公开(公告)号：EP1556338B1

公开(公告)日：2008-05-14

申请号：EP03769173.0

申请日：2003-10-21

申请人： Zentiva, a.s.

发明人： STEPANKOVA, HANA ,  HAJICEK, Josef ,  SIMEK, Stanislav

IPC分类号： C07C269/00 ,  C07C271/44 ,  C07C215/50

CPC分类号： C07C271/44 ,  C07B2200/07 ,  C07C215/50

摘要： The compound of formula (III), optionally its alkaline salt, is reacted with a compound of formula VII, wherein X is a leaving group, resulting in (S)-rivastigmine of formula II, which is then optionally converted into (S)-rivastigmine hydrogentartrade of formula I.

公开(公告)号：EP1653930B1

公开(公告)日：2007-12-19

申请号：EP04738465.6

申请日：2004-08-05

申请人： Zentiva, a.s.

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 ,  A61K31/40

CPC分类号： A61K31/40 ,  A61K9/2054 ,  A61K9/2866

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.

公开(公告)号：EP1723157B1

公开(公告)日：2007-11-28

申请号：EP05706666.4

申请日：2005-02-28

申请人： Zentiva, a.s.

发明人： RICHTER, Jindrich ,  JIRMAN, Josef ,  PETRICKOVA, Hana

IPC分类号： C07F9/58 ,  A61K31/663 ,  A61P19/00

CPC分类号： C07F9/582

摘要： The monosodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid in new amorphous forms, methods of preparation and a pharmaceutical formulation.

摘要翻译： 新的无定形形式的3-吡啶基-1-羟基亚乙基-1,1-二膦酸的单钠盐，制备方法和药物制剂。

公开(公告)号：EP1554279B1

公开(公告)日：2007-11-28

申请号：EP03755542.2

申请日：2003-10-21

申请人： Zentiva, a.s.

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- lH-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.

公开(公告)号：EP1758879A1

公开(公告)日：2007-03-07

申请号：EP05793945.6

申请日：2005-10-21

申请人： Zentiva, a.s.

发明人： RIDVAN, Ludek ,  HRUBY, Petr ,  PLACEK, Lukas ,  KUCHAR, Miroslav

IPC分类号： C07D333/20 ,  A61K31/38

CPC分类号： C07D333/20

摘要： A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt.

摘要翻译： 一种制备式（I）的（S）-N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺或其药学上可接受的盐的方法，其中（RS）-N， 使式（III）的3-（1-萘氧基）-3-（2-噻吩基）丙胺与光学活性酸反应，然后使该非对映异构体结晶，该非对映异构体通过与无机或有机 （S）-III的（S）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺，然后将其用氯甲酸烷基酯去甲基化，然后进行水解和任选的转化 式（I）化合物转化为其盐。

公开(公告)号：EP1387843B1

公开(公告)日：2007-02-28

申请号：EP02734989.3

申请日：2002-04-25

申请人： Zentiva, a.s.

发明人： HALAMA, Ales ,  HEJTMÁNKOVÁ, Ludmila ,  LUSTIG, Petr ,  RICHTER, Jindrich ,  SRSNOVÁ , Lucie ,  JIRMAN, Josef

IPC分类号： C07D417/12 ,  A61K31/4427 ,  A61P3/10

CPC分类号： C07D417/12 ,  Y02P20/55

摘要： A method for obtaining antidiabetic of formula (I), wherein the method comprises condensing of a 4-derivatized phenol or phenolate of general formula (II), wherein R is an amino group-containing organic residue, selected from the group comprising a residue of the following formula -NHR3, wherein R3 is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein Rb represents a carboxy group either in the free acid form or in the form of a salt or ester or another functional derivative or the nitrile group CN, and M represents a hydrogen or alkali metal atom, with a pyridine base of general formula (III), wherein Z is a leaving group other than a halogen, wherein, before or after carrying out the condensation, the following operations are carried out: (a) diazotizing the amino group present in organic residue R; (b) converting the diazotised residue R into a derivative of 2-halopropionate or 2-halopropionitrile of formula (B), wherein Rb is as defined above and X is a halogen; (c) cyclizing the derivative of 2-halopropionate or 2-halopropionitrile with thiourea; (d) hydrolysing the resulting imine thus giving pioglitazone of formula (I).

公开(公告)号：EP1696890A2

公开(公告)日：2006-09-06

申请号：EP04819574.7

申请日：2004-12-03

申请人： Zentiva, a.s.

发明人： VLADOVICOVA, Beate ,  LEHOCKY, Mikulas ,  KORMANOVA, Viera ,  HUBINOVA, Viera

IPC分类号： A61K9/32 ,  A61P25/22 ,  A61P25/24 ,  A61K31/137

CPC分类号： A61K9/2846

摘要： A venlafaxin containing coated tablet with controlled release, which contains venlafaxin, or its salt with an inorganic or carboxylic acid, in amounts from 20 to 60 weight %, and a hydrophilic polymer in amounts from 30 to 70 weight %, based on the weight of the core, in its core, and from 1 to 3 weight % of a water-poorly permeable or impermeable polymer in its coating, and a method of preparation thereof.

公开(公告)号：EP1554279A1

公开(公告)日：2005-07-20

申请号：EP03755542.2

申请日：2003-10-21

申请人： Zentiva, A.S.

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- lH-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.

公开(公告)号：EP2029587A2

公开(公告)日：2009-03-04

申请号：EP07764312.0

申请日：2007-06-21

申请人： Zentiva, A.S.

发明人： JIRMAN, Josef ,  JUNEK, Richard ,  LUSTIG, Petr ,  RICHTER, Jindrich ,  PLACEK, Lukas

IPC分类号： C07D453/02

CPC分类号： C07D453/02

摘要： A process for the preparation of (1 S)-QR)-I -azabicyclo[2.2.2.]oct-3-yl 3,4-dihydro-1-phenyl- 2(1H)-isoquinoline carboxylate by reacting (1S)-alkyl 1-phenyl-1, 2,3, 4-tetrahydro-2- isoquinoline carboxylate with 3-(R)-quinuclidol in an inert solvent, where a primary alkyl ester of the carboxylate whose alkyl length is C1-C4 is used and the reaction is catalyzed by a non-nucleophilic base.

摘要翻译： （1S）-QR）-1-氮杂二环[2.2.2]辛-3-基-3,4-二氢-1-苯基-2（1H） - 异喹啉羧酸酯的制备方法， - 烷基1-苯基-1,2,3,4-四氢-2-异喹啉羧酸酯与3-（R） - 奎宁醇在惰性溶剂中反应，其中使用烷基长度为C 1 -C 4的羧酸酯的伯烷基酯 并且反应由非亲核碱催化。

公开(公告)号：EP1996544A1

公开(公告)日：2008-12-03

申请号：EP05700507.6

申请日：2005-02-03

申请人： Zentiva, a.s.

发明人： HAJICEK, Josef ,  SLAVIKOVA, Marketa

IPC分类号： C07C303/40 ,  C07C311/37

CPC分类号： C07C311/46 ,  C07B2200/07 ,  C07C303/38 ,  Y02P20/55 ,  C07C311/37

摘要： A method of preparation of (R)-(-)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide of formula I and its use for production tamsulosin. A protective group is introduced to N-[(1R)-2­(4-methoxyphenyl)-1-methylethyl]-N- [(1 R)-1-phenylethyl)]amine and the resulting amide of formula IX is chlorosulfonated and the resulting sulfochloride is converted to a sulfonamide of formula X, from which the compound of formula I is obtained by hydrogenation.