公开(公告)号：EP2893919A1

公开(公告)日：2015-07-15

申请号：EP14000064.7

申请日：2014-01-09

申请人： SANOFI ,  Zentiva, a.s.

发明人： Mathieu, Amandine ,  Greco, Stephanie ,  Nakach, Mostafa ,  Bardet, Lionel ,  Authelin, Jean Rene ,  Skaria, Cyrus Victor ,  Beranek, Josef ,  Dammer, Ondrej ,  Krejcik, Lukas ,  Chalupova, Pavla ,  Dumicic, Aleksandra

IPC分类号： A61K9/14 ,  A61K31/5377

CPC分类号： A61K9/146 ,  A61K31/5377

摘要： The solid solution of aprepitant in a polymer, wherein the polymer is the co-polymer of polyvinyl caprolactam with polyvinyl acetate and polyethylene glycol and the weight ratio of aprepitant to the polymer is between 1:4 and 3:7, a process fro the preparation, and the corresponding pharmaceutical compositions and formulations.

摘要翻译： 聚乙烯吡咯烷酮在聚合物中的固溶体，其中聚合物是聚乙烯基己内酰胺与聚乙酸乙烯酯和聚乙二醇的共聚物，并且阿瑞消制剂与聚合物的重量比为1:4至3:7之间， ，以及相应的药物组合物和制剂。

公开(公告)号：EP2813212A1

公开(公告)日：2014-12-17

申请号：EP13002964.8

申请日：2013-06-10

申请人： Zentiva, a.s.

发明人： Stranska, Denisa ,  Erlebachova, Ivana ,  Kral, Vladimir ,  Sebek, Pavel ,  Beranek, Josef ,  Dumicic, Aleksandra ,  Sedmak, Gregor ,  Chvojka, Tomas

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K31/519

CPC分类号： A61K31/519 ,  A61K9/0051 ,  A61K9/2018 ,  A61K9/2077 ,  A61K9/4866 ,  A61K9/70 ,  A61K31/497 ,  A61K31/58

摘要： A process of manufacturing drug products using electrospinning technology,

摘要翻译： 使用静电纺丝技术制造药品的过程，

公开(公告)号：EP1558575B1

公开(公告)日：2009-04-22

申请号：EP03810732.2

申请日：2003-11-04

申请人： Zentiva, A.S

发明人： HERCEK, Richard ,  SKODA, Alojz ,  PROKSA, Bohumil

IPC分类号： C07D209/88

CPC分类号： C07D209/88

摘要： The invention solves a new method of preparation of Carvedilol for pharmaceutical use. In the synthesis of Carvedilol a reaction of 4-(oxirane-2-ylmethoxy)-9H-arbazole (II) with 2-(2-methoxyphenoxy)ethylamine salts (IV) in the presence of a base, in an alcohol having the number of carbons C2 to C5 as a solvent, at an elevated temperature, is used. After processing of the crude reaction mixture crude Carvedilol is obtained, which is purified by crystallization from ethylacetate with an addition of activated carbon and the final substance is formulated by crystallization from ethylacetate.

公开(公告)号：EP1711507B1

公开(公告)日：2008-12-03

申请号：EP05700509.2

申请日：2005-02-04

申请人： Zentiva, a.s.

发明人： RICHTER, Jindrich ,  JIRMAN, Josef

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

CPC分类号： C07F9/582

摘要： Crystalline monosodium salt of 3-pyridyl-1-hydroxyethylidene-1,1-bisphosphonic acid, having the X-ray pattern with characteristic interplanar distances 4.35; 8.44; 13.42 and 15.73 ú.

公开(公告)号：EP1554284B1

公开(公告)日：2008-10-22

申请号：EP03750270.5

申请日：2003-08-26

申请人： Zentiva, a.s.

发明人： VEVERKA, Miroslav ,  VODNY, Stefan ,  VEVERKOVA, Eva ,  HAJICEK, Josef ,  STEPANKOVA, Hana

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： A method for manufacturing hydrogen sulphate (alpha S) of the alpha-(2-chlorophenyl)-6,7­dihydro-thieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester (clopidogrel hydrogen sulphate) of formula I, in crystalline Form I, wherein the compound of formula is separated out of a solution of clopidogrel in the form of the free base or salt in a solvent selected from the series of primary, secondary or tertiary C1-C5 alcohols, their esters with Cl-C4 carboxylic acids, or optionally of mixtures thereof.

公开(公告)号：EP1968965A2

公开(公告)日：2008-09-17

申请号：EP06840860.8

申请日：2006-12-22

申请人： Zentiva, a.s.

发明人： RIDVAN, Ludek ,  JARRAH, Kamal ,  CINIBULK, Josef ,  ZATOPKOVA, Monika ,  PLACEK, Lukas

IPC分类号： C07D333/20

CPC分类号： C07D333/20

摘要： A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-mienyl)propylamine of Formula(l) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)-N, N-dimethyl-3-(l-naρhthyloxy)-3-(2-th1enyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(l-naphthyloxy)- 3-(2-thienyl)propylamine and D- tartaric acid (2:1), b) isolation of the salt (S)-N, N-dimethyl-3-(naphthyloxy)-3-(2- thienyl)propylamine/D- tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)-N, N-dimethyl-3-(l- naphthyloxy)-3-(2-thienyl) propylamine by action of an inorganic or organic base, c) demethylation of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2- thienyl) propylamine by action of an alkylchloroformate of formula C1COOR (R=C1-C5 alkyl, or C6-C12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetine base of formula I and optionally conversion of the base to a salt with the respective acid, or salt of a weak base.

公开(公告)号：EP1786808B1

公开(公告)日：2008-07-09

申请号：EP05773498.0

申请日：2005-08-31

申请人： Zentiva, a.s.

发明人： HALAMA, Ales ,  LUSTIG, Petr ,  JIRMAN, Josef

IPC分类号： C07D417/12

CPC分类号： C07D417/12

摘要： A method for the preparation of rosiglitazone of formula (I) by reduction of 5-[4-[2-(N-methyl- N-(2-ρyridyl)amino)ethoxy]-benzylidene]thiazolidine-2,4-dione of formula (II), the reduction being carried out using at least one borohydride of general formula MBH4, wherein M stands for a cation from the group of Na, Li, K, Zn and R4N, and R stands for a C1-C5 alkyl group, under the catalysis of cobalt salts in the presence of at least one complexing agent and a suitable solvent.

公开(公告)号：EP1922087A2

公开(公告)日：2008-05-21

申请号：EP06775676.7

申请日：2006-09-05

申请人： Zentiva, a.s.

发明人： ETRYCH, Tomas ,  CHYTIL, Petr ,  STUDENOVSKY, Martin ,  PECHAR, Michal ,  ULBRICH, Karel ,  RIHOVA, Blanka

IPC分类号： A61K47/48 ,  A61P35/00 ,  C08F220/58 ,  C08F8/34

CPC分类号： A61K47/58

摘要： A method for the preparation of polymeric conjugates of N-(2- hydroxypropyl)methacrylamide and a methacryloylaminoacylhydrazone of doxorubicin with pH-controlled release of the drug, comprising the following three steps of synthesis: a. preparation of a monomeric methacryloylaminoacylhydrazine, wherein the aminoacyl is derived from an amino acid or oligopeptide, by reaction of a methacryloyl halide with the respective peptide, amino acid, or a derivative thereof, and subsequent hydrazinolysis, b. synthesis of a polymeric precursor by direct copolymerization of N-(2- hydroxypropyl)methacrylamide with the methacryloylaminoacylhydrazine, and c. binding of doxorubicin to the polymeric precursor by reaction thereof with doxorubicin hydrochloride.

公开(公告)号：EP1782833A3

公开(公告)日：2008-03-19

申请号：EP06025316.8

申请日：2002-12-20

申请人： Zentiva, a.s.

发明人： Ulbrich, Karel ,  Etrych, Thomás ,  Rihova, Blanka, ,  Jelinkova, Markéta ,  Kovar, Marek

IPC分类号： A61K47/48

CPC分类号： A61K47/6883 ,  A61K47/65

摘要： Conjugates consisting of a polymeric carrier constituted by 30 to 3,000 monomer units linked to form a polymeric chain, composed of
a. 60 to 99 % of N -(2-hydroxypropyl)methacrylamide units
b. 1 to 25 % of units of methacryloylated hydrazones of α-amino acids, ε-amino acids, aromatic amino acids, or oligopeptides terminated with a molecule of an anthracycline cancerostatic
c. 0.5 to 15 % of units ofmethacryloylated α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides or their sodium salts, and optionally
d. 0.5 to 10 % of units of methacryloylated hydrazides of α-amino acids, ε-amino acids, aromatic amino acids or oligopeptides
e. 0.5 to 5 % of methacryloylated α-amino acids, ε-amino acids or oligopeptides terminated by a molecule of immunoglobulin or of a specific monoclonal or polyclonal antibody,

of the below given general formula, the individual structural units being disposed in a random manner in the chain and where x ranges from 20 to 3,000, a is from 1 to 750, b and c are each from 1 to 450, d ranges from 1 to 150, X is a residue of an amino acid or oligopeptide chosen from the following series: Gly, Ala, Leu, GlyGly, GlyLeuGly, GlyPheGly, GlyPheLeuGly, β-alanine, γ-amino butyric acid, ε-amino caproic acid (AKap), p-amino benzoic acid (AB), and S is an antibody selected from the following series: γ-globulin for i.v. administrations, autologous antibodies, antibodies anti-17-1A, anti-CA 15-3 and the like, linked to the polymeric chain by the marked structure.

公开(公告)号：EP1758879B1

公开(公告)日：2007-12-12

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.