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CIPLA LIMITED

CIPLA LIMITED Patent applications
Patent application numberTitlePublished
20120116071Rifaximin - 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
20120041199Process for the Preparation of Doxazosin and Salts Thereof - The present invention relates to a process for the preparation of doxazosin or salts thereof.02-16-2012
20110262378Rifaximin 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.10-27-2011
20110257418Process for Preparing Zanamivir and Intermediates for Use in the Process - The present invention provides a process for preparing methyl 5-acetamido-4-amino-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (V), which process comprises reducing methyl 5-acetamido-4-azido-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (IV) in the presence of a reducing agent selected from the group consisting of lithium aluminium hydride, sodium borohydride, zinc/ammonium chloride, zinc-ferric chloride and ferric chloride/sodium iodide. The present invention also provides compounds of formula (VIII) and (IX) which may be used in the synthesis of zanamivir. The present invention also provides processes for preparing compounds (VIII) and (IX) and processes involving their use, including in the synthesis of zanamivir.10-20-2011
20110250149Tiotropium Bromide Having a Low Degree of Crystallinity - The present invention provides tiotropium bromide having a low degree of crystallinity. The present invention also provides a complex of tiotropium bromide and polyvinylpyrrolidone, processes for preparing it and pharmaceutical formulations including it.10-13-2011
20110245499Process for Resolving Zopiclone - The present invention provides a process for the preparation of the dextrorotatory isomer of zopiclone (eszopiclone). The present invention also provides eszopiclone di-p-anisolyl-L-tartrate and eszopiclone diacetyl-L-tartrate, which are useful as intermediates in a process for preparing eszopiclone.10-06-2011
20110207938Process for the Preparation of Rufinamide - The present invention relates to a process for the preparation of rufinamide of formula I, which process comprises: (i) reacting a 2,6-difluorobenzylhalide of formula II, wherein X is chloride, bromide or iodide, with an azide to obtain 2-(azidomethyl)-1,3-difluorobenzene of formula III; (ii) reacting 2-(azidomethyl)-1,3-difluorobenzene of formula III with methyl propiolate to obtain methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid of formula IV; and (iii) reacting methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid of formula IV with ammonia to obtain rufinamide of formula I.08-25-2011
20110184174Processes for the Synthesis of Levocetirizine and Intermediates for Use Therein - The present invention provides a compound of formula (IV)07-28-2011
20110166237Process for the Synthesis of Arformoterol - The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein R07-07-2011
20110112292Crystalline 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
20110105763Process 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
20110104262Topical Combinations Comprising an Antimycotic Agent and an Antiviral Agent - There is provided a pharmaceutical composition comprising an antimycotic agent and an antiviral agent, useful for prophylaxis and/or treatment of an associated infection and/or disease and a method of manufacturing thereof.05-05-2011
20110077271Process 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
20110054218Process for the Synthesis of Propargylated Aminoindan Derivatives - A process for preparing a compound of formula (V) or its enantiomer, which comprises: 03-03-2011
20110034477Crystalline 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
20110028456Solid Pharmaceutical Dosage Form - A pharmaceutical composition comprising a solid unit dosage form comprising: one or more of pharmaceutically active ingredients selected from valacyclovir, olanzapine, voriconazole, topotecan, artesunate, amodiaquine, guggulosterone, ramipril, telmisartan, tibolone, atorvastatin, simvastatin, amlodipine, ezetimibe, fenofibrate, tacrolimus, valgancyclovir, valsartan, clopidrogel, estradiol, trenbolone, efavirenz, metformin, pseudoephedrine, verapamil, felodipine, valproic acid/sodium valproate, mesalamine, hydrochlorothiazide, levosulpiride, nelfinavir, cefixime and cefpodoxime proxetil in combination with a water insoluble polymer and/or a water soluble polymer. Methods for making the pharmaceutical composition are also disclosed.02-03-2011
20110015394Method 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
20110009450Crystalline form of benzothiophene compound and process for preparation thereof - Crystalline raloxifene hydrochloride in hydrated form, particularly the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and uses thereof.01-13-2011
20110008429Anti-Retroviral Combination - A pharmaceutical composition comprising a solid unit dosage form comprising: 01-13-2011
20110008412Oral Formulations for 5-HT-Receptor Agonists, Uses and Methods of Treatment Employing The Same - A pharmaceutically acceptable oral formulation comprising core material which comprises a therapeutically effective amount of a 5-HT-receptor agonist, or a pharmaceutically acceptable salt, solvate or derivative thereof, which core material is provided with a substantially water resistant coating comprising one or more substantially water resistant materials.01-13-2011
20100331289Combination of Azelastine and Steroids - A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.12-30-2010
20100298565Processes 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
20100285115Novel Antiretroviral Combination - The invention relates to pharmaceutical compositions containing a combination of atazanavir and ritonavir, to methods of making them, and their use in medicine.11-11-2010
20100222572PROCESSES 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
20100204493Process 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
20100204195Pharmaceutical Compositions and Process for Making Them - Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.08-12-2010
20100173921Antiretroviral Solid Oral Composition - The present invention provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with one or more excipients. The invention provides a composition which is smaller for a given amount of said active substance and possesses taste masking property and a process for preparing the composition. The present invention also provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with at least one water insoluble polymer, wherein the ratio of drug to polymer in the composition ranges from about 1:1 to about 1:6, and a process for preparing the composition.07-08-2010
20100160643Process 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
20100152229Process 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
20100137586Process 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
20100126507MULTI-DOSE INHALER DEVICE - The present invention provides an inhaler device (05-27-2010
20100113804Process 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
20100113790Process 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: R05-06-2010
20100113526Process 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
20100099887Process 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
20100094004Process 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
20100081688Process for the preparation of montelukast, and intermediates therefor - The invention relates to processes for making montelukast and to intermediates for use in the process, in particular compounds of formulas 2-7: L=OAc, OTs, OTf5OMs; where X=Cl, Br, I.04-01-2010
20100075999Process 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
20100063016Pharmaceutical Combinations - A pharmaceutical combination comprising (a) a combination of two or more bronchodilators; or (b) a combination of at least one bronchodilator in combination with at least one corticosteroid.03-11-2010
20100016605Process - 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
20090326028Process for the preparation of temozolomide and analogs - A process for the preparation of compounds of formula IA, where R═CH12-31-2009
20090325917Pharmaceutical Compositions and Nasal Spray Incorporating Anhydrous Mometasone Furoate - A stable aqueous pharmaceutical composition comprising anhydrous mometasone furoate and a pharmaceutically acceptable carrier.12-31-2009
20090320838DRY POWDER INHALER - An inhaler (12-31-2009
20090318397Combination of Azelastine and Steroids - A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.12-24-2009
20090312357Rifaximin - 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.12-17-2009
20090291143Combination of Azelastine and Steroids - A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.11-26-2009
20090221830Fexofenadine Polymorphs and Processes of Preparing the Same - Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.09-03-2009
20090187020Process And Intermediate For Preparation Of Donepezil - The invention relates to new compounds of formula (III):07-23-2009
20080234492Process for the Preparation of Carvedilol - A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The present invention further provides carvedilol of formula (I) prepared by a process as described above, and pharmaceutical compositions containing the same and therapeutic uses thereof.09-25-2008

Patent applications by CIPLA LIMITED