Class / Patent application number | Description | Number of patent applications / Date published |
544282000 | Ring nitrogen is shared by two cyclos | 26 |
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 |
20080214808 | Preparation of Aseptic 3-[2-[4-((6-Fluoro-1,2-Benzisoxazol-3-Yl)-1-Piperidinyl]-6,7,8,9-Tetrahydro-9-Hydroxy-2-Methyl-4H-Pyrido[1,2-a]Pyrimidin-4-One Palmitate Ester - The present invention concerns a process for preparing aseptic crystalline 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one palmitate ester (I) substantially free of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (II-a), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3 -yl)-1-piperidinyl]ethyl]-6,7-dihydro-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (II-b), and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-ethyl]-6,7,8,9-tetrahydro-2-methyl-9-pentadecyl-4H-pyrido[1,2-a]pyrimidin-4-one (III), and having an average particle size ranging from 20 to 150 μm. | 09-04-2008 |
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 |
20080262227 | PROCESS FOR MAKING RISPERIDONE AND INTERMEDIATES THEREFOR - The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). | 10-23-2008 |
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 |
20090156810 | SYNTHESIS OF PALIPERIDONE - A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). | 06-18-2009 |
20090171082 | MITOTIC KINESIN INHIBITORS - The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical compositions comprising such compounds, methods of treating cancer by the administration of such compositions, and processes for the preparation of the compounds. Compounds of the invention have the following formula: | 07-02-2009 |
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 |
20100004447 | PROCESS FOR PREPARATION OF 9-HYDROXY-3-(2-CHLOROETHYL)-2-METHYL-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE HYDROCHLORIDE - Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield. | 01-07-2010 |
20100010218 | SYNTHESIS OF PALIPERIDONE - A compound of formula (6) or an acid addition salt thereof | 01-14-2010 |
20100069633 | PALIPERIDONE KETONE - A compound of formula (7.2) or an acid addition salt thereof. | 03-18-2010 |
20100130740 | PROCESS FOR PREPARATION OF RISPERIDONE - The invention provides a more handy and environment friendly process for preparing risperidone, which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride with 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one in a basic aqueous solution or suspension. The concentration of alkaline metal carbonates in the basic aqueous solution or suspension is ranged from 15% to 40%. The reaction is carried out at a temperature range of 101-140° C. and the reaction is completed within 10 minutes to 2 hours. | 05-27-2010 |
20100267954 | PROCESS FOR THE PURIFICATION OF PALIPERIDONE - Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride. | 10-21-2010 |
20100298565 | Processes for the Preparation of Paliperidone and Pharmaceutically Acceptable Salts Thereof and Intermediates for Use in the Processes - The present invention relates to novel compounds of formula (VIII) and (X), processes for their preparation and their use in the preparation of paliperidone or a salt thereof. There is also provided by the present invention novel processes for preparing intermediates for use in the preparation of paliperidone or a salt thereof, and novel processes for preparing paliperidone or a salt thereof. | 11-25-2010 |
20100298566 | PROCESS FOR THE PREPARATION OF PALIPERIDONE AND ITS INTERMEDIATES - A process for the preparation of a psychotropic agent Paliperidone. Preferably, this invention relates to a method for the purification of Paliperidone by making its acid addition salts. | 11-25-2010 |
20110087024 | PROCESS FOR THE PREPARATION OF PALIPERIDONE INTERMEDIATES - The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone. | 04-14-2011 |
20110124863 | PROCESS TO PREPARE PALIPERIDONE AND INTERMEDIATES THEREOF - The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process. | 05-26-2011 |
20110213147 | New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-bacterial agents - The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: | 09-01-2011 |
20120165527 | PROCESS FOR THE PREPARATION OF PURE PALIPERIDONE - The present invention relates to an improved process for the preparation of pure Paliperidone of formula (I). The present invention more specifically provides an improved process for the preparation of pure Paliperidone which may contain impurities in the acceptable level of pharmacopoeia requirement specifically 3-{2-[4-(5-Fluoro-benzo[d]isoxazol-3-yl]-piperidin-1-yl]-ethyl}-2-methyl-7,8-dihydro- | 06-28-2012 |
20120259116 | Novel Process for the Preparation of Paliperidone - The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of | 10-11-2012 |
20140073787 | PREPARATION OF 3-[2-[4-((6-FLUORO-1, 2-BENZISOXAZOL-3-YL)-L-PIPERIDINYL)-6, 7, 8, 9-TETRAHYDRO-9-HYDROXY-2-METHYL-4H-PYRIDO[ 1, 2-A]-PYRIMIDIN-4-ONE (PALIPERIDONE) AND PALIPERIDONE PALMITATE. - An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester. | 03-13-2014 |
20140187776 | MIXTURES OF MESOIONIC PESTICIDES - Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, | 07-03-2014 |
20140343284 | MALONIC ACID DI-SALTS AND A METHOD FOR PREPARING MALONYL DIHALIDES - A compound of Formula 2 is disclosed | 11-20-2014 |
20150087832 | PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES - The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency. | 03-26-2015 |
20160176884 | Process for Making Beta 3 Agonists and Intermediates | 06-23-2016 |
20190144468 | NOVEL PROCESS | 05-16-2019 |