Class / Patent application number | Description | Number of patent applications / Date published |
546174000 | Having -C(=X)-, wherein X is chalcogen, attached indirectly to the quinoline ring system by nonionic bonding | 42 |
20080275243 | Process for the Preparation of Polymorphs, Solvates of Aripiprazole Using Aripiprazole Acid Salts - The present invention relates to the novel compounds Methyl 2-[(3S)-[3-[(2E)(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates (IV) wherein the halo is chloro, bromo, iodo, starting from the known compound Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1). Reaction of Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1) with thionyl chloride or with methane sulfonyl chloride—lithium bromide or with trimethyl chlorosilane—sodium iodide in presence or absence of base gives Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates. | 11-06-2008 |
20080306270 | Process for the Preparation of a Leukotriene Antagonist and Intermediates Thereof - It comprises a preparation process of Montelukast from a new intermediate compound of formula (VI), which is previously prepared by reaction of the corresponding sulfonate with 1-(mercaptomethyl)cyclopropyl)methanol. Compound (VI) is reacted with a Grignard reactant to convert the ester group into a tertiary alcohol, followed by conversion of the primary alcohol into a sulfonate, substitution of the sulfonate group by a cyano group, and finally transforming the cyano compound to the carboxilic acid compound by a hydrolysis reaction to afford Montelukast. Montelukast can also be prepared by a hydrolysis reaction of the corresponding amide. It also comprises new intermediate compounds useful in such preparation process. | 12-11-2008 |
20090018338 | Treatment of CRTH2-Mediated diseases and conditions - The present invention provides indole derivatives that antagonize prostaglandin D | 01-15-2009 |
20090093636 | PROCESS FOR MAKING MONTELUKAST AND INTERMEDIATES THEREFOR - A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: | 04-09-2009 |
20090099367 | Process for preparing a leukotriene antagonist - Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation. | 04-16-2009 |
20090171092 | Process for the Preparation of Montelukast and Its Pharmaceutically Acceptable Salts - An improved process for the preparation of Montelukast and its pharmaceutically acceptable salts comprises of reacting (S) Benzenepropanol α-[3-[2-(7-chloro2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy-1-methyl ethyl)-α-methane sulfonate compound of formula (II) with | 07-02-2009 |
20090182148 | PROCESS FOR THE MANUFACTURE OF MONTELUKAST SODIUM - An improved process for the manufacture of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, sodium salt [montelukast sodium(I)]. It consists of converting a vital intermediate 1-(mercaptomethyl)-cyclopropane acetic acid of formula IX, to a quaternary ammonium salt of formula X, using a suitable base in a suitable solvent at 0° C. to 50° C. followed by monometalation to provide an intermediate of formula XI and subsequent condensation of XI with 2-[2-[3-(S)-[3-[2-(7-chloro-2-quinolinyl)-ethenyl]phenyl]-3-methanesulphonyloxypropyl]phenyl]-2-propanol at 0 to −50° C. to afford 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid as the quaternary ammonium salt which is filtered, purified by crystallization from a suitable solvent and finally treated with a sodium base in a suitable solvent to generate montelukast sodium which is isolated by trituration with an antisolvent. The invention provides a convenient process for preparing montelukast sodium (I) in good yields and purities. | 07-16-2009 |
20090247759 | Purification process of Montelukast and its Amine Salts - It comprises a process for the purification of Montelukast, or its salts or its solvates, including any stereoisomer or mixture thereof, which comprises converting Montelukast acid or a solvate thereof, including any stereoisomer or mixtures thereof, into an amine salt selected from the group consisting of tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-α-phenylglycinol salt, in the presence of an appropriate solvent. It also comprises novel salts of Montelukast, in particular, tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-α-phenylglycinol salts. | 10-01-2009 |
20090270628 | PROCESS FOR MAKING MONTELUKAST INTERMEDIATES - A process for making a montelukast intermediate of formula (1) is achieved by reacting a compound of formula (2): | 10-29-2009 |
20090281323 | PROCESS FOR THE MANUFACTURE OF MONTELUKAST SODIUM - Process for the manufacture of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, sodium salt [montelukast sodium (I)] consisting of: i. Converting methyl 1-(mercaptomethyl)-cyclopropaneacetate to a metal salt (X) using a metal hydroxide, ii. Subjecting the metal salt (X) to monometallation to provide a dimetallide (XI). iii. Converting a diol of formula (II) to a mesylate of formula (III) and reacting (III) in situ with (XI) affordin the metal salt of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid. iv. Reacting the metal salt in-situ with a base and purifying to afford an amine salt (XII). v. Treating (XII) with a sodium base and precipitating out montelukast sodium (I). | 11-12-2009 |
20090326232 | Process for the Preparation of Leukotriene Receptor Antagonist (Montelukast Sodium) - The present invention relates to an improved process for the preparation of [R-(E)]-1-[[[1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]-cyclopropaneacetic acid, monosodium salt of Formula (I). | 12-31-2009 |
20100056793 | PROCESS FOR PURE MONTELUKAST SODIUM THROUGH PURE INTERMEDIATES AS WELL AS NOVEL AMINE SALTS - The present invention provides an improved process for the preparation of highly pure montelukast sodium through highly pure diol intermediate compound of formula (2) and (1)-(mercapto methyl)cyclopropane acetic acid methyl ester compound of formula (4) or mercaptomethyl cyclopropane acetic acid compound of formula (7). The present invention also provides novel organic amine salts of montelukast. | 03-04-2010 |
20100063291 | PROCESS FOR PREPARATION OF SOLID MONTELUKAST - A process for preparation of montelukast or a salt thereof is provided, the process including reacting a late intermediate compound which is 2-[1-[1-R-3-[2-(7 chloro quinolin-2-yl)vinyl [phenyl]-3-[2-methoxy carbonyl phenyl]propyl sulfonyl methyl]cyclo propyl]acetic acid or a salt thereof with methyl magnesium chloride or methyl magnesium bromide in an organic solvent. In one embodiment, the process includes reacting an earlier intermediate compound which is methyl 2-(3-R-(3-(2-(7-chloro 2-quinolinyl)-ethenyl)-3 hydroxy propyl)benzoate with methane sulfonyl chloride or toluene sulfonyl chloride to obtain a mesylated or tosylated derivative of the earlier intermediate compound; followed by a reaction of the mesylated or tosylated derivative with 1-mercapto methyl cyclopropane acetic acid in a polar solvent in a presence of a base to obtain the late intermediate compound. | 03-11-2010 |
20100076195 | PURIFICATION OF MONTELUKAST - The present invention provides methods of purifying montelukast, a new isolated impurity of montelukast, method for its isolation, and method of using montelukast impurity as a reference marker and a reference standard. | 03-25-2010 |
20100130745 | PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ETHENYLPHENYL ALCOHOLS - In one aspect, the present invention relates to a process for the preparation of an optically active alcohol of formula | 05-27-2010 |
20100152453 | Novel Compounds and Preparation for Montelukast Sodium - This invention relates to novel compounds and a process for preparation of montelukast sodium. | 06-17-2010 |
20100168432 | Process for the Preparation of Montelukast - The present invention relates to a process for the preparation of Montelukast or a salt thereof comprises, i) condensing Methyl-2-[3-[3-(2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-chloro propyljbenzoate obtained above with 1-(mercaptomethyl)cyclopropane acetic acid in presence of alkali carbonates such as Cesium Carbonate, followed by salification with organic amine ii) neutralizing the organic amine salt as obtained above with organic/inorganic acid followed by reaction with methylmagnesium chloride in the presence of Cerium Chloride followed by treatment with organic base yields montelukast amine salt iii) converting the montelukast amine salt to Montelukast Free acid iv) saltification of Montelukast free acid with Sodium hydroxide affords Montelukast Sodium. | 07-01-2010 |
20100174083 | METHOD FOR THE PREPARATION OF MONTELUKAST - A method of preparation of Montelukast of formula (I) by reaction of the compound of formula (III) and a compound of formula (IX), characterized in that the reaction is carried out in the presence of a base, an inert solvent and a component increasing selectivity of the process, especially of a polyether of general formula (XIII), wherein R stands for hydrogen or an alkyl and the value of n varies from 1 to 40, polyethyleneglycol of general formula (XIV), wherein n=1 to 40 or a crown-ether of formulae (XV), (XVI) or (XVII). | 07-08-2010 |
20100190987 | PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST - The tertiary alcohol α-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy-1-methylethyl)benzene-propanol, the (αS)-enantioner of which is an intermediate in the production of montelukast, is produced by reacting the novel lactone of formula (II) with a methylmagnesium halide in an ethereal solvent in the presence of lanthanum trichloride and lithium chloride. The lactone II can be prepared by reacting a corresponding hydroxyester with a Grignard reagent in the absence of a lanthanoid compound or with a strong base. | 07-29-2010 |
20100204476 | Process for preparing a leukotriene antagonist and an intermediate thereof - Dicyclohexylamine salt of formula (IIa) or a pharmaceutically acceptable solvate thereof, including a hydrate, and its process for preparation are provided. The invention also relates to processes for the preparation of montelukast of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, including a hydrate, based on the conversion of a salt of formula (IIa) into its form of free acid, followed by reaction with a compound of formula (III) CH3MgX, wherein X is halogen, in a suitable solvent, optionally in the presence of a Lewis acid. | 08-12-2010 |
20100267958 | METHOD FOR ISOLATION AND PURIFICATION OF MONTELUKAST - A method of isolation of Montelukast of formula I from reaction mixtures, comprising conversion of the crude sub-stance to well-crystallizing salts with primary amines in the environment of at least one organic solvent and acetonitrile, followed by re-crystallization of these salts with simultaneous removal of chemical impurities and use of the chemically pure salts of Montelukast with primary amines for direct transformation to the pharmaceutically useful amorphous form of Montelukast sodium of formula II. | 10-21-2010 |
20110034692 | SPECIFIC IMPURITIES OF MONTELUKAST - The subject-matter of the invention consists in a method of removing specific impurities of montelukast of formula (I), which occur due to chemical instability of the target substance and also contaminate the substance in the preparation process. Further, methods of isolation of specific impurities of montelukast defined by formulae (V-A), (IV-A), (XIIIa-A), (XIIIb-A) and analytic methods used for the control of the production of montelukast in the pharmaceutical quality. | 02-10-2011 |
20110040095 | PREPARATION OF MONTELUKAST AND ITS SALTS - Processes for preparing montelukast acid and its salts. | 02-17-2011 |
20110092708 | PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS THEREOF - The present invention relates to the alkyl amine salts of Montelukast and methods for their preparation and conversion of Montelukast amine salts to Montelukast or Montelukast alkali/alkaline salt. | 04-21-2011 |
20110105757 | METHOD FOR PREPARATION OF MONTELUKAST ACID IN IONIC LIQUID MEDIUM - The present invention relates to a method for preparing Montelukast acid or its sodium salt by reacting a thiol compound with a Montelukast intermediate in the presence of a base in a medium comprising an ionic liquid compound. In accordance with the inventive method, highly pure Montelukast acid or its sodium salt, which is advantageously used as a raw material in the preparation of Montelukast, a leukotriene antagonist, can be easily prepared in a high yield. | 05-05-2011 |
20110112300 | IMPROVED PROCESS FOR PREPARING MONTELUKAST AND SALTS THEREOF - A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with | 05-12-2011 |
20110137039 | PROCESS FOR THE PREPARATION OF MONTELUKAST AND ITS SALTS - The present invention relates to an improved process for the preparation of 1-[[[(IR)-I-[3[(IE)-2-(7chloro-2-quino-linyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid and its salts using Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoate. | 06-09-2011 |
20110166356 | METHOD FOR PREPARING MONTELUKAST SODIUM SALTS - Disclosed is a method for preparing a montelukast sodium salt of Formula 1. The method includes coupling a methanesulfonyl compound of Formula 2 below with a compound of Formula 3 below in the presence of a bistrimethylsilylamide alkali metal salt, further adding an alkali metal base thereto and hydrolyzing the mixture by heating to prepare a compound of Formula 4 below, reacting the compound of Formula 4 with 4-tert-butylcyclohexylamine, followed by purification, to prepare an amine salt of Formula 5, and converting the amine salt of Formula 5 into a sodium salt. | 07-07-2011 |
20110237798 | DIRECT CONVERSION OF PHENOLS INTO AMIDES AND ESTERS OF BENZOIC ACID - A method is provided for the preparation of an aromatic carboxylic acid aryl ester or an N-aryl aromatic carboxamide. The method comprises contacting an O,O-diaryl thiocarbonate or an O-aryl-N-aryl thiocarbamate with a reactant that regioselectively reacts with sulfur, which contact causes an O-neophyl rearrangement, thereby forming either the aromatic carboxylic acid aryl ester or the N-aryl aromatic carboxamide, respectively. | 09-29-2011 |
20120142931 | Purification of montelukast using simulated moving bed - This invention concerns generally with a process for purifying crude pharmaceutical compositions, wherein the crude pharmaceutical composition comprises a sodium salt of Montelukast | 06-07-2012 |
20120165535 | SYNTHETIC METHOD FOR MONTELUKAST SODIUM INTERMEDIATE - A synthesis method for preparing Montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In this method, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting the resultant product with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether. The present invention can easily obtain start materials and is applicable for mass production. | 06-28-2012 |
20120259121 | PROCESS FOR THE PREPARATION OF MONTELUKAST AND SALTS THEREOF - The present invention relates to an improved process for the preparation of Montelukast and pharmaceutical acceptable salts or derivatives thereof, in particular to a process for large scale production of Montelukast and salts thereof in high yield and high purity and pharmaceutical preparations containing said compounds. | 10-11-2012 |
20130184464 | NOVEL MONTELUKAST 4-HALOBENZYLAMINE SALT AND METHOD FOR PREPARING MONTELUKAST SODIUM SALT BY USING THE SAME - Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. | 07-18-2013 |
20130345429 | PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS - There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein R | 12-26-2013 |
20140206876 | 2-(Substituted ethynyl)quinoline Derivatives as mGLUr5 Antagonists - Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD). | 07-24-2014 |
20140350264 | Process for the Preparation of (5-Fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-Acetic Acid Esters - The invention relates to a process for the preparation of a compound of formula (I) wherein R | 11-27-2014 |
20150299127 | PROCESS FOR PREPARATION OF MONTELUKAST SODIUM - Disclosed is a process for the preparation of montelukast sodium. The process comprises a) reacting 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2-propanol with methane sulfonyl chloride and coupling the resultant mesylate compound with 1-(mercaptomethyl)cyclopropane acetic acid in presence of a base and free alkali source followed by saltification with an amine in a single step reaction and b) converting the montelukast amine salt to montelukast sodium salt. | 10-22-2015 |
20160074853 | LIGAND, NICKEL COMPLEX COMPRISING THE LIGAND, AND REACTION USING THE NICKEL COMPLEX - An object of the present invention is to provide a method for directly performing arylation (particularly α-arylation) of carbonyl or thiocarbonyl compounds using a more inexpensive phenol derivative and nickel catalyst. Another object of the present invention is to provide a novel nickel catalyst that can be used in this method, and a novel ligand of the nickel catalyst. The novel compounds of the present invention are a compound having a diphosphine skeleton in which a five- or six-membered heterocyclic ring is substituted with two dialkylphosphines and/or dicycloalkylphosphines, or a salt thereof, and a compound having the diphosphine skeleton that is bound to nickel. Moreover, coupling reaction of a carbonyl compound and a phenol derivative can be advanced in the presence of a nickel compound having a monodentate or bidentate dialkylphosphine and/or dicycloalkylphosphine skeleton. | 03-17-2016 |
546175000 | Nitrogen bonded directly to the -C(=X)- group | 4 |
20110230662 | RADIOLABELLED FLUOROBENZAMIDE ANALOGUES, THEIR SYNTHESIS AND USE IN DIAGNOSTIC IMAGING - Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with | 09-22-2011 |
20130109861 | TELOMERASE INHIBITORS AND A METHOD FOR THE PREPARATION THEREOF | 05-02-2013 |
20140179925 | METHODS FOR TREATING COGNITIVE DISORDERS USING 3-ARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES, 3-HETEROARYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS - Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 | 06-26-2014 |
20140221657 | ALPHA HELIX MIMETIC COMPOSITIONS FOR TREATING CANCER AND OTHER CBP/CATENIN-MEDIATED DISEASES AND CONDITIONS - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | 08-07-2014 |