Patents Assigned to LEK Pharmaceuticals d.d.
  • Patent number: 9212118
    Abstract: The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: December 15, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Jan Humljan, Nenad Maras
  • Patent number: 9174930
    Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: November 3, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Matej Sova, Zdenko Casar, Gaj Stavber
  • Patent number: 9150518
    Abstract: A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C1-C5 alkyl esters of rosuvastatin, preferably tert-butyl ester of rosuvastatin, with an organic nitrogen base, e.g. guanidines, amidines, amines and quaternary ammonium hydroxides, in the presence of water, optionally containing aprotic solvent, following the conversion of thus obtained rosuvastatin salt with a source of calcium to obtain rosuvastatin calcium, which is then isolated. An alternative process is disclosed, which comprises the conversion of numerous novel ammonium salts of rosuvastatin, preferably tert-octylammonium salt of rosuvastatin, with the source of calcium to desired commercial rosuvastatin calcium. Rosuvastatin calcium is an inhibitor of HMG CoA reductase, useful in the treatment of hyperlipidemia, hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: June 22, 2006
    Date of Patent: October 6, 2015
    Assignee: Lek Pharmaceuticals, D.D.
    Inventors: Marko Zlicar, Zdenko Casar
  • Patent number: 9149460
    Abstract: The present invention relates to coated particles and pharmaceutical dosage forms comprising the active substances sensitive to environmental influences. The coating of the present invention provides stability and protection of the active substance to environmental influences and in particular from oxidation and/or environmental humidity by coating.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: October 6, 2015
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Vlasta Humar, Mateja Burjak, Rok Grahek, Mateja Salobir, Janez Kerc, Klemen Kocevar
  • Patent number: 9089486
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of: a) providing a composition comprising ezetimibe, b) sieving a composition comprising a composition of step (a), c) shear mixing of the composition after step (b), preferably the mixing of the composition is carried out by high shear mixing, d) formulation into a dosage form. The present invention also relates to dosage forms containing ezetimibe and ezetimibe and simvastatin, which have been prepared according to the process according to the invention.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: July 28, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Janez Kerc, Miha Homar, Polona Jurkovic
  • Patent number: 9085538
    Abstract: The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: July 21, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Damjan Sterk, Marko Jukic
  • Publication number: 20150191475
    Abstract: The present invention relates to amorphous adducts of ticagrelor with divalent metal salts useful in the treatment or prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease.
    Type: Application
    Filed: July 3, 2013
    Publication date: July 9, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventor: Borut Zupancic
  • Patent number: 9067895
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: June 30, 2015
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Samo Andrensek, Jolanda Anzel, Marjeta Hocevar, Zdenko Casar
  • Publication number: 20150148533
    Abstract: The present invention relates to a process for preparing ?-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-?]pyrazin-7-yl compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 28, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Stefan Starcevic, Peter Mrak, Gregor Kopitar
  • Patent number: 8980585
    Abstract: Genetically modified strains of Streptomyces tsukubaensis (S. tsukubaensis) can be used for an improved fermentation process for the preparation of tacrolimus or a salt or derivative thereof by cultivation of these genetically modified strains. Novel genes allowing biosynthesis of allylmalonyl-CoA can be used for polyketide production with allylmalonyl extender unit.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: March 17, 2015
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Hrvoje Petkovic, Enej Kuscer, Stefan Fujs, Gregor Kopitar, Peter Mrak, Gregor Kosec
  • Publication number: 20150005498
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of Ticagrelor (TCG).
    Type: Application
    Filed: September 14, 2012
    Publication date: January 1, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nened Maras, Borut Zupancic
  • Publication number: 20140371449
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 18, 2014
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
  • Patent number: 8889873
    Abstract: The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: November 18, 2014
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Barbara Mohar, Renata Toplak Casar
  • Publication number: 20140288281
    Abstract: The present invention relates to a medium for the cultivation of eukaryotic cells, the medium comprising as (an) additive(s) DMSO, N-acetylmannosamine (NAcMan), N-acetylglucosamine (NAcGlc), or any combination of two or more of these additives, including the combination of NAcMan and NAcGlc.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 25, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventor: Tanja FICKO TRCEK
  • Publication number: 20140256747
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Publication number: 20140255989
    Abstract: The present invention relates to a medium for the cultivation of eukaryotic cells, the medium comprising as (an) additive(s) DMSO, N-acetylmannosamine (NAcMan), N-acetylglucosamine (NAcGlc), or any combination of two or more of these additives, including the combination of NAcMan and NAcGlc.
    Type: Application
    Filed: April 2, 2014
    Publication date: September 11, 2014
    Applicant: LEK Pharmaceuticals D.D.
    Inventor: Tanja FICKO TRCEK
  • Publication number: 20140248351
    Abstract: The present invention relates to a granulate and a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and stabilizer, in particular to a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and sucrose, polyethylene glycol, cyclodextrin, and combinations thereof and to a process for its preparation. The granulate and the pharmaceutical composition are particularly useful as a medicament, especially for the treatment of urinary incontinence. The present invention relates to use of sucrose, polyethylene glycol, cyclodextrin, and combinations thereof for stabilizing fesoterodine or a salt or a solvate thereof in a pharmaceutical composition.
    Type: Application
    Filed: April 10, 2012
    Publication date: September 4, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Sara Cesar, Klemen Naversnik, Tijana Stanic-Ljubin
  • Publication number: 20140213810
    Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.
    Type: Application
    Filed: April 6, 2012
    Publication date: July 31, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Matej Sova, Zdenko Casar, Gaj Stavber
  • Patent number: 8785674
    Abstract: A process for preparing a compound of formula VI wherein R1 and R6 is hydrogen, substituted or unsubstituted alkyl substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; R5 is B(OR2)(OR3), or wherein R2 and R3 independently from each other represent substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; or R2 and R3 cooperatively form a part of a 5- to 10-membered fused or unfused ring, optionally a chiral 5- to 10-membered fused or unfused ring; X is selected from Cl, Br, I; and * indicates a chiral center; is described.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: July 22, 2014
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Ivana Gazic Smilovic, Zdenko Casar
  • Publication number: 20140187558
    Abstract: The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 3, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Gaj Stavber