Class / Patent application number | Description | Number of patent applications / Date published |
548250000 | Tetrazoles (including hydrogenated) | 86 |
20080200687 | Preparation of Terazole Derivatives - The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula | 08-21-2008 |
20080234490 | Metal Salts of 2' - (1H-Tetrazol-5Yl) -1. 1'-Biphenyl-4-Carboxaldehyde - The invention relates to a method or process for the manufacture of blood pressure lowering agents, such as valsartan, novel intermediates as well as process steps in said synthesis. The method or process leads via the novel intermediate salts of the formula IA, | 09-25-2008 |
20090221836 | PROCESS FOR THE PREPARATION OF VALSARTAN AND PRECURSORS THEREOF - This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation. | 09-03-2009 |
20100041897 | Process for preparing a crystalline form of candesartan cilexetil - A process for preparing a crystalline form of candesartan cilexetil referred to as Form I, which has a content of Form II lower than 1% (w/w), is described. The process includes a seeding stage with a crystalline product, which mainly includes Form I, and a digestion stage. The invention also relates to the crystalline form, the pharmaceutical compositions containing it and its use for the preparation of a medicament for the treatment of hypertension. Candesartan cilexetil Form I has shown good stability under accelerated stability conditions, when the content of Form II is lower than 1% w/w. | 02-18-2010 |
20100048911 | ANTIOXIDANT INFLAMMATION MODULATORS: NOVEL DERIVATIVES OF OLEANOLIC ACID - Disclosed herein are novel oleanolic acid derivatives. Methods of preparing these compounds are also disclosed. The oleanolic acid derivatives of this invention may be used for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress. | 02-25-2010 |
20110015403 | PROCESS FOR PREPARING IODINATED AZOLES - The novel process for iodinating substituted azoles, especially for iodinating substituted 1H-tetrazoles and substituted 1H-triazoles, affords the desired compounds in high purity and with good yield. | 01-20-2011 |
20120059172 | NOVEL SOLVATE CRYSTALS - Acetone solvate crystals of trityl olmesartan medoxomil are provided. | 03-08-2012 |
548251000 | Chalcogen or nitrogen attached directly to the tetrazole ring by nonionic bonding | 12 |
20080200688 | Explosive complexes - Lead-free primary explosives of the formula [M | 08-21-2008 |
20080207914 | BIS-(1(2) H-TETRAZOL-5-YL)-AMINE MONOHYDRATE SYNTHESIS AND REACTION INTERMEDIATE - The present invention provides Bis-(1(2)H-tetrazol-5-YL)-amine compound, and safe and inexpensive methods for producing high quality Bis-(1(2)H-tetrazol-5-YL)-amine compound. Also provided are Bis-(1(2)H-tetrazol-5-YL)-amine intermediates, and methods for their preparation. The process of preparing Bis-(1(2)H-tetrazol-5-YL)-amine intermediate substantially combines dicyanamide salt, azide salt, solvent and acid at 40-70 C temperature. The process of preparing Bis-(1(2)H-tetrazol-5-YL)-amine anhydride and/or Bis-(1(2)H-tetrazol-5-YL)-amine monohydrate comprises heating the intermediate described above at ≧75 C and adding a second acid. | 08-28-2008 |
20100261912 | BIS-(1(2)H-TETRAZOL-5-YL)AMINE AND PRODUCTION METHOD THEREFOR - High-quality bis-(1(2)H-tetrazol-5-yl)amine and a method for easily, safely, and inexpensively producing the compound are provided. The method for producing bis-(1(2)H-tetrazol-5-yl)amine includes the steps of heating to 50 to 120° C. a solution mixture in which a necessary amount of an azide salt and a dicyanamide salt in an amount corresponding to 1 to 80 wt % of a necessary amount are added to a solvent, adding an acid in an amount of 1.54 to 2.22 chemical equivalents of the dicyanamide salt in the solution mixture to carry out a reaction at 50 to 120° C., and then adding an acid and a dicyanamide salt solution in which the remaining dicyanamide salt is dissolved in a solvent to promote the reaction. Bis-(1(2)H-tetrazol-5-yl)amine is obtained according to the production method. | 10-14-2010 |
20110046390 | Gas Generant Compositions - A novel compound, used for example, as a gas generating fuel, is defined as a compound having the structural formula of R | 02-24-2011 |
20120004419 | BIS-(1(2)H-TETRAZOL-5-YL) AMINE AND PRODUCTION METHOD THEREFOR - High-quality bis-(1(2)H-tetrazol-5-yl)amine and a method for easily, safely, and inexpensively producing the compound are provided. The method for producing bis-(1(2)H-tetrazol-5-yl)amine includes the steps of heating to 50 to 120° C. a solution mixture in which a necessary amount of an azide salt and a dicyanamide salt in an amount corresponding to 1 to 80 wt % of a necessary amount are added to a solvent, adding an acid in an amount of 1.54 to 2.22 chemical equivalents of the dicyanamide salt in the solution mixture to carry out a reaction at 50 to 120° C., and then adding an acid and a dicyanamide salt solution in which the remaining dicyanamide salt is dissolved in a solvent to promote the reaction. Bis-(1(2)H-tetrazol-5-yl)amine is obtained according to the production method. | 01-05-2012 |
20130190505 | Hydrothiolation of Unactivated Alkenes - The present invention is a method for promoting hydrothiolation of an unactivated alkenes with a thiol using gallium triflate. | 07-25-2013 |
20130317232 | ALTERNATIVE TO TETRAZENE - Embodiments of materials suitable for use as a replacement for Tetrazene and methods of preparing such materials are described. In one embodiment, the material comprises MTX-1, as well as simple salts or complexes derived therefrom. The methods of preparing such materials include combining Tetrazene and an acid to form a suspension, where the acid is nitric acid, sulfuric acid, perchloric acid, or hydrochloric acid. A nitrite salt may be added to the suspension, where the nitrite salt is sodium nitrite, lithium nitrite, potassium nitrite, an aqueous solution of sodium nitrite, an aqueous solution of lithium nitrite, or an aqueous solution of potassium nitrite. In some embodiments, the suspension is stirred until the suspension has a white appearance. | 11-28-2013 |
20140066630 | PROCESS FOR THE PREPARATION OF BIS-(1(2)H-TETRAZOL-5-YL)-AMINE MONOHYDRATE - A process for the preparation of Bis-(1(2)H-tetrazol-5-yl)-amine monohydrate. | 03-06-2014 |
20140171657 | ENERGETIC ACTIVE COMPOSITION COMPRISING A DIHYDROXYLAMMONIUM SALT OR DIAMMONIUM SALT OF A BISTETRAZOLEDIOL - The invention relates to an energetic active composition comprising a dihydroxylammonium salt or diammonium salt of 5,5′-bistetrazole-1,1′-diol, 5,5′-bistetrazole-1,2′-diol or 5,5′-bistetrazole-2,2′-diol or a mixture of at least two of these salts. | 06-19-2014 |
20140206885 | FACILE METHOD FOR PREPARATION OF 5-NITROTETRAZOLATES USING A FLOW SYSTEM - Described are methods for preparing salts of 5-nitrotetrazolate that include reacting aqueous solutions of 5-aminotetrazole, an acid, and sodium nitrite in a continuous flow system at an elevated temperature. | 07-24-2014 |
20150361057 | FACILE METHOD FOR PREPARATION OF 5-NITROTETRAZOLATES USING A BATCH SYSTEM - Described are methods for preparing salts of 5-nitrotetrazolate by reacting 5-aminotetrazole, an acid, and sodium nitrite in water in a batch reaction at an elevated temperature. As examples, the acid is nitric acid, sulfuric acid, perchloric acid, or hydrochloric acid, and the elevated temperature is at or above 65° C. | 12-17-2015 |
20160130238 | New Process to make non nucleosidal reverse transcriptase inhibitors (NNRTI) for the treatment of HIV - A chemical process that can form pharmaceutically acceptable medicaments NNRTI's for the treatment of HIV starting from thiotriazole compounds. The chemical process can form thiotetrazoles such as 2-((1-(naphthalen-1-yl)-1H-tetrazol-5-yl) thio)-N-(2-nitrophenyl)actetamide that is, a potent NNRTI with nanomolar activity. | 05-12-2016 |
548252000 | Chalcogen attached indirectly to the tetrazole ring by nonionic bonding | 63 |
20090111994 | Method for The Production of Losartan - The present invention relates to a novel process for preparing losartan, an imidazole derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2′-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazole, and pharmacologically active salts thereof. The invention further relates to novel intermediates which are suitable for preparing losartan and to novel processes for preparing intermediate compounds which are suitable for preparing losartan. | 04-30-2009 |
20090192318 | Method of preparation of N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-y1) [1,1'-biphenyl]-4-y1]methyl]-L-valine (valsartan) - From the starting 4-bromomethyl-2′-(1-triphenylmethyltetrazol-5-yl)biphenyl, N-[(2′(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester of formula 7 is obtained via a reaction with L-valine benzyl ester, and is converted to valsartan of formula I via a reaction with valeryl chloride and removing of protective groups. The method consists in converting, with hydrochloric acid, N-[(2′-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester of formula 7, obtained in the first stage, to N-[(2′-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-(L)-valine benzyl ester hydrochloride of formula III, which is optionally re-crystallized. | 07-30-2009 |
20090240060 | PROCESS FOR THE PREPARATION OF PURE IRBESARTAN - A process for the manufacturing of a pure irbesartan comprising converting irbesartan or a protected derivative thereof into an isolated hydrohalide acid addition salt, whereupon said hydrohalide acid addition salt is converted into the irbesartan is described. | 09-24-2009 |
20090306397 | Method for the production of substituted azoles - The novel process for preparing substituted azoles allows compounds of the general formula (I) and/or their salts and/or their acid addition compounds | 12-10-2009 |
20100190996 | Process for the Preparation of Losartan - The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan. | 07-29-2010 |
20100222597 | Process for the preparation of losartan - The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method. | 09-02-2010 |
20110098481 | NOVEL EP4 AGONIST - Provided is a compound represented by the formula (1): | 04-28-2011 |
20110172435 | Treatment Of Inflammatory Bowel Disease - Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I | 07-14-2011 |
20110184187 | PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES - The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives. | 07-28-2011 |
20120004420 | PROCESS FOR PREPARATION OF 1-ALKYL-5-BENZOYL-1H-TETRAZOLE DERIVATIVES - The present invention provides a process for preparation of 1-alkyl-5-benzoyl-1H-tetrazole derivative including a step 1 of reacting a ketoamide derivative represented by formula (I) (in formula (I), A represents a halogen atom or the like; n represents an integer of 0 to 5; Y represents an alkyl group) with a halogenating agent to obtain an imidoyl halide derivative represented by formula (II) (in formula (II), A, n and Y are as defined above; X represents a halogen atom); and a step 2 of reacting the imidoyl halide derivative represented by formula (II) with an azide represented by formula (III) (in formula (III), M represents an alkali metal or the like; m represents 1 or 2) to obtain a 1-alkyl-5-benzoyl-1H-tetrazole derivative represented by formula (IV) (in formula (IV), A, n and Y are as defined above). | 01-05-2012 |
20120330026 | PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES - The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives. | 12-27-2012 |
20140058113 | DEPROTECTION METHOD FOR PROTECTED HYDROXYL GROUP - To deprotect an alcoholic hydroxyl group protected by a t-butyldimethylsilyl group without influencing a functional group unstable to an acid. In the presence of a solvent, an alcohol having a hydroxyl group protected by a t-butyldimethylsilyl group is deprotected in the presence of an acid or an acid salt having a pKa of from 1.0 to 3.0 in water. | 02-27-2014 |
20150299145 | PROCESS FOR THE PREPARATION OF N-HYDROXY-1-(1-ALKYL-1H-TETRAZOL-5-YL)-1-PHENYLMETHANIMINE DERIVATIVES - The present invention relates to a process for the preparation of N-hydroxy-1-(1-alkyl-1H-tetrazol-5-yl)-1-phenylmethanimine derivatives of the general formula (I) | 10-22-2015 |
548253000 | The chalcogen, X, is in a -C(=X)- group | 50 |
20080214830 | Process for Producing 2-(N-Butyl)-3-[[2'-(Tetrazol-5-Yl)Biphenyl-4-Yl]Methyl]-I,3-Diazaspiro[4,4] Non-1-En-4-One - Disclosed herein a process for producing 2-(n-butyl)-3-[[2′-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one of formula (I) in pure form by using selective solvent system and cost efficient raw materials and reagents. | 09-04-2008 |
20080312451 | Process For the Preparation of Sartan Derivatives and Intermediates Useful in Such Process - The invention provides a process for the preparation of a sartan derivative of formula (I) (formula as filed in paper form) (I) wherein the substituents have the meaning indicated in the description, or a pharmaceutically acceptable salt thereof, comprising reacting 2-cyanophenylboronic acid or a derivative thereof with a p-halobenzyl-1H-imidazole derivative of formula (VI), (formula as filed in paper form) (VI) wherein (part of formula as filed in paper form), X, Y, R | 12-18-2008 |
20090018344 | PROCESS FOR THE PREPARATION OF CANDESARTAN CILEXETIL - The invention relates to process for the preparation of Candesartan cilexetil. More particularly, it relates to the preparation of pure candesartan cilexetil by the deprotection of Trityl candesartan cilexetil with inorganic acids. | 01-15-2009 |
20090111995 | Process for the manufacture valsartan - The present invention relates to a process for the manufacture of an angiotensin receptor blocker (ARB; also called angiotension II receptor antagonist or AT | 04-30-2009 |
20090131680 | PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL - The present invention relates to an improved process for the manufacture of olmesartan and pharmaceutically acceptable salts and esters thereof as an active ingredient of a medicament for the treatment of hypertension and related diseases and conditions. | 05-21-2009 |
20090203920 | METHOD FOR ISOLATING 5-SUBSTITUTED TETRAZOLES - The invention relates to a method for isolating 5-substituted tetrazoles of general formula (I) | 08-13-2009 |
20090203921 | PROCESSES FOR THE PREPARATION OF INTERMEDIATES OF VALSARTAN - The present invention relates to processes for the preparation of intermediates of valsartan. | 08-13-2009 |
20090216026 | Novel synthesis of irbesartan - Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid. | 08-27-2009 |
20090281326 | Process For the Preparation of Angiotensin II Antagonist - The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetra-zol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2′-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2′-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2′-(1-triphenylmethyl-tetra-=zol-5-yl)[1,1′biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2′-(1-H-tetrazol-5-yl)[1,1′biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by 11-12-2009 | |
20090318706 | Process for the Preparation of Candesartan Cilexetil - The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid. | 12-24-2009 |
20100056797 | Process for the Preparation of Irbesartan - The present invention relates to an improved process for the preparation of 2-n-butyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]-1,3-diazaspiro[4.4]non-1-en-4-one (Irbesartan) | 03-04-2010 |
20100076200 | Purification of olmesartan medoxomil - The present invention provides a process for purifying olmesartan medoxomil. | 03-25-2010 |
20100081826 | 7-PYRROLYL TETRACYCLINE COMPOUNDS AND METHODS OF USE THEREOF - A compound of Formula (I): | 04-01-2010 |
20100094023 | BENZOYLPYRAZOLES AND HERBICIDE - Benzoylpyrazoles represented by the following formula (I), and use thereof as herbicides. | 04-15-2010 |
20100113798 | PROCESS FOR PREPARATION OF IRBESARTAN - A process for the preparation of Irbesartan of formula (I) using the step of, | 05-06-2010 |
20100121072 | Candesartan cilexetil polymorphs - Provided are candesartan cilexetil forms and methods of their preparation. Also provided are pharmaceutical compositions prepared by combining at least one pharmaceutically-acceptable excipient with at least one candesartan cilexetil form of the invention. | 05-13-2010 |
20100152458 | COUPLING REACTIONS USEFUL IN THE PREPARATION OF (1H-TETRAZOL-5-YL) BIPHENYL DERIVATIVES - The present invention relates to a process for the manufacture of intermediates that may be used for the manufacture of ARBs (also called angiotension II receptor antagonists or AT | 06-17-2010 |
20100160643 | Process for Preparing Trityl Olmesartan Medoxomil and Olmesartan Medoxomil - A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, | 06-24-2010 |
20100160644 | NOVEL PROCESSES OF MAKING HYDROXY-1-AZO-DERIVATIVES AS TPO MIMETICS - Invented are novel processes of making hydroxy-1-azo-benzene derivatives as TPO mimetics. Also invented are novel intermediates used in the novel processes. Also invented are pharmaceutical compositions comprising compounds made by novel processes. | 06-24-2010 |
20100174091 | Process for the preparation of tetrazolytetrahydrocyclopentapyrazoles - A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R | 07-08-2010 |
20100197932 | PROCESS FOR PREPARING PURE VALSARTAN - An improved process for the preparation of substantially pure valsartan employing suitable reagents such as chelating agent and reaction conditions. | 08-05-2010 |
20100197933 | Process for the Preparation of Candesartan Cilexetil - The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid. | 08-05-2010 |
20100210852 | PROCESS FOR THE PREPARATION OF CANDESARTAN CILEXETIL - The present invention relates to an improved process for the preparation of tritylated candesartan acid of formula (I) | 08-19-2010 |
20100210853 | PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL - There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2′-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co-distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0° C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil. | 08-19-2010 |
20100234614 | PROCESS FOR PURE IRBESARTAN - The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3 -diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield. | 09-16-2010 |
20100249429 | PROCESS FOR THE MANUFACTURE OF VALSARTAN - The present invention relates to a process for the manufacture of an angiotensin receptor blocker (ARB; also called angiotension II receptor antagonist or AT | 09-30-2010 |
20100249430 | PROCESS FOR PREPARING VALSARTAN - The invention relates to novel compound of formula (IV), which is an organic acid salt of N-[(2′-cyanobipheny1-4-yl)methyl]-(L)-valine ester. This compound is an useful intermediate for process of preparation of Valsartan of formula (I), chemically known as (S)-N-(1-Carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2′-(1H-terazol-5-yl)biphenyl-4-ylmethyl]amine. This invention also relates to a process for preparing Valsartan using novel intermediate of formula (IV). | 09-30-2010 |
20110034701 | ONE POT PROCESS FOR THE PREPARATION OF CANDESARTAN - Present invention is to provide one pot synthesis of candesartan without isolating the ester intermediate. | 02-10-2011 |
20110092713 | METHOD FOR PRODUCING 1-BIPHENYLMETHYLIMIDAZOLE COMPOUND - The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. | 04-21-2011 |
20110105763 | Process for Preparing Valsartan - An N-[(2′-(1-triphenyl methyl tetrazole-5-yl)biphenyl]-4-yl]methyl]-L-valine benzyl ester organic salt of formula (IVA) wherein A represents an organic carboxylic acid, a process for its preparation and its use in the synthesis of valsartan or salts thereof. | 05-05-2011 |
20110275828 | PROCESS FOR THE PREPARATION OF IRBESARTAN - The present invention relates to a process for the preparation of 2-butyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]-1,3-diazaspiro[4,4]non-1-en-4-one by reaction of the corresponding nitrile with sodium azide and piperazine or its acid salt. | 11-10-2011 |
20120022268 | New Salt Hydrates - The invention relates to new forms of salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt. | 01-26-2012 |
20120029201 | PROCESS FOR THE PREPARATION OF CANDESARTAN CILEXETIL - The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid. | 02-02-2012 |
20120071665 | METHOD FOR PRODUCING OLMESARTAN MEDOXOMIL - A method for producing high-purity olmesartan medoxomil is provided in which a solvent containing water is used in steps of tritylation and DMDO esterification of olmesartan. | 03-22-2012 |
20120088919 | DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention relates to compounds having the formula: | 04-12-2012 |
20120116093 | ONE POT PROCESS FOR PREPARING 2-BUTYL-3-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1,3-DIAZASP- IRO [4, 4] NON-1-EN-4-ONE (IRBESARTAN) - A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent. | 05-10-2012 |
20120184750 | PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL - The present invention provides an improved process for the preparation of olmesartan medoxomil, which is free of OLM-acid and has lower amount of eliminate and acetic acid impurity. | 07-19-2012 |
20120184751 | POLYMORPHIC FORM OF OLMESARTAN MEDOXOMIL - The present invention relates to a polymorphic form of olmesartan medoxomil and a process for the preparation of crystalline olmesartan medoxomil. | 07-19-2012 |
20120238761 | PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS - The present invention relates to processes for the manufacture of an angiotensin receptor blocker (ARB; also called angiotension II receptor antagonist or AT | 09-20-2012 |
20120330027 | PROCESS FOR THE PREPARATION OF 5-SUBSTITUTED 1-ALKYLTETRAZOLES - The present invention relates to a process for the preparation of | 12-27-2012 |
20130131351 | GPR120 RECEPTOR AGONISTS AND USES THEREOF - GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. | 05-23-2013 |
20130144067 | PROCESS FOR THE PREPARATION OF VALSARTAN - The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (Ia), (Ib), and (Ic), which comprises: (i) condensing 2-(4′-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(1-oxopentyl)-N-[[2′-(2-tributyltinte-trazol-5-yl)-(1,1′-biphenyl)-4-yl]methyl]-(L)-valine methyl ester of formula (VHIb) free from thermal degradation impurity (Villa); (v) hydrolyzing the compound of formula (VHIb) in the presence of alkaline conditions to produce Valsartan (I). | 06-06-2013 |
20130190506 | PROCESS FOR OLMESARTAN MEDOXOMIL - The present invention provides a process for the preparation of substantially pure trityl olmesartan medoxomil. The present invention also provides a process for purification of trityl olmesartan medoxomil. The present invention further provides a process for purification of olmesartan medoxomil. | 07-25-2013 |
20140046075 | DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds of formula I: | 02-13-2014 |
20140179930 | PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL - The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I). | 06-26-2014 |
20140316142 | PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS AND INTERMEDIATES THEREOF - The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine of Formula 1 | 10-23-2014 |
20150291566 | NOVEL TETRAZOLO HYDRAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER - Provided are novel tetrazolo hydrazone derivatives or pharmaceutically acceptable salts thereof. The derivatives and the salts may inhibit the proliferation of cancer cells in a low molar concentration and inhibit the activity of cancer cells through the regulation of expression of apoptosis-related genes or the like, thus expressing excellent anti-cancer activity, and therefore, can be used effectively in preventing or treating cancer. | 10-15-2015 |
20150322021 | METHOD FOR PRODUCING 1-H-TETRAZOLE DERIVATIVE - The present invention provides a method for producing a 1H-tetrazole derivative by reacting an azide compound represented by general formula (II) and a cyanide compound represented by general formula (III) in a flow reactor to produce a compound represented by general formula (I) (wherein, Y represents an alkyl group, aryl group, arylalkyl group, substituted silyl group or substituted silylalkyl group, Z represents —CO—, —SO | 11-12-2015 |
20160102079 | ACETONE SOLVATE CRYSTALS OF TRITYL OMESARTAN MEDOXOMIL - Acetone solvate crystals of trityl olmesartan medoxomil are provided. | 04-14-2016 |
20160251338 | AMORPHOUS ALLISARTAN ISOPROXIL, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION CONTAINING AMORPHOUS ALLISARTAN ISOPROXIL | 09-01-2016 |
548254000 | Nitrogen attached indirectly to the tetrazole ring by nonionic bonding | 4 |
20090076281 | PROCESS FOR THE PREPARATION OF LOSARTAN AND ITS SALTS - The invention relates to the preparation of losartan and losartan potassium. More particularly, the invention relates to the preparation of losartan and losartan potassium in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans. | 03-19-2009 |
20090281327 | PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL - The present invention provides a process for the preparation of Olmesartan medoxomil] by condensing the ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate with 4-[2-(trityl tetrazol-5-yl)phenyl]benzyl bromide to obtain ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate and then hydrolyzing ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methyl imidazole-5-carboxylate to obtain trityl Olmesartan dihydrate followed by reacting trityl Olmesartan dihydrate with 4-chloromethyl-5-methyl-2-oxo-1,3-dioxolene to obtain trityl Olmesartan medoxomil and then deprotecting trityl Olmesartan medoxomil to obtain Olmesartan medoxomil. | 11-12-2009 |
20090281328 | PDK-1/AKT SIGNALING INHIBITORS - A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: | 11-12-2009 |
20100063299 | Process for Preparing Irbesartan - Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Irbesartan, or a pharmaceutically acceptable salt thereof, in high yield and purity. | 03-11-2010 |