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1. 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。

2. 发明申请

WO2008064615A2 CRYSTALLINE AND AMORPHOUS FORMS OF RIMONABANT AND PROCESSES FOR OBTAINING THEM 审中-公开
标题翻译：可溶性和非晶形式的晶体和方法获得它们
公开(公告)号：WO2008064615A2
公开(公告)日：2008-06-05
申请号：PCT/CZ2007000108
申请日：2007-12-03
申请人： ZENTIVA AS , 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 , A61P3/04 , A61P25/16 , A61P25/28 , A61P25/34
CPC分类号： C07D231/14
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-lH-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.
摘要翻译：利莫那班的新型结晶多晶型III和利莫那班的无定形形式。通过将利莫那班溶解在非质子极性溶剂如乙腈或四氢呋喃中制备结晶形式III，将溶液倒入水中并搅拌所得混合物。通过溶解式ROH的醇和其中R是烷基，如甲醇或异丙醇，并搅拌混合物制备利莫那班的无定形形式。得到式（I）的咪唑啉酮，使得式（III）的5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-1H-吡唑-3-羧酸的酯），其中R是C1-C5烷基，苯基或取代的苯基，优选甲基或乙基，在溶剂中，优选在溶剂中，从二乙醚，四氢呋喃，二恶烷，二氯甲烷，乙腈，甲苯或它们的混合物，或过量的N-氨基哌啶，与N-氨基哌啶一起，在0℃至所用溶剂或溶剂混合物的沸点下通过至少一种路易斯酸催化。还描述了含有上述形式的药物组合物和上述形式用于制备治疗肥胖症，治疗吸烟习惯或治疗阿尔茨海默病或帕金森病的药物的用途。

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

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。

5. 发明申请

WO2011124190A3 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：通过异构芳香硫醇通过其甲基酯的O-甲基化生产4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法
公开(公告)号：WO2011124190A3
公开(公告)日：2011-12-01
申请号：PCT/CZ2011000032
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 , C07C215/64
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 R1 and R2 are hydrogen (H) or methyl (CH3), by demethylation of their methylethers of general formula (II), wherein symbols R1 and R2 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：一种制备通式（I）的4-（2-（取代的）-1-（1-羟基环己基）乙基）苯酚的方法，其中符号R1和R2是氢（H）或甲基（CH3），通过脱甲基其通式（II）的甲醚，其中符号R1和R2具有与式（I）中相同的含义，通过在溶剂环境中用至少一当量的芳族硫醇加热至100至220℃; 反应是通过加入碱进行的，而芳族硫醇是非臭的。非臭味这一术语意味着臭气只能在极端情况下，即在例如含有物质的开放容器之上的合格化学品生产中达到的浓度是可察觉的; 该试剂应缺乏含有硫醇基团的低分子化合物典型的极不理想的“硫”特征; 即使在上述极端情况下，在类似条件下，其臭气也不会超过常用有机溶剂的强度。（式（I），（II））。

6. 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)

7. 发明申请

WO2011047643A1 METHOD FOR THE PREPARATION OF (LS)-6,7-DIMETHOXY-L-[2-(4-TRIFLUOROMETHYLPHENYL)ETHYL]- 1,2,3,4-TETRAHYDROISOQUINOLINE 审中-公开
标题翻译：制备（LS）-6,7-二甲基-L- [2-（4-三氟甲基苯基）乙基] -1,2,3,4-四氢喹啉酮的方法
公开(公告)号：WO2011047643A1
公开(公告)日：2011-04-28
申请号：PCT/CZ2010/000106
申请日：2010-10-14
申请人： ZENTIVA, K.S. , CERNY, Josef , RADL, Stanislav , REITMAJER, Josef
发明人： CERNY, Josef , RADL, Stanislav , REITMAJER, Josef
IPC分类号： C07D215/26
CPC分类号： C07D215/26
摘要： The solution relates to the substance (15)-6,7-dimethoxy-l-[2-(4- trifluoromethylphenyl)ethyl]-l,2,3,4-tetrahydroisoquinoline of formula I, containing the desired S-enantiomer in an enantiomeric excess higher than or equal to 98.0%. Another solution is a manufacturing process for the present substance of formula I, which is synthesized via reduction of 6,7-dimethoxy-l-[2-(4- trifluoromethylphenyl)ethyl]-3,4-dihydroisoquinoline of formula II free base or hydrochloride using (R,R)-N-(p-toluenesulfonyl)- 1,2-diphenylethanediamine (chloro)(p-cymene)ruthenium(π) as a catalyst or using a catalyst generated in situ out of a ruthenium complex and a chiral ligand, wherein the catalyst used is in an amount lower than or equal to 2 molar %, related to the reduced substance (II).
摘要翻译：该溶液涉及式I的物质（15）-6,7-二甲氧基-1- [2-（4-三氟甲基苯基）乙基] -1,2,3,4-四氢异喹啉，其中含有所需的S-对映异构体对映体过量高于或等于98.0％。另一种解决方案是式I的本物质的制备方法，其通过还原式II游离碱的6,7-二甲氧基-1- [2-（4-三氟甲基苯基）乙基] -3,4-二氢异喹啉和使用（R，R）-N-（对甲苯磺酰基）-1,2-二苯基乙二胺（氯）（对甲基异丙基苯）钌（p）作为催化剂或使用由钌络合物原位产生的催化剂和手性配体，其中使用的催化剂的量与还原物质（II）有关的量低于或等于2摩尔％。

8. 发明申请

WO2011006455A3 METHOD OF PREPARING DESVENLAFAXINE AND ITS SALTS 审中-公开
公开(公告)号：WO2011006455A3
公开(公告)日：2011-01-20
申请号：PCT/CZ2010/000074
申请日：2010-07-08
申请人： ZENTIVA, K.S. , HRUBY, Petr , RIDVAN, Ludek , RADL, Stanislav , PLACEK, Lukas
发明人： HRUBY, Petr , RIDVAN, Ludek , RADL, Stanislav , PLACEK, Lukas
IPC分类号： C07C213/00 , C07C213/10 , C07C215/64
摘要： A method for the preparation of 4-(2-(dimethylamino)-l-(l-hydroxycyclohexyl)ethyl) phenol of formula (I), known under generic name desvenlafaxine, and its pharmaceutically acceptable salts, which comprises (a) mixing of the starting material O -benzyldesvenlafaxine or its derivative of formula (II), wherein R is H, 4-methyl, 4-methoxy, 3,4-dimethoxy, 2-nitro, 4-nitro, 4-chloro, 4- bromo, 2,6-dichloro or 2,6-difluoro, in an organic solvent or a mixture of solvents, and subsequent dissolving of the starting material by decreasing the pH to a value of 3 to 8 by addition of an inorganic or organic acid, or dissolving of O -benzyldesvenlafaxine or its derivative of formula (II) in an organic solvent or a mixture of solvents, wherein the compound of formula (II) is in the form of a salt with an inorganic or organic acid and the pH of the solution has a value of 3 to 8, (b) converting O -benzyldesvenlafaxine or its derivative of formula (II) to desvenlafaxine I by catalytic hydrogenation on a Raney catalyst, (c) removing the catalyst from the desvenlafaxine solution by filtration and subsequent increasing the pH to a value of 8 to 11 by addition of an inorganic or organic base, (d) isolating the desvenlafaxine base I by filtration, (e) converting the desvenlafaxine base I to a pharmaceutically acceptable salt. Formulae (I), (II)

9. 发明申请

WO2009056077A3 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-HR-吡咯烷-5-基）乙酸（Lofofelone）的新方法
公开(公告)号：WO2009056077A3
公开(公告)日：2009-06-18
申请号：PCT/CZ2008000116
申请日：2008-09-29
申请人： ZENTIVA AS , 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-lH- pyrrolizine-5-yl)acetic acid of formula I, wherein 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl- 2,3-dihydro-lH-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 C1-C6 alkyl group, with the use of the Fenton reagent in the presence of a sulfoxide of formula R1-SO-R2, wherein R1 is an (un)branched C1-C12 alkyl group, R2 is either an (un)branched C1-C12 alkyl group, an aryl group or a substituted aryl group, or wherein R1, R2 are independently (C?2)mX(C?2)n, wherein X = CH2, O, S, NR3, m = 1-3, n = 1-3 and R3 is either an (un)branched C1-C12 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：式I的2-（6-（4-氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪-5-基）乙酸的制备方法，其中6-（4 - 氯苯基）-2,2-二甲基-7-苯基-2,3-二氢-1H-吡咯嗪用式VII的碘代衍生物进行烷基化，其中A是氰基CN或酯基COOR，其中R是（未）支化的C 1 -C 6烷基，使用Fenton试剂在式R 1 -SO-R 2的亚砜存在下进行，其中R 1是（非）支化的C 1 -C 12烷基，R 2 （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）mX（C 2）n，其中X = CH 2，O，S ，NR 3，m = 1-3，n = 1-3和R 3是（非）支链C 1 -C 12烷基，芳基或取代芳基，反应在所用亚砜的环境中进行或者在其与适合的溶剂的混合物中，在0℃至80℃的温度下，优选在10℃的温度下进行将所得式IV的酯或式VIII的腈直接水解或在腈的情况下经由式（IX）的酰胺水解为所需的式I产物。

10. 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.

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