Patents Assigned to LEK Pharmaceuticals d.d.
  • Publication number: 20160346207
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a solid pharmaceutical composition comprising androgen receptor antagonists, e.g. Enzalutamide or ARN-509, as well as to processes for preparing the same. The solid pharmaceutical compositions are useful in the treatment of prostate cancer.
    Type: Application
    Filed: February 4, 2015
    Publication date: December 1, 2016
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Rok Grahek, Andrija Lebar, Petra Draksler, Bostjan Petek, Jerneja Opara, Klemen Naversnik, Petra Bozic
  • Patent number: 9499857
    Abstract: The present invention relates to a method for selecting for cells or cell lines that produce a recombinant protein/polypeptide in high yields, the method allowing for the selection of high producer cells or cell lines in an early phase of cell line development, the method comprising the step of determining the nuclear DNA content of the cells or cell lines, wherein the level of the nuclear DNA content of the cells or cell lines positively correlates with the capacity of the cells or cell lines to produce the recombinant protein/polypeptide.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: November 22, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventor: Darja Obrstar
  • Patent number: 9493409
    Abstract: The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: November 15, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventor: Borut Zupancic
  • Patent number: 9469614
    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: Grant
    Filed: October 26, 2012
    Date of Patent: October 18, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Publication number: 20160289202
    Abstract: The present invention relates to 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate in crystalline form and to methods for the preparation thereof. In addition the present invention relates to solid pharmaceutical compositions for oral administration comprising an effective amount of the crystalline 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate. Moreover, the present invention relates to the use of crystalline 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate for the preparation of pharmaceutical compositions.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 6, 2016
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Andreas HOTTER, Robert ZIEGERT, Verena ADAMER, Arthur PICHLER
  • Patent number: 9453030
    Abstract: The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: September 27, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
  • Patent number: 9447188
    Abstract: The present invention relates to a method of controlling quality and quantity of posttranslational modification of a recombinantly produced polypeptide/protein (glycoprotein), wherein the posttranslational modification affects the glycosylation profile and/or the acidic variants profile, as manifested in CEX profiles, wherein the polypeptide/protein (glycoprotein) production is in eukaryotic host cells, the method comprising the following steps: a) cultivating the eukaryotic cells in a suitable medium under conditions which allow the expression of the polypeptide/protein, wherein the content of the dissolved CO2 (pCO2) in the medium is at a first value during the initial growth phase of the eukaryotic cells, allowing the eukaryotic cells to grow, and b) increasing or decreasing the content of the dissolved CO2 (pCO2) in the medium during the production phase of the eukaryotic cells to a second value.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: September 20, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Matja{hacek over (z)} Koncilja, Vatroslav Spudic, Sa{hacek over (s)}a Stojkovic, Matja{hacek over (z)} Tisu
  • Patent number: 9428562
    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: Grant
    Filed: April 2, 2014
    Date of Patent: August 30, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventor: Tanja Ficko Trcek
  • Patent number: 9388188
    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: Grant
    Filed: June 13, 2013
    Date of Patent: July 12, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Stefan Starcevic, Peter Mrak, Gregor Kopitar
  • Publication number: 20160194680
    Abstract: The present invention relates to a process for preparing chiral ?-aryl-?-aminobutyric acid compounds and derivatives thereof.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 7, 2016
    Applicant: Lek Pharmaceuticals D.D.
    Inventors: Stefan STARCEVIC, Peter MRAK, Gregor KOPITAR
  • Patent number: 9376397
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: June 28, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Janez Kosmrlj
  • Patent number: 9359617
    Abstract: The present invention describes new mammalian expression vectors comprising a novel combination of regulatory elements and one or more selection marker gene(s). The vector allows for incorporation of at least one, preferably two or more genes of interest, its/their subsequent expression, and for selection of transfected cells using, e.g., G418 and/or MTX. The pDGP?GOI vector as an example for a mammalian expression vector according to the present invention exhibits a 9555 bp sequence, one strand of which is represented by SEQ ID NO:2.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: June 7, 2016
    Assignee: LEK PHARMACEUTICALS D.D.
    Inventors: Andrej Francky, Dominik Gaser
  • Patent number: 9359385
    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: May 25, 2012
    Date of Patent: June 7, 2016
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Zdenko Casar, Gaj Stavber
  • Publication number: 20160145286
    Abstract: The present invention relates to non-stoichiometric crystalline hydrates of 1-(?-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene, processes for their preparation, and their use as medicaments. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel crystalline hydrates.
    Type: Application
    Filed: May 7, 2014
    Publication date: May 26, 2016
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Lovro Selic, Andreas Hotter, Christoph Langes, Ulrich Griesser
  • Publication number: 20160128946
    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: Application
    Filed: September 10, 2015
    Publication date: May 12, 2016
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Vlasta Humar, Mateja Burjak, Rok Grahek, Mateja Salobir, Janez Kerc, Klemen Kocevar
  • Patent number: 9315525
    Abstract: A process for producing bortezomib N-(pyrazin-2-yl)carbonyl-L-phenylalanine-L-leucine boronic acid) comprising the step of deprotecting the compound of formula XII: to yield bortezomib.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: April 19, 2016
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Ivana Gazic Smilovic, Zdenko Casar
  • Patent number: 9284320
    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: Grant
    Filed: July 3, 2013
    Date of Patent: March 15, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventor: Borut Zupancic
  • Patent number: 9278972
    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: Grant
    Filed: December 20, 2012
    Date of Patent: March 8, 2016
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
  • Publication number: 20160060215
    Abstract: The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
    Type: Application
    Filed: April 4, 2014
    Publication date: March 3, 2016
    Applicant: Lek Pharmaceuticals d.d.
    Inventor: Borut Zupancic
  • Patent number: 9221829
    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: Grant
    Filed: September 14, 2012
    Date of Patent: December 29, 2015
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Nened Maras, Borut Zupancic