Patents Assigned to LEK Pharmaceuticals d.d.
  • SYNTHESIS OF (S)-N-[2-(1,6,7,8-TETRAHYDRO-2H-INDENO-[5,4-B]FURAN-8-YL)ETHYL]PROPIONAMIDE
    Publication number: 20120071673
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon, and analogues thereof.
    Type: Application
    Filed: February 11, 2010
    Publication date: March 22, 2012
    Applicant: LEK Pharmaceuticals D.D.
    Inventor: Jerome Cluzeau
  • PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE AND SIMVASTATIN
    Publication number: 20120027854
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing simvastatin and ezetimibe, comprising the steps of providing a first composition containing simvastatin, providing a second composition containing ezetimibe, and forming a dosage form comprising at least two separate compartments, wherein one compartment is formed using either the first or the second composition and another compartment is formed using the other composition. The present invention also relates to a process for preparing dosage forms containing simvastatin and ezetimibe, wherein the process involves a direct compression step. Furthermore, the present invention belongs to a dosage form obtained by this process, comprising at least two separate compartments, wherein one compartment contains simvastatin and one compartment contains ezetimibe.
    Type: Application
    Filed: November 30, 2009
    Publication date: February 2, 2012
    Applicant: LEK Pharmaceuticals D.D.
    Inventors: Miha Homar, Mateja Burjak, Breda Husu-Kovacevic, Janez Kerc
  • CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING O-DESMETHYL-VENLAFAXINE
    Publication number: 20120027857
    Abstract: This invention relates to sustained release pharmaceutical compositions comprising O-desmethyl-venlafaxine, in particular to sustained pharmaceutical compositions comprising O-desmethyl-venlafaxine orotate and/or O-desmethyl-venlafaxine glucuronate.
    Type: Application
    Filed: November 26, 2009
    Publication date: February 2, 2012
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zrinka Abramovic, Zdenka Jerala-Strukelj, Igor Legen, Uros Klancar
  • KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
    Publication number: 20120022091
    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: Application
    Filed: February 1, 2010
    Publication date: January 26, 2012
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Janez Kosmrlj
  • Mammalian Expression Vector
    Publication number: 20110306090
    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: Application
    Filed: December 18, 2009
    Publication date: December 15, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Andrej Francky, Dominik Gaser
  • NEW CRYSTAL FORM OF SUNITINIB MALATE
    Publication number: 20110275690
    Abstract: A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described.
    Type: Application
    Filed: November 12, 2009
    Publication date: November 10, 2011
    Applicant: LEK Pharmaceuticals D.D.
    Inventor: Lovro Selic
  • Sirolimus formulation
    Patent number: 8053444
    Abstract: The present invention relates to a stable pharmaceutical composition that includes sirolimus. The pharmaceutical composition includes sirolimus in the amorphous form, a fatty acid ester, such as glyceryl behenate, and a pharmaceutically acceptable polymer wherein the fatty acid ester is present at a concentration of less than 10% w/w compared to the total weight of the composition.
    Type: Grant
    Filed: January 24, 2008
    Date of Patent: November 8, 2011
    Assignee: Lek Pharmaceuticals d.d.
    Inventors: Sebastjan Reven, Igor Legen, Zdenka Jerala-Strukelj
  • NOVEL EZETIMIBE FORMULATIONS
    Publication number: 20110262497
    Abstract: Formulations of ezetimibe are described, wherein attention is paid, alternatively or optionally in combination, to (i) the existence of ezetimibe in the form of primary particles, which when blended with a suitable hydrophilic excipient in particulate form are allowed adsorb on the surface of particles of the hydrophilic excipient; (ii) a selection of specific types of excipients; and/or (iii) a careful control of how the formulation of ezetimibe is obtained.
    Type: Application
    Filed: September 29, 2009
    Publication date: October 27, 2011
    Applicant: LEK Pharmaceuticals D.D.
    Inventors: Rade Injac, Sara Cesar
  • PROCESS FOR THE PREPARATION OR PURIFICATION OF OLMESARTAN MEDOXOMIL
    Publication number: 20110263666
    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: Application
    Filed: August 7, 2008
    Publication date: October 27, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Samo Pirc, Lovro Selic
  • Oxidative degradation products of atorvastatin calcium
    Patent number: 8044086
    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: July 15, 2005
    Date of Patent: October 25, 2011
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Rok Grahek, Darko Kocjan, Andrej Bastarda, Andrej Kocijan, Matjaz Kracun
  • PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL
    Publication number: 20110224271
    Abstract: The present invention relates to a process for the preparation and purification of trityl olmesartan medoxomil and olmesartan medoxomil.
    Type: Application
    Filed: August 7, 2008
    Publication date: September 15, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventor: Renata Toplak Casar
  • SYNTHESIS OF 6,7-DIHYDRO-1H-INDENO[5, 4-B] FURAN-8(2H)-ONE AS INTERMEDIATE IN THE PREPARATION OF REMELTEON
    Publication number: 20110184058
    Abstract: The present invention describes the preparation of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one, a key intermediate in preparation of ramelteon. The present invention also describes further preceding intermediate compounds useful for the synthesis of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one.
    Type: Application
    Filed: July 13, 2009
    Publication date: July 28, 2011
    Applicant: Lek Pharmaceuticals D.D.
    Inventor: Jerome Cluzeau
  • PROCESS FOR THE PREPARATION OF METHYL ESTER OF ROSUVASTATIN
    Publication number: 20110184172
    Abstract: Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.
    Type: Application
    Filed: August 1, 2008
    Publication date: July 28, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Andrej Bastarda, Rok Grahek, Martin Crnugelj
  • SYNTHESIS OF STATINS
    Publication number: 20110178295
    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: Application
    Filed: April 2, 2008
    Publication date: July 21, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Tomaz Mesar, Gregor Kopitar, Peter Mrak, Matej Oslaj
  • USE OF INHIBITOR OF BETA-LACTAMASES AND ITS COMBINATION WITH BETA-LACTAM ANTIBIOTICS
    Publication number: 20110172200
    Abstract: The present invention relates to a pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of Formula (I), compounds of Formula (I), the use of a therapeutically effective amount of one or more compounds of Formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.
    Type: Application
    Filed: January 28, 2009
    Publication date: July 14, 2011
    Applicant: LEK PHARMACEUTICALS D. D.
    Inventors: Andrej Prezelj, Uros Urleb, Gregr Vilfan
  • NEW TRINEM ANTIBIOTICS AND INHIBITORS OF BETA-LACTAMASES
    Publication number: 20110166118
    Abstract: The present invention relates to a compound of Formula (I) in particular compounds of formula (Ia), the use of a therapeutically effective amount of one or more compounds of formula (I) or (Ia) as a broad-spectrum antibiotic and the use of a pharmaceutical composition comprising said compounds for the treatment of bacterial infections in humans or animals.
    Type: Application
    Filed: June 18, 2009
    Publication date: July 7, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Ivan Plantan, Andrej Prezelj, Uros Urleb, Barbara Mohar, Michel Stephan
  • Synthesis of 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl and its use in preparation of angiotensin II antagonists
    Patent number: 7968727
    Abstract: 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2?-cyanobiphenyl or 4?-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: June 28, 2011
    Assignee: Lek Pharmaceuticals, D.D.
    Inventors: Anton Copar, Ljubomir Antoncic, Matej Antoncic
  • EZETIMIBE PROCESS AND COMPOSITION
    Publication number: 20110130378
    Abstract: The present invention describes a process for producing ezetimibe (EZT) from a protected compound, including a step of deprotecting the 4-(p-hydroxyphenyl) protection group by catalytic hydrogenation, wherein the catalyst is used in an amount of 0.7 wt.-% or lower, relative to the weight of the compound used for the deprotection reaction. After carrying out a step of deprotection reaction, the process preferably comprises: (a) the reaction product is dissolved or extracted in ethyl acetate, and (b) the ethyl acetate solution is washed with an aqueous salt solution. The invention further describes a process for obtaining pure EZT, wherein raw EZT is dissolved in a solvent at a concentration of lower than 0.1 g/ml, and a crystallization step is carried out from this solution.
    Type: Application
    Filed: May 26, 2009
    Publication date: June 2, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventor: Lovro Selic
  • SELF-MICROEMULSIFYING SYSTEMS INCORPORATED INTO LIQUID CORE MICROCAPSULES
    Publication number: 20110111042
    Abstract: The invention provides a microcapsule having a shell and a liquid core incorporating a self-microemulsifying system or a microemulsion, wherein the core comprises a lipophilic substance, at least one surfactant, an active agent, a gelling agent and optionally a cosolvent. Furthermore, a method for producing such microcapsules and pharmaceutical formulations comprising such microcapsules is provided.
    Type: Application
    Filed: April 21, 2009
    Publication date: May 12, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Janez Kerc, Miha Homar, Mirjana Gasperlin
  • TABLET COMPRISING EPROSARTAN MESYLATE
    Publication number: 20110112160
    Abstract: A tablet comprising eprosartan mesylate in only one form of either anhydrous or dihydrate form is described. In another aspect, a tablet is disclosed comprising eprosartan mesylate obtainable by direct compression, wherein eprosartan mesylate is provided in one primary form of being either anhydrous or dihydrate to the extent that the eprosartan mesylate shows a dissolution profile with a variability of dissolution from the different tablet samples of a set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution, measured using USP apparatus 2, placing the tablets in 1000 ml 0.1 M hydrochloric acid at 37±0.5° C. with paddle speed of 50 rpm.
    Type: Application
    Filed: April 8, 2009
    Publication date: May 12, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Igor Legen, Zdenka Jerala-Strukelj, Rade Injac