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1. 发明申请

WO2011124190A3 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：通过异构芳香硫醇通过其甲基酯的O-甲基化生产4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法
公开(公告)号：WO2011124190A3
公开(公告)日：2011-12-01
申请号：PCT/CZ2011000032
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 , C07C215/64
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 R1 and R2 are hydrogen (H) or methyl (CH3), by demethylation of their methylethers of general formula (II), wherein symbols R1 and R2 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：一种制备通式（I）的4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法，其中符号R1和R2是氢（H）或甲基（CH3），通过脱甲基其通式（II）的甲醚，其中符号R1和R2具有与式（I）中相同的含义，通过在溶剂环境中用至少一当量的芳族硫醇加热至100至220℃; 反应是通过加入碱进行的，而芳族硫醇是非臭的。非臭味这一术语意味着臭气只能在极端情况下，即在例如含有物质的开放容器之上的合格化学品生产中达到的浓度是可察觉的; 该试剂应缺乏含有硫醇基团的低分子化合物典型的极不理想的“硫”特征; 即使在上述极端情况下，在类似条件下，其臭气也不会超过常用有机溶剂的强度。（式（I），（II））。

2. 发明申请

WO2010088865A3 NEW SALTS OF DESVENLAFAXINE AND A METHOD OF THEIR PREPARATION 审中-公开
标题翻译： DESVENLAFAXINE的新盐及其制备方法
公开(公告)号：WO2010088865A3
公开(公告)日：2010-12-02
申请号：PCT/CZ2010000010
申请日：2010-02-03
申请人： ZENTIVA K S , RIDVAN LUDEK , HRUBY PETR , RADL STANISLAV , BRUSOVA HANA , KREJCIK LUKAS , PEKAREK TOMAS , CSOKOVA NATALIA , ZERZANOVA ANNA
发明人： RIDVAN LUDEK , HRUBY PETR , RADL STANISLAV , BRUSOVA HANA , KREJCIK LUKAS , PEKAREK TOMAS , CSOKOVA NATALIA , ZERZANOVA ANNA
IPC分类号： C07C51/41 , C07C55/07 , C07C213/08 , C07C215/64
CPC分类号： A61K31/205 , C07B2200/13 , C07C51/412 , C07C55/07 , C07C213/08 , C07C213/10 , C07C215/52 , C07C215/64 , C07C2601/14
摘要： The invention deals with new salts of the desvenlafaxine base of formula (I) with oxalic acid, the new salts being the hydrogen oxalate of formula (II) in the proportion of desvenlafaxine : oxalic acid of 1 : 1 and hemioxalate of formula (III) in the proportion of desvenlafaxine : oxalic acid of 2 : 1.
摘要翻译：本发明涉及式（I）的去甲文拉法辛碱与草酸的新盐，新盐为式（II）的草酸氢草酸，其比例为去甲文拉法辛：草酸1:1和式（III）草酸半草酸酯比例为2:1的去甲文拉法辛：草酸。

3. 发明申请

WO2011006455A2 METHOD OF PREPARING DESVENLAFAXINE AND ITS SALTS 审中-公开
标题翻译：制备DESVENLAFAXINE及其盐的方法
公开(公告)号：WO2011006455A2
公开(公告)日：2011-01-20
申请号：PCT/CZ2010000074
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
CPC分类号： C07C213/10 , C07C213/00 , C07C2601/14 , 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)
摘要翻译：制备式（I）的4-（2-（二甲基氨基）-1-（1-羟基环己基）乙基）苯酚的方法，其通称为去甲文拉法辛，及其药学上可接受的盐，其包含（a）其中R是H，4-甲基，4-甲氧基，3,4-二甲氧基，2-硝基，4-硝基，4-氯代，4-溴代，4-甲氧基，4-氯代苯基， 2,6-二氯或2,6-二氟在有机溶剂或溶剂混合物中反应，随后通过加入无机酸或有机酸将pH值降至3〜8来溶解原料，或者将O-苄基去甲文拉法辛或其式（II）的衍生物溶解在有机溶剂或溶剂混合物中，其中式（II）化合物为与无机或有机酸形成的盐的形式，并且溶液的pH （b）通过在Ra上催化氢化将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）通过过滤从去甲文拉法辛溶液中除去催化剂，随后通过加入无机或有机碱将pH值升高至8至11，（d）通过过滤分离去甲文拉法辛碱I，（e）将去甲文拉法辛碱I转化为药学上可接受的盐。式（I），（II）

4. 发明申请

WO2008064615A2 CRYSTALLINE AND AMORPHOUS FORMS OF RIMONABANT AND PROCESSES FOR OBTAINING THEM 审中-公开
标题翻译：可溶性和非晶形式的晶体和方法获得它们
公开(公告)号：WO2008064615A2
公开(公告)日：2008-06-05
申请号：PCT/CZ2007000108
申请日：2007-12-03
申请人： ZENTIVA AS , 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 , A61P3/04 , A61P25/16 , A61P25/28 , A61P25/34
CPC分类号： C07D231/14
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-lH-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.
摘要翻译：利莫那班的新型结晶多晶型III和利莫那班的无定形形式。通过将利莫那班溶解在非质子极性溶剂如乙腈或四氢呋喃中制备结晶形式III，将溶液倒入水中并搅拌所得混合物。通过溶解式ROH的醇和其中R是烷基，如甲醇或异丙醇，并搅拌混合物制备利莫那班的无定形形式。得到式（I）的咪唑啉酮，使得式（III）的5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-1H-吡唑-3-羧酸的酯），其中R是C1-C5烷基，苯基或取代的苯基，优选甲基或乙基，在溶剂中，优选在溶剂中，从二乙醚，四氢呋喃，二恶烷，二氯甲烷，乙腈，甲苯或它们的混合物，或过量的N-氨基哌啶，与N-氨基哌啶一起，在0℃至所用溶剂或溶剂混合物的沸点下通过至少一种路易斯酸催化。还描述了含有上述形式的药物组合物和上述形式用于制备治疗肥胖症，治疗吸烟习惯或治疗阿尔茨海默病或帕金森病的药物的用途。

5. 发明专利

IL237884D0 A method of preparing a highly pure potassium salt of azilsartan medoxomil 未知
公开(公告)号：IL237884D0
公开(公告)日：2015-05-31
申请号：IL23788415
申请日：2015-03-22
申请人： ZENTIVA KS , ONDREJ DAMMER , STACH JAN , KRULIS RADIM , CERNY JOSEF , RIDVAN LUDEK , KREJCIK LUKAS , RADL STANISLAV
发明人： ONDREJ DAMMER , STACH JAN , KRULIS RADIM , CERNY JOSEF , RIDVAN LUDEK , KREJCIK LUKAS , RADL STANISLAV
IPC分类号： C07D20060101
摘要： A method of preparing the potassium salt of azilsartan medoxomil of formula I, in which a solvate of azilsartan medoxomil of formula II with a solvent selected from the group that consists of dimethyl acetamide or N-methyl pyrrolidone or their mixtures with other solvents is prepared, or re-crystallized from dimethyl acetamide or N-methyl pyrrolidine or their mixtures with other solvents, and, in the next step, converted to the potassium salt using a potassium source in a suitable solvent.

6. 发明申请

WO2007076733A3 A METHOD FOR THE PREPARATION OF (S)-N-MET?YL-3-(l-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE HYDROCHLORIDE (DULOXETINE) 审中-公开
标题翻译：制备（S）-N-METγY-3-（1-萘基）-3-（2-噻吩基）丙酰胺氢氯化物（DULOXETINE）的方法
公开(公告)号：WO2007076733A3
公开(公告)日：2007-08-23
申请号：PCT/CZ2006000096
申请日：2006-12-22
申请人： ZENTIVA AS , RIDVAN LUDEK , JARRAH KAMAL , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
发明人： RIDVAN LUDEK , JARRAH KAMAL , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-mienyl)propylamine of Formula(l) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)-N, N-dimethyl-3-(l-na?hthyloxy)-3-(2-th1enyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(l-naphthyloxy)- 3-(2-thienyl)propylamine and D- tartaric acid (2:1), b) isolation of the salt (S)-N, N-dimethyl-3-(naphthyloxy)-3-(2- thienyl)propylamine/D- tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)-N, N-dimethyl-3-(l- naphthyloxy)-3-(2-thienyl) propylamine by action of an inorganic or organic base, c) demethylation of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2- thienyl) propylamine by action of an alkylchloroformate of formula C1COOR (R=C 1 -C 5 alkyl, or C 6 -C 12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetine base of formula I and optionally conversion of the base to a salt with the respective acid, or salt of a weak base.
摘要翻译：制备式（1）的（S）-N-甲基-3-（1-萘氧基）-3-（2-甲基）丙胺及其药学上可接受的盐的方法，其包括a）（RS）-N ，N-二甲基-3-（1-萘基氧基）-3-（2-烯基）丙胺与旋光性D-酒石酸或衍生自D-酒石酸的酸盐形成N，N的非对映异构体盐的混合物 - 二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺和D-酒石酸（2:1），b）分离盐（S）-N，N-二甲基-3-（萘氧基）-3-（2-噻吩基）丙胺/ D-酒石酸盐（2:1），由有机溶剂，水或其混合物中的非对映异构体盐的混合物和（S）-N，N-二甲基-3- （1-萘氧基）-3-（2-噻吩基）丙胺通过无机或有机碱的作用，c）（S）-N，N-二甲基-3-（1-萘氧基）-3-（2- 噻吩基）丙胺，通过式C1COOR（R = C 1 -C 5烷基）或C 6 -C 6烷基的氯甲酸烷基酯的作用， 12芳基或烷基芳基），特别是ph 烯丙基，乙基或甲基氯甲酸酯，以及d）式I的度洛西汀碱的水解释放和任选地将碱与弱酸的盐或弱碱转化成盐。

7. 发明申请

WO2008067781B1 A METHOD OF PURIFICATION OF (S)-N-METHYL-3-(1-NAPHTYLOXY)-3-(2-THIENYL) PROPYLAMINE HYDROCHLORIDE (DULOXETINE) 审中-公开
标题翻译：（S）-N-甲基-3-（1-萘基氧基）-3-（2-噻吩基）丙胺盐酸盐（杜冷丁）的纯化方法
公开(公告)号：WO2008067781B1
公开(公告)日：2008-10-02
申请号：PCT/CZ2007000109
申请日：2007-12-05
申请人： ZENTIVA AS , RIDVAN LUDEK , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
发明人： RIDVAN LUDEK , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
IPC分类号： C07D333/20 , A61K31/381 , A61P25/24
CPC分类号： C07D333/20
摘要： A method of purification of (5)-7V-methyl-3-(l-naphtyloxy)-3-(2-thienyl) propylamine hydrochloride of formula I, comprising (a) transformation of the substance of formula I to its free base by the action of an organic or inorganic base in an aqueous environment; and (b) transformation of the base of the substance of formula I to crystalline hydrochloride by the action of hydrochloric acid or gaseous HCl in an organic solvent or a mixture of organic solvents. A method of purification of (S)-N-methyl-3-(l-naphtyloxy)-3-(2-thienyl) propylamine hydrochloride of formula I, comprising dissolution of this substance in a minimum quantity of methanol containing 0 to 50% of water and its transformation back to the solid phase (precipitation) by addition of a less polar solvent.
摘要翻译：一种纯化式（I）的（5）-N-甲基-3-（1-萘基氧基）-3-（2-噻吩基）丙胺盐酸盐的方法，包括：（a）通过将式I的物质转化为其游离碱，有机或无机碱在含水环境中的作用; 和（b）通过盐酸或气态HCl在有机溶剂或有机溶剂混合物中的作用将式I物质的碱转化为结晶盐酸盐。一种纯化式I的（S）-N-甲基-3-（1-萘基氧基）-3-（2-噻吩基）丙胺盐酸盐的方法，包括将该物质溶解于最少量的含有0至50％通过加入极性较低的溶剂将其转化回固相（沉淀）。

8. 发明申请

WO2008104134A2 A METHOD FOR THE PREPARATION OF ZOLMITRIPTAN 审中-公开
标题翻译：一种制备ZOLMITRIPTAN的方法
公开(公告)号：WO2008104134A2
公开(公告)日：2008-09-04
申请号：PCT/CZ2008000021
申请日：2008-02-25
申请人： ZENTIVA AS , VOSLAR MICHAL , ZATOPKOVA MONIKA , RIDVAN LUDEK , PEKAREK TOMAS
发明人： VOSLAR MICHAL , ZATOPKOVA MONIKA , RIDVAN LUDEK , PEKAREK TOMAS
IPC分类号： C07D413/06
CPC分类号： C07D413/06
摘要： In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4- hydrazinobenzyl)-l,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14 % by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111°C in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm - 1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm - 1, characteristic for toluene.
摘要翻译：在式III的唑来曲坦的制备中，将重氮盐还原成式IV的（5）-4-（4-肼基苄基）-1,3-恶唑烷-2-酮的方法是以更浓缩的混合物和效果在碱金属亚硫酸盐上，优选二亚硫酸钠。唑来曲坦甲苯溶剂化物，其特征在于根据气相色谱测定的甲苯含量为9至14重量％，并且在重量分析记录中在约111℃的温度下具有最大的相应质量损失。唑来曲坦甲苯溶剂化物，在1443和1354cm -1的波数下显示出强拉曼带，其具有内置甲苯的佐米曲坦的晶格特征，以及在1004和786cm处的进一步标记的带甲苯的特征。

9. 发明申请

WO2008067781A3 A METHOD OF PURIFICATION OF (S)-N-METHYL-3-(1-NAPHTYLOXY)-3-(2-THIENYL) PROPYLAMINE HYDROCHLORIDE (DULOXETINE) 审中-公开
公开(公告)号：WO2008067781A3
公开(公告)日：2008-07-24
申请号：PCT/CZ2007000109
申请日：2007-12-05
申请人： ZENTIVA AS , RIDVAN LUDEK , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
发明人： RIDVAN LUDEK , CINIBULK JOSEF , ZATOPKOVA MONIKA , PLACEK LUKAS
IPC分类号： C07D333/20 , A61K31/381 , A61P25/24
CPC分类号： C07D333/20
摘要： A method of purification of (5)-7V-methyl-3-(l-naphtyloxy)-3-(2-thienyl) propylamine hydrochloride of formula I, comprising (a) transformation of the substance of formula I to its free base by the action of an organic or inorganic base in an aqueous environment; and (b) transformation of the base of the substance of formula I to crystalline hydrochloride by the action of hydrochloric acid or gaseous HCl in an organic solvent or a mixture of organic solvents. A method of purification of (S)-N-methyl-3-(l-naphtyloxy)-3-(2-thienyl) propylamine hydrochloride of formula I, comprising dissolution of this substance in a minimum quantity of methanol containing 0 to 50% of water and its transformation back to the solid phase (precipitation) by addition of a less polar solvent.

10. 发明专利

IL244848D0 Dihydrogenphosphate salt of tenofovir disoproxil 未知
公开(公告)号：IL244848D0
公开(公告)日：2016-05-31
申请号：IL24484816
申请日：2016-03-31
申请人： ZENTIVA KS , DAMMER ONDREJ , RIDVAN LUDEK , KRAL VLADIMIR , HOLAN JAN , ZAPADLO MICHAL , BERANEK JOSEF
发明人： DAMMER ONDREJ , RIDVAN LUDEK , KRAL VLADIMIR , HOLAN JAN , ZAPADLO MICHAL , BERANEK JOSEF
IPC分类号： C07F20060101
摘要： Tenofovir disoproxil dihydrogenphosphate, showing the following characteristic reflections in the XRPD measured by CuK± emission 5,6; 7,7; 12,4; 13,6; 16,4; 22,4 a 25,4 ± 0,2 ° 2¸, and methods for the preparation thereof.

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