György
György Báthori, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100021927 | CHOLESTEROL LOADED INSECT CELL MEMBRANES AS TEST SYSTEMS FOR ABC TRANSPORTER PROTEINS - The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane. | 01-28-2010 |
György Báthori, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100021927 | CHOLESTEROL LOADED INSECT CELL MEMBRANES AS TEST SYSTEMS FOR ABC TRANSPORTER PROTEINS - The invention provides for a novel cholesterol loaded insect cell membrane preparation having an increased cholesterol level as compared to physiological cholesterol levels of insect cell membranes or to control insect cell membrane preparations without cholesterol loading, wherein said cholesterol loaded membrane preparation comprises an ABC transporter protein having an increased substrate transport activity due to increased cholesterol level of the membrane. The invention also relates to reagent kits comprising the preparations of the invention. The invention also relates to methods for manufacturing said preparations and methods for measuring any type of activity of the ABC transporters present in the cholesterol loaded membranes as well as studying or testing compounds and interaction of compounds and ABC transporters, in this assay systems. The invention also provides for a test system useful for testing whether ABC transporter proteins can be activated by cholesterol in an insect cell membrane. | 01-28-2010 |
György Clememtis, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090306117 | ROSUVASTATIN ZINC SALT - The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1). | 12-10-2009 |
György Clememtis, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090306117 | ROSUVASTATIN ZINC SALT - The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1). | 12-10-2009 |
György Clementis, Siofok HU
| Patent application number | Description | Published |
|---|---|---|
| 20130225695 | METHOD FOR PREPARATION OF AN EXCIPIENT SUITABLE FOR PHARMACEUTICAL USE - The present invention is related to a method for purifying diatomaceous earth wherein the natural colloidal structure of the material is retained, which comprises preparing a suspension of diatomaceous earth in a liquid wherein diatomaceous earth is insoluble, separating diatomaceous earth from the suspension, treating diatomaceous earth with an inorganic or organic acid, heat-treating the thus obtained product at a temperature not higher than 300° C., subjecting the product obtained to oxidative treatment and drying the purified product. | 08-29-2013 |
György Cselik, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20120157620 | AMINE-EPOXY ADDUCTS AND THEIR USE FOR PREPARING POLYUREA AND POLYUREA-POLYURETHANE COATINGS - The invention relates to amine-epoxy adducts with symmetrical and asymmetrical structures based on one hand on aliphatic, cycloaliphatic, araliphatic or aromatic mono-, di- and triamines, and on the other hand on aliphatic, cycloaliphatic and aromatic, mono-, di- or polyepoxy compounds, having an average molecular mass (M | 06-21-2012 |
György Dormán, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100267711 | METHOD OF ENHANCING CELLULAR PRODUCTION OF MOLECULAR CHAPERONE, HYDROXYLAMINE DERIVATIVES USEFUL FOR ENHANCING THE CHAPERONE PRODUCTION AND THE PREPARATION THEREOF - A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). | 10-21-2010 |
| 20130303572 | NOVEL INHIBITORS OF MATRIX METALLOPROTEINASES - Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: | 11-14-2013 |
György Dormán, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100267711 | METHOD OF ENHANCING CELLULAR PRODUCTION OF MOLECULAR CHAPERONE, HYDROXYLAMINE DERIVATIVES USEFUL FOR ENHANCING THE CHAPERONE PRODUCTION AND THE PREPARATION THEREOF - A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). | 10-21-2010 |
| 20130303572 | NOVEL INHIBITORS OF MATRIX METALLOPROTEINASES - Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: | 11-14-2013 |
György Haraszati, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20120261848 | METHOD TO CREATE REMOVABLE DENTAL PROSTHESIS, AND THE DENTAL PROSTHESIS MAKING THEREOF - The subject of the invention is a method to create removable dental prosthesis, and the dental prosthesis making thereof, which solution is suitable for quick and efficient production of removable dental prostheses. | 10-18-2012 |
György Juhász, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100296096 | IMAGING OPTICAL INSPECTION DEVICE WITH A PINHOLE CAMERA - The invention relates to an imaging optical inspection setup for inspecting a sample ( | 11-25-2010 |
| 20120324368 | Object transfer method using gesture-based computing device - A file transfer method is operative in a mobile computing device having a display interface that supports gesture-based control operations. The mobile computing device includes a remote access client. One or more other computers associated with the user each maintain connections to a Web-based remote access service. The user desires to copy and/or move resources between first and second of his or her connected computers. According to the file transfer method, after receipt of data indicating a first gesture requesting a copy or move operation with respect to the resource in the file system, an overview of one or more target devices is displayed. The overview is a folder level view of all folders and files located on the target devices, which are the one or more other computers also having a connection (or capable of having a connection) to the Web-based remote access service. In addition to displaying the folder-level view, an additional display element is shown. This display element is a representation of the resource from which the copy or move operation has been requested. The display element is displayed as an overlay, and it is adapted to be selectively positioned (by the user) in the overview using a gesture. Thereafter, and upon receipt of data indicating a second gesture that has caused the representation to be positioned over an available transfer location within a computer connected to the Web-based remote access service, the copy or move operation is completed. | 12-20-2012 |
György Juhász, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100296096 | IMAGING OPTICAL INSPECTION DEVICE WITH A PINHOLE CAMERA - The invention relates to an imaging optical inspection setup for inspecting a sample ( | 11-25-2010 |
| 20120324368 | Object transfer method using gesture-based computing device - A file transfer method is operative in a mobile computing device having a display interface that supports gesture-based control operations. The mobile computing device includes a remote access client. One or more other computers associated with the user each maintain connections to a Web-based remote access service. The user desires to copy and/or move resources between first and second of his or her connected computers. According to the file transfer method, after receipt of data indicating a first gesture requesting a copy or move operation with respect to the resource in the file system, an overview of one or more target devices is displayed. The overview is a folder level view of all folders and files located on the target devices, which are the one or more other computers also having a connection (or capable of having a connection) to the Web-based remote access service. In addition to displaying the folder-level view, an additional display element is shown. This display element is a representation of the resource from which the copy or move operation has been requested. The display element is displayed as an overlay, and it is adapted to be selectively positioned (by the user) in the overview using a gesture. Thereafter, and upon receipt of data indicating a second gesture that has caused the representation to be positioned over an available transfer location within a computer connected to the Web-based remote access service, the copy or move operation is completed. | 12-20-2012 |
György Kaptay, Miskolc HU
| Patent application number | Description | Published |
|---|---|---|
| 20110185855 | METHOD TO PRODUCE MONOTECTIC DISPERSED METALLIC ALLOYS - The invention relates to a method for producing monotectic alloys with finely dispersed and homogeneously distributed second phase particles from two or more starting metals or alloys, in which the two or more metals or alloys are melted together or separately and the two or more, practically immiscible liquid metallic alloys are mixed to disperse the alloy of lower volume ratio with the other alloy of higher volume ratio, then the system is cooled below the eutectic temperature. The characteristic feature of the method is that at least one of the starting alloys contains stabilizing solid particles. | 08-04-2011 |
György Kaszás, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100065202 | Procedure of Manufacturing a Neutron-Guiding Flat Surface - The subject of the invention is a procedure for manufacturing a neutron-guiding flat surface of low waviness in the course of which a thin plate coated by a material suitable for neutron reflection, advantageously of multilayered structure, is glued onto a significantly thicker carrier surface. The procedure is characterised by placing the thin neutron-reflecting plate onto a base surface of low flatness, typically of the order of magnitude of 10 | 03-18-2010 |
György Kaszás, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100065202 | Procedure of Manufacturing a Neutron-Guiding Flat Surface - The subject of the invention is a procedure for manufacturing a neutron-guiding flat surface of low waviness in the course of which a thin plate coated by a material suitable for neutron reflection, advantageously of multilayered structure, is glued onto a significantly thicker carrier surface. The procedure is characterised by placing the thin neutron-reflecting plate onto a base surface of low flatness, typically of the order of magnitude of 10 | 03-18-2010 |
György Kéri, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090298842 | Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor - Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier. | 12-03-2009 |
| 20110318409 | FRACTIONS OF WHEAT GERM FERMENT - The invention concerns wheat germ ferment, its biologically active fractions, the process for their production, the pharmaceutical preparations containing them and their uses. | 12-29-2011 |
| 20120258968 | 4-PHENYLAMINO-PYRIMIDINE DERIVATIVES HAVING PROTEIN KINASE INHIBITOR ACTIVITY - The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein | 10-11-2012 |
| 20120277231 | QUINOLINYLOXYPHENYLSULFONAMIDES - The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases. | 11-01-2012 |
György Kéri, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20080207677 | Napthyridine Compounds As Rock Inhibitors - The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis. | 08-28-2008 |
| 20080214583 | 7H-Pyrrolo[2,3-D]Pyrimidine Derivatives, As Well As Their Therapeutically Acceptable Salts, Pharmaceutical Preparations Containing Them And Process For Production The Active Agent - The invention relates to new 7H-pyrrolo[2,3-d]pyrimidine derivatives, as well as their therapeutically acceptable salts, pharmaceutical preparations containing them and process for producing the active agent. The pharmaceutical preparation is adventageously antiphlogistic and analgetic one, a preparation reducing neuropathic hyperalgesia and rheumatic arthritis, a preparation for hindering destruction of bones chondrus, being applicable for treatment of other diseases, which may be connected with other inflammatory processes e.g. asthma, eczema or psoriasis. | 09-04-2008 |
| 20090018149 | 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and methods for medical intervention against mycobacterial infections - Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases. | 01-15-2009 |
| 20090298842 | Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor - Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier. | 12-03-2009 |
| 20120164132 | Anticancer and immunomodulating molecules and fractions containing said molecules, and process for preparing said fractions and said molecules from fermented vegetal material, and their uses - Biologically active substances and fractions of wheat germ ferment/fermented wheat germ extract (FWGE), including formulation A250, the processes for their production, the pharmaceutical preparations containing them, and their uses. | 06-28-2012 |
| 20140057911 | NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS - Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents. | 02-27-2014 |
| 20140336191 | QUINOLINYLOXYPHENYLSULFONAMIDES - The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases. | 11-13-2014 |
György KeserÜ, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090312299 | Isolated Isomers of Norelgestromin and Methods of Making and Using the Same - The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions. | 12-17-2009 |
György KeserÜ, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090312299 | Isolated Isomers of Norelgestromin and Methods of Making and Using the Same - The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions. | 12-17-2009 |
György Krasznai, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090215757 | Process for Preparation of High-Purity Meloxicam and Meloxicam Potassium Salt - The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam. | 08-27-2009 |
| 20130281694 | METHOD FOR PREPARING ROSUVASTATIN SALTS - The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S,6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates. | 10-24-2013 |
| 20130338360 | METHOD FOR THE PREPARATION OF HIGH-PURITY PHARMACEUTICAL INTERMEDIATES - The present invention is related to intermediates useful in the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid and polymorphs of said intermediates, methods for preparation thereof and use thereof. | 12-19-2013 |
| 20140142303 | PROCESS FOR THE PREPARATION OF A RIVAROXABAN AND INTERMEDIATES FORMED IN SAID PROCESS - The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The process is characterized by the reactions according to claim | 05-22-2014 |
György Krasznai, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090215757 | Process for Preparation of High-Purity Meloxicam and Meloxicam Potassium Salt - The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam. | 08-27-2009 |
| 20120035162 | PROCESS FOR PREPARATION OF HIGH-PURITY MELOXICAM AND MELOXICAM POTASSIUM SALT - The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam. | 02-09-2012 |
György Levay, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100075975 | MEDICAMENT FOR THE ENHANCEMENT OF COGNITIVE FUNCTION AND NEUROPROTECTION - The invention relates the use of 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]isoxazole-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3-(2H) pyridazinone of the Formula (I) | 03-25-2010 |
György Lévay, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090306144 | PYRIDINE DERIVATIVES OF ALKYL OXINDOLES AS 5-HT7 RECEPTOR ACTIVE AGENTS - New 3,3-disubstituted indol-2-one derivatives of the general formula (I) | 12-10-2009 |
György Panyi, Debrecen HU
| Patent application number | Description | Published |
|---|---|---|
| 20110059064 | Vm23 and Vm24, two scorpion peptides that block human T-lymphocyte potassium channels (sub-type Kv1.3) w/High Selectivity and Decrease the in vivo DTH-responses in Rats - Potassium channels Kv1.3 are known to be implicated in immunological diseases and graft rejections. Disclosed are peptides capable of blocking with high affinity and specificity potassium channels Kv1.3, their pharmaceutical compositions, and methods for their use to block Kv1.3 potassium channels, to treat various immunological conditions and to diagnostic applications. Methods for their chemical synthesis and correct folding are also disclosed. Exemplary peptides correspond to protein components (Vm23 and Vm24) isolated from the venom of the Mexican scorpion | 03-10-2011 |
| 20150087603 | MODIFIED PEPTIDE TOXINS - The invention relates to toxin peptides capable of selectively inhibiting a Kv1.3 potassium channel protein. The toxin peptides of the invention are modified anuroctonus scorpion toxin peptides. | 03-26-2015 |
György Panyi, Debrecen HU
| Patent application number | Description | Published |
|---|---|---|
| 20110059064 | Vm23 and Vm24, two scorpion peptides that block human T-lymphocyte potassium channels (sub-type Kv1.3) w/High Selectivity and Decrease the in vivo DTH-responses in Rats - Potassium channels Kv1.3 are known to be implicated in immunological diseases and graft rejections. Disclosed are peptides capable of blocking with high affinity and specificity potassium channels Kv1.3, their pharmaceutical compositions, and methods for their use to block Kv1.3 potassium channels, to treat various immunological conditions and to diagnostic applications. Methods for their chemical synthesis and correct folding are also disclosed. Exemplary peptides correspond to protein components (Vm23 and Vm24) isolated from the venom of the Mexican scorpion | 03-10-2011 |
György Rabloczky, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100048627 | SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE PREVENTION OR TREATMENT OF DIABETES - The invention refers to a synergistic pharmaceutical combination which comprises (a) a first pharmaceutical composition containing an antidiabetic or anti-hyperlipidemic active agent and one or more conventional carrier(s), and (b) a second pharmaceutical composition containing a hydroximic acid derivative of the formula I and one or more conventional carrier(s). The pharmaceutical combination is suitable for the prevention or treatment of, among others, diabetes mellitus. | 02-25-2010 |
György Rabloczky, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100048627 | SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE PREVENTION OR TREATMENT OF DIABETES - The invention refers to a synergistic pharmaceutical combination which comprises (a) a first pharmaceutical composition containing an antidiabetic or anti-hyperlipidemic active agent and one or more conventional carrier(s), and (b) a second pharmaceutical composition containing a hydroximic acid derivative of the formula I and one or more conventional carrier(s). The pharmaceutical combination is suitable for the prevention or treatment of, among others, diabetes mellitus. | 02-25-2010 |
György Ruzsics, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20120330018 | PROCESS FOR PREPARING PHARMACEUTICAL COMPOUNDS AND INTERMEDIATE COMPOUNDS - The object of the present invention is a process for preparing the 2-acetoxy-5-(2-fluor-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]pyridine (prasugrel) of the formula (I). The process starts form crystalline 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI). Further objects of the present invention are two novel crystalline forms of 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI) and the use thereof for preparing the compound of the formula (V) and process preparing thereof. | 12-27-2012 |
| 20130030183 | PROCESS FOR PREPARING A PHARMACEUTICAL COMPOUND - The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents. | 01-31-2013 |
György Visky, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20100137622 | INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11beta-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-- DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS - The present invention relates to a process for the synthesis of the known 17-acetoxy-11-β-[4-(dimethyl amino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-ethandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process has the following steps: i) formation of an epoxide; ii) addition of hydrogen cyanide; iii) silylation of a hydroxyl group; iv) reaction with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of a hydroxyl group with trimethyl chlorosilane; vi) reaction with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of a hydroxyl group with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of a hydroxyl group with acetic anhydride in the presence of perchloric acid, and in given case, purification by chromatography. The invention also relates to new intermediates of the process. | 06-03-2010 |
György Visky, Budapest HU
| Patent application number | Description | Published |
|---|---|---|
| 20090187032 | INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17alpha-ACETOXY-11beta-[4-(N,N-DIMETHYL-AMINO)-PHENYL]-19-NORPREGNA-4,9-D- IENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS - The present invention relates to a new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process. | 07-23-2009 |
| 20100137622 | INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11beta-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-- DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS - The present invention relates to a process for the synthesis of the known 17-acetoxy-11-β-[4-(dimethyl amino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-ethandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process has the following steps: i) formation of an epoxide; ii) addition of hydrogen cyanide; iii) silylation of a hydroxyl group; iv) reaction with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of a hydroxyl group with trimethyl chlorosilane; vi) reaction with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of a hydroxyl group with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of a hydroxyl group with acetic anhydride in the presence of perchloric acid, and in given case, purification by chromatography. The invention also relates to new intermediates of the process. | 06-03-2010 |