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1. 发明申请

WO02088120B1 METHOD FOR OBTAINING PIOGLITAZONE AS AN ANTIDIABETIC AGENT 审中-公开
标题翻译：获得PIOGLITAZONE作为抗真菌剂的方法
公开(公告)号：WO02088120B1
公开(公告)日：2004-02-26
申请号：PCT/CZ0200024
申请日：2002-04-25
申请人： LECIVA A S , HALAMA ALES , HEJTMANKOVA LUDMILA , LUSTIG PETR , RICHTER JINDRICH , SRSNOVA LUCIE , JIRMAN JOSEF
发明人： HALAMA ALES , HEJTMANKOVA LUDMILA , LUSTIG PETR , RICHTER JINDRICH , SRSNOVA LUCIE , JIRMAN JOSEF
IPC分类号： A61K31/4427 , A61P3/10 , 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 , wherein R is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein R 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 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是氢或保护基，其在进一步处理之前被除去，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）将重氮化的残基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。

2. 发明申请

WO2007147374A3 PROCESS FOR THE PREPARATION OF SOLIFENACIN 审中-公开
标题翻译：制备辛伐他汀的方法
公开(公告)号：WO2007147374A3
公开(公告)日：2008-04-17
申请号：PCT/CZ2007000061
申请日：2007-06-21
申请人： ZENTIVA AS , JIRMAN JOSEF , JUNEK RICHARD , LUSTIG PETR , RICHTER JINDRICH , PLACEK LUKAS
发明人： JIRMAN JOSEF , JUNEK RICHARD , LUSTIG PETR , RICHTER JINDRICH , PLACEK LUKAS
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A process for the preparation of (1 S)-QR)-I -azabicyclo[2.2.2.]oct-3-yl 3,4-dihydro-1-phenyl- 2(1H)-isoquinoline carboxylate by reacting (1S)-alkyl 1-phenyl-1, 2,3, 4-tetrahydro-2- isoquinoline carboxylate with 3-(R)-quinuclidol in an inert solvent, where a primary alkyl ester of the carboxylate whose alkyl length is C 1 -C 4 is used and the reaction is catalyzed by a non-nucleophilic base.
摘要翻译：（1S）-QR）-1-氮杂双环[2.2.2]辛-3-基3,4-二氢-1-苯基-2（1H） - 异喹啉羧酸酯的制备方法， - 烷基1-苯基-1,2,3,4-四氢-2-异喹啉羧酸酯与3-（R） - 奎宁二醇在惰性溶剂中反应，其中烷基长度为C 1的羧酸酯的伯烷基酯使用C 3 S 4并且该反应由非亲核碱催化。

3. 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。

4. 发明申请

WO2009111998A3 SPECIFIC IMPURITIES OF MONTELUKAST 审中-公开
标题翻译： MONTELUKAST的具体特点
公开(公告)号：WO2009111998A3
公开(公告)日：2010-03-25
申请号：PCT/CZ2009000038
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 , A61K31/47 , A61P37/00 , C07D405/10
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。

5. 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。

6. 发明申请

WO2009012734A2 NEW SALTS OF BAZEDOXIFENE 审中-公开
标题翻译： BAZEDOXIFENE的新盐
公开(公告)号：WO2009012734A2
公开(公告)日：2009-01-29
申请号：PCT/CZ2008000089
申请日：2008-07-24
申请人： ZENTIVA AS , JIRMAN JOSEF , RICHTER JINDRICH
发明人： JIRMAN JOSEF , RICHTER JINDRICH
CPC分类号： C07D209/12
摘要： The invention deals with new crystalline salts of bazedoxifene, by means of which a high API quality can be achieved in a high yield.
摘要翻译：本发明涉及巴西多昔芬的新结晶盐，借此可以以高产率实现高API质量。

7. 发明申请

WO2008077357A3 A METHOD FOR THE PREPARATION OF SOLIFENACIN 审中-公开
标题翻译：一种制备溶胶蛋白的方法
公开(公告)号：WO2008077357A3
公开(公告)日：2008-08-14
申请号：PCT/CZ2007000119
申请日：2007-12-21
申请人： ZENTIVA AS , JIRMAN JOSEF , JUNEK RICHARD
发明人： JIRMAN JOSEF , JUNEK RICHARD
IPC分类号： C07D453/00
CPC分类号： C07D453/00
摘要： A method of preparing (lS)-(3R)-l-azabicyclo[2.2.2]oct-3-yl 3,4-dihydro-l-phenyl-2(lH)- isoquinoline carboxylate (solifenacin) or its pharmaceutically acceptable salts with high optic purity, wherein the crude solifenacin base is transformed to the hydrogen tartrate, which is then optionally transformed to another pharmaceutically acceptable salt or the base of solifenacin. A crystalline salt of solifenacin hydrogen tartrate.
摘要翻译：制备（1S） - （3R）-1-氮杂双环[2.2.2]辛-3-基3,4-二氢-1-苯基-2（1H） - 异喹啉羧酸盐（solifenacin）或其药学上可接受的盐具有高的光学纯度，其中将粗的索非那新碱转化为酒石酸氢盐，然后将其任选转化为另一种药学上可接受的盐或索非那星的碱。酒石酸索非那新的结晶盐。

8. 发明专利

CS245088B1 METHOD OF N-BENZOYLED THIOUREAS PRODUCTION 未知
公开(公告)号：CS245088B1
公开(公告)日：1986-08-14
申请号：CS167085
申请日：1985-03-11
申请人： JIRMAN JOSEF
发明人： JIRMAN JOSEF
IPC分类号： C07C335/04 , C07C157/12

9. 发明专利

CS245852B1 CYLINDRICAL HEATING BODY FOR VACUUM BAKING OVENS 未知
公开(公告)号：CS245852B1
公开(公告)日：1986-10-16
申请号：CS17283
申请日：1983-01-11
申请人： JIRMAN JOSEF , DOHNAL JIRI , POTOCEK JAROSLAV , HAMACEK LUDEK , ZITNANSKY MARCEL
发明人： JIRMAN JOSEF , DOHNAL JIRI , POTOCEK JAROSLAV , HAMACEK LUDEK , ZITNANSKY MARCEL
IPC分类号： H05B3/64

10. 发明专利

SK14452003A3 Method for obtaining pioglitazone as an antidiabetic agent 未知
公开(公告)号：SK14452003A3
公开(公告)日：2004-04-06
申请号：SK14452003
申请日：2002-04-25
申请人： LECIVA A S
发明人： HALAMA ALES , HEJTMANKOVA LUDMILA , LUSTIG PETR , RICHTER JINDRICH , SRSNOVA LUCIE , JIRMAN JOSEF
IPC分类号： A61K31/4427 , A61P3/10 , C07D417/12
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)

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