Patents Assigned to LEK Pharmaceuticals d.d.
  • Patent number: 8604194
    Abstract: Novel pharmaceutically acceptable salts of desvenlafaxine with physiologically ubiquitous ions selected from sugar acids and vitamins, processes for their preparation, pharmaceutical compositions containing them and uses therefor are described.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: December 10, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Furlan Borut, Anton Copar
  • Publication number: 20130317100
    Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 28, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Frank Richter, Erwin Schreiner, Samo Pirc, Anton Copar
  • Patent number: 8592490
    Abstract: Self-microemulsifying drug delivery systems and microemulsions used to enhance the solubility of pharmaceutical ingredients comprising a polyoxyethylene sorbitan fatty acid ester emulsifier; a fatty acid ester co-emulsifier and an oil.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: November 26, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Igor Legen, Janez Kerc, Polona Jurkovic
  • Patent number: 8592474
    Abstract: The present invention relates to a process for the preparation and purification of olmesartan medoxomil hydrohalide salts and optionally converting them to olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.
    Type: Grant
    Filed: August 7, 2008
    Date of Patent: November 26, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Samo Pirc, Lovro Selic
  • Publication number: 20130302816
    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: Application
    Filed: November 9, 2011
    Publication date: November 14, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventor: Darja Obrstar
  • Patent number: 8580246
    Abstract: The present invention provides a new stable pharmaceutical composition of granulocyte-colony stimulating factor (G-CSF).
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: November 12, 2013
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Barbara Podobnik, Vladka Gaberc Porekar, Viktor Menart
  • Publication number: 20130259935
    Abstract: The present invention relates to the field of a pharmaceutical technology. More specifically, the present invention relates to a pharmaceutical composition comprising glimepiride and a surface active agent. Surface active agent obtainable by reacting castor oil or hydrogenated castor oil with ethylene oxide, preferably hydrogenated castor oil, substantially improves dissolution glimepiride active pharmaceutical ingredient and at the same time, when both formulated into a pharmaceutical composition, ensures satisfying or exceeding other parameters like for example stability, hardness, friability and handling of said pharmaceutical composition.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 3, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Miha Jaklic, Sebastjan Reven
  • Publication number: 20130202713
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for coating a particle comprising a pharmaceutically active ingredient (API) comprising the steps of providing a composition comprising carbonate ions, phosphate ions, or a mixture thereof, providing a particle comprising an API, and precipitating a carbonate salt, a phosphate salt or a mixture thereof onto said particles. The present invention is also directed to a particle comprising an API, wherein the particle is coated with a coating comprising a carbonate salt, phosphate salt, or mixture thereof, and to a pharmaceutical composition comprising said particles. Moreover, the present invention is also directed to the use of said particles for preparing a medicament.
    Type: Application
    Filed: December 20, 2010
    Publication date: August 8, 2013
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Marjan Bele, Miran Gaberscek, Janko Jamnik, Milena Zorko, Uros Maver, Klemen Kocevar
  • Publication number: 20130197082
    Abstract: A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.
    Type: Application
    Filed: March 8, 2011
    Publication date: August 1, 2013
    Applicant: Lek Pharmaceuticals D.D.
    Inventor: Damjan Sterk
  • Patent number: 8471045
    Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: June 25, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Zdenko Casar, Tomaz Mesar, Gregor Kopitar, Peter Mrak, Matej Oslaj
  • Patent number: 8445693
    Abstract: One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: May 21, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Zdenko Casar, Anton Copar, Jerome Cluzeau, Andrej Premrl
  • Publication number: 20130115301
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for coating a particle comprising a pharmaceutically active ingredient (API) comprising the steps of providing a composition comprising carbonate ions, phosphate ions, or a mixture thereof, providing a particle comprising an API, and precipitating a carbonate salt, a phosphate salt or a mixture thereof onto said particles. The present invention is also directed to a particle comprising an API, wherein the particle is coated with a coating comprising a carbonate salt, phosphate salt, or mixture thereof, and to a pharmaceutical composition comprising said particles.
    Type: Application
    Filed: December 20, 2010
    Publication date: May 9, 2013
    Applicants: LEK PHARMACEUTICALS D.D.
    Inventors: Marjan Bele, Miran Gaberscek, Uros Maver, Klemen Kocevar
  • Patent number: 8435938
    Abstract: The new pure vancomycin hydrochloride substantially free of impurities known in commercially available products is described. The term “substantially free of impurities” designates a purity of vancomycin hydrochloride between about 97% and about 99%, particularly between about 98% and about 99%, preferably about 99%, as determined by HPLC analytical method as directed in U.S.P., NF 27th revision, 22 (2004). The new pure vancomycin hydrochloride (vancomycin B hydrochloride) contains less than 0.7% of total impurities, namely, only one impurity exceeds 0.3%. The new process for the purification of crude vancomycin by displacement chromatography is described by which the desired pure antibiotic according to the present invention is produced, based on the finding that high purity of the vancomycin hydrochloride is obtained using low selected pH values of the mobile phase between 3.9 and 4.2.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: May 7, 2013
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Rok Grahek, Andrej Bastarda
  • Patent number: 8410285
    Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: April 2, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
  • Patent number: 8404870
    Abstract: The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.
    Type: Grant
    Filed: January 20, 2009
    Date of Patent: March 26, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Jerome Cluzeau, Zdenko Casar, Peter Mrak, Matej Oslaj, Gregor Kopitar
  • Publication number: 20130059002
    Abstract: The present invention relates to a pharmaceutical composition, preferably a pharmaceutical dosage form, comprising at least two separate compartments, wherein one compartment contains a composition comprising metformin or a pharmaceutically acceptable salt thereof and wherein another compartment contains a composition comprising sitagliptin. The present invention also relates to a process for preparing dosage forms comprising metformin or a pharmaceutically acceptable salt thereof and sitagliptin or a pharmaceutically acceptable salt thereof, the process comprising the steps of: a) providing one composition containing metformin or a pharmaceutically acceptable salt thereof and optionally also sitagliptin, b) providing a further composition containing sitagliptin or a pharmaceutically acceptable salt thereof and optionally also metformin, and c) combining the compositions to form compartments.
    Type: Application
    Filed: February 9, 2011
    Publication date: March 7, 2013
    Applicant: Lek Pharmaceuticals D.D.
    Inventors: Polona Smrdel, Tijana Stanic Ljubin, Luka Peternel, Uros Klancar
  • Patent number: 8389695
    Abstract: The invention relates to a modifying agent comprising a water soluble polymer, wherein the water soluble polymer comprises at least one reactive selenium group, said reactive selenium group being capable of reacting with a thiol group thereby forming an —Se—S— bond. Furthermore, the invention relates to a method for producing said modifying agents and their use in the modification of pharmaceutically active agents, e.g. G-CSF. Additionally, the invention concerns conjugates comprising a water-soluble polymer and a pharmaceutically active agent, wherein the water-soluble polymer is linked via a S—Se-bond to agent and a method for their production and their use as medicaments. Finally, the invention concerns a pharmaceutical composition comprising the inventive conjugates.
    Type: Grant
    Filed: February 13, 2009
    Date of Patent: March 5, 2013
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Menci Kunstelj, Gabriela Ambrozic, Vladka Gaberc Porekar, Veronika Verbic
  • Patent number: 8367848
    Abstract: Present invention refers to the process of preparing amorphous atorvastatin calcium without intermediate isolation of crystal or undefined mixture of crystal and amorphous atorvastatin calcium, respectively. Forming of calcium atorvastatin salt is carried out in a mixture of chlorinated organic solvent or cyclic hydrocarbon solvent, respectively, the non-hydroxylic organic solvent, and water, the source of calcium ions is calcium acetate or calcium chloride, respectively.
    Type: Grant
    Filed: April 9, 2004
    Date of Patent: February 5, 2013
    Assignee: LEK Pharmaceuticals D.D.
    Inventors: Ljubomir Antoncic, Gorazd Sorsak, Anton Copar
  • Patent number: 8362259
    Abstract: There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: January 29, 2013
    Assignee: Lek Pharmaceuticals, D.D.
    Inventor: Renata Toplak Casar
  • Publication number: 20130018065
    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-methyl-methanesulfonylamino)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: Application
    Filed: December 15, 2010
    Publication date: January 17, 2013
    Applicant: Lek Pharmaceuticals D.D.
    Inventors: Samo Andrensek, Jolanda Anzel, Marjeta Hocevar, Zdenko Casar