Patent application number | Description | Published |
20090270633 | Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-triazol-1-yl)methyl] benzonitrile and 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile intermediate - The present invention relates to a process for the preparation of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile (letrozole), substantially free from its isomeric impurity. The preparation involves reaction of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile with 4-fluorobenzonitrile in the presence of an organic solvent and a silicon amine. The present invention also relates to a process for the preparation of 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile which involves: (a) the reaction of a 4-halomethyl benzonitrile with 1,2,4-triazole in the presence of cesium carbonate and an organic solvent to obtain a reaction mass comprising 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile of formula II; and (b) precipitation of 4-[1-(1,2,4-triazole-1-yl)methyl]benzonitrile (II) from the reaction mass using a suitable organic solvent. | 10-29-2009 |
20090325915 | Crystalline Levosalbutamol Sulphate and Polymorphic Forms Thereof - The invention provides three polymorphic forms of crystalline levosalbutamol sulphate designated herein as Forms I, II and III. | 12-31-2009 |
20090326028 | Process for the preparation of temozolomide and analogs - A process for the preparation of compounds of formula IA, where R═CH | 12-31-2009 |
20100016605 | Process - A one-pot process for the preparation of pantoprazole sodium by reacting 2-chloro methyl 3,4-dimethoxy pyridine hydrochloride with 2-mercapto-5-difluoromethoxy benzimidazole in an organic solvent system in presence of a phase transfer catalyst and further treating with aqueous sodium hypohalite solution comprising sodium hydroxide to obtain pantoprazole sodium in high yield and purity. The process for conversion of pantoprazole sodium to pantoprazole sodium sesquihydrate and also pantoprazole sodium monohydrate are also disclosed herein. | 01-21-2010 |
20100075999 | Process for the Preparation of Ethyl-N-(2,3-Dichloro-6-Nitrobenzyl)Glycine Hydrochloride - The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V): | 03-25-2010 |
20100094004 | Process for Preparation of Erlotinib and its Pharmaceutically Acceptable Salts - A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4˜halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. | 04-15-2010 |
20100099887 | Process for the Preparation of Pure Anastrozole - A process for the preparation of anastrozole which comprises: a) brominating 3,5-bis(2-cyanoprop-2-yl)toluene (II) in an organic solvent using a brominating agent to obtain 3,5-bis(2-cyanoprop-2-yl)benzylbromide (III); b) heating the reaction mass of step a) to the reflux temperature of the organic solvent for a period of time no longer than 3 hours; c) isolating and purifying the bromo intermediate (III) using an organic solvent; d) alkylating the bromo intermediate in the presence of a base, optionally a phase transfer catalyst, a 1,2,4-triazole and an organic solvent to obtain anastrozole; and e) isolating and purifying the anastrozole from an organic solvent. | 04-22-2010 |
20100113526 | Process for the Preparation of Esomeprazole Magnesium Dihydrate - A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole. | 05-06-2010 |
20100113790 | Process for Preparing Isomers of Carmoterol - A process for preparing a compound of formula (III) comprising condensing an oxiranyl compound of formula (I) with an amine of formula (II) or a salt thereof wherein: R | 05-06-2010 |
20100113804 | Process for Preparing Dorzolamide - There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxy sulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid. | 05-06-2010 |
20100137586 | Process for the Preparation of Gefitinib - There is provided a compound of formula (III), and a process for preparing a compound of formula (V) comprising converting a compound of formula (III) to the compound (V), wherein (X) is fluoro, chloro, bromo or iodo. There is also provided a process for preparing a compound of formula (XI) comprising converting a compound of formula (X) to the compound (XI). The compounds (V) and (XI) so prepared may be used in a process for preparing gefitinib. | 06-03-2010 |
20100152229 | Process for the Synthesis of Moxifloxacin Hydrochloride - A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II): | 06-17-2010 |
20100160643 | Process for Preparing Trityl Olmesartan Medoxomil and Olmesartan Medoxomil - A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, | 06-24-2010 |
20100190797 | CRYSTALLINE POLYMOPHIC FORMS OF ZOPICLONE, PROCESSES FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL COMPOSITIONS - Disclosed are processes for the preparation of crystalline polymorphic forms of zopiclone and their pharmaceutical compositions for use as a sedative. | 07-29-2010 |
20100204493 | Process for the Preparation of Escitalopram - The present invention provides a novel process for the preparation of a compound of Formula III, and novel processes for preparing escitalopram using the compound of Formula III. | 08-12-2010 |
20100222572 | PROCESSES FOR THE PREPARATION OF CICLESONIDE AND ITS CRYSTAL MODIFICATION - Improved processes for the synthesis of ciclesonide, chemically termed as [11β,16α(R)]-16,17-[(cyclohexylmethylene)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione and its crystal modification. | 09-02-2010 |
20100298565 | Processes for the Preparation of Paliperidone and Pharmaceutically Acceptable Salts Thereof and Intermediates for Use in the Processes - The present invention relates to novel compounds of formula (VIII) and (X), processes for their preparation and their use in the preparation of paliperidone or a salt thereof. There is also provided by the present invention novel processes for preparing intermediates for use in the preparation of paliperidone or a salt thereof, and novel processes for preparing paliperidone or a salt thereof. | 11-25-2010 |
20110015394 | Method of Synthesis of Bosentan, Its Polymorphic Forms and Its Salts - The present invention relates to alkaline earth metal salts of bosentan, anyhdrous bosentan, polymorphic forms thereof, amorphous bosentan and processes for preparing them. The present invention further relates to a process for the preparation of bosentan and its pharmaceutically acceptable salts. | 01-20-2011 |
20110034477 | Crystalline Polymorph of Doxazosin Mesylate (Form IV) and Process for Preparation Thereof - Crystalline Form IV of doxazosin mesylate, a process for its preparation and uses thereof. | 02-10-2011 |
20110054218 | Process for the Synthesis of Propargylated Aminoindan Derivatives - A process for preparing a compound of formula (V) or its enantiomer, which comprises:
| 03-03-2011 |
20110077271 | Process for the Preparation of Donepezil Hydrochloride - The present invention provides a process for preparing donepezil or a salt thereof, the process comprising reducing a 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methylene]pyridonium halide of formula II, wherein X is bromide or chloride, in the presence of an ionic compound, a solvent, a catalyst and a source of hydrogen, to form donepezil and optionally converting the donepezil to the salt thereof. | 03-31-2011 |
20110105763 | Process for Preparing Valsartan - An N-[(2′-(1-triphenyl methyl tetrazole-5-yl)biphenyl]-4-yl]methyl]-L-valine benzyl ester organic salt of formula (IVA) wherein A represents an organic carboxylic acid, a process for its preparation and its use in the synthesis of valsartan or salts thereof. | 05-05-2011 |
20110112292 | Crystalline Form of Tenofovir Disoproxil and a Process for Its Preparation - Crystalline Form C of tenofovir disoproxil, salts thereof and a process for its preparation. The process involves adding a solution comprising tenofovir disoproxil and an organic solvent to salt-saturated water, whereby the crystalline Form C of tenofovir disoproxil precipitates. The crystalline Form C of tenofovir disoproxil may be converted to a salt thereof. There is also provided a process for purifying a crude product comprising tenofovir monoisoproxil and tenofovir disoproxil. | 05-12-2011 |
20120116071 | Rifaximin - Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa. | 05-10-2012 |
20120157544 | Process for the Preparation of O-Desmethyl Venlafaxine and Intermediate for Use Therein - The present invention relates to a compound of formula A, wherein R is alkyl. | 06-21-2012 |
20120165524 | Process for Preparing Levosimendan and Intermediates for Use in the Process - In an embodiment, the present invention provides a process for preparing (−)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II | 06-28-2012 |
20120220778 | Process for the synthesis of naratriptan - The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR | 08-30-2012 |
20120232091 | Polymorphic Forms of Manidipine - The invention relates to various new polymorphic forms of manidipine and pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of the polymorphic forms of manidipine and pharmaceutically acceptable salts thereof. | 09-13-2012 |
20130029945 | Darunavir Polymorph and Process for Preparation Thereof - There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent. | 01-31-2013 |
20130150587 | Process for the Preparation of Esomeprazole Magnesium Dihydrate - A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1H-benzimidazole. | 06-13-2013 |
20130150588 | Salts and Polymorphs of Dexrabeprazole - The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation. | 06-13-2013 |
20130160761 | Pharmaceutical Aerosol Composition - A pharmaceutical aerosol composition comprising at least one hydrofluoroalkane propellant; at least one active agent complexed with an adjuvant; and, optionally, at least one pharmaceutically acceptable excipient. | 06-27-2013 |
20130165686 | Process for the Preparation of Nateglinide - The present invention relates to a process for the preparation of substantially pure nateglinide of formula (I), substantially free from the cis-isomer and L-enantiomer and preparation of enantiomerically pure nateglinide form B, directly from the hydrolysis of a (−)-N-(trans-4-isopropylcyclohexyl-1-carbonyl)-D-phenylalanine alkyl ester in a ketonic solvent or water or mixture thereof. | 06-27-2013 |
20140128419 | Rifaximin - Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa. | 05-08-2014 |
20140194624 | Process for Preparation of Erlotinib and its Pharmaceutically Acceptable Salts - A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4-halo-6,7-bis(2-methoxyethoxy)quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. | 07-10-2014 |
20140200228 | PROCESS FOR THE PREPARATION OF PALIPERIDONE - The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) | 07-17-2014 |
20140256004 | Process for the Preparation of an Endothelin Receptor Antagonist - The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use. | 09-11-2014 |
20150037275 | RIFAXIMIN COMPLEXES - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex. | 02-05-2015 |
20150045382 | RIFAXIMIN COMPLEXES - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex. | 02-12-2015 |
20150080579 | Salts and Polymorphs of Dexrabeprazole - The present invention provides dexrabeprazole magnesium hydrate and a process for its preparation. The present invention also provides a magnesium, calcium or potassium salt of dexrabeprazole, optionally in amorphous form, and processes for its preparation. | 03-19-2015 |