| Medichem, S.A. Patent applications |
| Patent application number | Title | Published |
|---|
| 20120111098 | 2- ACETAMIDE - The invention relates to 2-{2-amino-3-[hydroxy(phenyl)methyl]phenyl}acetamide, a process for its preparation, and its use as a reference marker and reference standard for analyzing the purity of nepafenac. | 05-10-2012 |
| 20120004239 | Process for Preparing Quinoxaline Derivatives - The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof. | 01-05-2012 |
| 20110313200 | New Method for Obtaining an Aminoindan Mesylate Derivative - The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate five of any alkyl mesylates, including isopropyl mesylate. The invention further relates to processes for purifying rasagiline mesylate to obtain a product free of alkyl mesylates, and to the thus obtained rasagiline mesylate. | 12-22-2011 |
| 20110295037 | PROCESSES FOR PREPARING CINACALCET HYDROCHLORIDE AND POLYMORPHIC FORMS THEREOF - The invention relates to cinacalcet hydrochloride, new polymorphic crystalline forms of cinacalcet hydrochloride, amorphous cinacalcet hydrochloride and synthetic processes for their preparation. | 12-01-2011 |
| 20110189241 | Process For Controlling The Particle Size of A [3-(Trifluoromethyl)Phenyl]-1-Aminopropane Derivative - The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation. | 08-04-2011 |
| 20110159096 | 1-(1H-1,2,4-Triazol-1-YL)Butan-2-OL Derivative For Pharmaceutical Use, and The Use Of a 1-(1H-1,2,4-Triazol-1-YL)Butan-2-OL Derivative With Substantially Undefined Crystal Shape For Preparing Said 1-(1H-1,2,4-Triazol-1-YL)Butan-2-OL Derivative - The present invention relates to voriconazole, processes of preparing voriconazole, and pharmaceutical compositions and therapeutic uses thereof. In particular, the present invention also relates to voriconazole prepared from voriconazole having a substantially undefined shape and/or crystal habit. The invention further relates to voriconazole having a modified sphericity factor and/or specific surface area and/or Sauter diameter compared to voriconazole known from the prior art. | 06-30-2011 |
| 20110105788 | Polymorphic Form of an Aminoindan Mesylate Derivative - The invention relates to a polymorphic form of rasagiline mesylate, and to processes for preparing the same. | 05-05-2011 |
| 20110105750 | Salts of a Pyrazino[2,3-h][3]Benzazepine Derivative - This invention provides novel dicarboxylic acid salt forms of varenicline, wherein the acid is selected from maleic acid, fumaric acid, adipic acid, galactaric acid and malic acid. This invention provides also a carboxylic acid salt form of varenicline, wherein the acid is S-2-pyrrolidinon-5-carboxylic acid. This invention also provides methods for making these salt forms. | 05-05-2011 |
| 20110092738 | PROCESS FOR PREPARING 3,3-DIARYLPROPYLAMINES - Described is a process of preparing a pure solid or crystalline racemic 3,3-diarylpropylamine compound and the compounds formed thereof. The solid and crystalline forms of racemic 3,3-diarylpropylamine compound are especially suitable for producing highly pure 3,3-diarylpropylamine salts such as tolterodine tartrate. Also described are the highly pure solid or crystalline forms of racemic tolterodine, racemic tolterodine salt and tolterodine tartrate. | 04-21-2011 |
| 20110034731 | Solid Forms Of An N-(Phenylmethyl)Propanamide Derivative And Processes Of Preparation - The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide. | 02-10-2011 |
| 20100305359 | Processes For Preparing A Substituted Gamma-Amino Acid - The present invention is related to processes suitable for industrial synthesis of pregabalin from (R)-(−)-3-(carbamoylmethyl)-5-methylhexanoic using sodium hypochlorite as described herein. In addition, the present invention is related to pregabalin which is substantially free of impurities and pharmaceutical compositions comprising pregabalin. | 12-02-2010 |
| 20100286410 | Polymorphic Forms Of A 3-Pyrrole Substituted 2-Indolinone - The invention relates to new crystalline polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (i.e., sunitinib base), including Form I, Form II, and Form IV, processes for preparing crystalline polymorphic forms of sunitinib base, and pharmaceutically acceptable salts of new crystalline polymorphic forms of sunitinib base and pharmaceutical compositions comprising new crystalline polymorphic forms of sunitinib base, salts of new crystalline polymorphic forms of sunitinib base and mixtures thereof. | 11-11-2010 |
| 20100267988 | PROCESSES FOR PREPARING INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION OF CINACALCET - The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates. | 10-21-2010 |
| 20100234469 | New Crystals Of A Benzoylbenzeneacetamide Derivative - The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations. | 09-16-2010 |
| 20100168414 | PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF - The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe. | 07-01-2010 |
| 20100137619 | CRYSTALLINE POLYMORPHIC FORMS OF OLOPATADINE HYDROCHLORIDE AND PROCESSES FOR THEIR PREPARATION - The invention relates to new polymorphic forms of olopatadine hydrochloride, designated herein as olopatadine hydrochloride Forms A and B, and methods of preparing, purifying and treating them. | 06-03-2010 |
| 20100121108 | PROCESS FOR SYNTHESIZING DESVENLAFAXINE FREE BASE AND SALTS OR SOLVATES THEREOF - The invention relates generally to an improved process for manufacturing desvenlafaxine free base and salts or solvates thereof. | 05-13-2010 |
| 20100069637 | CRYSTALLINE SALT FORMS OF A 5,6,7,8-TETRAHYDRO-1,2,4-TRIAZOLO[4,3-a]PYRAZINE DERIVATIVE - This invention provides novel crystalline acid salt forms of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, i.e. sitagliptin, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same. | 03-18-2010 |
| 20100056784 | PROCESS FOR THE PREPARATION OF VORICONAZOLE - The present invention relates to an improved process for the preparation of Voriconazole. | 03-04-2010 |
| 20090318697 | PROCESS FOR PREPARING A PIPERAZINE DERIVATIVE - Disclosed is a process for preparing purified ranolazine of formula (I), which is indicated for the chronic treatment of angina, comprising reacting 1-[(2,6-dimethylphenyl)aminocarbonyl]piperazine with 1-phenoxy-2,3-epoxypropane in an inert solvent followed by precipitating the ranolazine. | 12-24-2009 |
| 20090318525 | Process For Preparing A 3-Pyrrole Substituted 2-Indolinone Malate Salt - The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib. | 12-24-2009 |
| 20090312575 | Process For Preparing A Benzoylbenzeneacetamide Derivative - Disclosed is a process for preparing anti-inflammatory compound nepafenac comprising preparing a compound of formula (V) wherein a N-halosuccinimide is used as the halogenating agent, followed by desulfurization using Raney Nickel. Also disclosed is a polymorphic form B of 2-amino-3-benzoyl-α-(methylthio)-benzeneacetamide (i.e., a compound of formula (V) wherein R is methyl | 12-17-2009 |
| 20090306406 | METHOD FOR PREPARING 1,3-DISUBSTITUTED PYRROLIDINE COMPOUNDS - A process for preparing substituted pyrrolidine compounds, including (5)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst. | 12-10-2009 |
| 20090275780 | PROCESS FOR CONTROLLING THE PARTICLE SIZE OF A 3-(TRIFLUOROMETHYL)PHENYL]-1-AMINOPROPANE DERIVATIVE - The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation. | 11-05-2009 |
| 20090247542 | SYNTHESES AND PREPARATIONS OF POLYMORPHS OF CRYSTALLINE ARIPIPRAZOLE - The invention relates to polymorphic crystalline forms of aripiprazole, synthetic processes for their preparation and pharmaceutical compositions containing the same. These crystalline forms of aripiprazole can be readily milled and can be easily combined with various pharmaceutical adjuvants without effecting changes to their crystalline structure when, for example, pressed into tablet or capsule form. | 10-01-2009 |
| 20090093645 | SYNTHESIS AND PREPARATIONS OF DULOXETINE SALTS - The invention relates to an improved process for the preparation of duloxetine hydrochloride. | 04-09-2009 |
| 20090076281 | PROCESS FOR THE PREPARATION OF LOSARTAN AND ITS SALTS - The invention relates to the preparation of losartan and losartan potassium. More particularly, the invention relates to the preparation of losartan and losartan potassium in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans. | 03-19-2009 |
| 20090076262 | PROCESS FOR PREPARING QUETIAPINE AND QUETIAPINE FUMARATE - The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations. | 03-19-2009 |
| 20090023922 | PROCESS FOR PREPARING VORICONAZOLE, NEW POLYMORPHIC FORM OF INTERMEDIATE THEREOF, AND USES THEREOF - The present invention relates to an improved process for preparation of Voriconazole and Voriconazole (1R)-(−)-10-camphorsulfonate. | 01-22-2009 |
| 20090018346 | Amorphous Form Of Darifenacin Hydrobromide And Processes For The Preparation Thereof - The present invention relates to amorphous form darifenacin hydrobromide and processes therefor. In addition, the present invention relates to compositions comprising amorphous form darifenacin hydrobromide. | 01-15-2009 |
| 20080312455 | Method For Determining Enantiomeric Purity Of Darifenacin And Intermediates - The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): | 12-18-2008 |
| 20080306257 | Syntheses and Preparations of Narwedine and Related Novel Compounds - The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved) to yield (−)-narwedine and which is the biogenic precursor of (−)-galanthamine) and the use thereof as a starting material for producing (−)-galanthamine. The invention further includes processes for preparing (−)-galanthamine and (−)-galanthamine hydrobromide, as well as related novel compounds. | 12-11-2008 |
| 20080262089 | Process for the Preparation of Tamsulosin - The invention includes an improved process for producing tamsulosin comprising reacting 5-(2-aminopropyl)-2-methoxybenzenesulfonamide with 2-(o-ethoxyphenoxy)ethyl bromide in an organic phosphite solvent to obtain tamsulosin. Optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide can be employed to produce optically pure (R)-tamsulosin product. The organic phosphite solvent utilized in the reaction can include tri-alkyl phosphites such as triethyl phosphite, trimethyl phosphite, and tributyl phosphite. Additionally, processes for producing tamsulosin having a low concentration of by-product contaminants, such as 5-((R)-2-{Bis-[2-(2-ethoxyphenoxy)ethyl]amino}-propyl)-2-methoxybenzenesulfonamide, and the use of such by-products to monitor the chemical purity of tamsulosin, are provided. | 10-23-2008 |
| 20080262043 | Solid Crystalline Form of Pantoprazole Free Acid, Salts Derived Therefrom and Process for Their Preparation - The invention relates, in general, to a new solid crystalline form of pantoprazole free acid (denominated “Form III”), salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and methods for producing the same. The invention further includes formulating pantoprazole free acid Form III, salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and/or in vivo cleavable prodrugs thereof (collectively “the compounds of the invention”) into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans. | 10-23-2008 |
| 20080242697 | Process for the synthesis of solifenacin - The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof. | 10-02-2008 |
| 20080214822 | Process For the Preparation of a Leukotriene Antagonist - The present invention relates to a novel process for the preparation of montelukast sodium, a compound of Formula (1b) and precursors thereof. The invention further concerns the free acid of this compound in crystalline form, obtainable for the first time by the new process. | 09-04-2008 |
| 20080207896 | Process For the Manufacture of Mirtazapine - Improved process for manufacturing mirtazapine. A process is described for preparing mirtazapine starting from a compound of formula (II), which is subjected to a ring cyclization, obtaining mirtazapine for pharmaceutical use in crystalline and anhydrous form. | 08-28-2008 |
