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1. 发明申请

WO2014000719A1 NOVEL PHARMACEUTICAL SOLID FORMS OF (1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4DIFLUOROPHENYL)CYCLOPROPYLAMINO]-5-(PROPYLTHIO)-3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDIN-3YL]-5-(2-HYDROXYETHOXY)CYCLOPENTANE-L,2-DIOL 审中-公开
标题翻译：（1S，2S，3R，5S）-3- [7 - [（1R，2S）-2-（3,4-二氟苯基）环丙基氨基] -5-（丙基）-3H- [ 3]三唑并[4,5-d]嘧啶-3-基] -5-（2-羟基乙氧基）环戊烷-1,2-二醇
公开(公告)号：WO2014000719A1
公开(公告)日：2014-01-03
申请号：PCT/CZ2012/000059
申请日：2012-06-29
申请人： ZENTIVA, K.S. , MOHAMED, Sharmarke , HEJTMANKOVA, Ludmila , RIDVAN, Ludek , TKADLECOVA, Marcela , DAMMER, Ondrej
发明人： MOHAMED, Sharmarke , HEJTMANKOVA, Ludmila , RIDVAN, Ludek , TKADLECOVA, Marcela , DAMMER, Ondrej
IPC分类号： C07D487/04 , A61K31/519 , A61P7/02
CPC分类号： C07D487/04
摘要： Solid state structures of (1S,2S,3R,5S)-3-[7-[1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino]-5- (propylthio)-3H-[1,23]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol (hereafter referred to as Ticagrelor) in the form of a stable 3-hydroxy-2-naphthoic acid co-crystal solid form as well as a 1,4-dioxane solvate, and processes for the preparation thereof.
摘要翻译：（1S，2S，3R，5S）-3- [7- [1R，2S）-2-（3,4-二氟苯基）环丙基氨基] -5-（丙硫基）-3H- [1,23] 三唑并[4,5-d]嘧啶-3-基] -5-（2-羟基乙氧基）环戊烷-1,2-二醇（以下称为替卡格雷）为稳定的3-羟基-2-萘甲酸共晶固体形式以及1,4-二烷溶剂化物，及其制备方法。

2. 发明申请

WO2008145075A2 METHOD FOR THE PREPARATION OF LASOFOXIFENE 审中-公开
标题翻译：制备乳酸菌的方法
公开(公告)号：WO2008145075A2
公开(公告)日：2008-12-04
申请号：PCT/CZ2008/000058
申请日：2008-05-28
申请人： ZENTIVA, A.S. , LUSTIG, Petr , HEJTMANKOVA, Ludmila
发明人： LUSTIG, Petr , HEJTMANKOVA, Ludmila
CPC分类号： C07D295/088
摘要： A method of preparing (-)-cis-(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]- 5,6,7,8-tetrahydronaphthalen-2-ol D-tartrate - lasofoxifene of formula 1, comprising the following steps a) Preparation of cis-1- {2-[4-(2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalen-1-yl)-phenoxy]ethyl}pyrrolidine of formula (3) by alkylation of cis-1-(4-hydroxyphenyl)-2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalene with 1-(2-chloroethyl)pyrrolidine base or its salt, b) Deprotection of the hydroxyl group in the substance of formula (3) by the effect of hydrobromic acid generating cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol hydrobromide of formula (2a), c) Conversion of the substance of formula (2a) into cis-6-phenyl-5-[4-(2-pyrrolidin-1- ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol of formula (2b), d) Preparation of lasofoxifene of formula (1) by conversion into the corresponding diasteroisomer by reaction with D-tartaric acid and crystallization.
摘要翻译：制备（ - ） - 顺式 - （5R，6S）-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇的方法 D-酒石酸盐 - 式1的拉索昔芬，包括以下步骤a）顺式-1- {2- [4-（2-苯基-6-甲氧基-1,2,3,4-四氢萘-1-基）（4-羟基苯基）-2-苯基-6-甲氧基-1,2,3,4-四氢化萘与1-（2-氯乙基）吡咯烷的烷基化反应制得式（3）的3-（苯氧基）乙基} 碱或其盐，b）通过产生氢溴酸的顺式-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] - 吡咯烷酮的作用，使式（3）物质中的羟基脱保护，式（2a）的5,6,7,8-四氢萘-2-醇氢溴酸盐，c）将式（2a）物质转化成顺式-6-苯基-5- [4-（2-吡咯烷-1-基）乙酰氧基）苯基] -5,6,7,8-四氢萘-2-醇，d）通过与D-酒石酸反应转化成相应的非对映异构体并结晶，制备式（1）的拉莫昔芬。

3. 发明申请

WO2008017278A2 CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：结晶酒石酸酒石酸盐和含有相同物质的药物组合物
公开(公告)号：WO2008017278A2
公开(公告)日：2008-02-14
申请号：PCT/CZ2007/000078
申请日：2007-08-09
申请人： ZENTIVA, A.S. , SVOBODA, Martin , JAMPILEK, Josef , KACIRKOVA, Martina , TOMASEK, Vaclav , LEHOCKY, Mikulas , HEJTMANKOVA, Ludmila , VOSATKA, Vaclav
发明人： SVOBODA, Martin , JAMPILEK, Josef , KACIRKOVA, Martina , TOMASEK, Vaclav , LEHOCKY, Mikulas , HEJTMANKOVA, Ludmila , VOSATKA, Vaclav
IPC分类号： C07C213/10 , C07C215/54 , A61K31/137
CPC分类号： C07C215/54 , C07C213/10
摘要： A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-ρhenylρropyl]-4-methyl-phenol with (2R,3R)-2,3-dihydroxybutanedioic acid, known under the name R-tolterodine tartarate, wherein: a) at least 90 % of all crystals are present in a size smaller than 30 μm, b) at least 40 % of crystalline matter are smaller than 250 μm, c) the maximum size of crystals does not exceed 800 μm, d) the salt contains less than 0.1 weight % of the undesirable enantiomer S-tolterodine tartarate, e) analytical test for sulfate ashes (Pharm. Eur.) provides a value lower than 0.1%. The method of its preparation involves at least one crystallization from water. A pharmaceutical composition containing tolterodine or its pharmaceutically acceptable salts further contains a filler, a disintegrant and a lubricant, said composition being free of ions of alkaline earth metals.
摘要翻译：（2R，3R）-2,2-二甲基苯胺的2 - [（1R）-3- [双（1-甲基乙基）氨基] -1-苯基丙基] -4-甲基 - 苯酚的晶体盐，其中：a）全部晶体的至少90％以小于30μm的尺寸存在，b）至少40％的晶体物质小于250μm， c）晶体的最大尺寸不超过800μm，d）盐含有小于0.1重量％的不希望的对映体S-托特罗定酒石酸盐，e）硫酸盐灰分（欧洲药典）的分析测试提供的值低于 0.1％。其制备方法涉及至少一次从水中结晶。包含托特罗定或其药学上可接受的盐的药物组合物还含有填充剂，崩解剂和润滑剂，所述组合物不含碱土金属离子。

4. 发明申请

WO2012142983A1 OPTICALLY ACTIVE SALTS OF (3AR,4S,6R,6AS)-6-AMINO-2,2-DIMETHYLTETRAHYDRO-3AH- CYCLOPENTA-[D] [1,3]DIOXOL-4-OL AND A METHOD OF THEIR PREPARATION 审中-公开
标题翻译：（3AR，4S，6R，6AS）-6-氨基-2,2-二甲基四氢呋喃-3H-环丙基 - [D] [1,3]二氧杂环戊烯-4-醇的光活性盐及其制备方法
公开(公告)号：WO2012142983A1
公开(公告)日：2012-10-26
申请号：PCT/CZ2012/000036
申请日：2012-04-19
申请人： ZENTIVA, K.S. , LUSTIG, Petr , HEJTMANKOVA, Ludmila
发明人： LUSTIG, Petr , HEJTMANKOVA, Ludmila
IPC分类号： C07B57/00 , C07C59/50 , C07C59/56 , C07D317/44
CPC分类号： C07D317/44 , C07B57/00 , C07B2200/07 , C07C51/412 , C07C59/50 , C07C59/56
摘要： Diastereomeric salts of the compound of formula I with D-(-)-mandelic and R-(-)-3- chloromandelic acid, a method of for the preparation thereof and their use in the synthesis of the drug ticagrelor.
摘要翻译：式I化合物与D-（ - ） - 扁桃酸和R - （ - ） - 3-氯扁桃酸的非对映异构体盐，其制备方法及其在合成药物替卡格雷中的用途。

5. 发明申请

WO2008017278B1 CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：金属托乐定和其含有的药物组合物
公开(公告)号：WO2008017278B1
公开(公告)日：2008-08-28
申请号：PCT/CZ2007000078
申请日：2007-08-09
申请人： ZENTIVA AS , SVOBODA MARTIN , JAMPILEK JOSEF , KACIRKOVA MARTINA , TOMASEK VACLAV , LEHOCKY MIKULAS , HEJTMANKOVA LUDMILA , VOSATKA VACLAV
发明人： SVOBODA MARTIN , JAMPILEK JOSEF , KACIRKOVA MARTINA , TOMASEK VACLAV , LEHOCKY MIKULAS , HEJTMANKOVA LUDMILA , VOSATKA VACLAV
IPC分类号： C07C213/10 , A61K31/137 , C07C215/54
CPC分类号： C07C215/54 , C07C213/10
摘要： A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-?henyl?ropyl]-4-methyl-phenol with (2R,3R)-2,3-dihydroxybutanedioic acid, known under the name R-tolterodine tartarate, wherein: a) at least 90 % of all crystals are present in a size smaller than 30 µm, b) at least 40 % of crystalline matter are smaller than 250 µm, c) the maximum size of crystals does not exceed 800 µm, d) the salt contains less than 0.1 weight % of the undesirable enantiomer S-tolterodine tartarate, e) analytical test for sulfate ashes (Pharm. Eur.) provides a value lower than 0.1%. The method of its preparation involves at least one crystallization from water. A pharmaceutical composition containing tolterodine or its pharmaceutically acceptable salts further contains a filler, a disintegrant and a lubricant, said composition being free of ions of alkaline earth metals.
摘要翻译： 2 - [（1R）-3- [双（1-甲基乙基）氨基] -1-苯基乙酰基] -4-甲基 - 苯酚与（2R，3R）-2,3-二羟基丁二酸的结晶盐，以名称R-tolterodine酒石酸盐，其中：a）至少90％的晶体以小于30μm的尺寸存在，b）至少40％的结晶物质小于250μm，c）最大尺寸的晶体不超过800μm，d）盐含有小于0.1重量％的不需要的对映体S-托特罗定酒石酸酯，e）硫酸盐灰分析（Pharm.Eur。）的分析测试提供的值低于0.1％。其制备方法涉及至少一种从水中的结晶。含有托特罗定或其药学上可接受的盐的药物组合物还含有填料，崩解剂和润滑剂，所述组合物不含碱土金属的离子。

6. 发明申请

WO2009094957A1 A METHOD FOR THE PREPARATION OF DARIFENACIN HYDROGEN BROMIDE 审中-公开
标题翻译：一种制备DARIFENACIN氢溴化物的方法
公开(公告)号：WO2009094957A1
公开(公告)日：2009-08-06
申请号：PCT/CZ2009/000003
申请日：2009-01-14
申请人： ZENTIVA, K.S. , HEJTMANKOVA Ludmila , JIRMAN, Josef
发明人： HEJTMANKOVA Ludmila , JIRMAN, Josef
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： A method of preparing (3S)-l-[2-(2,3-dihydro-5-benzofuranyl)ethyl}-α,α-diphenyl-3- pyrrolidine acetamide hydrogen bromide, wherein 3-(S)-(I -carbamoyl- 1,1- diphenylmethyl)pyrrolidine or its salt with an organic acid is alkylated in the presence of an inorganic base with 5-(2-bromoethyl)-2,3-dihydrobenzofurane in a heterogeneous system of the solvents water and an organic solvent selected from C6 to C9 aliphatic, alicyclic or aromatic hydrocarbons, after separation of the two phases the crude darifenacin base is isolated, which is converted to the hydrobromide by addition of a C3 to C9 ketone or C3 to C9 alcohol and concentrated hydrobromic acid.
摘要翻译：制备（3S）-1- [2-（2,3-二氢-5-苯并呋喃基）乙基}-α，α-二苯基-3-吡咯烷乙酰胺溴化氢的方法，其中3-（S） - （I- 氨基甲酰基-1,1-二苯基甲基）吡咯烷或其与有机酸的盐在无机碱与5-（2-溴乙基）-2,3-二氢苯并呋喃的存在下在溶剂水和有机物的异质体系中烷基化溶剂选自C6至C9脂族，脂环族或芳族烃，分离两相后，分离粗制的达赖芬酸碱，通过加入C3至C9酮或C3至C9醇和浓氢溴酸将其转化为氢溴酸盐。

7. 发明申请

WO2008145075A3 METHOD FOR THE PREPARATION OF LASOFOXIFENE AND CRYSTALLINE INTERMEDIATES USED THEREIN 审中-公开
标题翻译：用于制备乳酸的方法及其使用的晶体中间体
公开(公告)号：WO2008145075A3
公开(公告)日：2009-03-19
申请号：PCT/CZ2008000058
申请日：2008-05-28
申请人： ZENTIVA AS , LUSTIG PETR , HEJTMANKOVA LUDMILA
发明人： LUSTIG PETR , HEJTMANKOVA LUDMILA
IPC分类号： C07D295/088
CPC分类号： C07D295/088
摘要： A method of preparing (-)-cis-(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]- 5,6,7,8-tetrahydronaphthalen-2-ol D-tartrate - lasofoxifene of formula 1, comprising the following steps a) Preparation of cis-1- {2-[4-(2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalen-1-yl)-phenoxy]ethyl}pyrrolidine of formula (3) by alkylation of cis-1-(4-hydroxyphenyl)-2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalene with 1-(2-chloroethyl)pyrrolidine base or its salt, b) Deprotection of the hydroxyl group in the substance of formula (3) by the effect of hydrobromic acid generating cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol hydrobromide of formula (2a), c) Conversion of the substance of formula (2a) into cis-6-phenyl-5-[4-(2-pyrrolidin-1- ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol of formula (2b), d) Preparation of lasofoxifene of formula (1) by conversion into the corresponding diasteroisomer by reaction with D-tartaric acid and crystallization.
摘要翻译：制备（ - ） - 顺式 - （5R，6S）-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] -5,6,7,8-四氢萘-2-醇的方法 D-酒石酸盐 - 式1的拉索昔芬，包括以下步骤a）顺式-1- {2- [4-（2-苯基-6-甲氧基-1,2,3,4-四氢萘-1-基）（4-羟基苯基）-2-苯基-6-甲氧基-1,2,3,4-四氢化萘与1-（2-氯乙基）吡咯烷的烷基化反应制得式（3）的3-（苯氧基）乙基} 碱或其盐，b）通过产生氢溴酸的顺式-6-苯基-5- [4-（2-吡咯烷-1-基乙氧基）苯基] - 吡咯烷酮的作用，使式（3）物质中的羟基脱保护，式（2a）的5,6,7,8-四氢萘-2-醇氢溴酸盐，c）将式（2a）物质转化成顺式-6-苯基-5- [4-（2-吡咯烷-1-基）乙酰氧基）苯基] -5,6,7,8-四氢萘-2-醇，d）通过与D-酒石酸反应转化成相应的非对映异构体并结晶，制备式（1）的拉莫昔芬。

8. 发明申请

WO2008017278A3 CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：结晶酒石酸酒石酸盐和含有相同物质的药物组合物
公开(公告)号：WO2008017278A3
公开(公告)日：2008-07-10
申请号：PCT/CZ2007000078
申请日：2007-08-09
申请人： ZENTIVA AS , SVOBODA MARTIN , JAMPILEK JOSEF , KACIRKOVA MARTINA , TOMASEK VACLAV , LEHOCKY MIKULAS , HEJTMANKOVA LUDMILA , VOSATKA VACLAV
发明人： SVOBODA MARTIN , JAMPILEK JOSEF , KACIRKOVA MARTINA , TOMASEK VACLAV , LEHOCKY MIKULAS , HEJTMANKOVA LUDMILA , VOSATKA VACLAV
IPC分类号： C07C213/10 , A61K31/137 , C07C215/54
CPC分类号： C07C215/54 , C07C213/10
摘要： A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-?henyl?ropyl]-4-methyl-phenol with (2R,3R)-2,3-dihydroxybutanedioic acid, known under the name R-tolterodine tartarate, wherein: a) at least 90 % of all crystals are present in a size smaller than 30 µm, b) at least 40 % of crystalline matter are smaller than 250 µm, c) the maximum size of crystals does not exceed 800 µm, d) the salt contains less than 0.1 weight % of the undesirable enantiomer S-tolterodine tartarate, e) analytical test for sulfate ashes (Pharm. Eur.) provides a value lower than 0.1%. The method of its preparation involves at least one crystallization from water. A pharmaceutical composition containing tolterodine or its pharmaceutically acceptable salts further contains a filler, a disintegrant and a lubricant, said composition being free of ions of alkaline earth metals.
摘要翻译： 2 - [（1R）-3- [双（1-甲基乙基）氨基] -1-苯基丙基] -4-甲基 - 苯酚与（2R，3R）-2,3-二羟基丁二酸的结晶盐，以名称R-托特罗定酒石酸盐公知，其中：a）全部晶体的至少90％以小于30μm的尺寸存在，b）至少40％的晶体物质小于250μm，c）最大尺寸的晶体不超过800μm，d）盐含有小于0.1重量％的不良对映体S-托特罗定酒石酸盐，e）硫酸盐灰分（欧洲药典）的分析测试提供的值低于0.1％。其制备方法涉及至少一次从水中结晶。含有托特罗定或其药学上可接受的盐的药物组合物还含有填充剂，崩解剂和润滑剂，所述组合物不含碱土金属离子。

9. 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。

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