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1. 发明申请

WO2005021535A2 A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP 审中-公开
标题翻译：一种去除三苯基甲烷保护基团的方法
公开(公告)号：WO2005021535A2
公开(公告)日：2005-03-10
申请号：PCT/CZ2004/000051
申请日：2004-08-26
申请人： ZENTIVA, a.s. , RADL, Stanislav , STACH, Jan , KLECAN, Ondrej
发明人： RADL, Stanislav , STACH, Jan , KLECAN, Ondrej
IPC分类号： 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)-1 H -tetrazoles of general formula I wherein R represents the groups of formulae and where R 1 , R 2 and R 3 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 2 and R 3 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1-三苯甲基-5-（4'-烯基甲基-1,1'-联苯-2-基）-1H-苯并三唑基甲酸酯中除去三苯基甲烷保护基团的方法，通式I的四唑类，其中R代表下式的基团，并且其中R 1，R 2和R 3可以是H，卤素，直链或支链的C 1 -C 5烷基，C 1 -C 5羟基烷基，C 1 -C 5烷氧基，C 1 -C 5烷氧基甲基或苄基，或者其中R 2和R 3为氢，可以通过在简单的无水C1-C5醇中在中性或微碱性介质中进行溶剂分解而一起形成饱和或不饱和的C5-C7环，任选未取代或取代的芳环。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西酯的钾盐。

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

WO2012069025A1 (5-METHYL-2-OXO-1,3-DIOXOL-4-YLMETHYL)-4-(1-HYDROXY-1-METHYL-PROPYL)-2-PROPYL-1-[2'- (1H-TETRAZOL-5-YL)BIPHENYL-4-YL-METHYL]IMIDAZOLE-5-CARBOXYLATE AS AN IMPURITY OF OLMESARTAN MEDOXOMIL AND A METHOD OF ITS PREPARATION 审中-公开
标题翻译：（5-甲基-2-氧代-1,3-二氧代-4-甲基乙基）-4-（1-羟基-1-甲基 - 丙基）-2-丙基-1- [2' - （1H-四唑-5 -YL）联苯-4-基甲基]咪唑-5-羧酸甲酯作为奥美沙坦的消毒剂及其制备方法
公开(公告)号：WO2012069025A1
公开(公告)日：2012-05-31
申请号：PCT/CZ2011/000112
申请日：2011-11-23
申请人： ZENTIVA, K.S. , STACH, Jan , PLACEK, Lukas , KRULIS, Radim , RADL, Stanislav , CERNY, Josef
发明人： STACH, Jan , PLACEK, Lukas , KRULIS, Radim , RADL, Stanislav , CERNY, Josef
IPC分类号： C07D233/90 , C07D403/10 , C07D405/14 , G01N30/00
CPC分类号： C07D405/14 , C07D233/90 , C07D403/10
摘要： The compound of formula VI and a method of its preparation, and intermediates of its preparation. Use of these intermediates as standards in analysis of the angiotensin II antagonist olmesartan medoxomil of formula I and of intermediates of its production.
摘要翻译：式Ⅵ化合物及其制备方法及其制备中间体。使用这些中间体作为分析式I的血管紧张素II拮抗剂奥美沙坦酯和其制备中间体的标准。

4. 发明申请

WO2007048361A1 A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP FROM PRECURSORS OF ANTIHYPERTENSIVE DRUGS 审中-公开
标题翻译：从抗生素药物前驱物中除去三苯甲基保护基团的方法
公开(公告)号：WO2007048361A1
公开(公告)日：2007-05-03
申请号：PCT/CZ2006/000073
申请日：2006-10-25
申请人： ZENTIVA, A.S. , RADL, Stanislav , STACH, Jan
发明人： RADL, Stanislav , STACH, Jan
IPC分类号： C07D403/10 , C07D405/14
CPC分类号： C07D403/10 , C07D405/14 , Y02P20/55
摘要： A method of removing the triphenylmethane protecting group from precursors of antihypertensive drugs of general formula I, wherein R is a metabolically degradable group, B is a heterocyclic moiety with one or two 5- or 6-membered rings at least one of which contains two nitrogen heteroatoms, in which the compound of formula I is reacted with water in the presence of a solvent which is partially or completely miscible with water.
摘要翻译：从通式I的抗高血压药物的前体除去三苯甲烷保护基团的方法，其中R是可代谢降解的基团，B是具有一个或两个5-或6-元环的杂环部分，其中至少一个含有两个氮杂原子，其中式I化合物在与水部分或完全混溶的溶剂的存在下与水反应。

5. 发明申请

WO2011088806A3 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
公开(公告)号：WO2011088806A3
公开(公告)日：2011-07-28
申请号：PCT/CZ2011/000003
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
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)

6. 发明申请

WO2009006860A3 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
公开(公告)号：WO2009006860A3
公开(公告)日：2009-01-15
申请号：PCT/CZ2008/000080
申请日：2008-07-08
申请人： ZENTIVA A.S. , STACH, Jan , RADL, Stanislav , CINIBULK, Josef , STRELEC, Ivo , JARRAH, Kamal
发明人： STACH, Jan , RADL, Stanislav , CINIBULK, Josef , STRELEC, Ivo , JARRAH, Kamal
IPC分类号： C07D235/18
摘要： A carboxylic acid of the general formula R 1 COOH, wherein R 1 is the hydrogen atom or a C 1 -C 4 alkyl, is added to a solution of the potassium salt of telmisartan in an alcohol of the formula R 2 OH with the water content lower than 2%, wherein R 2 is ethyl or methyl.

7. 发明申请

WO2005068435A1 TITLE OF INVENTION: A METHOD OF PREPARATION OF THE HEMI-CALCIUM SALT OF (E)-7-[4-(4FLUOROPHENYL)-6-ISOPROPYL-2- [METHYL(METHYLSULFONVL)AMINOLPYRIMIDIN-5-YL](3R,5S)-3 ,5-, DIHVDROXY-6-HEPTENOIC ACID 审中-公开
标题翻译：（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]吡啶-5-基]（3R，5S）的盐酸盐的制备方法技术领域本发明涉及）-3,5-，DIHVDROXY-6-HEPTENOIC ACID
公开(公告)号：WO2005068435A1
公开(公告)日：2005-07-28
申请号：PCT/CZ2004/000088
申请日：2004-12-17
申请人： ZENTIVA, a. s. , SEBEK, Pavel , RADL, Stanislav , STACH, Jan
发明人： SEBEK, Pavel , RADL, Stanislav , STACH, Jan
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： A method of preparation of the hemi-calcium salt of rosuvastatin of formula (I) consists in extracting an aqueous solution of the sodium or potassium salt of (E)-7-[4-(4-fluorophenyl)-6isopropyl-2- [methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxy-6-heptenoic acid, with optional admixture of sodium or potassium hydroxide or other sodium or potassium salts having inorganic anions, with an organic solvent, incompletely miscible with water, selected from the series of R 1 COOR 2 , R 1 COR 2 and R 1 OH, wherein R 1 and R 2 independently represent hydrogen or a residue of a C 1 -C 10 aliphatic hydrocarbon, C 6 aromatic hydrocarbon, C 5 or C 6 cyclic hydrocarbon, or a combination of an aliphatic and aromatic or cyclic hydrocarbon, the extract being subsequently shaken with an aqueous solution of an inorganic or C 1 -C 5 organic calcium salt, and the product of formula I is further isolated by cooling and/or adding an anti-solvent and filtration, and optionally, is converted into its amorphous form.
摘要翻译：制备式（I）的瑞舒伐他汀的半钙盐的方法在于提取（E）-7- [4-（4-氟苯基） - 异丙基-2- [（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）-3,5-二羟基-6-庚烯酸，具有任选的氢氧化钠或氢氧化钾或其它具有无机阴离子的钠盐或钾盐的混合物，选自R 1 COOR 2，R 1 COR 2和R 1 OH的不完全与水混溶的有机溶剂，其中R 1和R 2独立地表示氢或C 1 -C 10脂族烃，C 6芳族烃，C 5或C 6环烃或脂族和芳族或环烃的组合的残基，随后与无机或C 1 -C 5有机物的水溶液一起摇动该提取物钙盐，并且式I的产物通过冷却和/或加入抗溶剂进一步分离并过滤，并且任选地被转化为其无定形形式。

8. 发明申请

WO2005011638A3 METHODS FOR THE STABILIZATION OF ATORVASTATIN 审中-公开
公开(公告)号：WO2005011638A3
公开(公告)日：2005-02-10
申请号：PCT/CZ2004/000045
申请日：2004-08-05
申请人： ZENTIVA, A. S. , 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
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.

9. 发明申请

WO2003068739A1 METHOD OF MANUFACTURING AN AMORPHOUS FORM OF THE HEMI-CALCIUM SALT OF (3R, 5R) 7- 3-PHENYL-4-PHENYLCARBAMOYL-2-(4-FLUOROPHENYL)-5-ISOPROPYL-PYRROL-1-YL!-3, 5-DIHYDROXYHEPTANOIC ACID (ATORVASTATIN) 审中-公开
标题翻译：制备（3R，5R）7- 3-苯基-4-苯基乙酰基-2-（4-氟苯基）-5-异丙基 - 吡咯-1-基] -3,5,5-三甲氧基苯酚的盐酸盐的非晶形式的方法 -DIHYDROXYHEPTANOIC ACID（ATORVASTATIN）
公开(公告)号：WO2003068739A1
公开(公告)日：2003-08-21
申请号：PCT/CZ2003/000007
申请日：2003-01-30
申请人： LECIVA, a.s. , RADL, Stanislav , STACH, Jan
发明人： RADL, Stanislav , STACH, Jan
IPC分类号： C07D207/34
CPC分类号： C07D207/337
摘要： A method of manufacturing an amorphous form of the hemi-calcium salt of (3R, 5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid of formula (I), in which (3R, 5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid or its salt with a cation M + wherein M + is either a cation of an alkali metal or an ammonium cation of formula R n N (+) H (4-n) wherein R is lower C 1 -C 5 alkyl, n may reach values ranging between 0 and 3, is, without isolating the intermediate in the form of the hemi-calcium salt or of another salt, acid or lactone, converted, in a solution, by the treatment with the calcium salt or calcium hydroxide, or a calcium C 1 -C 5 alcoholate, to the hemi-calcium salt, and the latter is precipitated with a C 1 -C 5 hydrocarbon or dialkylether of formula R 1 OR 2 , wherein each of R 1 and R 2 is a C 1 -C 5 alkyl group. The starting acid or its salt is prepared starting from (3R, 5R) tert-butyl (6-{2-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl]-ethyl}-2,2-dimethyl-[1,3]dioxane-4-yl)-acetate of formula II.
摘要翻译：制备（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（3H） - 嘧啶的半钙盐的无定形形式的方法（I）的5-二羟基庚酸，其中（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] 5-羟基庚酸或其盐与阳离子M +，其中M +是碱金属的阳离子或式RnN（+）H（4-n）的铵阳离子，其中R为低级C1-C5烷基，n可达到值范围在0和3之间，是不分离半钙盐或另一种盐，酸或内酯形式的中间体，在溶液中通过用钙盐或氢氧化钙处理或钙 C1-C5醇化物与半钙盐反应，后者用式R1OR2的C1-C5烃或二烷基醚沉淀，其中R1和R2各自为C1-C5烷基。起始酸或其盐由（3R，5R）（6- {2- [3-苯基-4-苯基氨基甲酰基-2-（4-氟苯基）-5-异丙基 - 吡咯-1-基 ] - 乙基} -2,2-二甲基 - [1,3]二氧杂环己烷-4-基） - 乙酸乙酯。

10. 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）

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