI), where X stands for a chlorine or bromine atom, with trialkylamine hydrohalides of chemical formula R 1 R 2 R 3 N*HX, where R 1 , R 2 and R 3 independently stand for a linear or branched alkyl with 1 to 6 carbon atoms, substituents R 1 and R 2 can be connected with a bridge and form a cycle with 2 to 6 carbon atoms, or can be connected with an ether bond, X stands for a chlorine or bromine atom. The invention also deals with analytical standards and analytical methods used for the control of the production process and final quality of vildagliptin.
摘要翻译：本发明涉及一种制备化学高纯度和药用维格列汀（I）的新方法，包括对目标物质的生产过程和质量的分析控制。新发现的方法是基于化学式（VI）的1-卤代乙酰基-2-（S） - 吡咯烷甲酰胺的混合物的制备和分离，其中X表示氯或溴原子，其中化学式为三烷基胺氢卤化物 R1R2R3N * HX，其中R1，R2和R3独立地表示具有1至6个碳原子的直链或支链烷基，取代基R1和R2可以与桥连接并形成具有2至6个碳原子的循环，或可以连接具有醚键，X表示氯或溴原子。本发明还涉及用于控制生产过程和维格列汀的最终质量的分析标准和分析方法。

6. 发明申请

WO2009006861A3 A METHOD FOR ISOLATION AND PURIFICATION OF MONTELUKAST 审中-公开
公开(公告)号：WO2009006861A3
公开(公告)日：2009-01-15
申请号：PCT/CZ2008/000081
申请日：2008-07-08
申请人： ZENTIVA, A.S. , HALAMA, Ales , JIRMAN, Josef , PETRICKOVA, Hana
发明人： HALAMA, Ales , JIRMAN, Josef , PETRICKOVA, Hana
IPC分类号： C07D215/18
摘要： A method of isolation of Montelukast of formula I from reaction mixtures, comprising conversion of the crude substance to well-crystallizing salts with primary amines in the environment of at least one organic solvent and acetonitrile, followed by re-crystallization of these salts with simultaneous removal of chemical impurities and use of the chemically pure salts of Montelukast with primary amines for direct transformation to the pharmaceutically useful amorphous form of Montelukast sodium of formula II.

7. 发明申请

WO2006010345A1 SALT OF OXALIC ACID WITH 5-[4-[2-(N-METHYL-N-(2-PYRIDYL)-AMINO)ETHOXY]BENZYL]THIAZOLIDIN-2,4-DIONE AND A METHOD OF ITS PREPARATION AND ITS USE 审中-公开
标题翻译：盐酸与5- [4- [2-（N-甲基-N-（2-吡啶基） - 氨基）乙氧基]苄基]噻唑烷-2,4-二酮及其制备方法及其用途
公开(公告)号：WO2006010345A1
公开(公告)日：2006-02-02
申请号：PCT/CZ2005/000058
申请日：2005-07-20
申请人： ZENTIVA, A.S. , HALAMA, Ales
发明人： HALAMA, Ales
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： The salt of oxalic acid with 5-[4-[2-( N -methyl- N -(2-pyridyl)amino)-ethoxy]-benzyl]-thiazolidin-2,4-dione of formula III including its tautomers and solvates. The method of preparation of the salt of oxalic acid with 5-[4-[2-( N -methyl- N -(2-pyridyl)amino)-ethoxy]benzyl]thiazolidin-2,4-dione consists in a reaction of 5-[4-[2-( N -methyl- N -(2-pyridyl)-amino)ethoxy]benzyl]thiazolidin-2,4-dione of formula I with oxalic acid, the reaction being carried out in a solution in organic solvent or its mixture with water.
摘要翻译：草酸盐与式III的5- [4- [2-（N-甲基-N-（2-吡啶基）氨基） - 乙氧基] - 苄基] - 噻唑烷-2,4-二酮的盐，包括其互变异构体和溶剂合物。用5- [4- [2-（N-甲基-N-（2-吡啶基）氨基） - 乙氧基]苄基]噻唑烷-2,4-二酮制备草酸盐的方法在于具有式I的5- [4- [2-（N-甲基-N-（2-吡啶基） - 氨基）乙氧基]苄基]噻唑烷-2,4-二酮与草酸反应，该反应在有机溶剂或其与水的混合物。

8. 发明申请

WO2010022690A3 A METHOD OF PREPARATION OF HIGHLY PURE VILDAGLIPTIN 审中-公开
标题翻译：一种制备高纯度VILDAGLIPTIN的方法
公开(公告)号：WO2010022690A3
公开(公告)日：2010-11-11
申请号：PCT/CZ2009000105
申请日：2009-08-25
申请人： ZENTIVA K S , HALAMA ALES , KAFKOVA BOZENA , CHVOJKA TOMAS
发明人： HALAMA ALES , KAFKOVA BOZENA , CHVOJKA TOMAS
IPC分类号： C07D207/16
CPC分类号： C07D207/16
摘要： The present invention deals with a new method of preparation of chemically highly pure and pharmaceutically usable vildagliptin (I), including analytic control of the production process and quality of the target substance. The newly found process is based on the preparation and isolation of a mixture of l-haloacetyl-2-(S)-pyrrolidine carboxamide of chemical formula (VI), where X stands for a chlorine or bromine atom, with trialkylamine hydrohalides of chemical formula R1R2R3N*HX, where R1, R2 and R3 independently stand for a linear or branched alkyl with 1 to 6 carbon atoms, substituents R1 and R2 can be connected with a bridge and form a cycle with 2 to 6 carbon atoms, or can be connected with an ether bond, X stands for a chlorine or bromine atom. The invention also deals with analytical standards and analytical methods used for the control of the production process and final quality of vildagliptin.
摘要翻译：本发明涉及制备化学高纯度和药学可用的维格列汀（I）的新方法，包括对目标物质的生产过程和质量的分析控制。新发现的方法基于制备和分离化学式（VI）的1-卤代乙酰基-2-（S） - 吡咯烷甲酰胺（其中X代表氯或溴原子）与三烷基胺氢卤化物的化学式 R 1 R 2 R 3 N * HX，其中R 1，R 2和R 3独立地代表具有1至6个碳原子的直链或支链烷基，取代基R 1和R 2可以与桥连接并形成具有2至6个碳原子的环，或可以连接用醚键，X代表氯或溴原子。本发明还涉及用于控制维格列汀的生产过程和最终质量的分析标准和分析方法。

9. 发明申请

WO2008083635B1 A METHOD FOR THE PREPARATION OF MONTELUKAST 审中-公开
标题翻译：一种制备MONTELUKAST的方法
公开(公告)号：WO2008083635B1
公开(公告)日：2008-10-09
申请号：PCT/CZ2008000002
申请日：2008-01-08
申请人： ZENTIVA AS , HALAMA ALES , JIRMAN JOSEF
发明人： HALAMA ALES , JIRMAN JOSEF
IPC分类号： C07D215/18 , C07D323/00
CPC分类号： C07D215/18 , C07D323/00
摘要： A method of preparation of Montelukast of formula (I) by reaction of the compound of formula (III) and a compound of formula (IX), characterized in that the reaction is carried out in the presence of a base, an inert solvent and a component increasing selectivity of the process, especially of a polyether of general formula (XIII), wherein R stands for hydrogen or an alkyl and the value of n varies from 1 to 40, polyethyleneglycol of general formula (XIV), wherein n=l to 40 or a crown-ether of formulae (XV), (XVI) or (XVII).
摘要翻译：通过式（III）化合物与式（IX）化合物的反应制备式（I）的孟鲁司他的方法，其特征在于反应在碱，惰性溶剂和组分增加了该方法的选择性，特别是通式（XIII）的聚醚，其中R代表氢或烷基，n的值在1至40之间，通式（XIV）的聚乙二醇，其中n = 1至 40或式（XV），（XVI）或（XVII）的冠醚。

10. 发明申请

WO2006125402A1 A PROCESS FOR THE CRYSTALLIZATION OF ROSIGLITAZONE AND ITS DERIVATIVES FROM MIXED SOLVENTS 审中-公开
标题翻译： ROSIGLITAZONE及其衍生物从混合溶剂中的结晶过程
公开(公告)号：WO2006125402A1
公开(公告)日：2006-11-30
申请号：PCT/CZ2006/000034
申请日：2006-05-19
申请人： ZENTIVA, A.S. , HALAMA, Ales , RICHTER, Jlndrich
发明人： HALAMA, Ales , RICHTER, Jlndrich
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Crystallization of rosiglitazone of formula (I), its penultimate of formula (II), or salts with acids of formula (III), wherein HX stands for a mineral or carboxylic acid, is carried out from mixed organic solvents, consisting of mixtures of carboxylic acids, particularly formic acid, acetic acid or propionic acid, with aliphatic alcohols, particularly methanol, ethanol, 1-propanol, 2- propanol, butanols or amyl alcohols.
摘要翻译：式（I）的罗格列酮，其倒数第二式（II）的结晶或与式（III）的酸的盐，其中HX代表矿物或羧酸，由混合的有机溶剂进行，所述混合有机溶剂由羧酸酸，特别是甲酸，乙酸或丙酸，与脂族醇，特别是甲醇，乙醇，1-丙醇，2-丙醇，丁醇或戊醇。

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