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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

WO2014023270A1 SALTS OR CO-CRYSTALS OF ETHYL N-[2-AMINO-4-[(4-FLUOROPHENYL)METHYLAMINO]-PHENYL]CARBAMATE 审中-公开
标题翻译：乙基N- [2-氨基-4- [[（4-氟苯基）甲基] - 苯基]碳酸酯的钠盐或共晶体
公开(公告)号：WO2014023270A1
公开(公告)日：2014-02-13
申请号：PCT/CZ2012/000077
申请日：2012-08-09
申请人： ZENTIVA, K.S. , RIDVAN, Ludek , KISS, Violetta , KLECAN, Ondrej , TKADLECOVA, Marcela , DAMMER, Ondrej , KREJCIK, Lukas
发明人： RIDVAN, Ludek , KISS, Violetta , KLECAN, Ondrej , TKADLECOVA, Marcela , DAMMER, Ondrej , KREJCIK, Lukas
IPC分类号： C07C271/28 , A61K31/325
CPC分类号： C07C269/08 , C07B2200/13 , C07C271/28
摘要： A salt or co-crystal of ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]- phenyl]carbamate and one acid selected from the group consisting of hydrobromic acid, hydrochloric acid, methanesulphonic acid, benzenesulphonic acid, fumaric acid and salicylic acid.
摘要翻译： N- [2-氨基-4 - [（4-氟苯基）甲基氨基] - 苯基]氨基甲酸乙酯和一种选自氢溴酸，盐酸，甲磺酸，苯磺酸，富马酸和水杨酸。

3. 发明申请

WO2012146371A1 PHARMACEUTICALLY ACCEPTABLE COCRYSTALS OF N-[2-(7-METHOXY-1-NAPHTYL)ETHYL]ACETAMIDE AND METHODS OF THEIR PREPARATION 审中-公开
标题翻译： N- [2-（7-甲氧基-1-己酰基）乙基]乙酰胺的药物可接受的结晶及其制备方法
公开(公告)号：WO2012146371A1
公开(公告)日：2012-11-01
申请号：PCT/EP2012/001761
申请日：2012-04-25
申请人： ZENTIVA, K.S. , MILLER, Gary James , RIDVAN, Ludek , RICHTER, Jindrich , DAMMER, Ondrej , CHVOJKA, Tomas , PEKAREK, Tomas , HEYSE, Winfried , NAGEL, Norbert
发明人： MILLER, Gary James , RIDVAN, Ludek , RICHTER, Jindrich , DAMMER, Ondrej , CHVOJKA, Tomas , PEKAREK, Tomas , HEYSE, Winfried , NAGEL, Norbert
IPC分类号： A61K31/165 , A61K31/185 , A61K31/194 , C07C57/145 , C07C59/265 , C07C233/18 , C07C309/29 , A61P25/24
CPC分类号： C07C233/25 , C07B2200/13 , C07C57/145 , C07C59/265 , C07C231/22 , C07C233/18 , C07C309/29
摘要： The present invention relates to novel solid forms of agomelatine (I), specifically novel pharmaceutically acceptable cocrystals thereof, as well as to methods of preparing them. Three pharmaceutically acceptable cocrystals of (I) that have physicochemical properties acceptable for pharmaceutical development were obtained.
摘要翻译：本发明涉及新型固体形式的agomelatine（I），特别是其新颖的药学上可接受的共晶，以及其制备方法。获得了具有药学开发可接受的物理化学性质的（I）药学上可接受的三种共晶体。

4. 发明申请

WO2012097764A1 METASTABLE CRYSTAL FORMS OF AGOMELATINE 审中-公开
标题翻译： AGOMELATINE的金属晶体形式
公开(公告)号：WO2012097764A1
公开(公告)日：2012-07-26
申请号：PCT/CZ2012/000007
申请日：2012-01-17
申请人： ZENTIVA, K.S. , RICHTER, Jindrich , RIDVAN, Ludek , REZAC, Jaroslav , DAMMER, Ondrej
发明人： RICHTER, Jindrich , RIDVAN, Ludek , REZAC, Jaroslav , DAMMER, Ondrej
IPC分类号： C07C231/24 , C07C233/18
CPC分类号： C07C231/24 , C07B2200/13 , C07C233/18
摘要： The invention provides a method for the preparation of chemically and polymorphously stable composition of agomelatine, based on a metastable form of agomelatine represented by the chemical formula (1), as well as a reproducible method of preparation of the known metastable form 1 of agomelatine. Other aspects of the invention comprise new metastable crystal forms JR 1, JR2, JR3 and JR4 of agomelatine and their use in a polymorphously stable pharmaceutical composition.
摘要翻译：本发明提供了一种基于由化学式（1）表示的亚稳定形式的阿米苏定的化学和多晶稳定组成的agomelatine的制备方法，以及制备阿格美林的已知亚稳态1的可重现的方法。本发明的其他方面包括阿格美拉汀的新型亚稳态晶形JR 1，JR2，JR3和JR4及其在多晶稳定药物组合物中的用途。

5. 发明申请

WO2011006455A3 METHOD OF PREPARING DESVENLAFAXINE AND ITS SALTS 审中-公开
公开(公告)号：WO2011006455A3
公开(公告)日：2011-01-20
申请号：PCT/CZ2010/000074
申请日：2010-07-08
申请人： ZENTIVA, K.S. , HRUBY, Petr , RIDVAN, Ludek , RADL, Stanislav , PLACEK, Lukas
发明人： HRUBY, Petr , RIDVAN, Ludek , RADL, Stanislav , PLACEK, Lukas
IPC分类号： C07C213/00 , C07C213/10 , C07C215/64
摘要： A method for the preparation of 4-(2-(dimethylamino)-l-(l-hydroxycyclohexyl)ethyl) phenol of formula (I), known under generic name desvenlafaxine, and its pharmaceutically acceptable salts, which comprises (a) mixing of the starting material O -benzyldesvenlafaxine or its derivative of formula (II), wherein R is H, 4-methyl, 4-methoxy, 3,4-dimethoxy, 2-nitro, 4-nitro, 4-chloro, 4- bromo, 2,6-dichloro or 2,6-difluoro, in an organic solvent or a mixture of solvents, and subsequent dissolving of the starting material by decreasing the pH to a value of 3 to 8 by addition of an inorganic or organic acid, or dissolving of O -benzyldesvenlafaxine or its derivative of formula (II) in an organic solvent or a mixture of solvents, wherein the compound of formula (II) is in the form of a salt with an inorganic or organic acid and the pH of the solution has a value of 3 to 8, (b) converting O -benzyldesvenlafaxine or its derivative of formula (II) to desvenlafaxine I by catalytic hydrogenation on a Raney catalyst, (c) removing the catalyst from the desvenlafaxine solution by filtration and subsequent increasing the pH to a value of 8 to 11 by addition of an inorganic or organic base, (d) isolating the desvenlafaxine base I by filtration, (e) converting the desvenlafaxine base I to a pharmaceutically acceptable salt. Formulae (I), (II)

6. 发明申请

WO2011124190A2 METHOD OF PRODUCING 4-(2-(SUBSTITUTED)-1-(1-HYDROXYCYCLOHEXYL)ETHYL)PHENOLS BY O- DEMETHYLATION OF THEIR METHYLETHERS BY MEANS OF INODOROUS AROMATIC THIOLS 审中-公开
标题翻译：通过甲基醚的非离子型芳香族硫醇的O-甲基化制备4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法
公开(公告)号：WO2011124190A2
公开(公告)日：2011-10-13
申请号：PCT/CZ2011/000032
申请日：2011-04-06
申请人： ZENTIVA, K.S. , RADL, Stanislav , RIDVAN, Ludek , KLECAN, Ondrej , HRUBY, Petr
发明人： RADL, Stanislav , RIDVAN, Ludek , KLECAN, Ondrej , HRUBY, Petr
IPC分类号： C07C213/00
CPC分类号： C07C213/00 , C07C2601/14 , C07C215/64
摘要： A method of producing 4-(2-(substituted)-l-(l-hydroxycyclohexyl)ethyl)phenols of general formula (I), wherein the symbols R 1 and R 2 are hydrogen (H) or methyl (CH 3 ), by demethylation of their methylethers of general formula (II), wherein symbols R 1 and R 2 have the same meaning as in formula (I), by heating to 100 to 220 °C with at least one equivalent of an aromatic thiol in the environment of solvents; the reaction is carried out with addition of a base and the aromatic thiol is non- stinking. The term non-stinking means that the stink is only perceptible in concentrations reached in a qualified chemical production in extreme situations only, i.e., for example, above an opened vessel containing the substance; the agent should lack extremely disagreeable "sulphur" character typical of low-molecular compounds containing thiol groups; and even in the above mentioned extreme situations its stink does not exceed intensity of commonly used organic solvents under similar conditions. (Formulae (I), (II)).
摘要翻译：制备通式（I）的4-（2-（取代）-1-（1-羟基环己基）乙基）酚的方法，其中符号R 1，和R 2是氢（H）或甲基（CH 3），通过其通式（II）的甲基醚的去甲基化，其中符号R 1， R 2和R 2具有与式（I）中相同的含义，通过在溶剂环境中用至少1当量的芳族硫醇加热至100至220℃; 该反应在加入碱的情况下进行并且芳族硫醇不发臭。术语“不发臭”是指只有在极端情况下合格的化学品生产达到的浓度才可以察觉臭味，例如，在含有该物质的开放容器上方; 试剂应该缺乏极度不愉快的“硫” 性质典型的含有巯基的低分子化合物; 即使在上述极端情况下，其臭味也不会超过类似条件下常用有机溶剂的强度。（式（I），（II））。

7. 发明申请

WO2010060390A1 A METHOD OF PREPARATION OF DESVENLAFAXINE AND ITS SALTS 审中-公开
标题翻译：一种拟南芥和其盐的制备方法
公开(公告)号：WO2010060390A1
公开(公告)日：2010-06-03
申请号：PCT/CZ2009/000140
申请日：2009-11-26
申请人： ZENTIVA, K.S. , RIDVAN, Ludek , RADL, Stanislav
发明人： RIDVAN, Ludek , RADL, Stanislav
IPC分类号： C07C213/00 , C07C215/64
CPC分类号： C07C213/00 , C07C2601/14 , C07C215/64
摘要： A method of preparation of 4-(2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl)phenol of formula (I), known under the generic name desvenlafaxine, and its pharmaceutically acceptable salts, which comprises (a) stirring up O -benzyl desvenlafaxine or its derivative of formula (II), or its salt, where R is selected from H, 4-methyl, 4-methoxy, 3,4-dimethoxy, 2-nitro, 4-nitro, 4-chloro, 4-bromo, 2,6-dichloro and 2,6-difluoro, in an organic solvent or a mixture of organic solvents, followed by dissolution of the starting substance at pH 3 to 8; (b) transformation of O -benzyl desvenlafaxine or its derivative of formula (II) to desvenlafaxine (I) by catalytic hydrogenation; (c) removing the catalyst from the desvenlafaxine solution with the pH value of 3 to 8 by filtration, followed by increasing pH to a value higher than 8 and lower than 11 by addition of an inorganic or organic base; (d) isolation of desvenlafaxine base (I) by filtration; and (e) transformation of desvenlafaxine base (I) to a pharmaceutically acceptable salt.
摘要翻译：制备通式（I）的通式（I）的4-（2-（二甲基氨基）-1-（1-羟基环己基）乙基）苯酚及其药学上可接受的盐的方法，其包括（a）搅拌其中R选自H，4-甲基，4-甲氧基，3,4-二甲氧基，2-硝基，4-硝基，4-氯， 4-溴，2,6-二氯和2,6-二氟，在有机溶剂或有机溶剂的混合物中，然后将起始物质在pH 3至8下溶解; （b）通过催化氢化将O-苄基去甲文拉法辛或其式（II）的衍生物转化为去甲文拉法辛（I）; （c）通过过滤将pH值为3至8的去甲文拉法辛溶液中的催化剂除去，然后通过加入无机或有机碱将pH升高至高于8且小于11; （d）通过过滤分离去甲文拉法辛碱（I）; 和（e）将去甲文拉法辛碱（I）转化为药学上可接受的盐。

8. 发明申请

WO2011026449A1 A METHOD OF CRYSTALLIZATION OF (S)-N-METHYL-3-(1-NAPHTHYLOXY)-3- (2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE) 审中-公开
标题翻译：（S）-N-甲基-3-（1-萘基）-3-（2-噻吩基）丙基氯化氢（DULOXETINE）的结晶方法
公开(公告)号：WO2011026449A1
公开(公告)日：2011-03-10
申请号：PCT/CZ2010/000099
申请日：2010-09-02
申请人： ZENTIVA, K.S. , RIDVAN, Ludek , CINIBULK, Josef , GRUNWALDOVA, Veronika , BRUSOVA, Hana
发明人： RIDVAN, Ludek , CINIBULK, Josef , GRUNWALDOVA, Veronika , BRUSOVA, Hana
IPC分类号： C07D333/16 , C07D333/20
CPC分类号： C07D333/16 , C07D333/20
摘要： ( S)-N -Methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine hydrochloride of formula (I) is crystallized in such a way that suspension of duloxetine in a mixture of an aprotic solvent and a protic solvent is stirred at an increased temperature under simultaneous reduction of the volume proportion of the protic solvent.
摘要翻译：式（I）的（S）-N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺盐酸盐以如下方式结晶：使度洛西汀在非质子溶剂和质子溶剂在升高的温度下搅拌，同时降低质子溶剂的体积比例。

9. 发明申请

WO2008064615A3 CRYSTALLINE AND AMORPHOUS FORMS OF RIMONABANT AND PROCESSES FOR OBTAINING THEM 审中-公开
公开(公告)号：WO2008064615A3
公开(公告)日：2008-06-05
申请号：PCT/CZ2007/000108
申请日：2007-12-03
申请人： ZENTIVA, A.S. , RADL, Stanislav , RIDVAN, Ludek , CERNY, Josef , HRUBY, Petr , PETRICKOVA, Hana , HAVLICEK, Jaroslav , PEKAREK, Tomas
发明人： RADL, Stanislav , RIDVAN, Ludek , CERNY, Josef , HRUBY, Petr , PETRICKOVA, Hana , HAVLICEK, Jaroslav , PEKAREK, Tomas
IPC分类号： C07D231/14 , A61K31/454 , A61P25/16 , A61P25/28 , A61P25/34 , A61P3/04
摘要： Novel crystalline polymorphic Form III of rimonabant and an amorphous form of rimonabant. Crystalline form III of rimonabant is prepared by dissolving rimonabant in an aprotic polar solvent such as acetonitrile or tetrahydrofuran, pouring the solution into water and stirring the resulting mixture. Amorphous form of rimonabant is prepared by dissolving in and alcohol of formula ROH, wherein R is an alkyl, such as methanol or isopropyl alcohol, and stirring the mixture. Rimonabant of formula (I) is obtained in such a way that an ester of 5-(4-chlorophenyl)-l-(2,4-dichlorophenyl)-4-methyl-l H -pyrazole-3-carboxylic acid of formula (III), wherein R is a Cl-C5 alkyl group, phenyl group or a substituted phenyl group, preferably methyl or ethyl, is reacted, in a solvent, preferably in a solvent from the group of diethyl ether, tetrahydrofuran, dioxan, dichloromethane, acetonitrile, toluene or their mixtures, or in an excess of N -aminopiperidine, with N -aminopiperidine with catalysis by at least one Lewis acid at a temperature from 0° C to the boiling point of the solvent or mixture of solvents used. Pharmaceutical compositions containing the above forms and use of the above forms for the manufacture of a medicament the treatment of obesity, for curing of the habit of smoking or for the treatment of Alzheimer or Parkinson diseases are also described.

10. 发明申请

WO2007009405A1 A METHOD FOR THE PREPARATION OF (R)-N-METHYL-3-(2-METHYLPHENOXY)-3-PHENYLPROPYLAMINE HYDROCHLORIDE (ATOMOXETINE) 审中-公开
标题翻译：制备（R）-N-甲基-3-（2-甲基苯氧基）-3-苯基丙烯酰胺氯化氢（ATOMOXETINE）的方法
公开(公告)号：WO2007009405A1
公开(公告)日：2007-01-25
申请号：PCT/CZ2005/000091
申请日：2005-12-01
申请人： ZENTIVA, A.S. , RIDVAN, Ludek , HRUBY, Petr , RADL, Stanislav , ZATOPKOVA, Monika , PLACEK, Lukas
发明人： RIDVAN, Ludek , HRUBY, Petr , RADL, Stanislav , ZATOPKOVA, Monika , PLACEK, Lukas
IPC分类号： C07C213/06 , C07C215/30
CPC分类号： C07C213/06 , C07C217/44
摘要： Racemic N -benzyl- N -methyl-3-(2-methylphenoxy)-3-phenylproρylamine (VIII) is an intermediate for obtaining atomoxetine. Racemic N -benzyl- N -methyl-3-(2-methylphenoxy)-3- phenylpropylamine (VIII) further reacts in a solution of an organic solvent with an optically active acid producing a mixture of diastereoisomers, which are subsequently resolved by crystallization and converted to the respective (R) and (S) enantiomers of N-benzyl-N-methyl- 3-(2-methylphenoxy)-3-phenylpropylamine by treatment with an organic or inorganic base. The (R)-enantiomer of N-methyl-3-(2-methylphenoxy)-3-phenylpropylamine ((R)-VIII) is further subjected to debenzylation by means of an alkyl or aryl chloro formate yielding an alkyl/aryl (R)-3-(2-methylphenoxy)-3-phenylpropylmethylcarbamate ((R)-IX), which is then hydrolyzed in the basic environment yielding the base of (R)-N-methyl-3-(2-methylphenoxy)- 3-phenylpropaneamine, which is finally converted to (R)-N-methyl-3-(2-methylphenoxy)-3- phenylpropanamine hydrochloride ((R)-I) by treatment with hydrochloric acid.
摘要翻译：外消旋N-苄基-N-甲基-3-（2-甲基苯氧基）-3-苯基丙基胺（VIII）是获得阿托西汀的中间体。外消旋N-苄基-N-甲基-3-（2-甲基苯氧基）-3-苯基丙胺（VIII）进一步在有机溶剂与光学活性酸的溶液中反应，产生非对映异构体的混合物，其随后通过结晶和通过用有机或无机碱处理转化成N-苄基-N-甲基-3-（2-甲基苯氧基）-3-苯基丙胺的各自的（R）和（S）对映异构体。 N-甲基-3-（2-甲基苯氧基）-3-苯基丙基胺（（R）-VIII）的（R） - 对映异构体进一步通过烷基或芳基氯甲酸酯进行脱苄基，得到烷基/芳基（R ）-3-（2-甲基苯氧基）-3-苯基丙基甲基氨基甲酸酯（（R）-IX），然后在碱性环境中水解，得到（R）-N-甲基-3-（2-甲基苯氧基） - 苯基丙胺，最后通过用盐酸处理转化为（R）-N-甲基-3-（2-甲基苯氧基）-3-苯基丙胺盐酸盐（（R）-I）。

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