Patent application number | Description | Published |
20080200676 | Process for the synthesis of CMHTP and intermediates thereof - The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone. | 08-21-2008 |
20080207726 | Process for the purification of carvedilol or its salts thereof - The present invention provides processes for reducing bis impurities ((1,1′-[2-(2-methoxyphenoxy)ethyl]iminobis-[3-(9H-carbazol-4-yloxy)]-propan-2-ol)), in particular Bis 1 and Bis 2, in carvedilol preparations. The process may comprise (a) combining carvedilol base with phosphoric acid in ethanol to obtain a reaction mixture; and (b) precipitating carvedilol phosphate from the reaction mixture, where the carvedilol phosphate comprises low levels of Bis 1 and Bis 2. | 08-28-2008 |
20080207923 | Pure DNT-maleate and methods of preparation thereof - (S)—N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine maleate (DNT-maleate) and polymorphs of DNT-maleate, compositions of DNT-maleate and its polymorphs, processes for the preparation of DNT-maleate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-maleate are provided. Processes for preparing chemically pure duloxetine and chemically pure duloxetine intermediates are also provided. In addition, chemically pure DNT and salts thereof are provided. | 08-28-2008 |
20080214809 | Process for the synthesis of CMHTP and intermediates thereof - The present invention provides processes of preparing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate. | 09-04-2008 |
20080281100 | Pure paliperidone and processes for preparing thereof - The present invention provides pure paliperidone comprising less than about 0.1%, preferably less than about 0.05% and more preferably less than about 0.02%, impurity X as well as purification processes to obtain thereof. | 11-13-2008 |
20090012316 | Crystal forms of (S)-(+)-N,N-dimethyl-3-(1-Napathalenyloxy)-3-(2-thienyl)propanamine oxalate and the preparation thereof - DNT-Oxal crystalline forms and processes for making DNT-Oxal crystalline forms are provided. | 01-08-2009 |
20090035829 | Enzymatic process for the preparation of paliperidone and its intermediate CMHTP - The present invention provides a process for the preparation of a 4H-pyrrido[1,2-a]-pyrimidin-4-one derivative, wherein the 4H-pyrrido[1,2-a]-pyrimidin-4-one derivative is Paliperidone or 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (‘CMHTP’), said process comprising enzymatically hydroxylating Risperidone or 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (‘ClMTTP’), respectively, with at least one oxidoreductase enzyme; and optionally isolating or purifying the Paliperidone or CMHTP, wherein the at least one oxidoreductase enzyme is selected from the group of peroxidases, dioxygenases, monooxygenases and any combination thereof. | 02-05-2009 |
20090209757 | Processes for the preparation and purification of paliperidone palmitate - The present invention encompasses processes for the preparation and purification of paliperidone palmitate. | 08-20-2009 |
20090270620 | Processes for preparing crystal forms of 9-hydroxy-risperidone (paliperidone) - The present invention is related to processes for the preparation of paliperidone crystalline Form II. The invention also provides a paliperidone crystalline Form II containing isopropyl alcohol, and processes for preparing the same. | 10-29-2009 |
20090286844 | Carvedilol phosphate - The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof. | 11-19-2009 |