Patent application number | Description | Published |
20080293938 | Novel Process for the Preparation of Didanosine Using Novel Intermediates - present invention relates to novel crystalline alkali metal and alkaline earth metal salts of 2′,3′-dideoxy-2′,3′-didehydroinosine. The present invention also provides a novel process for preparation of didanosine in high yield and purity using novel intermediates. Thus, for example, 5′-O-acetyl-2′,3′-dideoxy-2′,3′-didehydroinosine is reacted with monomethyl amine to give 2′,3′-dideoxy-2′,3′-didehydro inosine, which is then reacted with sodium hydroxide and crystallized to give crystalline 2′,3′-dideoxy-2′,3′-didehydroinosine sodium salt. 2′,3′-Dideoxy-2′,3′-didehydroinosine sodium salt is hydrogenated using raney nickel catalyst in aqueous medium and then neutralized with hydrochloric acid to yield didanosine. | 11-27-2008 |
20090054682 | PROCESS FOR OSELTAMIVIR PHOSPHATE - The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate. | 02-26-2009 |
20090149670 | PROCESS FOR OBTAINING PURE OSELTAMIVIR - The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity. | 06-11-2009 |
20090177009 | PROCESS OF MAKING SERTRALINE FORM II - The present invention discloses novel and improved processes for preparation of sertraline hydrochloride crystalline form II. Thus, for example, sertraline free base is dissolved in isoamyl alcohol at 25-30° C., pH of the mass is adjusted to 2.0 with conc. hydrochloric acid (36%) at 25-30° C. and then stirred for 14 hours at 25-30° C. Filtered the solid and dried at 65° C. for 4 hours to give sertraline hydrochloride crystalline form II. The present invention also provides a novel process for preparation of sertraline hydrochloride crystalline form I. | 07-09-2009 |
20090177010 | PROCESS OF MAKING SERTRALINE FORM I - The present invention discloses novel and improved processes for preparation of sertraline hydrochloride crystalline form II. Thus, for example, sertraline free base is dissolved in isoamyl alcohol at 25-30° C., pH of the mass is adjusted to 2.0 with conc. hydrochloric acid (36%) at 25-30° C. and then stirred for 14 hours at 25-30° C. Filtered the solid and dried at 65° C. for 4 hours to give sertraline hydrochloride crystalline form II. The present invention also provides a novel process for preparation of sertraline hydrochloride crystalline form I. | 07-09-2009 |
20090197907 | NOVEL CRYSTALLINE FORM OF RUPATADINE FREE BASE - The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof. | 08-06-2009 |
20100076022 | NOVEL POLYMORPHS OF RIMONABANT - The present invention discloses novel and stable polymorphs of rimonabant, its hydrates and solvates, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention further discloses a novel and stable amorphous form of rimonabant, process for its preparation and a pharmaceutical composition comprising it. The present invention also provides an improved process for the preparation of rimonabant crystalline Form II. Thus, for example, rimonabant is dissolved in methylene dichloride, stirred for 10 minutes at 25-30° C. and then the solvent distilled off under vacuum at 40° C. The resulting residue is stirred with water and the separated solid is collected at 25-30° C. to give a stable crystalline rimonabant hydrate. | 03-25-2010 |
20100076197 | PROCESS FOR RIMONABANT - The present invention provides an improved and commercially viable process for the preparation of rimonabant substantially free of amide impurity, namely 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxamide and its pharmaceutically acceptable acid addition salts thereof. Thus, for example, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxylic acid chloride is reacted with 1-aminopiperidine in the presence of a base and optionally a phase transfer catalyst is used such as tetra-butylammonium bromide in a biphasic reaction medium containing water and a water-immiscible solvent to obtain pure rimonabant. | 03-25-2010 |
20100137632 | PROCESS FOR OSELTAMIVIR PHOSPHATE - The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate. | 06-03-2010 |
20100210868 | PROCESS FOR OBTAINING PURE OSELTAMIVIR - The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity. | 08-19-2010 |
20110137034 | PROCESS 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 |
20110294839 | NOVEL 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 |
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 |
20120015987 | NOVEL 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 |
20120035211 | NOVEL 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 |
20120115857 | Novel Polymorphs of Efavirenz - The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz. | 05-10-2012 |
20120178930 | NOVEL POLYMORPHS OF RALTEGRAVIR POTASSIUM - The present invention provides novel polymorphs of raltegravir potassium, processes for their preparation and pharmaceutical compositions comprising them. Thus for example, raltegravir potassium was added to water and stirred for 15 minutes, the solution was filtered on hiflo bed and the bed washed with water, the resulting solution was subjected to freeze drying at −180 deg C. for 13 hours to give raltegravir potassium amorphous form. | 07-12-2012 |
20120232069 | PROCESS FOR PREPARING EFAVIRENZ POLYMORPH - The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25° C.-30° C., the solution was slowly added to water at 0° C.-5° C., the separated solid was filtered, washed with mixture of acetone and water and dried at 25° C.-35° C. under below 65% relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1. | 09-13-2012 |
20120271047 | Novel Polymorphs of Efavirenz - The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz. | 10-25-2012 |
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 |
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 |
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 |
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 |