Entries |
Document | Title | Date |
20100324287 | PROCESS FOR PHOSPHONIC ACID - The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases. | 12-23-2010 |
20110009629 | PREPARATION OF MORPHOLINE DERIVATIVES - This invention relates to processes and intermediates for the stereoselective morpholine derivatives. The invention in particular allows the stereoselective preparation of the drugs aprepitant and fosaprepitant. | 01-13-2011 |
20110190491 | S-TRIAZOLE ALPHA- MERCAPTOACETANILIDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE - A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO | 08-04-2011 |
20110313157 | S-TRIAZOLYL ALPHA-MERCAPTO ACETANILIDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE - A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO | 12-22-2011 |
20120277426 | PROCESS FOR THE PREPARATION OF CRYSTALLINE APREPITANT HAVING FORM I CONTENT - The present invention provides a process for preparation of crystalline aprepitant having not more than 15% by weight of Form I content which comprises, a) dissolving aprepitant in a suitable solvent to obtain a solution, b) cooling the solution to 10-15° C., c) optionally seeding the solution with aprepitant Form I crystals, d) adding an anti-solvent to the solution, and e) isolating crystalline aprepitant having not more than 15% by weight of Form I content. | 11-01-2012 |
20130109853 | PREPARATION METHOD OF 5-[[2(R)-[1(R)-[3,5-BIS(TRIFLUOROMETHYL) PHENYL]ETHOXY]-3(S)-4-FLUOROPHENYL-4-MORPHOLINYL]METHYL]-1,2-DIHYDRO-3H-1- ,2,4-TRIAZOLE-3-ONE | 05-02-2013 |
20130345418 | PROCESS FOR PURIFICATION OF APREPITANT - The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenypethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C. to give pure aprepitant substantially free of its diastereomeric impurity. | 12-26-2013 |
20140107337 | PROCESS FOR FOSAPREPITANT - The present invention provides a novel process for reducing palladium content in fosaprepitant dimeglumine. | 04-17-2014 |
20140288301 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound. | 09-25-2014 |
20150087828 | 4-SUBSTITUENT-2-HYDROXYLMORPHOLINE-3-ONE AND PREPARATION METHOD THEREOF - A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. | 03-26-2015 |
20160031867 | AN IMPROVED PROCESS FOR THE PREPARATION OF APREPITANT - The present invention provides a process for the preparation of 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (Aprepitant) comprising condensation of 2-(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(S)-(4-fluorophenyl)morpholine hydrochloride salt with 2-(2-chloro-1-iminoethyl)hydrazinecarboxylic acid methyl ester to obtain the reaction mixture containing 2-[2-[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]-1-iminoethyl]hydrazinecarboxylic acid methyl ester, which is in-situ cyclized in the presence of dimethylsulfoxide and a polar protic solvent at a low temperature to yield aprepitant having purity ≧99.5%. | 02-04-2016 |