Abstract: A method for preparing 1-(4-methanesulfonamidophenoxy)-2-[N-(4-methanesulfonamidophenethyl)-N-methylamino]ethane (Dofetilide) of formula I by sulfonylation of 1-(4-aminophenoxy)-2-[N-(4-aminophenethyl)-N-methylamino]ethane of formula II with N-methylsulfonyl-N?-methylimidazolium chloride of formula III.
Abstract: A method for preparing 1-(4-methanesulfonamidophenoxy)-2-[N-(4-methanesulfonamidophenethyl)-N-methylamino]ethane (Dofetilide) of formula I by sulfonylation of 1-(4-aminophenoxy)-2-[N-(4-aminophenethyl)-N-methylamino]ethane of formula II with N-methylsulfonyl-N?-methylimidazolium chloride of formula III.
Abstract: The invention relates to a compound which is, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine, which is a selective A2A adenosine receptor agonist in myocardial imaging. The new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E) is characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°; and further characterized by a DSC scan showing marked endotherm in the range of 258 to 264° C.; and further characterized by a specific IR spectra.
Type:
Grant
Filed:
June 27, 2013
Date of Patent:
September 13, 2016
Assignee:
Farmak, a.s.
Inventors:
Lubomir Kvapil, Pavel Hradil, Martin Grepl, Petr Slezar, Barbora Dvorakova
Abstract: A method of preparation of N-(1-benzo[b]thien-2-ylethyl)-N-hydroxyurea of formula (I) with the use of a reaction of 1-(benzo[b]thien-2-yl)-ethanol of formula (II) with hydroxyurea of formula (III) in organic solvents, organic acids, their mixtures or in mixtures thereof with water, being catalyzed by strongly acidic cation exchangers or various hydrogen sulphates.
Type:
Grant
Filed:
April 6, 2009
Date of Patent:
January 13, 2015
Assignee:
Farmak, A.S.
Inventors:
Kamil Koristek, Pavel Hradil, Martin Grepl, Petr Slezar
Abstract: A new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E), characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°, and further characterized by DSC showing marked endotherm in the range of 258 to 264° C.
Type:
Application
Filed:
June 27, 2013
Publication date:
October 30, 2014
Applicant:
Farmak, a.s.
Inventors:
Lubomir KVAPIL, Pavel HRADIL, Martin GREPL, Petr SLEZAR, Barbora DVORAKOVA
Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
July 16, 2013
Assignee:
Farmak, A.S.
Inventors:
Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
Abstract: A method for preparing 4-[3,5-bis(2-hydroxyphenyl )-[1,2,4]triazol-1-yl]benzoic acid of formula (I) by reaction of 2-(2-hydroxyphenyl)benz[e][1,3]oxazin-4-one of formula (II) with 4-hydrazinobenzoic acid of formula (III) in an organic acid or in a mixture of an organic acid and an organic solvent.
Type:
Grant
Filed:
June 16, 2008
Date of Patent:
March 6, 2012
Assignee:
Farmak, A S
Inventors:
Radek Melnicky, Pavel Hradil, Lubomir Kvapil, Martin Grepl, Petr Slezar
Abstract: A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1 -piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C1 to C6 alcohol used.
Type:
Grant
Filed:
August 31, 2006
Date of Patent:
October 11, 2011
Assignee:
Farmak, A.S.
Inventors:
Pavel Hradil, Lubomir Kvapil, Roman Gabriel, Martin Grepl, Jan Novotny, Petr Slezar, Radek Melnicky
Abstract: A process for preparing optically pure enantiomers of R-(?)tamsulosin of formiula Ia and S-(+)tamsulosin of formula Ib by resolving racemic tamsulosin of formula I by means of (IR)-(?)-camphor-10-sulfonic acid and (1S)-(+)-camphor-10-sulfonic acid, resp., in an environment of organic solvents, water or mixtures thereof.
Type:
Grant
Filed:
October 8, 2003
Date of Patent:
April 4, 2006
Assignee:
Farmak, a.s.
Inventors:
Pavel Hradil, Miroslav Urbasek, Lubomir Kvapil, Petr Slezar