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.
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
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
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.
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.
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.
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
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: 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
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
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
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.
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
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
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
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.
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
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.
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