专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

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. 发明授权

EP1704144B1 A METHOD OF PREPARATION OF THE HEMI-CALCIUM SALT OF (E)-7- [4-(4-FLUOROPHENYL)-6-ISOPROPYL-2- [ME THYL(METHYLSULFONYL)AMINO]PYRIMIDIN-5-YL](3R,5S)-3,5-DIHYDROXY-6-HEPTENOIC ACID 有权
标题翻译： PROCESS FOR（E）的半钙盐的制备-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）-3,5- 二羟基-6-庚
公开(公告)号：EP1704144B1
公开(公告)日：2007-02-07
申请号：EP04821059.5
申请日：2004-12-17
申请人： Zentiva, a.s.
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)-6-isopropyl-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 R1COOR2, R1COR2 and R1OH, wherein R1 and R2 independently represent hydrogen or a residue of a C1-C10 aliphatic hydrocarbon, C6 aromatic hydrocarbon, C5 or C6 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 C1-C5 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.

8. 发明公开

EP1594839A2 METHODE OF MANUFACTURING GLIMEPIRIDE AND THE RESPECTIVE INTERMEDIATE 审中-公开
标题翻译：用于生产格列美脲和相关中间体
公开(公告)号：EP1594839A2
公开(公告)日：2005-11-16
申请号：EP04712991.1
申请日：2004-02-20
申请人： Zentiva, a.s.
发明人： RADL, Stanislav , JARRAH, Kamal
IPC分类号： C07D207/38 , C07C211/35
CPC分类号： C07C211/35 , C07B2200/07 , C07D207/38
摘要： A method of manufacturing glimepiride of formula I wherein trans-4-methylcyclohexylamine pivalate of formula (VII) is reacted, either directly or after conversion to trans-4-methylcyclohexylamine or to its another salt, with an alkyl [4-(2-{[(3-ethyl-4-methyl-2-oxo-2,5-dihydro-lH-pyrrol-l yl)carbonyl]amino)ethyl)phenyl]-sulfonyl carbamate of general formula (IV) wherein R is a C1-C5 alkyl, giving glimepiride of formula I. trans-4-Methylcyclohexylamine pivalate of formula (VII).

9. 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.

10. 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）。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式