Patent application number | Description | Published |
20110313035 | POLYMORPHS OF DARUNAVIR - The present invention provides novel solvated forms of darunavir and processes for there preparation. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form. | 12-22-2011 |
20120197021 | OPTICAL RESOLUTION OF SUBSTITUTED 2-(2-PYRIDINYLMETHYLSULPHINYL)-1H-BENZIMIDAZOLES - The present invention relates to process for preparation of optical resolution of substituted 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles either as a single enantiomer or in an enantiomerically enriched form. Thus, for example, R-1,1′-binaphtyl-2-2′-diyl hydrogen phosphate was reacted with 2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (Lansoprazole) in a mixture of benzene and cyclohexane to obtain diasteremeric complexes. The diasteremeric complexes were subjected to fractional crystallization to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole.R-1,1′-binaphthyl-2-2′-diyl hydrogen phosphate. The separated isomer was treated with sodium bicarbonate in a mixture of ethyl acetate and water to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (dexlansoprazole). | 08-02-2012 |
20120215003 | PROCESS FOR THE RESOLUTION OF OMEPRAZOLE - The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL. | 08-23-2012 |
20130131090 | SALTS OF LAPATINIB - The present invention provides novel dioxalate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel monobesylate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of monohydrate form of lapatinib ditosylate. The present invention further provides a process for the preparation of anhydrous form of lapatinib ditosylate. | 05-23-2013 |
20130178654 | PROCESS FOR CINACALCET HYDROCHLORIDE - 3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride. | 07-11-2013 |
20130190368 | NOVEL POLYMORPHS OF FEBUXOSTAT - The present invention provides a novel 1,4-dioxane solvate form of febuxostat and process for its preparation. The present invention also provides novel crystalline forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. | 07-25-2013 |
20130190490 | PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES - The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. | 07-25-2013 |
20130211091 | CRYSTALLINE FORMS OF MARAVIROC PHOSPHATE AND PROCESS FOR MARAVIROC AMORPHOUS FORM - The present invention provides novel crystalline forms of maraviroc phosphate, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides novel process for the preparation of maraviroc amorphous form and pharmaceutical composition comprising it. | 08-15-2013 |
20130237563 | NOVEL POLYMORPHS OF PITAVASTATIN CALCIUM - The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it. | 09-12-2013 |
20130245052 | NOVEL POLYMORPH OF NILOTINIB HYDROCHLORIDE - The present invention provides a novel crystalline form of nilotinib hydrochloride, process for its preparation and pharmaceutical compositions comprising it. | 09-19-2013 |
20130245262 | PROCESS FOR THE PREPARATION OF PAZOPANIB USING NOVEL INTERMEDIATE - The present invention provides a commercially viable process for preparing pazopanib and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate. The present invention also provides a process for the purification of pazopanib hydrochloride. | 09-19-2013 |
20140046062 | PROCESS FOR NUCLEOSIDES - The present invention relates to improved process for the preparation of lamivudine or emtricitabine. Thus, (1′R,2′S,5′R)-menthyl-5(R,S)-acetoxy-[1,3]-oxathiolane-2(R)-carboxylate is reacted with N-propinoyl cytosine in hexamethyl disilazane and then added trityl perchlorate to obtain a solid containing (1′R,2′S,5′R)-menthyl-5S-(N-4″-propionylcytosin-1″-yl)-[1,3]-oxathiolane-2R-carboxylate. The solid obtained above is reacted with methane sulfonic acid to obtain (2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-[1,3]-oxathiolane-2-carboxylic acid, 2S-isopropyl-5R-methyl-1R-cyclohexyl ester. The above compound is reduced with sodium borohydride to obtain lamivudine. | 02-13-2014 |
20140066468 | AMORPHOUS FORM OF LOPINAVIR AND RITONAVIR MIXTURE - The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it. | 03-06-2014 |
20140100252 | AMORPHOUS RITONAVIR CO-PRECIPITATED - The present invention relates to amorphous ritonavir co-precipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it. | 04-10-2014 |
20140107337 | PROCESS FOR FOSAPREPITANT - The present invention provides a novel process for reducing palladium content in fosaprepitant dimeglumine. | 04-17-2014 |
20140112992 | PROCESS FOR FEBUXOSTAT - The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 μm, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles. | 04-24-2014 |
20140121384 | PROCESS FOR BENDAMUSTINE HYDROCHLORIDE - The present invention provides a process for the preparation of 1H-benzimidazol-1-methyl-5-N,N-di(2-hydroxyethyl)-2-butanoic acid ethyl ester. The present invention also provides a process for the preparation of bendamustine hydrochloride. The present invention further provides a process for the purification of bendamustine hydrochloride. | 05-01-2014 |
20140200356 | POLYMORPHS OF DARUNAVIR - The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form. | 07-17-2014 |
20140235859 | PROCESS FOR THE RESOLUTION OF OMEPRAZOLE - The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL. | 08-21-2014 |
20140350038 | RILPIVIRINE HYDROCHLORIDE - The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it. | 11-27-2014 |
20150025040 | NOVEL POLYMORPHS OF FOSAMPRENAVIR CALCIUM - Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium. The pharmaceutical composition may comprse substantially pure amorphous fosamprenavir calcium and pharmaceutically acceptable excipients. | 01-22-2015 |
20150080420 | AMORPHOUS FORM OF LOPINAVIR AND RITONAVIR MIXTURE - The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it. | 03-19-2015 |
20150133670 | PROCESS FOR SORAFENIB TOSYLATE POLYMORPH III - The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III. | 05-14-2015 |
20150141457 | ELVITEGRAVIR SOLID DISPERSION - The present invention provides a novel amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. In a preferred embodiment the process for the preparation of amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier comprises: preparing a solution comprising a mixture of elvitegravir and one or more pharmaceutically acceptable carriers selected from copovidone, ethyl cellulose, hydroxypropyl methylcellulose, polyethylene glycol, span 20 or soluplus in a solvent; and removing the solvent from the solution obtained; adding hydrocarbon solvent to the residual solid; and isolating amorphous solid dispersion of elvitegravir in combination with a pharmaceutically acceptable carrier. | 05-21-2015 |
20150182458 | RUFINAMIDE SOLID DISPERSION - The present invention provides a solid dispersion of rufinamide in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. | 07-02-2015 |
20150183751 | PROCESS FOR RILPIVIRINE USING NOVEL INTERMEDIATE - The present invention provides a commercially viable process for preparing rilpivirine and its pharmaceutically acceptable acid addition salts thereof in high yields using novel intermediate. | 07-02-2015 |
20150183767 | NOVEL POLYMORPHS OF AZILSARTAN MEDOXOMIL - The present invention provides a novel amorphous Form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel crystalline Forms of azilsartan medoxomil, processes for their preparations and pharmaceutical compositions comprising them. The present invention further provides a novel amorphous Form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a novel process for the preparation of azilsartan medoxomil potassium crystalline Form II. | 07-02-2015 |
20150252045 | PROCESS FOR PRALATREXATE - The present invention provides a novel process for the purification of alpha-propargylhomoterephthalic acid dimethyl ester substantially free of homoterephthalic acid dimethyl ester. The present invention also provides a novel process for the purification of pralatrexate. | 09-10-2015 |
20150290199 | LINAGLIPTIN SOLID DISPERSION - The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. | 10-15-2015 |
20150291574 | NOVEL POLYMORPHS OF AZILSARTAN - The present invention provides a novel crystalline Form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides a novel crystalline Form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. | 10-15-2015 |