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HETERO RESEARCH FOUNDATION

HETERO RESEARCH FOUNDATION Patent applications
Patent application numberTitlePublished
20120107397PHARMACEUTICAL COMPOSITIONS OF VALSARTAN - The present invention relates to the stable pharmaceutical composition comprising valsartan or a pharmaceutically acceptable salt thereof with mannitol as a filler and povidone as binder. The present invention also relate to the valsartan or pharmaceutically acceptable salt thereof in combination with hydrochlorothiazide or amlodipine or both; and optionally one or more additional excipients.05-03-2012
20120077772SOLID ORAL DOSAGE FORMS OF LAMIVUDINE - The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also relate to the combination of lamivudine and other Anti-HIV agents. Thus, for example, the present invention provides a stable tablet formulation comprising lamivudine, isomalt, crospovidone, calcium stearate and opadry white.03-29-2012
20120035211NOVEL POLYMORPHS OF SAQUINAVIR - The present invention provides novel polymorphs of saquinavir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides a process for purification of saquinavir. The present invention further provides a novel process for preparation of known saquinavir crystalline form I.02-09-2012
20120015987NOVEL POLYMORPH OF ATAZANAVIR SULFATE - The present invention provides a novel crystalline form of atazanavir sulfate, process for its preparation and to pharmaceutical composition containing it. In accordance with the present invention atazanavir sulfate was dissolved in methanol, to the solution was added ethyl acetate, the solid obtained was collected by filtration and dried to give atazanavir sulfate crystalline form H1.01-19-2012
20110313035POLYMORPHS 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
20110306647NOVEL POLYMORPHS OF SUNITINIB MALATE - The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about −90 deg C. for 8 hours to give sunitinib malate crystalline form III.12-15-2011
20110294839NOVEL POLYMORPHS OF LOPINAVIR - The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100° C. for 10 hours to give lopinavir desolvated crystalline form H1.12-01-2011
20110263865POLYMORPHS OF ZOLMITRIPTAN - The present invention provides a novel isopropyl acetate solvate form of zolmitriptan, and a process for its preparation thereof. The present invention also provides a process for preparation of zolmitriptan polymorph A. Thus, for example, zolmitriptan isopropanol solvate was dissolved in isopropyl acetate at 25 deg C, the contents were heated to reflux for 30 minutes and the separated solid was filtered, washed with isopropyl acetate to give zolmitriptan isopropyl acetate solvate.10-27-2011
20110245497OPTICAL RESOLUTION OF SUBSTITUTED 1, 3-OXATHIOLANE NUCLEOSIDES - Cis(±)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone is reacted with S(+)-1,1′-binaphthyl-2,2′-diyl hydrogen phosphate in methanol to obtain diastereomeric compounds. The diastereomeric compounds are subjected to selective crystallization to obtain (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1′-binaphthyl-2,2′-diyl hydrogen phosphate. (2R-Cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone 1,1′-binaphthyl-2,2′-diyl hydrogen phosphate is treated with hydrochloric acid in water to obtain (2R-cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone.10-06-2011
20110237822PROCESS FOR PREPARATION OF VALSARTAN INTERMEDIATE - The present invention provides a process for preparation of a key intermediate of valsartan in a pure form and use of this intermediate for the preparation of valsartan or a pharmaceutically acceptable salt in pure form.09-29-2011
20110213155OPTICAL PURIFICATION OF ESOMEPRAZOLE - The present invention relates to process for optical purification of esomeprazole or a salt thereof. Thus, esomeprazole sodium having 20 to 1% R-omeprazole by weight of the sum of the contents of esomeprazole and R-omeprazole is precipitated from a solvent selected from an alcohol or a mixture of alcohols and the precipitated solid is collected to obtain optically pure esomeprazole sodium.09-01-2011
20110212990NOVEL POLYMORPH OF MOXIFLOXACIN HYDROCHLORIDE - The present invention relates to novel polymorph of moxifloxacin hydrochloride, processes for its preparation and to pharmaceutical compositions containing it. Thus, for example moxifloxacin hydrochloride is suspended in methanol and water and the p09-01-2011
20110137034PROCESS FOR PREPARING LAMIVUDINE POLYMORPH FORM - The invention relates to a process for the preparation of stable lamivudine polymorph form and to a composition comprising thereof.06-09-2011
20110054186PROCESS FOR EPROSARTAN INTERMEDIATE - The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-butyl-5-formyl-1H-imidazole-1-yl]methyl]benzoic acid methyl ester is reacted with ethyl 2-carboxy-3-(2-thienyl)propionate in the presence of piperidinium propionate in diisopropyl ether or a mixture of n-hexane and a solvent selected from toluene and cyclohexane, optionally purifying the crude compound to obtain (E)-α-[[2-butyl-1-[[4-(methoxy carbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester substantially free of 3-(2-thienyl)propanoic acid ethyl ester impurity.03-03-2011
20110015196LUPEOL-TYPE TRITERPENE DERIVATIVES AS ANTIVIRALS - The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.01-20-2011
20100210853PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL - There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2′-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co-distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0° C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil.08-19-2010

Patent applications by HETERO RESEARCH FOUNDATION