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1. 发明申请

WO2011088806A2 A METHOD OF INDUSTRIAL PRODUCTION OF AN AMORPHOUS FORM OF ATORVASTATIN WITH A HIGH SPECIFIC SURFACE AREA AND ITS USE IN A DOSAGE FORM 审中-公开
标题翻译：一种工业生产具有高比表面积的阿托伐他汀的非晶形式的方法及其在剂型中的用途
公开(公告)号：WO2011088806A2
公开(公告)日：2011-07-28
申请号：PCT/CZ2011000003
申请日：2011-01-12
申请人： ZENTIVA K S , STACH JAN , HOLAN MARTIN , HAVLICEK JAROSLAV , SIMEK STANISLAV , LINEK JAN , BRUSOVA HANA , RADL STANISLAV , DUBOVSKA MICHAELA , PROKOPOVA ALENA , RIHA JAROSLAV , SEBEK PAVEL
发明人： STACH JAN , HOLAN MARTIN , HAVLICEK JAROSLAV , SIMEK STANISLAV , LINEK JAN , BRUSOVA HANA , RADL STANISLAV , DUBOVSKA MICHAELA , PROKOPOVA ALENA , RIHA JAROSLAV , SEBEK PAVEL
IPC分类号： C07D207/34 , A61K31/40 , A61P3/06
CPC分类号： C07D207/34
摘要： The invention deals with an amorphous form of the hemicalcium salt of (3R,5R) 7-[3-phenyl- 4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-y1]-3,5-dihydroxyheptanoic acid (atorvastatin of formula I) with a high specific surface area, based on controlled precipitation, and its use in a medical dosage form. (I)
摘要翻译：本发明涉及（3R，5R）7- [3-苯基-4-苯基氨基甲酰基-2-（4-氟苯基）-5-异丙基吡咯-1-基] -3,5-二羟基庚酸的半钙盐基于受控沉淀的具有高比表面积的酸（式I的阿托伐他汀）及其在医药剂型中的用途。（一世）

2. 发明申请

WO2005011638A2 METHODS FOR THE STABILIZATION OF ATORVASTATIN 审中-公开
标题翻译：用于稳定阿托伐他汀的方法
公开(公告)号：WO2005011638A2
公开(公告)日：2005-02-10
申请号：PCT/CZ2004000045
申请日：2004-08-05
申请人： ZENTIVA AS , SEBEK PAVEL , PROKOPOVA ALENA , SVOBODA EDUARD , RADL STANISLAV , STACH JAN , SVOBODA MARTIN , KOVACIK ANDREJ , DANKO ADRIAN , PETRO ROMAN , STRIZINEC MIROSLAV
发明人： SEBEK PAVEL , PROKOPOVA ALENA , SVOBODA EDUARD , RADL STANISLAV , STACH JAN , SVOBODA MARTIN , KOVACIK ANDREJ , DANKO ADRIAN , PETRO ROMAN , STRIZINEC MIROSLAV
IPC分类号： A61K9/20 , A61K9/28 , A61K31/40
CPC分类号： A61K31/40 , A61K9/2054 , A61K9/2866
摘要： Stabilization of the pharmaceutical active solid substance atorvastatin alone or in a mixture with other solid substances embedded in a gaseous mixture is carried out in such a manner that in the surrounding gaseous mixture a partial pressure of oxygen of at most 2 kPa, preferably less than 1 kPa, more preferably less than 0.4 kPa is maintained. The corresponding partial pressure is achieved either by use of oxygen absorbers, by packaging under a pressure of 0.3 - 10 kPa, or by packaging under a slight overpressure of an inert gas, preferably nitrogen, the gas being introduced, by means of nozzles, into the cavities, optionally also into the space of the press roller and of the wiper station.
摘要翻译：药物活性固体物质阿托伐他汀单独或与包埋在气体混合物中的其它固体物质的混合物中的稳定化以这样的方式进行，即在周围的气体混合物中氧分压至多2kPa，优选小于1 kPa，更优选小于0.4kPa。通过使用氧气吸收器，通过在0.3-10kPa的压力下包装，或者通过在稍微超压的惰性气体，优选氮气下包装来实现相应的分压，通过喷嘴将气体引入腔体，可选地也进入压辊和擦拭器站的空间中。

3. 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。

4. 发明申请

WO2011063773A3 CRYSTALLINE AND AMORPHOUS FORMS OF ALMOREXANT HYDROCHLORIDE AND A METHOD OF THEIR PREPARATION 审中-公开
标题翻译：氢氧氯化物的晶体和非晶形态及其制备方法
公开(公告)号：WO2011063773A3
公开(公告)日：2012-02-02
申请号：PCT/CZ2010000119
申请日：2010-11-24
申请人： ZENTIVA K S , RADL STANISLAV , CERNY JOSEF , BRUSOVA HANA
发明人： RADL STANISLAV , CERNY JOSEF , BRUSOVA HANA
IPC分类号： C07D217/18 , A61K31/472 , A61P25/20
CPC分类号： C07D217/18
摘要： The invention relates to crystalline and amorphous forms of (2R)-2-{(1S)-6,7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl] -3,4-dihydro- 1H-isoquinolin-2-yl} -N-methyl-2-phenyl- acetamide hydrochloride (I) (almorexant) and a method of their preparation.
摘要翻译：本发明涉及（2R）-2 - {（1S）-6,7-二甲氧基-1- [2-（4-三氟甲基 - 苯基） - 乙基] -3,4-二氢-1H- 异喹啉-2-基} -N-甲基-2-苯基 - 乙酰胺盐酸盐（I）（异氰酸酯）及其制备方法。

5. 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。

6. 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））。

7. 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）

8. 发明申请

WO2009006860A2 A METHOD OF MANUFACTURING 4'-[[4-METHYL-6-(1-METHYL-1H-BENZIMIDAZOL-2-YL)-2-PROPYL-1H-BENZIMIDAZOL-1YL]METHYL]BIPHENYL-2-CARBOXYLIC ACID (TELMISARTAN) 审中-公开
标题翻译：制备4' - [[4-甲基-6-（1-甲基-1H-苯并咪唑-2-基）-2-丙基-1H-苯并咪唑-1-基]甲基]联苯-2-羧酸（TELMISARTAN）
公开(公告)号：WO2009006860A2
公开(公告)日：2009-01-15
申请号：PCT/CZ2008000080
申请日：2008-07-08
申请人： ZENTIVA AS , STACH JAN , RADL STANISLAV , CINIBULK JOSEF , STRELEC IVO , JARRAH KAMAL
发明人： STACH JAN , RADL STANISLAV , CINIBULK JOSEF , STRELEC IVO , JARRAH KAMAL
CPC分类号： C07D235/14
摘要： A carboxylic acid of the general formula R1COOH, wherein R1 is the hydrogen atom or a C1-C4 alkyl, is added to a solution of the potassium salt of telmisartan in an alcohol of the formula R2OH with the water content lower than 2%, wherein R2 is ethyl or methyl.
摘要翻译：将通式为R 1 COOH的羧酸（其中R 1为氢原子或C 1 -C 4烷基）加入到替米沙坦钾盐在式R2OH醇中的含水量低于2％的溶液中，其中 R2是乙基或甲基。

9. 发明申请

WO2005021535A3 A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP 审中-公开
标题翻译：一种去除三苯甲基保护基团的方法
公开(公告)号：WO2005021535A3
公开(公告)日：2005-06-09
申请号：PCT/CZ2004000051
申请日：2004-08-26
申请人： ZENTIVA AS , RADL STANISLAV , STACH JAN , KLECAN ONDREJ
发明人： RADL STANISLAV , STACH JAN , KLECAN ONDREJ
IPC分类号： C07D257/04 , C07D403/10
CPC分类号： C07D257/04 , C07D403/10 , Y02P20/55
摘要： A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1'-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R , R and R can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R and R can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
摘要翻译：从通式I的1-三苯基甲基-5-（4'-取代甲基-1,1'-联苯-2-基）-1H-四唑中除去三苯基甲烷保护基的方法，其中R表示式的基团和其中R 1，R 2和R 3可以是H，卤素，无支链或支链C 1 -C 5烷基，C 1 -C 5羟烷基，C 1 -C 5烷氧基，C 1 -C 5烷氧基甲基或苄基，或其中 R 2和R 3可以一起形成饱和或不饱和的C 5 -C 7环，任选未取代或取代的芳环，通过在中性或微碱性介质中的简单的无水C1至C5醇中溶剂解来进行。该方法适用于制备药物，如氯沙坦，厄贝沙坦或缬沙坦或坎地沙坦酯的钾盐。

10. 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.

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