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11. 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。

12. 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.

13. 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。

14. 发明申请

WO2004101534A1 A METHOD OF PREPARATION OF N-(1-OXOPENTYL)-N-[[2'-(1H-TETRAZOL-5-y1) [1,1'-BIPHENYL] -4-y1]METHYL]-L-VALINE (VALSARTAN) 审中-公开
标题翻译：制备N-（1-氧代戊基）-N - [[2' - （1H-四唑-5-y1）[1,1'-联苯]] -4-y] [甲基] -L-缬氨酸（VALSARTAN ）
公开(公告)号：WO2004101534A1
公开(公告)日：2004-11-25
申请号：PCT/CZ2004/000029
申请日：2004-05-14
申请人： ZENTIVA, a. s. , RADL, Stanislav , STACH, Jan , DEDINOVA, Eva
发明人： RADL, Stanislav , STACH, Jan , DEDINOVA, Eva
IPC分类号： C07D257/04
CPC分类号： C07D257/04 , Y02P20/55
摘要： From the starting 4-bromomethyl-2'-(1-triphenylmethyltetrazol-5-yl)biphenyl, N-[(2'(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester of formula 7 is obtained via a reaction with L-valine benzyl ester, and is converted to valsartan of formula I via a reaction with valeryl chloride and removing of protective groups. The method consists in converting, with hydrochloric acid, N-[(2'-(l-triphenylmethyl-tetrazol-5-yl)biphenyl-4yl)methyl]-(L)-valine benzyl ester of formula 7, obtained in the first stage, to N -[(2'-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester hydrochloride of formula III, which is optionally re-crystallized.
摘要翻译：从起始的4-溴甲基-2' - （1-三苯基甲基四唑-5-基）联苯，N - [（2'（1-三苯基甲基 - 四唑-5-基）联苯-4-基）甲基] - （L）通过与L-缬氨酸苄酯的反应获得式7的缬氨酸苄酯，并通过与戊酰氯反应和除去保护基团而转化成式I的缬沙坦。该方法包括用盐酸转化得自式7的N - [（2' - （1-三苯甲基 - 四唑-5-基）联苯-4-基）甲基] - （L） - 缬氨酸苄基酯转化为式III的N - [（2' - （1-三苯基甲基 - 四唑-5-基）联苯-4-基）甲基] - （L） - 缬氨酸苄酯盐酸盐，其任选地重结晶。

15. 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.

16. 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）。

17. 发明申请

WO2012139535A1 A METHOD OF PREPARING 2-ETHOXY-1-((2'-(5-OXO-4,5-DIHYDRO-1,2,4-OXADIAZOL-3-YL)BIPHENYL- 4-YL)METHYL)-1H-BENZO[D]IMIDAZOLE-7-CARBOXYLATES AND CONVERSION THEREOF TO AZILSARTAN 审中-公开
标题翻译：制备2-乙氧基-1 - （（2' - （5-氧代-4,5-二氢-1,2,4-氧杂环丁烷-3-基）联苯-4-基）甲基）-1H-苯并咪唑的方法 [D]咪唑-7-羧酸酯及其转化为AZILSARTAN
公开(公告)号：WO2012139535A1
公开(公告)日：2012-10-18
申请号：PCT/CZ2012/000030
申请日：2012-04-04
申请人： ZENTIVA, K.S. , RADL, Stanislav , STACH, Jan
发明人： RADL, Stanislav , STACH, Jan
IPC分类号： C07D413/10
CPC分类号： C07D413/10
摘要： An improved method of preparing alkyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro- 1,2,4-oxadiazol-3- yl)biphenyl-4-yl)methyl)-1 H -benzo[ d ]imidazole-7-carboxylates of formula (I), wherein R is either a branched or unbranched C 1 -C 4 alkyl, ArCH 2, Ar 2 CH, or Ar 3 C, wherein Ar is a substituted or unsubstituted phenyl, and of conversion thereof to azilsartan of formula (II). This compound is an efficient angiotensin II AT1 receptor antagonist, which is used in the form of the prodrug azilsartan medoxomil of formula (III) in the treatment of hypertension.
摘要翻译：制备2-乙氧基-1 - （（2' - （5-氧代-4,5-二氢-1,2,4-恶二唑-3-基）联苯-4-基）甲基） - 甲基）-1H - 苯并[d]咪唑-7-羧酸酯，其中R是支链或非支链C 1 -C 4烷基，ArCH 2，Ar 2 CH或Ar 3 C，其中Ar是取代或未取代的苯基，并且其转化为式（II）的叠氮化物。该化合物是一种有效的血管紧张素II AT1受体拮抗剂，其用于治疗高血压的式（III）的前药阿齐沙坦酯的形式。

18. 发明申请

WO2012055380A1 A METHOD OF OBTAINING OLMESARTAN MEDOXOMIL 审中-公开
标题翻译：一种获得奥美沙坦的方法
公开(公告)号：WO2012055380A1
公开(公告)日：2012-05-03
申请号：PCT/CZ2011/000104
申请日：2011-10-21
申请人： ZENTIVA, K. S. , STACH, Jan , JARRAH, Kamal , KRULIS, Radim , RADL, Stanislav , CERNY, Josef
发明人： STACH, Jan , JARRAH, Kamal , KRULIS, Radim , RADL, Stanislav , CERNY, Josef
IPC分类号： C07D405/14
CPC分类号： C07D405/14
摘要： A method of obtaining olmesartan medoxomil of formula I, comprising the following steps: a) detritylation of trityl olmesartan medoxomil in the presence of an organic acid and water, to give olmesartan medoxomil and trityl alcohol; b) addition of water and separation of the resulting trityl alcohol; c) addition of a water-miscible aprotic solvent; d) addition of water, to give crystalline olmesartan medoxomil; e) isolation of crystalline olmesartan medoxomil of formula I. A pharmaceutical composition comprising olmesartan medoxomil of formula I obtained by the above described method.
摘要翻译：一种获得式I的奥美沙坦酯的方法，包括以下步骤：a）在有机酸和水的存在下三苯甲基奥美沙坦酯的脱硝，得到奥美沙坦酯和三苯甲醇; b）加入水并分离得到的三苯甲醇; c）加入水混溶性非质子溶剂; d）加水，得到结晶奥美沙坦酯; e）分离式I的结晶奥美沙坦酯。包含通过上述方法获得的式I的奥美沙坦酯的药物组合物。

19. 发明申请

WO2012139536A1 A METHOD OF PREPARING 2-ETHOXY-1-((2'-(5-OXO-4,5-DIHYDRO-1,2,4-OXADIAZOL-3-YL)BIPHENYL- 4-YL)METHYL)-1H-BENZO[D]IMIDAZOLE-7-CARBOXYLATES AND CONVERSION THEREOF TO AZILSARTAN 审中-公开
标题翻译：制备2-乙氧基-1 - （（2' - （5-氧代-4,5-二氢-1,2,4-氧杂环丁烷-3-基）联苯-4-基）甲基）-1H-苯并咪唑的方法 [D]咪唑-7-羧酸酯及其转化为AZILSARTAN
公开(公告)号：WO2012139536A1
公开(公告)日：2012-10-18
申请号：PCT/CZ2012/000031
申请日：2012-04-04
申请人： ZENTIVA, K.S. , RADL, Stanislav
发明人： RADL, Stanislav
IPC分类号： C07D413/10
CPC分类号： C07D413/10
摘要： A method of preparing alkyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro- 1,2,4-oxadiazol-3- yl)biphenyl-4-yl)methyl)-1 H -benzo[ d ]imidazole-7-carboxylates of the general formula I, wherein R is either a branched or unbranched C 1 -C 4 alkyl, ArCH 2 , Ar 2 CH, or Ar 3 C, wherein Ar is a substituted or unsubstituted phenyl, in which an alkyl 2-ethoxy-1 -((2'- ((hydroxyamino)iminomethyl)biphenyl-4-yl)methyl)- 1 H -benzo[ d ]imidazole-7-carboxylate of the general formula V is reacted with a cyclization agent in a solvent in the presence of suitable bases. (I) (V)
摘要翻译：制备2-乙氧基-1 - （（2' - （5-氧代-4,5-二氢-1,2,4-恶二唑-3-基）联苯-4-基）甲基）苯并[d]咪唑-7-羧酸酯，其中R是支链或非支链C 1 -C 4烷基，ArCH 2，Ar 2 CH或Ar 3 C，其中Ar是取代或未取代的苯基，其中烷基2- 将通式V的乙氧基-1 - （（2' - （（羟基氨基）亚氨基甲基）联苯-4-基）甲基）-1H-苯并[d]咪唑-7-羧酸酯与环化剂在溶剂中存在合适的碱基。（I）（V）

20. 发明申请

WO2010088865A2 NEW SALTS OF DESVENLAFAXINE AND A METHOD OF THEIR PREPARATION 审中-公开
标题翻译：维生素D的新盐及其制备方法
公开(公告)号：WO2010088865A2
公开(公告)日：2010-08-12
申请号：PCT/CZ2010/000010
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
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，新盐是式（II）的草酸氢盐，其中去甲文拉法辛：草酸为1:1，式（III）的次氯酸盐以去甲文拉法辛：草酸为2：1的比例。

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