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11. 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。

12. 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。

13. 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。

14. 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。

15. 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。

16. 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。

17. 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。

18. 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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