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.
Abstract: The present invention relates to process to prepare ?-aminobutyryl compounds having ?-amino acid core structural moieties and optionally having ?-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.
Type:
Grant
Filed:
June 3, 2011
Date of Patent:
July 1, 2014
Assignee:
Lek Pharmaceuticals D.D.
Inventors:
Damjan Sterk, Matjaz Ustar, Marko Zlicar
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:
Grant
Filed:
February 9, 2011
Date of Patent:
June 24, 2014
Assignee:
Lek Pharmaceuticals D.D.
Inventors:
Polona Smrdel, Tijana Stanic Ljubin, Luka Peternel, Uros Klancar
Abstract: The invention relates to a pharmaceutical composition, which comprises at least one active agent and which further comprises a binder and/or a retarding agent, wherein the binder swells in an acidic medium, and the retarding agent retards the release of the active agent in an acidic or alkaline medium.
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.
Abstract: A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions.
Type:
Application
Filed:
January 17, 2014
Publication date:
May 15, 2014
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Adnan Beso, Igor Legen, Sebastjan Reven
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.
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.
Abstract: A process for the preparation of amorphous atorvastatin calcium. The process includes providing a reaction mixture having a pH between 6.5 and 8.0 containing a sodium salt of atorvastatin and tetrahydrofuran. A non-cyclic chlorinated organic solvent selected from the group consisting of dichloromethane, trichloroethane, tetrachloroethane and chloroform or addition of cyclic hydrocarbon solvent selected from the group consisting of cyclohexane, cyclopentane and methyl cyclohexane is added to provide a mixture of organic solvents. An equivalent or an excess quantity of a source of calcium ions selected from the group consisting of calcium acetate and calcium chloride is added. Amorphous atorvastatin calcium is isolated from an organic phase comprising the mixture of organic solvents.
Type:
Grant
Filed:
March 4, 2009
Date of Patent:
April 15, 2014
Assignee:
LEK Pharmaceutical D.D.
Inventors:
Ljubomir Antoncic, Gorazd Sorsak, Anton Copar
Abstract: Pharmaceutically acceptable salts of sunitinib, processes of making sunitinib salts, as well as related pharmaceuticals and methods of treating are described.
Abstract: A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions.
Type:
Grant
Filed:
June 14, 2007
Date of Patent:
April 1, 2014
Assignee:
Lek Pharmaceuticals D.D.
Inventors:
Adnan Beso, Igor Legen, Sebastjan Reven
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:
Application
Filed:
April 12, 2012
Publication date:
March 27, 2014
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Matjaz Koncilja, Vatroslav Spudic, Sasa Stojkovic, Matjaz Tisu
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:
Application
Filed:
July 25, 2011
Publication date:
February 20, 2014
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Zdenko Casar, Damjan Sterk, Marko Jukic
Abstract: A pharmaceutical composition comprises a combination of thiazolidinedione or a pharmaceutically acceptable salt thereof as a first pharmaceutically active ingredient and a second pharmaceutically active ingredient different from thiazolidinedione, wherein the amount of said second pharmaceutically ingredient is larger than that of the first pharmaceutically active ingredient, and wherein the combination of said first and second pharmaceutically active ingredients are provided by a first granulate comprising the first and second pharmaceutically active ingredients and optionally at least one excipient, said first granulate being present in a second granulate comprising a further pharmaceutical excipient.
Type:
Application
Filed:
October 7, 2011
Publication date:
February 13, 2014
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Tijana Stanic Ljubin, Rok Staric, Simon Skubin
Abstract: A sustained release pharmaceutical composition comprising coating comprising at least one water-insoluble permeable polymer and at least one water soluble polymer and homogenous cores containing only tolterodine or a salt thereof and microcrystalline cellulose is described.
Abstract: A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallization of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.
Abstract: The present invention discloses a process for preparing an active pharmaceutical ingredient (API) or intermediates thereof, notably particular step in the synthesis of an intermediate useful for example in the preparation of statins, by using an enzyme capable of catalyzing oxidation or dehydrogenation. The invention further provides an expression system effectively translating said enzyme. In addition, the invention relates to a specific use of such enzyme for preparing API or intermediate thereof, and in particular for preparing statin or intermediate thereof.
Type:
Application
Filed:
December 20, 2011
Publication date:
December 19, 2013
Applicant:
LEK PHARMACEUTICALS D.D
Inventors:
Peter Mrak, Tadeja Zohar, Matej Oslaj, Gregor Kopitar
Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing a pharmaceutical composition comprising a pharmaceutically active ingredient (API) that is poorly soluble in water, a pharmaceutical composition obtained according to said process, to a dosage form comprising said pharmaceutical composition and to the use of said dosage forms for the treatment of hypercholesterolemia.
Type:
Application
Filed:
December 21, 2011
Publication date:
December 19, 2013
Applicant:
LEK PHARMACEUTICALS D.D.
Inventors:
Rok Staric, Simon Skubin, Miha Homar, Bostjan Markun, Sandra Berglez, Petra Kralj, Marija Boskovic