Class / Patent application number | Description | Number of patent applications / Date published |
546114000 | Ring sulfur in the bicyclo ring system | 65 |
20080207907 | Process For Pd-Catalysed C-N Coupling In Specific Solvent Systems - The invention relates to a novel process for the Pd catalysed formation of C—N bonds between an aryl halide or an aryloxysulphonyl compound and an amine in specific solvent systems, and also to the use of these solvent systems for C—N couplings. | 08-28-2008 |
20080214821 | Method of Preparing Clopidogrel and Intermediates Used Therein - Optically pure clopidogrel can be prepared in a high yield by optically resolving a racemic form of the compound of formula (II) using an optically active amine to form the optically active form of the compound of formula (III) or its acid-addition salt; and methylating the compound of formula (III) or its acid-addition salt. | 09-04-2008 |
20080249311 | Preparation of Clopidogrel and Its Analogues Methyl Tetrahydrothienopyridine Acetate Compuunds - The present invention disclosed a preparation method of Clopidogrel (X=2-Cl) and its analogues of methyl tetrahydrothienopyridine acetate (I) by using halogen phenyl acetonitrile (VIII) as starting material and tetrahydrothienopyridine acetonitrile (IV), tetrahydrothienopyridine acetate (V) as key intermediates, and further using kinetic resolution to prepare the optical active Clopidogrel and compounds of methyl tetrahydrothenopridine acetate of formula (XII). The Clopidogrel of present invention is a novel high effective and safety drug for inhibition of platelet aggregation. This invention applied systematic technique of racemization of unwanted optical active enantiomer, recover recycle and reuse of resolution agent etc., with greater economic advantages and suitable for commercial scale industrial production. | 10-09-2008 |
20080287679 | Process for preparing clopidogrel - The present invention encompasses processes for the preparation of optically pure clopidogrel camphorsulfonic acid salt without the need to isolate or recover (±) clopidogrel. | 11-20-2008 |
20080300409 | Crystalline clopidogrel hydrobromide and processes for preparation thereof - Provided are crystalline forms of clopidogrel hydrobromide and processes for their preparation. | 12-04-2008 |
20080306268 | Crystalline clopidogrel hydrobromide and processes for preparation thereof - Provided are crystalline forms of clopidogrel hydrobromide and processes for their preparation. | 12-11-2008 |
20090036683 | METHOD FOR PREPARING CLOPIDOGREL 1,5-NAPHTHALENEDISULFONATE OR HYDRATE THEREOF - The present invention relates to a method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof, which comprises reacting a clopidogrel-acid addition salt with disodium 1,5-naphthalenedisulfonate or its hydrate in water, or a mixture of water and an organic solvent. High quality clopidogrel 1,5-naphthalenedisulfonate can be prepared by the inventive method by way of using non-corrosive disodium 1,5-naphthalenedisulfonate. | 02-05-2009 |
20090093635 | PROCESS FOR MAKING POLYMORPH FROM I OF (S) - (+) -METHYL-ALPHA- (2-CHLOROPHENYL) -6, 7-DYHIDRO-THIENO- [3, 2-c] PYRIDINE-5 (4H) -ACETATE HYDROGEN SULFATE - The invention relates to a process for the preparation of the pharmaceutically applicable polymorph Form I of (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]-pyridine-5(4H)-acetate hydrogen sulfate of formula I; by reacting (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate and sulfuric acid in the presence of solvents which comprises dissolving (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate in an ether; mixing this solution with a solution of a C | 04-09-2009 |
20090099363 | PROCESS FOR THE PREPARATION OF POLYMORPHIC FORMS OF CLOPIDOGREL HYDROGEN SULFATE - The present invention relates to a novel process for the preparation of polymorphic forms of clopidogrel hydrogen sulfate, namely methyl(+)-(S)-α-(o-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetate hydrogen sulfate of formula (I). Particularly the present invention relates to the process for the preparation of form (I) and amorphous clopidogrel hydrogen sulfate. | 04-16-2009 |
20090187022 | Crystalline clopidogrel hydrobromide and processes for preparation thereof - Provided are crystalline forms of clopidogrel hydrobromide and processes for their preparation. | 07-23-2009 |
20090192313 | PROCESS FOR PRODUCING 5-METHYL-4,5,6,7-TETRAHYDROTHIAZOLO[5,4-c]PYRIDINE-2-CARBOXYLIC ACID - 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof, [F14] | 07-30-2009 |
20090221827 | PROCESSES FOR THE PREPARATION OF DIFFERENT FORMS OF (S)-(+)-CLOPIDOGREL BESYLATE - Disclosed herein are the improved processes for the preparation of different forms of (S)-(+)-Clopidogrel besylate, pharmaceutical compositions containing them and their use in medicine. | 09-03-2009 |
20090234123 | Processes For The Preparation Of Clopidogrel Hydrogen Sulfate Polymorphic Form I - Processes for the preparation of clopidogrel hydrogen sulfate of polymorphic form I are described which include use of specific solvents and process measures to avoid formation of undesired by-products. | 09-17-2009 |
20090275755 | Process for the Preparation of S-(+)-Clopidogrel by Optical Resolution - The present invention relates to a process for the preparation of S-(+)-clopidogrel by an optical resolution and, more particularly, to a process for the preparation of S-(+)-clopidogrel represented by the following formula 1 with high optical purity by converting a clopidogrel racemic carboxylic acid into a diastereomeric salt using a (+)-cinchonine for optical resolution, extracting an S-(+)-clopidogrel carboxylic acid from the diastereomeric salt using a suitable solvent under an acidic condition and then reacting the S-(+)-clopidogrel carboxylic acid with methanol. | 11-05-2009 |
20090286984 | Processes and intermediates for preparing fused heterocyclic kinase inhibitors - This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level. | 11-19-2009 |
20090318701 | METHOD PREPARATION CLOPIDOGREL AND INTERMEDIATES USED THEREIN - Optically pure clopidogrel can be prepared in a high yield by optically resolving a racemic form of the compound of formula (II) using an optically active amine to form the optically active form of the compound of formula (III) or its acid-addition salt; and methylating the compound of formula (III) or its acid-addition salt. | 12-24-2009 |
20100004453 | PROCESS FOR PREPARATION OF METHYL-(+)-(S)-ALPHA-(2-CHLOROPHENYL)-6, 7-DIHYDROTHIENO[3,2-C]PYRIDINE-5 (4H) -ACETIC ACID METHYL ESTER OR SALTS THEREOF HAVING HIGHER CHIRAL PURITY AND PRODUCTS THEREOF - A process for preparation of Methyl-(+)-(S)-alpha-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester or salts thereof [clopidogrel or salts thereof of Formula (I)] having higher chiral purity and products thereof is provided. A process for purification of the compound prepared is also provided to enhance its efficacy by enhancing its optical rotation and chiral purity. In Formula (I), R is selected from a group comprising alkyl, alkoxy, hydroxy, amine etc., and R | 01-07-2010 |
20100016594 | PROCESS FOR THE PREPARATION OF CLOPIDOGREL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS - The present invention provides a process for the preparation of clopidogrel and its pharmaceutically acceptable salts thereof comprises the resolving racemic methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate by the salt formation of methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate with excess levorotatory camphor-10-sulfonic acid to get a maximum yield of camphor sulphonate salt of methyl S-(+)-alpha-5-(4,5,6,7-tetrahydro[3,2-e]thienopyridyl)(2-chlorophenyl)-acetate and transforming the camphor sulphonate salt to clopidogrel or its pharmaceutically acceptable salts thereof. | 01-21-2010 |
20100016595 | PROCESS FOR PREPARING (S)-(+)-CLOPIDOGREL BASE AND ITS SALTS - Processes for the preparation of Methyl (+)-(S)-(2-chlorophenyl)-(6,7dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate [Clopidogrel base, (I)] and their various pharmaceutically acceptable salts. | 01-21-2010 |
20100076192 | PROCESS FOR PRODUCING 5-METHYL-4,5,6,7-TETRAHYDROTHIAZOLO[5,4-c]PYRIDINE-2-CARBOXYLIC ACID - 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (6) or a salt thereof, | 03-25-2010 |
20100081824 | Processes For the preparation of different forms of (S)-(+)-Clopidogrel besylate - Improved processes for the preparation of different forms of (S)-(+)-Clopidogrel besylate, pharmaceutical compositions containing them and their use in medicine. | 04-01-2010 |
20100094013 | PROCESS FOR PRODUCTION OF PRASUGREL HYDROCHLORIDE HAVING HIGH PURITY - An object of the present invention is to provide prasugrel hydrochloride with a reduced content of CATP, and the like. | 04-15-2010 |
20100145053 | MODIFIED RELEASE CLOPIDOGREL FORMULATION - A once daily dosage form comprising Clopidogrel or a salt of Clopidogrel equivalent to 50 mg to 150 mg Clopidogrel is disclosed. Said dosage form provides at least one of the following in vivo plasma profile of Clopidogrel selected from:
| 06-10-2010 |
20100160635 | INDUSTRIAL PROCESS FOR PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE - An improved process for the manufacture of Clopidogrel starting from 2-(2-thienyl)ethylamine, which eliminates the isolation of an unstable intermediate like 2-(2-thienyl)ethyl formimine by subjecting it to a one pot cyclization to get 4,5,6,7-tetrahydrothieno (3,2-c) pyridine of Formula II and further reacting with halo-compound of formula III (where X is Cl or Br) at 20 to 90° C. temperature characterized in a solvent like water and/or dichloroethane in presence of organic or inorganic bases is disclosed herein. This inventions also discloses Crystalline Form I of (+)-(S)-clopidogrel hydrogen sulphate and its preparation thereof. | 06-24-2010 |
20100197923 | SALTS OF CLOPIDOGREL AND PROCESS FOR PREPARATION - Disclosed are new salts of Clopidogrel viz. Clopidogrel mesylate, Clopidogrel besylate and Clopidogrel tosylate, methods for their preparation and pharmaceutical compositions containing them and their use in medicine. | 08-05-2010 |
20100216999 | PROCESS FOR PREPARATION OF PURE POLYMORPHIC FORM 1 OF CLOPIDOGREL HYDROGENSULFATE - Process for the preparation of substantially pure polymorphic Form 1 of clopidogrel hydrogensulfate, wherein the reaction of optically active clopidogrel base with sulfuric acid is carried out in the mixture of at least two solvents, chosen from group I, comprising aliphatic ethers, and from group II, comprising ketones, esters of C | 08-26-2010 |
20100228033 | METHOD OF MANUFACTURING 5-[2-CYCLOPROPYL-1-(2-FLUOROPHENYL)-2-OXOETHYL]-4,5,6,7-TETRAHYDROTHIENO[- 3,2-C]PYRIDIN-2-YL ACETATE (PRASUGREL) - A method of manufacturing 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate, known under the INN name prasugrel of formula (I), in which the substance of formula (VI) is reacted with a cyclopropyl magnesium halide to produce the substance of formula (V), which reacted with methanesulfonyl chloride to give the methanesulfonate of formula (IV), which is further reacted with the compound of formula (III) to be converted the substance of formula (II) and the latter is converted to the substance of formula (I) with an acetylation agent. | 09-09-2010 |
20100261908 | PROCESSES FOR THE PREPARATION OF PRASUGREL , AND ITS SALTS AND POLYMORPHS - Processes for the preparation of prasugrel and its pharmaceutically acceptable salts thereof. Also disclosed are polymorphic forms of prasugrel hydrochloride and processes for their preparation. | 10-14-2010 |
20100274020 | PROCESS FOR THE PREPARATION OF PHARMACEUTICAL INTERMEDIATES - The invention relates to a process for the preparation of cyclopropyl benzyl ketone compounds of formula (II) wherein R | 10-28-2010 |
20110040093 | PROCESS FOR THE PREPARATION OF PHARMACEUTICAL INTERMEDIATE - The invention relates to a process for the preparation of compounds of general formula (III), wherein R represents fluorine or chlorine atom and X represents chlorine or bromine atom, by halogenation of cyclopropyl benzyl ketone of general formula (II), wherein R represents fluorine or chlorine atom and the halogenation is carried out in the mixture of aqueous hydrogen halide and aqueous hydrogen peroxide in the presence of a water miscible solvent or in the presence of a phase transfer catalyst; or the halogenation is carried out in the mixture of sulfuric acid and an alkali metal salt of aqueous hydrogen halide. The process can be applied preferably on industrial scale. | 02-17-2011 |
20110054177 | PROCESS FOR PRODUCING 5-METHYL-4,5,6,7-TETRAHYDROTHIAZOLO[5,4-c]PYRIDINE-2-CARBOXYLIC ACID - 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof, | 03-03-2011 |
20110087028 | METHOD FOR PREPARING CLOPIDOGREL AND ITS DERIVATIVES - The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenyl glycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives. Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed. | 04-14-2011 |
20110118467 | PROCESS FOR THE PREPARATION OF CLOPIDOGREL HYDROGEN SULFATE CRYSTALLINE FORM I - The present invention relates to a process for the preparation of clopidogrel and, more particularly, to an improved process for the preparation of clopidogrel hydrogen sulfate crystalline Form I by addition of dilute sulfuric acid to a solution of clopidogrel free base in butyl acetate. | 05-19-2011 |
20110144343 | PROCESS FOR PREPARING CANNABINOID RECEPTOR LIGANDS - A process for the preparation of compounds of formula (I) or a salt thereof | 06-16-2011 |
20110166354 | METHOD FOR PRODUCING OPTICALLY ACTIVE AMINO ACID DERIVATIVE - The present application relates to a method for producing an optically active α-amino acid derivative, comprising steps of reacting an α-haloester derivative represented by the general formula (1): | 07-07-2011 |
20110184177 | CXCR2 INHIBITORS - The invention relates to compounds of the formula I: | 07-28-2011 |
20110190502 | PROCESS FOR THE PREPARATION OF S-CLOPIDOGREL - A process for the preparation of (S)-Clopidogrel free base or a pharmaceutically acceptable salt thereof by the racemization of the undesired (R)-Clopidogrel in the presence of a suitable base followed by resolution with camphor sulfonate salt and further treatment with an inorganic acid to yield the title compound. | 08-04-2011 |
20110201814 | METHOD FOR PRODUCING SOLID PREPARATION - A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which comprises a step wherein a composition containing the compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying mechanical stress to the composition. The compound of the formula (I) is as follows: | 08-18-2011 |
20110257401 | PROCESS FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID - It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and/or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-α-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent. | 10-20-2011 |
20110263858 | PROCESS FOR THE PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE FORM I - The present invention relates to a process for the preparation of Form 1 of (+)-(S)-∞-(2-Chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester hydrogen sulphate commonly known as clopidogrel bisulphate. The present invention further relates to a process for reducing the residual amount of methyl isobutyl ketone and controlling the amount of mesityl oxide in clopidogrel hydrogen sulphate Form 1 by washing with ethyl acetate. Formula (I). | 10-27-2011 |
20110275821 | METHOD FOR PRODUCING DIAMINE DERIVATIVE - The present invention provides a method for producing a compound represented by formula (A), the method comprising the steps of: (a) mixing a compound represented by formula (B) with p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate at less than 1 molar equivalent with respect to the compound represented by formula (B) in a solvent under heating; (b) adding additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to the mixed solution under cooling, wherein the additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate is added in such an amount that the total molar equivalent thereof with the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate of step (a) is 1 molar equivalent or more with respect to the compound represented by formula (B) of step (a); and (c) subsequently allowing the mixed solution to crystallize to obtain the compound represented by formula (A). | 11-10-2011 |
20110282064 | METHOD FOR THE MANUFACTURE OF HIGHLY PURE PRASUGREL - The invention deals with preparation of the substance prasugrel, using 3-cyclopropyl-1-(2-fluorophenyl)-3-oxopropyl methanesulfonate for alkylation of 2-oxo-thienotetrahydropyridine, which may be in the form of a salt, e.g. with hydrochloric acid or p-toluenesulfonic acid. The resulting compound of formula II is acylated, preferably with acetanhydride, preferably directly in the reaction mixture without isolation, and the produced prasugrel of formula I can then be crystallized directly from the reaction mixture. | 11-17-2011 |
20120035369 | METHOD FOR PRODUCING OPTICALLY ACTIVE DIAMINE DERIVATIVE - The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a method for industrially producing a compound (1) or a compound (4), comprising: [Step 1]: adding a quaternary ammonium salt and a metal azide salt to water to prepare an aqueous solution of an azidification reagent complex comprising quaternary ammonium salt-metal azide salt, and subsequently dehydrating the aqueous solution using an aromatic hydrocarbon solvent to form a mixed solution of the azidification reagent complex comprising quaternary ammonium salt-metal azide salt and the aromatic hydrocarbon solvent with a water content of 0.2% or less; and [Step 2]: adding, to the mixed solution prepared in [Step 1], a compound (2) wherein L represents a leaving group. | 02-09-2012 |
20120041206 | PROCESS FOR PRODUCING DIAMINE DERIVATIVE - The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a process for industrially producing a compound (1) represented by the following formula (1): | 02-16-2012 |
20120077980 | METHOD FOR PRODUCING A SOLID PREPARATION - A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which includes a step wherein a composition containing the compound represented by the formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying a mechanical stress to the composition. The compound of the formula (I) is as follows: | 03-29-2012 |
20120095234 | PROCESSES AND INTERMEDIATES FOR PREPARING FUSED HETEROCYCLIC KINASE INHIBITORS - This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level. | 04-19-2012 |
20120142927 | METHOD FOR PREPARING PRASUGREL - The present invention relates to a method for synthesizing prasugrel, comprising, the following steps: converting o-fluorobenzyl cyclopropyl ketone into α-cyclopropylcarbonyl-2-fluorobenzyl halide (compound 2) using dibromohydantoinhydantoin as halogenation reagent and acetic acid as solvent, then 2-oxo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine p-toluenesulfonate (compound 4) is obtained with high yield by a concerted catalysis using a phase transfer catalyst and an inorganic salt, then is condensed and acylated to obtain prasugrel as a gum. The present invention also provides a method for purifying prasugrel comprising crystallizing using alcohols as a crystallization solvent to obtain prasugrel crystals with a high purity. | 06-07-2012 |
20120203002 | Crystalline Forms of Kinase Inhibitors - Salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer. | 08-09-2012 |
20120232274 | PROCESS FOR PREPARATION OF CLOPIODOGREL BISULFATE FORM-1 - An improved process for preparing crystalline form-1 of (S)-methyl 2-(2-chlorophenyl)-2-{6,7-dihydrothieno[3,2-c]pyridine-5(4H)-yl}acetate bisulfate (clopidogrel bisulfate) of formula I is provided The preparation comprises the straight conversion of an uncyclized material of (S)-methyl 2-[2-(thiophen-2-yl)ethylamino]-2-(2-chlorophenyl) acetate hydrochloride into clopidogrel bisulfate crystalline form-1 without any degradation of clopidogrel base | 09-13-2012 |
20120330018 | PROCESS FOR PREPARING PHARMACEUTICAL COMPOUNDS AND INTERMEDIATE COMPOUNDS - The object of the present invention is a process for preparing the 2-acetoxy-5-(2-fluor-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]pyridine (prasugrel) of the formula (I). The process starts form crystalline 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI). Further objects of the present invention are two novel crystalline forms of 5-trityl-4,5,6,7-tetrahydro-tieno[3,2-c]pyridine of the formula (VI) and the use thereof for preparing the compound of the formula (V) and process preparing thereof. | 12-27-2012 |
20130005979 | THIENOPYRIDINE DERIVATIVE, METHOD FOR PRODUCING SAME AND ORGANIC SEMICONDUCTOR DEVICE USING SAME - This invention relates to a novel thienopyridine derivative represented by formula (1), which is useful as an organic semiconductor device, such as an organic thin film transistor element, and the invention also relates to method for producing the thienopyridine derivative represented by formula (1): | 01-03-2013 |
20130030183 | PROCESS FOR PREPARING A PHARMACEUTICAL COMPOUND - The object of the present invention is a one-pot process for preparing the 2-acetoxy-5-(2-fluoro-α-cyclopropyl-carbonyl-benzyl)-4,5,6,7-tetrahydro-4H-tieno[3,2-c]-pyridine (prasugrel) of the formula (I) by reacting the 5,6,7,7a-tetrahydro-4H-tieno[3,2-c]-pyridine-2-on of the formula (II) with 2-bromo-1-cyclopropyl-2-(2-fluorophenyl)-etanone of the formula (III) or with 2-chloro-1-cyclopropyl-2-(2-fluorphenyl)-etanone of the formula (IIIa) and acetylating of the formed compound of the formula (IV), wherein the reaction is carried out in the presence of an organic base with an acetylation agent without isolating the compound of the formula (IV). The coupling and acetylation are carried out in the presence of the same organic base such as triethylamine, N,N-diisopropyl-ethylamine or pyridine. At the end of the process the prasugrel of the formula (I) is purified by recrystallization from an organic solvent or a mixture of solvents. | 01-31-2013 |
20130053569 | PROCESS FOR THE PREPARATION OF PRASUGREL HCL SALT - The present invention relates to process for the preparation of Prasugrel HCl having formula (I). | 02-28-2013 |
20130144061 | PROCESS FOR PREPARING A COMPOUND BY A NOVEL SANDMEYER-LIKE REACTION USING A NITROXIDE RADICAL COMPOUND AS A REACTION CATALYST - The present invention provides a novel process for preparing a substituted aromatic compound such as an aromatic halo compound or a salt thereof through a transformation reaction of an aromatic diazonium salt from an aromatic amino compound at stable high yields utilizing a novel Sandmeyer-like reaction using a nitroxide radical compound as a reaction catalyst. | 06-06-2013 |
20130165657 | PROCESS FOR PREPARATION OF OPTICALLY ACTIVE DIAMINE DERIVATIVE SALT - The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group. | 06-27-2013 |
20130310564 | Processes and Intermediates for Preparing Fused Heterocyclic Kinase Inhibitors - This invention relates to intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level. | 11-21-2013 |
20130345428 | METHOD FOR PRODUCTION OF PRASUGREL HYDROCHLORIDE HAVING HIGH PURITY - A method for producing prasugrel hydrochloride with a reduced content of 2-acetoxy-5-[5-chloro-1-(2-fluorophenyl)-2-oxopentyl]-4,5,6,7-tetrahydrothieno[3,2-6]pyridine by carrying out the following steps: | 12-26-2013 |
20140142311 | METHOD FOR PREPARING PRASUGREL - The present invention relates to a method for synthesizing prasugrel, comprising the following steps: converting o-fluorobenzyl cyclopropyl ketone into α-cyclopropylcarbonyl-2-fluorobenzyl halide (compound 2) using dibromohydantoinhydantoin as halogenation reagent and acetic acid as solvent, then 2-oxo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine p-toluenesulfonate (compound 4) is obtained with high yield by a concerted catalysis using a phase transfer catalyst and an inorganic salt, then is condensed and acylated to obtain prasugrel as a gum. The present invention also provides a method for purifying prasugrel comprising crystallizing using alcohols as a crystallization solvent to obtain prasugrel crystals with a high purity. | 05-22-2014 |
20140206872 | FLUORESCENT DYE - There is provided a fluorescent dye which can improve the fluorescent intensity at the time of labeling to thereby detect a biomolecule with higher sensitivity. The fluorescent dye of the present invention includes a nitrogen cation-containing group or a nitrogen-containing group. Its high water solubility can improve the rate of labeling for a biomolecule to thereby detect a biomolecule with high sensitivity. | 07-24-2014 |
20150025243 | FORMULATIONS CONTAINING CLOPIDOGREL AND SULFOALKYL ETHER CYCLODEXTRIN AND METHODS OF USE - The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution. The compositions herein can be administered perorally or parenterally and provide substantial pharmacokinetic, pharmacodynamic and/or therapeutic advantages over a tablet composition administered perorally and excluding SAE-CD. | 01-22-2015 |
20150344388 | HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES - The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. | 12-03-2015 |
20150344389 | CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES - The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents. | 12-03-2015 |
20150353577 | METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE - It is an object of the present invention to provide a method for efficiently producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which is important as an intermediate compound for the production of an FXa-inhibiting compound. A method for producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which comprises treating an (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid with 1,3-dibromo-5,5-dimethylhydantoin or N-bromosuccinimide in a solvent. | 12-10-2015 |
20160009715 | FUSED HETEROCYCLIC COMPOUND | 01-14-2016 |
20160016974 | PREPARATION METHOD OF OPTICALLY ACTIVE DIAMINE COMPOUND - The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (1f) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, R | 01-21-2016 |