| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 544297000 | Nitrogen attached directly at 2-position by nonionic bonding and sulfur bonded directly to the nitrogen | 48 |
| 20080207903 | Chemical Process - A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (A chemical formula should be inserted here—please see paper copy enclosed herewith) I via a Heck reaction is described. Intermediates useful in the process and processes for making said intermediates are also described. | 08-28-2008 |
| 20080221323 | Production of Rosuvastatin Calcium Salt - An improved process for the manufacture of (E)-7-[4-(4-flurophenyl)-6-isopropyl-2-[methyl(methylsulfony)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, Formula (1), which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described. | 09-11-2008 |
| 20080221324 | Novel Processes For The Preparation Of A 2H-Chromene - The present invention relates to novel processes for the preparation of the compound of formula I (Iclaprim), related to dihydrofolate reductase inhibitors | 09-11-2008 |
| 20080249306 | Method for the Production of Statins - The present invention relates to a process for the production of statins, which are known as HMG-CoA reductase inhibitors. A few of the intermediate compounds for use in the process in accordance with the invention are novel compounds and the invention also relates to these novel intermediate compounds. | 10-09-2008 |
| 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 |
| 20090069563 | Rosuvastatin intermediates and their preparation - Provided are processes and intermediates for preparation of rosuvastatin. | 03-12-2009 |
| 20090076271 | Process for preparing intermediates of HMG-CoA reductase inhibitors - The present invention relates to intermediates of rosuvastatin and processes for the production thereof. | 03-19-2009 |
| 20090209759 | AUTOMATED ITERATIVE DRUG DISCOVERY AND SYNTHESIS - The present invention relates to methods and systems for de novo iterative synthesis, an automated iterative drug discovery method and system providing for rapid identification and synthesis of novel compounds. | 08-20-2009 |
| 20090275752 | Novel Process for Statins and its Pharmaceutically Acceptable Salts Thereof - Novel process for statins and its pharmaceutically acceptable salts thereof represented by general formula (I). | 11-05-2009 |
| 20090299065 | PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS - A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt. | 12-03-2009 |
| 20090312547 | PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM FIELD OF THE INVENTION - The present invention relates to an improved process for preparing (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium of Formula (I). | 12-17-2009 |
| 20100010219 | METHOD FOR PRODUCING PYRROLIDINE COMPOUND - Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. | 01-14-2010 |
| 20100016590 | NILOTINIB INTERMEDIATES AND PREPARATION THEREOF - Intermediates of Nilotinib were prepared, including, for example, 3-(trifluoromethyl-5-(4-methyl-1H-imidazole-1-yl)-benzeneamine; 3-(4-(pyridin-3-yl)pyrimidin-2-ylamino) -4-methylbenzoyl halogen dihydrochloride; and N-(3-Bromo-5-trifluoromethylphenyl)-4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzamide. Nilotinib.3HCl and its crystalline forms are also described. | 01-21-2010 |
| 20100029940 | PROCESS FOR PREPARING ROSUVASTATIN CALCIUM - The present invention relates to an improved process for preparing (2E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-propenal of Formula I which is an intermediate useful in the preparation of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methyl-sulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoicacid] calcium salt of Formula II | 02-04-2010 |
| 20100056783 | Novel Process for the Preparation of Statins and their Pharmaceutically Acceptable Salts thereof - Novel process for the preparation of statins and their pharmaceutically acceptable salts thereof represented by the general formula-(1) through novel intermediate compounds of general formula-(4). | 03-04-2010 |
| 20100063281 | DIPHENYL AMINE DERIVATIVES HAVING LUMINESCENCE PROPERTY - The present invention relates to diphenyl amine derivatives having luminescent properties, and particularly to diphenyl amines substituted with various electron-donating or electron-withdrawing groups. The compounds of the present invention show blue or blue-green luminescence, and luminescence of the compounds herein can be achieved by UV or visible light, thus being useful as a fluorescent dye or fluorescent material for an organic electroluminescence device or display. | 03-11-2010 |
| 20100145046 | Substituted 3-hydroxy-delta-lactones from epoxides - Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-δ-lactones and β-lactones are disclosed. | 06-10-2010 |
| 20100174075 | USE OF NITRIC OXIDE-RELEASING STATINS IN THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION - The present invention relates to the use of nitric oxide-releasing statins of formula (I) for the treatment of pulmonary arterial hypertension. | 07-08-2010 |
| 20100197916 | DIASTEREOMERIC PURIFICATION OF ROSUVASTATIN - The invention relates to diastereomerically pure rosuvastatin and processes for preparing diastereomerically pure rosuvastatin and its intermediates. | 08-05-2010 |
| 20100228028 | PROCESSES FOR THE MANUFACTURE OF ROSUVASTATIN AND INTERMEDIATES - A process for the manufacture of a compound of formula (V), useful for making rosuvastatin, by a stereoselective aldol reaction is described. Novel intermediates and processes to make them are also described. | 09-09-2010 |
| 20100274014 | PROCESS FOR MANUFACTURING ROSUVASTATIN POTASSIUM AND CRYSTALLINE AND AMORPHOUS FORMS THEREOF - A process of manufacturing of Rosuvastatin Potassium of formula (I) | 10-28-2010 |
| 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 |
| 20110065920 | PROCESS FOR PREPARING PENTANOIC DIACID DERIVATIVES - The present invention relates to a process for preparing pentanoic diacid derivatives useful for preparing pyrimidine derivatives, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin. | 03-17-2011 |
| 20110124864 | PREPARATION METHOD OF ROSUVASTATIN CALCIUM AND ITS INTERMEDIATES - A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided. | 05-26-2011 |
| 20110137033 | PROCESS FOR PREPARING (4,6-DIMETHYLPYRIMIDIN-2-YL)PHENYLAMINE (PYRIMETHANIL) - A process for preparing (4,6-dimethylpyrimidin-2-yl)phenylamine (pyrimethanil) of the formula | 06-09-2011 |
| 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 |
| 20110178296 | Process for preparing pyrimidine propenaldehyde - The present invention relates to an improved process for preparing (2E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-propenal of formula (I), which is an useful intermediate in the preparation of Rosuvastatin. | 07-21-2011 |
| 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 |
| 20110269961 | PROCESS FOR SYNTHESIS OF PHENOXY DIAMINOPYRIMIDINE DERIVATIVES - A method for preparing a compound of formula k | 11-03-2011 |
| 20110295005 | PROCESS FOR PREPARING PYRIMIDINE DERIVATIVES - The present invention relates to a process for preparing pyrimidine derivatives of the formula V, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin. | 12-01-2011 |
| 20110301348 | Process for the Manufacture of the Calcium Salt of Rosuvastatin (E)-7-[4-(4-Fluorophenyl)-6-Isopropyl-2-[Methyl(Methylsulfonyl)Amino]-Pyr- imidin-5-yl](3R,5S)-3,5-Dihydroxyhept-6-Enoic Acid and Crystalline Intermediates Thereof - A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) | 12-08-2011 |
| 20110319617 | Rosuvastatin and Atorvastatin Derivatives - This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues. | 12-29-2011 |
| 20120004408 | Use of Rosuvastatin Lactols as Medicaments - This invention relates to the discovery of novel rosuvastatin analogues. More specifically, the invention relates to novel rosuvastatin analogues which have utility in treating conditions treatable by the inhibition of HMG-CoA reductase. | 01-05-2012 |
| 20120136151 | NOVEL METHOD FOR PREPARING ROSUVASTATIN, INTERMEDIATE COMPOUNDS USEFUL FOR PREPARING SAME, AND METHOD FOR PREPARING SAME - The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate. | 05-31-2012 |
| 20120323005 | Process For The Preparation Of Amide Intermediates And Their Use Thereof - The present invention relates to an improved process for the preparation of amide intermediates useful in the preparation of cholesterol reducing agents. | 12-20-2012 |
| 20130066074 | PROCESS FOR THE PREPARATION OF PROPENAL INTERMEDIATE AND DERIVATIVES THEREOF - The present invention provides an improved process for the preparation of (E)-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methyl methanesulfon-amide, which is a useful intermediate for the preparation of (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl methylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy hept-6-enoic acid, commonly known as Rosuvastatin. | 03-14-2013 |
| 20130096303 | PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF - The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R | 04-18-2013 |
| 20130150579 | NOVEL INTERMEDIATES FOR THE PREPARATION OF HMG-CoA REDUCTASE INHIBITORS - The present invention provides a process for preparing novel intermediates of Formula wherein, R | 06-13-2013 |
| 20130197224 | PREPARATION METHOD OF ROSUVASTATIN CALCIUM AND ITS INTERMEDIATES - A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided. | 08-01-2013 |
| 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 |
| 20130296561 | PROCESS FOR THE PREPARATION OF STATINS IN THE PRESENCE OF BASE - The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin. | 11-07-2013 |
| 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 |
| 20140107339 | SUBSTITUTED 3-HYDROXY-DELTA-LACTONES FROM EPOXIDES - Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-δ-lactones and β-lactones are disclosed. | 04-17-2014 |
| 20140316135 | Process and Intermediate Compounds Useful in the Preparation of Statins, Particularly Rosuvastatin - Provided are a compound of formula (5) and a process for its preparation | 10-23-2014 |
| 20140357864 | PROCESS FOR THE PREPARATION OF A STATIN PRECURSOR - The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament. | 12-04-2014 |
| 20160052864 | AMINE SALTS OF PITAVASTATIN AND ROSUVASTATIN - The present invention relates to unsaturated amine salts of HMG-CoA reductase inhibitors, to a method of producing said amine salts and to the use of said amine salts in the production of pharmaceutically acceptable salts of HMG-CoA reductase inhibitors. | 02-25-2016 |
| 20160075664 | AMINE SALTS OF PITAVASTATIN AND ROSUVASTATIN - The present invention relates to oxygen-comprising amine salts of HMG-CoA reductase inhibitors, to a method of producing said amine salts and to the use of said amine salts in the production of pharmaceutically acceptable salts of HMG-CoA reductase inhibitors. | 03-17-2016 |
| 20160185734 | METHOD FOR PRODUCING OPTICALLY ACTIVE 5-HYDROXY-3-KETOESTER - The object of the present invention is to provide a method for producing in high yield with high stereoselectivity an optically active 5-hydroxy-3-ketoester compound which is useful as an intermediate for a pharmaceutical. A novel method for producing an optically active 5-hydroxy-3-ketoester compound in which an asymmetric aldol reaction by use of 1,3-diene compound is carried out in the presence of an optically active binaphthol-titanium complex together with a substituted nitrogen-containing 5 or 6-membered aromatic heterocyclic compound to obtain an optically active 5-hydroxy-3-ketoester compound in high yield with high stereoselectivity; and a novel production intermediate having a crystalline form. | 06-30-2016 |
