LEK Pharmaceuticals D.D. Patent applications |
Patent application number | Title | Published |
20160128946 | Coated Particles And Pharmaceutical Dosage Forms - 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. | 05-12-2016 |
20160060215 | New Process For The Synthesis Of 1-(2-((2,4-Dimethylphenyl)Thio)Phenyl)Piperazine - 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. | 03-03-2016 |
20150191475 | Ticagrelor Adducts With Divalent Metal Salts - 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. | 07-09-2015 |
20150148533 | New Synthetic Route For The Preparation Of Beta-aminobutyryl Substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-alpha]Pyrazin-7-yl Compounds - The present invention relates to a process for preparing □-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-α]pyrazin-7-yl compounds. | 05-28-2015 |
20140371449 | Synthesis of Triazolopyrimidine Compounds - 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. | 12-18-2014 |
20140288281 | PRODUCTION OF GLYCOPROTEINS WITH LOW N-GLYCOLYLNEURAMINIC ACID (NEU5GC) CONTENT - 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. | 09-25-2014 |
20140256747 | Synthesis of Triazolopyrimidine Compounds - 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. | 09-11-2014 |
20140255989 | PRODUCTION OF GLYCOPROTEINS WITH LOW N-GLYCOLYLNEURAMINIC ACID (NEU5GC) CONTENT - 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. | 09-11-2014 |
20140248351 | PHARMACEUTICAL COMPOSITION COMPRISING FESOTERODINE - The present invention relates to a granulate and a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and stabilizer, in particular to a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and sucrose, polyethylene glycol, cyclodextrin, and combinations thereof and to a process for its preparation. The granulate and the pharmaceutical composition are particularly useful as a medicament, especially for the treatment of urinary incontinence. The present invention relates to use of sucrose, polyethylene glycol, cyclodextrin, and combinations thereof for stabilizing fesoterodine or a salt or a solvate thereof in a pharmaceutical composition. | 09-04-2014 |
20140213810 | PREPARATION OF SITAGLIPTIN INTERMEDIATES - 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. | 07-31-2014 |
20140187558 | PREPARATION OF SITAGLIPTIN INTERMEDIATES - 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. | 07-03-2014 |
20140135368 | SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF - 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. | 05-15-2014 |
20140134247 | PHARMACEUTICAL COMPOSITION - A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions. | 05-15-2014 |
20140087423 | Method for Controlling the Main Complex N-Glycan Structures and the Acidic Variants and Variability in Bioprocesses Producing Recombinant Proteins - 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 CO | 03-27-2014 |
20140051854 | PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF STATINS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - 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. | 02-20-2014 |
20140044783 | PHARMACEUTICAL COMPOSITION COMPRISING A THIAZOLIDINEDIONE - 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. | 02-13-2014 |
20130338131 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING A LOW SOLUBLE PHARMACEUTICALLY ACTIVE INGREDIENT - 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. | 12-19-2013 |
20130337485 | ENZYMATIC SYNTHESIS OF ACTIVE PHARMACEUTICAL INGREDIENT AND INTERMEDIATES THEREOF - 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. | 12-19-2013 |
20130317100 | PROCESS FOR THE PREPARATION OF 3-AROYL-5-AMINOBENZOFURAN DERIVATIVES - 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. | 11-28-2013 |
20130302816 | NUCLEAR DNA CONTENT OF CHO CELL LINES AS A SELECTION CRITERION IN SCREENING OF THE BEST RECOMBINANT PROTEIN PRODUCERS - 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. | 11-14-2013 |
20130259935 | PHARMACEUTICAL COMPOSITIONS COMPRISING GLIMEPIRIDE AND POLYETHYLENE GLYCOL CASTOR OIL - 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. | 10-03-2013 |
20130202713 | COATING OF PARTICLES COMPRISING A PHARMACEUTICALLY ACTIVE INGREDIENT WITH A CARBONATE SALT OR PHOSPHATE SALT - 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. | 08-08-2013 |
20130197082 | SHORT SYNTHESIS OF TOLTERODINE, INTERMEDIATES AND METABOLITES - 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. | 08-01-2013 |
20130115301 | COATING OF PARTICLES COMPRISING A PHARMACEUTICALLY ACTIVE INGREDIENT WITH A CARBONATE SALT OR PHOSPHATE SALT - 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. | 05-09-2013 |
20130059002 | PHARMACEUTICAL COMPOSITIONS COMPRISING A COMBINATION OF METFORMIN AND SITAGLIPTIN - 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. | 03-07-2013 |
20130018065 | PROCESSES FOR THE PREPARATION OF KEY INTERMEDIATE FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOFAANM Andrensek; SamoAACI LjubljanaAACO SIAAGP Andrensek; Samo Ljubljana SIAANM Anzel; JolandaAACI LjubljanaAACO SIAAGP Anzel; Jolanda Ljubljana SIAANM Hocevar; MarjetaAACI LjubljanaAACO SIAAGP Hocevar; Marjeta Ljubljana SIAANM Casar; ZdenkoAACI LjubljanaAACO SIAAGP Casar; Zdenko Ljubljana SI - 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. | 01-17-2013 |
20120295316 | PROCESS FOR PREPARATION OF TACROLIMUS - Genetically modified strains of | 11-22-2012 |
20120231993 | NEW SYNTHETIC ROUTE FOR THE PREPARATION OF ALPHA-AMINO BORONIC ACID DERIVATIVES via SUBSTITUTED ALK-1-YNES - The present invention relates in general to the field of organic chemistry and in particular to the preparation of α-amino boronic acid derivatives. | 09-13-2012 |
20120220794 | PROCESS FOR HYDROGENATION OF HALOGENOALKENES WITHOUT DEHALOGENATION - The present invention relates in general to the field of organic chemistry and in particular to the preparation of halogenoalkanes. | 08-30-2012 |
20120196333 | SYNTHESIS OF STATINS - 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. | 08-02-2012 |
20120149895 | PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS - The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin. | 06-14-2012 |
20120135976 | PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE - The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of:
| 05-31-2012 |
20120088774 | ACTIVE PHARMACEUTICAL INGREDIENT ADSORBED ON SOLID SUPPORT - The present invention belongs to the field of pharmaceutical industry and relates to dosage forms comprising active pharmaceutical ingredients (API) such as tadalafil, simvastatin, fenofibrate and lovastatin that are practically insoluble in water, adsorbed on a carrier. Furthermore it relates to an adsorbate comprising API being practically insoluble in water and to a process for the preparation of said adsorbate with non-polar solvent (s) such as chlorinated hydrocarbon, diisopropylethes and hexane. Furthermore the invention relates to a process for the preparation of the dosage form, as well as to the use of the adsorbate for the preparation of the dosage form. Moreover it relates to the dosage form for use in the treatment of erectile dysfunction, human immunodeficiency virus (HIV) infections and/or Acquired Immune Deficiency Syndrome (AIDS). | 04-12-2012 |
20120087953 | PHARMACEUTICAL COMPOSITIONS OF ACTIVE PHARMACEUTICAL INGREDIENT COMPRISING SULPHONYLUREA MOIETY WITH EXCELLENT DISSOLUTION PROPERTIES - The present invention provides a pharmaceutical composition comprising at least one active pharmaceutical ingredient comprising sulphonylurea moiety, wherein the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is intimately mixed with a basic agent. The weight ratio of the basic agent and the at least one active pharmaceutical ingredient comprising sulphonylurea moiety is from 2.5:1 to 50:1, preferably from 2.5:1 to 25:1, more preferably from 3.5:1 to 15:1, yet more preferably from 3.5:1 to 10:1. The pharmaceutical composition can be obtained by simply mixing active pharmaceutical ingredient comprising sulphonylurea moiety and the basic agent in the aforementioned weight ratio, optionally in the presence of the granulation liquid. Alternatively, the pharmaceutical composition can be obtained by at least partially or fully dissolving the compounds in the granulation liquid or solvent, and at least partly precipitating them. The invention provides improved dissolution properties of the active pharmaceutical ingredient comprising sulphonylurea moiety. | 04-12-2012 |
20120083526 | SYNTHESIS OF 1-(2,3-DIHYDROBENZOFURAN-4-YL)ETHANONE AS INTERMEDIATE IN THE PREPARATION OF RAMELTEON - The present invention relates in general to the field of organic chemistry and in particular to the preparation of 1-(2,3-dihydrobenzofuran-4-yl)ethanone, an intermediate in preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon. | 04-05-2012 |
20120077760 | NOVEL SALTS OF SITAGLIPTIN - The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them. | 03-29-2012 |
20120071673 | SYNTHESIS OF (S)-N-[2-(1,6,7,8-TETRAHYDRO-2H-INDENO-[5,4-B]FURAN-8-YL)ETHYL]PROPIONAMI- DE - 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. | 03-22-2012 |
20120027857 | CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING O-DESMETHYL-VENLAFAXINE - 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. | 02-02-2012 |
20120027854 | PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE AND SIMVASTATIN - 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. Finally, the present invention relates to a combination dosage form comprising a combination of simvastatin and ezetimibe present in two separate compartments of the dosage form. | 02-02-2012 |
20120022091 | KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - 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. | 01-26-2012 |
20110306090 | Mammalian Expression Vector - 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 pDGPΔGOI 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. | 12-15-2011 |
20110275690 | NEW CRYSTAL FORM OF SUNITINIB MALATE - A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described. | 11-10-2011 |
20110263666 | PROCESS FOR THE PREPARATION OR PURIFICATION OF OLMESARTAN MEDOXOMIL - 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. | 10-27-2011 |
20110262497 | NOVEL EZETIMIBE FORMULATIONS - 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. | 10-27-2011 |
20110224271 | PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL - The present invention relates to a process for the preparation and purification of trityl olmesartan medoxomil and olmesartan medoxomil. | 09-15-2011 |
20110184172 | PROCESS FOR THE PREPARATION OF METHYL ESTER OF ROSUVASTATIN - 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. | 07-28-2011 |
20110184058 | SYNTHESIS OF 6,7-DIHYDRO-1H-INDENO[5, 4-B] FURAN-8(2H)-ONE AS INTERMEDIATE IN THE PREPARATION OF REMELTEON - 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. | 07-28-2011 |
20110178295 | SYNTHESIS OF STATINS - 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. | 07-21-2011 |
20110166118 | NEW TRINEM ANTIBIOTICS AND INHIBITORS OF BETA-LACTAMASES - 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. | 07-07-2011 |
20110130378 | EZETIMIBE PROCESS AND COMPOSITION - 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. These measures, respectively alone and particularly in combination contribute to attain ezetimibe (EZT) free of critical impurities described herein, and thus to use exceptionally pure ezetimibe (EZT) to be formulated into a pharmaceutical composition together with a pharmaceutically acceptable carrier or excipient. | 06-02-2011 |
20110112160 | TABLET COMPRISING EPROSARTAN MESYLATE - 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. Further described is a set of samples of tablets, wherein each comprises eprosartan mesylate as an active ingredient, wherein the eprosartan mesylate shows a dissolution profile with a variability of dissolution from different tablet samples of the set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution. A tablet can be prepared by using a process, comprising providing eprosartan mesylate in only one primary form of being either anhydrous or dihydrate, optionally subjecting eprosartan mesylate to dry granulation process, and a direct compression while maintaining said only one primary form; or by process comprising mixing eprosartan mesylate in particulate form with excipients or additives, wherein the prepared whole dry formulation or granulation of eprosartan mesylate has a water activity of less than 0.62, preferably less than 0.60 and more preferably less than 0.50, respectively determined at room temperature, and subsequently tabletting. Suitable prophylactic and/or therapeutic uses are also described. | 05-12-2011 |
20110111042 | SELF-MICROEMULSIFYING SYSTEMS INCORPORATED INTO LIQUID CORE MICROCAPSULES - 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. | 05-12-2011 |
20110105539 | 2'-HALOBIPHENYL-4-YL INTERMEDIATES IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS - 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. Further described is use of in line analytics for monitoring the aforementioned reactions, process for preparing a pharmaceutical composition and/or dosage for, or use in preparing a medicament. | 05-05-2011 |
20110098329 | CATALYZED CARBONYLATION IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS - 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. | 04-28-2011 |
20110092420 | SELENIUM CONTAINING MODIFYING AGENTS AND CONJUGATES - 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. | 04-21-2011 |
20110068497 | PREPARATION OF NANOPARTICLES BY USING A VIBRATING NOZZLE DEVICE - A method for preparing nanoparticles is provided, which comprises the steps of dissolving a polymer and, optionally, at least one additional ingredient, in an organic solvent, passing the solution through a vibrating nozzle and dropping the solution through the electrical field into an aqueous solution, which is stirred, such that nanoparticles are formed by the rapid diffusion of the solvent. | 03-24-2011 |
20110046375 | ((2S,4R)-4,6-DIHYDROXYTETRAHYDRO-2H-PYRAN-2-YL)METHYL CARBOXYLATE AND PROCESS FOR THE PRODUCTION THEREOF - 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. | 02-24-2011 |
20110033534 | CONTROLLED RELEASE TAMSULOSIN HYDROCHLORIDE TABLETS AND A PROCESS OF MAKING THEM - The present invention relates to a controlled release preparation of tamsulosin hydrochloride comprising hydroxypropylcellulose and polyethylene oxide, and the process for making such pharmaceutical composition. | 02-10-2011 |
20110021631 | Method of preparing stabilized pharmaceutical compositions comprising active ingredients susceptible to conversion to alternate polymorph forms - A process is described for the preparation of a pharmaceutical comprising an active pharmaceutical ingredient capable of existing in multiple polymorphic forms, wherein the process comprises a step of preparation of a wet phase comprising the active pharmaceutical ingredient and microcrystalline cellulose and a liquid, wherein in the wet phase has a weight ratio of active pharmaceutical ingredient to microcrystalline cellulose above 1.0 or a weight ratio of active pharmaceutical ingredient to liquid above 1.0. | 01-27-2011 |
20110008439 | DULOXETIN COMPOSITION - The present invention relates to a stable pharmaceutical pellet composition comprising duloxetine or a pharmaceutically acceptable salt thereof and a method for making such composition. In particular, the composition comprises duloxetine hydrochloride and a separating layer comprising a water soluble inorganic salt. | 01-13-2011 |
20100331356 | SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS - 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. | 12-30-2010 |
20100305087 | ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY - A combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support, wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed. | 12-02-2010 |
20100297227 | PHARMACEUTICAL COMPOSITION COMPRISING AT LEAST ONE ACTIVE AGENT AND A BINDER, WHICH SWELLS IN AN ACIDIC MEDIA - 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. | 11-25-2010 |
20100234473 | PROCESS FOR PREPARATION OF 3-(2-HYDROXY-5-SUBSTITUTED PHENYL)-N-ALKYL-3-PHENYLPROPYLAMINES - A new process for preparation of 3-(2-hydroxy-5-substituted phenyl)-N,alkyl-3-phenylpropylamines from cinnamyl chloride via N-alky-3-phenylprop-2-en-1-amine has been developed. | 09-16-2010 |
20100219063 | OXIDATIVE DEGENERATION PRODUCTS OF ATORVASTATIN CALCIUM - 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. | 09-02-2010 |
20100183714 | GASTRORESISTANT PHARMACEUTICAL DOSAGE FORM COMPRISING N-(2-(2- PHTHALIMIDOETHOXY)-ACETYL)-L-ALANYL-D-GLUTAMIC ACID (LK-423) - The present invention relates to the pharmaceutical dosage forms which enable a controlled and/or a targeted delivery of an active substance to the selected regions of gastrointestinal tract of humans or animals. The pharmaceutical dosage forms preferably comprises the active substance N-(2(2-phthalimidoethoxy)-acetyl)-L-alanyl-D-glutamic acid (designated as LK 423). Methods of treatment of chronic inflammatory diseases of gastrointestinal tract of humans and/or animals by using the pharmaceutical dosage forms of the invention are disclosed. | 07-22-2010 |
20100172969 | HOT-MELT MICROPELLETS - The present invention provides a method of making solid micropellets of which at least 75% by weight have a diameter less than 500 μm comprising (i) melting one or more binders; and (ii) combining the one or more binders melted in step (i) with a pharmaceutically active ingredient to form solid micropellets. Solid micropellets obtainable by this method are also provided. The invention has particular utility for improving the solubility of poorly water-soluble pharmaceutically active ingredients. | 07-08-2010 |
20100087652 | S-Omeprazole Magnesium - The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1% by weight as determined by high performance liquid chromatography (HPLC). | 04-08-2010 |
20100076025 | PROCESS FOR SOLVENT REMOVAL FROM OMEPRAZOLE SALTS - The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole. | 03-25-2010 |
20100056605 | OXIDATIVE DEGRADATION PRODUCTS OF ATORVASTATIN CALCIUM - 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. | 03-04-2010 |
20100048509 | Pharmaceutical Composition Comprising Perindopril - The present invention provides a stable pharmaceutical composition comprising an inclusion complex of perindopril, a microcrystalline cellulose having a low moisture content and/or a silicified microcrystalline cellulose having a low moisture content, and optionally other pharmaceutically acceptable excipients. | 02-25-2010 |
20100034887 | Bursting Pellets - In the present invention, a new pharmaceutical formulation of bursting pellets comprising in the core a high dose of a low potency active substance which is poorly soluble in water is described. Release of the active substance from the core takes place within minutes. | 02-11-2010 |
20100021419 | Stable Pharmaceutical Composition Comprising Granulocyte-Colony Stimulating Factor - The present invention provides a new stable pharmaceutical composition of granulocyte-colony stimulating factor (G-CSF). | 01-28-2010 |
20100016614 | PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE - The present invention relates to a new process for the preparation of pure perindopril erbumine. The present invention also relates to a new process for the preparation of crystalline form D of perindopril erbumine. | 01-21-2010 |
20100016370 | PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE MAGNESIUM IN A STABLE FORM - 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. | 01-21-2010 |
20090318521 | Synthesis of 4-Bromomethyl-2'-Formylbiphenyl and 4-Bromomethyl-2'-Hydroxymethylbiphenyl and Its Use in Preparation of Giotensin II Antagonists - 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. | 12-24-2009 |
20090291136 | Multiple Unit Tablets - The present invention relates to multiple unit tablets comprising multiple units compacted together with at least two tablet filler-binders and optionally other pharmaceutically acceptable excipients, wherein at least one of said tablet filler-binder is a tablet filler-binder having mean particle size-to-mean multiple unit size ratio from 10% to 40%, and at least one of said tablet filler-binder is a tablet filler-binder having mean particle size-to-mean multiple unit size ratio from 1% to 10%. | 11-26-2009 |
20090264497 | STABLE PHARMACEUTICAL FORMULATION COMPRISING A HMG-COA REDUCTASE INHIBITOR - Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to | 10-22-2009 |
20090238871 | PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising an ester of 4-(1-hydroxy-1-methylethyl)-2 propyl-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid characterized in that when exposed to 75% relative humidity at 40° in open dish for one month the total amount of related substances does not increase more than 1% is described. | 09-24-2009 |
20090234139 | Novel Process - A novel process for the preparation of 1′-hydroxy-2′-substituted cyclohexyl azetidin-2-one compound of formula 2, which is important intermediate in the synthesis of trinems, is described by epoxide ring opening of (3S,4R)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-4-[(1′R,2′S,3′R)-1′,2′-epoxycyclohexan-3′-yl]azetidin-2-one of formula 1 with the nucleophile compound of formula RYH, where nucleophile may act as solvent itself if the nucleophile is in the liquid form, in a suitable solvent and in the presence of a suitable catalyst from the group of salt of trifluoromethane sulfonic acid, preferably ytterbium (III) trifluoromethanesulfonate, stannous (II) trifluoromethanesulfonate or dysprosium (III) trifluoromethanesulfonate, under a) ultrasonic irradiation or b) under microwave irradiation of the reaction mixture following by isolation and purification of the desired compound. A variant of the novel process describes ring epoxide opening of the starting compound of formula 1 with the compound of formula NH | 09-17-2009 |
20090221646 | CRYSTALLINE SOLVATE OF OMEPRAZOLE SODIUM - The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent. | 09-03-2009 |
20090214642 | COATED FORMULATIONS FOR TOLTERODINE - 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. | 08-27-2009 |
20090208573 | NOVEL POLYMORPH FORM OF IRBESARTAN - New form of irbesartan having favourable chargeability is prepared from the alcoholic/etheric or ketonic solution of irbesartan after slow cooling with sporadic or light agitation and alternatively new crystalline form of an acid addition salt of irbesartan is prepared from the aqueous solution of a sodium salt of irbesartan after strongly acidifying aforesaid solution and subsequently adjusting pH with an alkali. Those are used in manufacturing a pharmaceutical composition. | 08-20-2009 |
20090202636 | Pharmaceutical Composition - A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions. | 08-13-2009 |
20090176849 | Process for the preparation of 2-alkyl-1-((2'-substituted-biphenyl-4-yl) Methyl)-imidazole, dihydroimidazole or benzimidazloe derivatives - The invention relates to a new process for the preparation of sartans 2-butyl-3-[[2′-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1′-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one is disclosed, which proceeds via novel intermediate, 4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]phenylboronic acid (Formula (II)) or its analogs. Compound (II) reacts with 5-(2-bromophenyl)-1-(triphenylmethyl)-1H-tetrazole (III) in the presence of catalyst, using conditions of Suzuki reaction, to give trityl irbesartan (I), whereas analogs to compound (II) may give candesartan, valsartan, telmisartan, losartan and olmesartan. | 07-09-2009 |
20090111839 | Process for Preparing Amorphous Rosuvastatin Calcium of Impurities - A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C | 04-30-2009 |
20090093499 | Pharmaceutical composition - A chemically stable formulation of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R, 5S)-3,5-dihydroxyhept-6-enoic acid or a pharmaceutically-acceptable salt thereof for oral use, such as tablets, capsules, powders, granules has been developed using the substances which stabilize against formation of degradation products: lactone and oxidation product. | 04-09-2009 |
20090012140 | Preparation of Telmisartan Salts with Improved Solubility - New alkali and earth-alkali salts of telmisartan in amorphous form and a new crystalline sodium salt of telmisartan have been prepared by preparing a solution despite low solubility of telmisartan and rapidly vacuum evaporating to dryness. | 01-08-2009 |
20080306135 | Process for the Preparation of Crystalline Perindopril - The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof. | 12-11-2008 |
20080300406 | Process for the Synthesis of Hmg-Coa Reductase Inhibitors - A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis. | 12-04-2008 |
20080299193 | Pharmaceutical composition comprising eszoplicone - The present invention relates to a stable pharmaceutical composition of eszopiclone with a defined particle size. | 12-04-2008 |
20080293924 | Process For the Isolation and/or Purification of Proteins - The invention relates to the process for the isolation and/or purification of biologically active proteins, preferably TNF-alpha or TNF-alpha analogues. The process of the present invention results in the production of high yields of proteins, preferably TNF-alpha or TNF alpha analogues with a purity of greater than 98%. The described process is particularly suitable for the industrial production of proteins, preferably TNF-alpha or TNF-alpha analogues. | 11-27-2008 |
20080255170 | Process for the Synthesis of Rosuvastatin Calcium - Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain. | 10-16-2008 |
20080214637 | Process for the Synthesis of Tetrazoles - A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent. | 09-04-2008 |