Abstract: 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 ?-amino acids, ?-amino acids, aromatic amino acids or oligopeptides terminated with a molecule of an anthracycline cancerostatic, c) 0.5 to 15% of units of methacryloylated ?-amino acids, ?-amino acids, aromatic amino acids or oligopeptides or their sodium salts.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
April 5, 2011
Assignee:
Zentiva, k.s.
Inventors:
Karel Ulbrich, Tomas Etrych, Blanka Rihova, Marketa Jelinkova, Marek Kovar
Abstract: The subject-matter of the invention consists in a method of removing specific impurities of montelukast of formula (I), which occur due to chemical instability of the target substance and also contaminate the substance in the preparation process. Further, methods of isolation of specific impurities of montelukast defined by formulae (V-A), (IV-A), (XIIIa-A), (XIIIb-A) and analytic methods used for the control of the production of montelukast in the pharmaceutical quality.
Type:
Application
Filed:
March 11, 2009
Publication date:
February 10, 2011
Applicant:
ZENTIVA, K.S.
Inventors:
Ales Halama, Olga Bouskova, Petr Gibala, Josef Jirman
Abstract: Racemization of the R(?) isomer of the (2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester (Formula II) (also called R clopidogrel) is performed via conversion of a portion thereof to the S(+)isomer and it takes place in an organic solvent selected from alcohols, esters, ketones or ethers, or in their mixtures, in the presence of a base selected from substances of formula R1R2R3R4N+OH? wherein R1, R2, R3 and R4 are identical or different substituents selected from C1-C5 alkyls or C5, C6 cycloalkyls or aryls, C7-C9 alkyl-cycloalkyls or alkyl-aryls, the molar ratio of the base to the starting substance being 1:1 to 1:10., OMe Cl I Cl<VOMe II.
Type:
Grant
Filed:
March 3, 2006
Date of Patent:
July 13, 2010
Assignee:
Zentiva k s
Inventors:
Josef Hajicek, Hana Stepankova, Jan Kalivoda
Abstract: A method for manufacturing hydrogen sulphate (alpha S) of the alpha-(2-chlorophenyl)-6,7dihydrothieno[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 C1-C4 carboxylic acids, or optionally of mixtures thereof.
Type:
Grant
Filed:
August 26, 2003
Date of Patent:
May 11, 2010
Assignee:
Zentiva, k.s.
Inventors:
Miroslav Veverka, Stefan Vodny, Eva Veverkova, Josef Hajicek, Hana Stepankova
Abstract: A method of preparation of (S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)-N,N-dimethyl-3-(1-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-(1-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.
Type:
Grant
Filed:
October 21, 2005
Date of Patent:
May 4, 2010
Assignee:
Zentiva k.s.
Inventors:
Ludek Ridvan, Petr Hruby, Lukas Placek, Miroslav Kuchar
Abstract: 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-[(1R)-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.