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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

WO2009056077A2 A NEW METHOD OF MANUFACTURING 2-(6-(4-CHLOROPHENYL)-2,2-DIMETHYL-7-PHENYL-2,3-DIHYDRO-LH-PYRROLIZINE-5-YL)ACETIC ACID (LICOFELONE) 审中-公开
标题翻译：制备2-（6-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-4-羟基吡咯烷-5-基）乙酸（LICOFELONE）的新方法
公开(公告)号：WO2009056077A2
公开(公告)日：2009-05-07
申请号：PCT/CZ2008/000116
申请日：2008-09-29
申请人： ZENTIVA, A.S. , RADL, Stanislav , KLECAN, Ondrej
发明人： RADL, Stanislav , KLECAN, Ondrej
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A method of manufacturing 2-(6-(4-chlorophenyl)-2,2-dirnethyl-7-phenyl-2,3-dihydro-l H - pyrrolizine-5-yl)acetic acid of formula I, wherein 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl- 2,3-dihydro-l H -pyrrolizine of formula II is alkylated with a iodo derivative of formula VII, wherein A is either the cyano group CN or an ester group COOR, wherein R is an (un)branched C 1 -C 6 alkyl group, with the use of the Fenton reagent in the presence of a sulfoxide of formula R 1 -SO-R 2 , wherein R 1 is an (un)branched C 1 -C 12 alkyl group, R 2 is either an (un)branched C 1 -C 12 alkyl group, an aryl group or a substituted aryl group, or wherein R 1 , R 2 are independently (CΗ 2 ) m X(CΗ 2 ) n , wherein X = CH 2 , O, S, NR 3 , m = 1-3, n = 1-3 and R 3 is either an (un)branched C 1 -C 12 alkyl group, an aryl group or a substituted aryl group, the reaction being carried out in the environment of the sulfoxide used or in its mixture with suitable solvents at a temperature of O 0C to 80 °C, preferably at temperatures in the range of 10 to 40 °C, and the resulting ester of formula IV or nitrile of formula VIII is hydrolyzed to the desired product of formula I either directly or in the case of the nitrile via the amide of formula (IX).
摘要翻译：制备式I的2-（6-（4-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪-5-基）乙酸的方法，其中6-（4 - 氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪与式Ⅶ的碘衍生物烷基化，其中A为氰基CN或酯基COOR，其中R是（未）支化的C 1 -C 6烷基，在式R1-SO-R2的亚砜存在下使用芬顿试剂，其中R 1是（未）支化的C 1 -C 12烷基，R 2 是（未）支链C 1 -C 12烷基，芳基或取代芳基，或其中R 1，R 2独立地为（C 2）m X（C 2）n，其中X = CH 2，O，S ，NR 3，m = 1-3，n = 1-3，并且R 3是（未）支化的C 1 -C 12烷基，芳基或取代的芳基，所述反应在所用亚砜的环境中进行或在其合适的溶剂中，在0℃至80℃的温度下，优选在10℃的温度范围内将所得到的式IV的酯或式VIII的腈直接或通过式（IX）的酰胺直接或在腈的情况下水解成所需的式I的产物。

3. 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。

4. 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.

5. 发明申请

WO2008151584A1 METHOD FOR THE PREPARATION OF HIGH PURITY ALMOTRIPTAN 审中-公开
标题翻译：用于制备高纯度ALMOTRIPTAN的方法
公开(公告)号：WO2008151584A1
公开(公告)日：2008-12-18
申请号：PCT/CZ2008/000067
申请日：2008-06-13
申请人： ZENTIVA, A.S. , RIDVAN, Ludek , HRUBY, Petr , STACH, Jan , RADL, Stanislav , VOSLAR, Michal , PETRICKOVA, Hana , TISOVSKA, Lucie , ZATOPKOVA, Monika
发明人： RIDVAN, Ludek , HRUBY, Petr , STACH, Jan , RADL, Stanislav , VOSLAR, Michal , PETRICKOVA, Hana , TISOVSKA, Lucie , ZATOPKOVA, Monika
IPC分类号： C07D401/12
CPC分类号： C07D209/14
摘要： A method for the preparation and purification of the substance of formula (I), i.e. 3-[2- (dimethylamino)ethyl]-5-(1-pyrrolidinylsulfonylmethyl)-1 H- indole, which comprises (a) conversion of 4-(1-pyrrolidinylsulfonylmethyl)phenylhydrazine of formula (III) by reaction with an organic or inorganic acid to a salt that is insoluble or poorly soluble in water, which is converted to 3-(2-aminoethyl)-5-(1-pyrrolidinylsulfonylmethyl)indole of formula (VII), which is further converted without isolation to a solution of the almotriptan base, which provides a crystalline salt of almotriptan with an organic or inorganic acid; (b) conversion of the salt of almotriptan to the almotriptan base, which separates from the solution in the crystalline form; (c) purification of the almotriptan base by crystallization from an organic solvent.
摘要翻译：制备和纯化式（I）物质的方法，即3- [2-（二甲基氨基）乙基] -5-（1-吡咯烷基磺酰基甲基）-1H-吲哚，其包括（a）4- 通过与有机或无机酸反应成不溶于水或难溶于水的盐，转化成3-（2-氨基乙基）-5-（1-吡咯烷基磺酰基甲基）吲哚，得到式（III）的1-吡咯烷基磺酰基甲基）苯肼式（VII）化合物，其不经分离进一步转化为阿莫曲坦碱的溶液，其提供阿莫曲坦与结构的有机或无机酸的盐; （b）将阿莫曲坦盐转化为阿米托糖碱，其以结晶形式与溶液分离; （c）通过从有机溶剂中结晶来纯化阿莫曲坦碱。

6. 发明申请

WO2007000121A1 A METHOD FOR THE PRODUCTION OF THE HEMI-CALCIUM SALT OF (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]PYRIMIDIN-5-YL](3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC 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]嘧啶-5-基]（3R，5S）的硫酸钙的生产方法）-3,5-二羟基庚-6-烯酸
公开(公告)号：WO2007000121A1
公开(公告)日：2007-01-04
申请号：PCT/CZ2006/000039
申请日：2006-06-08
申请人： ZENTIVA, a.s. , RADL, Stanislav , STACH, Jan , KLVANA, Robert , JIRMAN, Josef
发明人： RADL, Stanislav , STACH, Jan , KLVANA, Robert , JIRMAN, Josef
IPC分类号： C07D239/42 , A61K31/505
CPC分类号： C07D239/42 , Y02P20/55
摘要： A method of producing the hemi-calcium salt of rosuvastatin, i.e. of ( E )-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3 R ,5 S )-3,5-dihydroxyhept-6-enoic acid of formula (I), in the crystalline or amorphous solid state, wherein a) the lactone of formula (IV), or ester or amid of general formulae (V) or (XIII), wherein X is either oxygen or amino group, R 1 CR 2 is a protecting group, wherein R 1 and R 2 are preferably selected from C 1 to C 3 alkyls, and R is an alkyl selected from C 1 to C 10 alkyls, preferably methyl, ethyl or tert-butyl, after removing the protecting group in the case of the compound of formula (V), ia converted, by alkaline hydrolysis with an alkali metal or Ca 2+ base, into a salt of rosuvastatin, b) in the case that an alkali metal base was used in step (a), the resulting alkali salt of rosuvastatin is converted into the calcium salt of rosuvastatin by reaction with a calcium salt in aqueous environment, c) crude calcium salt of rosuvastatin of formula (I) is extracted into a solvent partially miscible with water selected from the group including R 1 COOR 2 , R 1 COR 2 , or R 1 OH, wherein R 1 and R 2 independently mean hydrogen or a residue of a C 1 to 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, d) the solution of the calcium salt of rosuvastatin prepared according to step (c) is further washed with water, and e) the product of formula (I) is isolated by cooling the solution and filtration, or by adding an anti-solvent and filtration, or by spraying into the stream of an inert gas.
摘要翻译：（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R）的半舒康的半钙盐的制备方法，式（I）的5S）-3,5-二羟基庚-6-烯酸，其结构或无定形固态，其中a）式（Ⅳ）的内酯，或通式（Ⅴ）或（XIII），其中X为氧或氨基，R 1为CR 2为保护基，其中R 1和R 2为 > 2优选选自C 1至C 3烷基，R是选自C 1至C 3烷基的烷基，在式（V）化合物的情况下除去保护基后，通过碱金属或碱金属碱性水解转化，优选甲基，乙基或叔丁基，优选甲基，乙基或叔丁基， 2 +底物转化为罗苏伐他汀的盐，b）在步骤（a）中使用碱金属碱的情况下，将所得的瑞舒伐他汀碱盐转化为罗苏伐他汀的钙盐他汀类药物通过在水性环境中与钙盐反应，c）式（I）的瑞舒伐他汀的粗钙盐被萃取到与选自以下的水部分混溶的溶剂中：R＆lt; 2，R 1，R 2，或R 1 OH，其中R 1和R 2， SUP> 2独立地表示氢或C 1至C 10脂族烃，C 6芳烃，C 5或C 6环状烃，或脂族和芳族或环状烃的组合，d）根据步骤（c）制备的瑞舒伐他汀钙盐溶液，进一步用水洗涤，e）通过冷却溶液和过滤，或通过加入反溶剂和过滤，或通过喷雾入惰性气体流来分离式（I）的产物。

7. 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））。

8. 发明申请

WO2004037824A1 PROCESS FOR THE PREPARATION OF ZALEPLON 审中-公开
标题翻译：制备ZALEPLON的方法
公开(公告)号：WO2004037824A1
公开(公告)日：2004-05-06
申请号：PCT/CZ2003/000057
申请日：2003-10-21
申请人： ZENTIVA, A.S. , RADL, Stanislav
发明人： RADL, Stanislav
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： N -[3-(3-Dimethylamino-acryloyl)-phenyl]- N -ethyl-acetamide is reacted with 5-amino- l H -pyrazol-4-carbonitrile in a medium comprising a solution of hydrochloric or hydrobromic acid in a C1-C5 alcohol, or in a C4-C6 aliphatic or cyclic ether, or in a C2-C5 alkoxyalcohol, or in a 5- to 6-membered aromatic heterocyclic solvent, containing 1-2 oxygen atoms, or in mixtures thereof with water, thus forming ZALEPLON.
摘要翻译： N- [3-（3-二甲基氨基 - 丙烯酰基） - 苯基] -N-乙基 - 乙酰胺与5-氨基-1H-吡唑-4-甲腈在含有盐酸或氢溴酸溶液的介质中反应， C5醇，或C4-C6脂肪族或环状醚，或C2-C5烷氧基醇，或含有1-2个氧原子或与水混合的5-至6-元芳族杂环溶剂，因此形成ZALEPLON。

9. 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。

10. 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)

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