- Novel and efficient debenzylation of N-benzyltetrazole derivatives with the rosenmund catalyst
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The Rosenmund catalyst (Pd/BaSO4) was found to efficiently catalyze debenzylation of N-benzyltetrazole derivatives with ammonium formate by catalytic transfer hydrogenation under mild conditions. The protocol has been applied to functionalized substrates to provide various angiotensin II receptor blockers in excellent yields.
- Seki, Masahiko
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Read Online
- Efficient synthesis of losartan, a nonpeptide angiotensin II receptor antagonist
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A highly efficient, convergent approach to the synthesis of the angiotensin II receptor antagonist losartan (1) is described. Directed ortho-metalation of 2-trityl-5-phenyltetrazole provides the key boronic acid intermediate 10 for palladium-catalyzed biaryl coupling with bromide 5 obtained from the regioselective alkylation of the chloroimidazole 2. This methodology overcomes many of the drawbacks associated with previously reported syntheses.
- Larsen,King,Chen,Corley,Foster,Roberts,Yang,Lieberman,Reamer,Tschaen,Verhoeven,Reider,Lo,Rossano,Brookes,Meloni,Moore,Arnett
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Read Online
- Unusual detritylation of tritylated tetrazole in Sartan molecules
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Tritylated tetrazole of 2a underwent unusual detritylation under basic reaction condition during the synthesis of methyl ether of olmesartan medoxomil 1. The unusual detritylation was found to be a common feature in the case of all tetrazole containing Sartan molecules (3-7).
- Srimurugan, Sankareswaran,Suresh, Paulsamy,Babu, Balaji,Hiriyanna, Salmara Ganeshbhat,Pati, Hari Narayan
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Read Online
- Preparation method of losartan
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The invention provides a preparation method of losartan, wherein the preparation method comprises the steps: reacting a nitrile intermediate shown in the specification with an azide reagent in a solvent, adding an inorganic alkali aqueous solution selected from carbonate or bicarbonate, washing, and separating out an intermediate material layer; and further separating the intermediate material layer to obtain losartan. The azide ions after the reaction can be basically and completely removed by using the conventional inorganic alkali solution, the removal effect is good, the preparation process is simple and convenient, the operation conditions are mild and easy to control, and the method is suitable for large-scale industrial production.
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Paragraph 0033-0042
(2021/04/21)
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- Method for preparing high-purity losartan
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The invention relates to a method for preparing high-purity losartan. The method comprises steps as follows: (1), a losartan crude product is added to an organic solvent or a mixed solvent of an organic solvent and water, and the mixture is heated to reach 20-80 DEG C and stirred; (2), the system is cooled directly or cooled after water is added or cooled to 0-5 DEG C after a part of solvent is evaporated, a material is precipitated, filtered and dried, and losartan is obtained, wherein the organic solvent used in the step (1) is any one of tetrahydrofuran, butanone, acetone and methyl alcohol or is a mixed solvent of any one of the four solvents and water. The losartan obtained with the method has high purity, any individual impurity can be reduced to 0.2% or even under 0.1%, the purity of the losartan can reach 99.5%, the cost of the method is lower, the refining yield is high, and the method is very simple in operation, environment-friendly and suitable for industrial production.
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Paragraph 0020-0034
(2020/10/19)
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- Preparation method of losartan
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The invention provides a preparation method of losartan. The losartan is prepared by reacting a cyano-containing intermediate as shown in a formula (I), which is described in the specification, with an azide reagent in toluene in the presence of a catalyst. After the reaction is finished, azide ions are removed through the following procedures: adding water to divide a reaction system into three layers, separating out a middle layer, adding n-butyl alcohol into the middle layer for dilution, and adding triphenylphosphine into the obtained diluted solution to remove the residual azide ions in the diluted solution. According to the preparation method, sodium nitrite is not needed, so formation of the genotoxic impurity nitrosamine is fundamentally eradicated; the obtained target losartan isgood in purity and high in yield; and the method is simple and convenient in preparation process, mild and easily controllable in operation conditions, good in safety, and suitable for large-scale industrial production.
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Paragraph 0054-0059
(2019/11/29)
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- Nickel-Catalyzed Denitrogenative ortho-Arylation of Benzotriazinones with Organic Boronic Acids: an Efficient Route to Losartan and Irbesartan Drug Molecules
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Denitrogenative ortho-arylation, vinylation and methylation of 1,2,3-benzotriazin-4-(3H)-ones with organic boronic acids catalyzed by nickel complexes to give a wide range of o-substituted benzamides were demonstrated. Further, the catalytic reaction is successfully applied to the synthesis of the popular hypertensive drugs losartan and irbesartan in high yields. (Figure presented.).
- Thorat, Vijaykumar H.,Upadhyay, Nitinkumar Satyadev,Cheng, Chien-Hong
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p. 4784 - 4789
(2018/11/10)
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- A trityl protecting group by removing method of preparing losartan medicine
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The invention discloses a method for preparation of a Sartan drug by removal of a triphenylmethyl protective group. The method includes: under the catalysis of an insoluble weak acid, subjecting a Sartan prodrug and methanol to deprotection reaction, and after complete reaction, conducting aftertreatment to obtain the Sartan drug. The method has the characteristics of low cost, few side product, high quality product, and simple aftertreatment. At the same time, montmorillonite can be taken as insoluble weak acid, and the cost is low, thus being convenient for industrial production.
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Paragraph 0032-0039; 0047-0051
(2018/07/30)
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- Sartan compound discoloration method
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The invention relates to a sartan compound discoloration method. The method comprises the following steps: adding irbesartan or losartan crude products containing pigment impurities into solvent, and dissolving; and adding hydroboration reagent, stirring for discoloration, and crystallizing through dissociation, cooling, distillation and other means to obtain white losartan or irbesartan. The method has the advantages of mild reaction conditions, short operating cycle, high discoloration efficiency and environment friendliness, and is suitable for industrial production.
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Paragraph 0020; 0022; 0028
(2017/07/08)
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- High-purity Losartan preparation method
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The invention provides a high-purity Losartan preparation method. The method comprises the following steps: adding a catalyst having a structural formula as shown in Formula A into organic solvent, dropwisely adding acid, and stirring to perform salification; and adding a compound 1, sodium azide and tetrabutylammonium bromide into the system, heating, reacting with stirring, and performing posttreatment to obtain high-purity Losartan. The Losartan obtained by the invention is high in purity and favorable in appearance; the purity can be up to 98.4%; and the content of a single impurity can be reduced to 0.2%. The method is low in cost and high in yield; and meanwhile, the method provided by the invention is simple to operate and environment-friendly, thereby being suitable for industrial production.
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Paragraph 0030-0032; 0034; 0038; 0041; 0044; 0047; 0050-0059
(2017/09/02)
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- Pd(ii)-catalyzed, controllable C-H mono-/diarylation of aryl tetrazoles: Concise synthesis of Losartan
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A palladium(ii)-catalyzed C-H arylation directed by tetrazole, a metabolically stable surrogate for the carboxylic acid group in drug design, has been developed. Excellent mono-/di-selectivity was achieved through adjustment of the protecting site on the tetrazole ring. The synthetic utility of this new transformation was demonstrated in the concise total synthesis of Losartan. This journal is
- Ding, Yan-Jun,Li, Yan,Dai, Sheng-Yu,Lan, Quan,Wang, Xi-Sheng
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p. 3198 - 3201
(2015/03/18)
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- DEPROTECTION METHOD FOR TETRAZOLE COMPOUND
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The present invention relates to a method of deprotecting a tetrazole compound, useful as an intermediate for angiotensin II receptor blockers, and provides a novel production method of angiotensin II receptor blockers. Provided is a production method of a compound represented by the formula [3] or [4] or a salt thereof, including (i) reducing a compound represented by the formula [1] or [2] or a salt thereof in the presence of a metal catalyst and an alkaline earth metal salt, or (ii) reacting the compound with a particular amount of Br?nsted acid: wherein each symbol is as defined in the present specification.
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- An efficient and green synthetic route to losartan
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A practical, efficient and green process for the preparation of losartan, an antihypertensive drug, has been developed with an overall yield of 58.6%. The key step is the synthesis of the two key intermediates 2-butyl-4-chloro-3H-imidazole-5-carbaldehyde (BCFI) and 2-cyano-4'-methyl biphenyl (OTBN). BCFI was synthesised from valeronitrile and acetyl chloride by three steps with an overall yield of 69%; OTBN was obtained in 86% yield by the coupling of o-chlorobenzonitrile with p-methylphenylmagnesium chloride in tetrahydrofuran in the presence of manganese chloride and chlorotrimethylsilane. The above route was successfully operated in at a pilot-plant operation.
- Shuangxia, Feng,Zheng, Gu,Yelv, Tang,Hui, Liu,Guofang, Jiang
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p. 451 - 454
(2015/11/03)
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- PROCESS FOR PRODUCTION OF BIPHENYL DERIVATIVE
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The invention provides a production method of a biaryltetrazole derivative useful as an intermediate for an angiotensin II receptor antagonist. The method comprises reacting an aryltetrazole derivative with a benzene derivative, deprotecting or reducing the resulting compound, and halogenating the deprotected or reduced compound
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Page/Page column 32
(2012/09/22)
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- NOVEL ZINC AZIDE COMPLEX AND A PROCESS FOR PREPARING TETRAZOLE DERIVATIVES USING THE SAME
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The present invention relates to a novel zinc azide complex. The present invention also relates to a process for preparing 5-substituted-1H-tetrazole derivatives from nitrile derivatives by using the zinc azide complex. According to the present invention, in particular, pharmaceutically active compounds for treating hypertension or intermediates useful for preparation thereof can be prepared effectively.
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Page/Page column 10
(2012/11/13)
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- An efficient, commercially viable, and safe process for preparation of losartan potassium, an angiotensin II receptor antagonist
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An efficient, commercially viable and safe process for the preparation of losartan potassium, an antihypertensive drug substance, with an overall yield of 55.5% and ～99.9% purity (including five chemical reactions and two recrystallizations) and meeting all other regulatory requirements is described. Formation and control of all the possible impurities are also described.
- Madasu, Suri Babu,Vekariya,Koteswaramma, Ch,Islam, Aminul,Sanasi, Paul Douglas,Korupolu, Raghu Babu
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p. 2025 - 2030
(2013/02/25)
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- Synthesis of angiotensin II receptor blockers by means of a catalytic system for C-H Activation
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A highly efficient catalytic system for C-H activation has been worked out that involves inexpensive RuCl3·xH2O and a specific amount of PPh3. This procedure has been successfully applied to a practical synthesis of angiotensin II receptor blockers (ARBs). The residual ruthenium that existed in the reaction mixture was thoroughly removed by treatment with properly selected metal scavengers. The new process permits ready access to the important class of drugs in a highly atom-economical and sustainable manner (Figure presented).
- Seki, Masahiko,Nagahama, Masaki
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p. 10198 - 10206
(2012/02/03)
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- PHARMACEUTICAL PREPARATION CONTAINING NON-DIHYDROPYRIDINE CALCIUM CHANNEL BLOCKER AND ANGIOTENSIN-2 RECEPTOR BLOCKER
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The present invention provides a pharmaceutical formulation comprising an immediate-release compartment containing an angiotensin-2 receptor blocker (ARB) as a pharmacologically active ingredient and an extended-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. Since the disclosed formulation enables the release of the two ingredients at a different time, it reduces side effects and increases the effects of the drug more than the case of separately administering the ingredients each at the same time. In addition, the formulation maximizes the effects of drug at the time of day when the complication risk of cardiovascular system diseases is highest.
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- AN IMPROVED PROCESS FOR PREPARING LOSARTAN POTASSIUM
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The present invention relates to an improved process for preparing Losartan Potassium of formula (I).
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Page/Page column 12
(2010/04/06)
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- Process for the Preparation of Losartan
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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.
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Page/Page column 7-8
(2010/08/07)
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- Process for the preparation of losartan
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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.
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Page/Page column 8
(2010/09/07)
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- METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTION GROUP
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The present invention relates to a method of removing triphenylmethane protection group. The method for preparing biphenyl benzoic acid derivatives of the present invention is economically advantageous and very excellent in the aspect of improving process in that: process safety is secured by using acidic ion exchange resin in the presence of organic solvent instead of using highly corrosive acid; the reaction takes much less time than do the conventional reactions which use only anhydrous methanol and few sub-reaction does occur; and the ion-exchange resin of the present invention is excellent for mass-processing because the resin can be collected and recycled only by filtration after being used.
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Page/Page column 17-18
(2010/07/02)
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- INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS
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The present invention relates to novel substituted biphenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists, to a process for the synthesis of them and to a process for the conversion thereof to said molecules.
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Page/Page column 29
(2010/11/30)
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- METHOD FOR PREPARING LOSARTAN
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The present invention relates to a simple and efficient method for preparing losartan, which comprises the steps of reacting a nitrile compound with triethylamine hydrochloride and sodium azide in an organic solvent; and crystallizing losartan directly from the reaction solution.
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Page/Page column 6; 7
(2008/06/13)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LOSARTAN
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The invention relates to an improved process for the preparation of Losartan. Which comprises reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and alkali, and reducing resulting cyano aldehyde to get cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan .
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Page/Page column 9; 13; 16-17
(2008/06/13)
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- AN IMPROVED PROCESS FOR THE MANUFACTURE OF LOSARTAN POTASSIUM
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The present invention relates to an improved process for the manufacture of Losartan potassium. The process comprises of condensation of 2-butyl-4-chloro-5-formyl imidazole with 2-cyano-4-bromomethyl biphenyl in a biphasic solvent system under phase transfer catalysis followed by insitu reduction using sodium borohydride. The obtained product is converted to Losartan by treating with sodium azide and an amine salt. Losartan is then converted to its potassium salt by treating it with potassium hydroxide in alcohol.
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Page/Page column 13-14
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF LOSARTAN
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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 get cyano aldehyde, reacting the cyano aldehyde sodium azide in the presence of tributyl tin chloride to form aldehyde tetrazole , reducing the aldehyde tetrazole with sodium borohydride to give Losartan and , if desired , converting it to its potassium salt by known method .
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Page/Page column 16-17; 19-20
(2008/06/13)
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- A process for the preparation of sartan derivates and intermediates useful in such process
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The invention provides a process for the preparation of a sartan derivative of formula (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), wherein , X, Y, R1 and R2 are as defined above, and Z is I, Br or Cl, in the presence of a transition metal catalyst and an inorganic or organic base. The invention also provides new intermediates of formula (V), wherein M is an alkali metal or an NR4R5R6R7 group; and of formula (II)
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Page/Page column 9
(2008/06/13)
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- A process for the preparation of losartan derivatives by chlorination and reduction of the respective 1H-imidazole-5-carbaldehydes
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The invention provides a process for the preparation of a sartan derivative of formula (I): wherein R = C2-C7 straight or branched alkyl or C3-C9 cycloalkyl, or a pharmaceutically acceptable salt thereof, comprising the steps of chlorinating and reducing, in any order, a compound of formula (III): wherein R is defined as above to form a compound of formula (VI), wherein R is defined as above and then deprotecting said compound of formula (VI) to obtain the sartan derivative of formula (I), and optionally converting said sartan derivative into one of its pharmaceutically acceptable salts. A preferred embodiment of this invention is a process for the preparation of losartan and, particularly, its potassium salt.
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Page/Page column 11
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF LOSARTAN AND ITS SALTS
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The invention relates to the preparation of losartan and its salts (e.g., losartan potassium). More particularly, the invention relates to the preparation of losartan and its salts (e.g., losartan potassium) in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating losartan, its salts (e.g., losartan potassium ) and/or in vivo cleavable prodrugs thereof (collectively "the compounds of the invention") into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.
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Page/Page column 12
(2008/06/13)
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- Process for preparing losartan
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A process for preparing losartan, comprising reacting trityl losartan with an aqueous acid.
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Page/Page column 3
(2008/06/13)
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- PROCESS FOR PRODUCING BIPHENYL-TETRAZOLE COMPOUNDS
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A process for producing biphenyl-tetrazole compounds in pure form by deprotecting compounds of the following formula (II): proposes to use acids in an alcohol-ketone-water mixture and/or a mixture of alcohol-alcohol-keton-water to remove the Ph3C-protecting group.
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Page/Page column 10-11
(2008/06/13)
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- METHOD FOR PRODUCING BIPHENYL-TETRAZOLE COMPOUNDS
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A method for producing biphenyl-tetrazole compounds by deprotecting compounds of the formula (II) proposes to use hydroxylammonium salts to remove the Ph3C-protecting group.
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Page/Page column 11-12
(2008/06/13)
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- METHOD FOR THE PRODUCTION OF LOSARTAN
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The invention relates to a novel method for the production of losartan, an imidazol derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol and the pharmacologically active salts thereof. The invention also relates to novel intermediate products which are suitable for the production of losartan, and to novel methods for the production of intermediate compounds which are suitable for the production of losartan. One aspect of the invention is a method for the production of a compound of general formula (I), which can arise as an intermediate step in the inventive representation of losartan.
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Page/Page column 16; 18; 20; 29
(2008/06/13)
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- PROCESS FOR THE SYNTHESIS OF TETRAZOLES
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A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.
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Page/Page column 10
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES
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The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
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Page/Page column 51-52
(2008/06/13)
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- Phenyltetrazole compounds
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Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.
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Page/Page column 6
(2010/02/12)
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- PROCESS FOR THE PREPARATION OF LOSARTAN POTASSIUM FORM I
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The present invention relates to a novel method for preparing trityl losartan and losartan potassium form I.
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Page/Page column 13
(2008/06/13)
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- A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP
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A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1‘-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R1, R2 and R3 can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R2 and R3 can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
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Page/Page column 10
(2008/06/13)
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- Phenyltetrazole compounds
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Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.
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Page/Page column 4
(2010/02/11)
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- Process for preparing 2,4,5-trisubstituted imidazoles from N-acylated alpha-amino nitriles
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The invention is a process for preparing an imidazole of formula I which comprises treating an N-acylated α-amino nitrile with a phosphine and a carbon tetrahalide of the formula CX4, wherein X is Cl or Br, to form a haloimidazole of the formula wherein R1 is selected from the group consisting of hydrogen, C1-6alkyl, —CH2-aryl, and aryl; and R2 is selected from the group consisting of hydrogen, C1-6alkyl, —CH2—O-aryl and aryl; and X is selected from the group consisting of Cl and Br.
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- PREPARATION OF NEW PHARMACEUTICALLY SUITABLE SALT OF LOSARTAN AND FORMS THEREOF WITH NEW PURIFICATION AND ISOLATION METHODS
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Pharmaceutically suitable crystalline and amorphous alkali and earth-alkali salts of 2-n-butyl-4-chloro-5-h idroxymethyl-1-[[2'-(1 H-tetrazole-5-yl)[1.1'-biphenyl]-4-yl]-1 H-imidazole have been prepared and new manufacturing, purification and isolation procedure for said salts in high purity have been described. Stable pharmaceutical compositions containing new crystalline potassium salts of 2-n-butyl-4-chloro-5-hidroxymethyl-1-[[2'-(1 H-tetrazole-5-yl)[1.1'-biphenyl]-4-yl]-1 H-imidazole have been prepared.
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Page/Page column 51-52
(2008/06/13)
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- PROCESSES FOR PREPARING LOSARTAN AND LOSARTAN POTASSIUM
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Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.
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Page/Page column 16
(2008/06/13)
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- Use of an angiotensin II receptor antagonist for the preparation of drugs to increase the survival rate of renal transplant patients
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The present invention relates to the use, for the preparation of drugs to increase the survival rate of transplant patients, including renal and heart transplant patients, of a therapeutically effective amount of an angiotension II receptor antagonist compound, such as the class of substituted imidazoles represented by formula (I) and in particular by losartan potassium, 2-butyl-4-chloro-[(2′-tetrazol-5-yl)biphenyl-4-il]methyl]-5-(hydroxymethyl)imidazole potassium salt.
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- Crystalline or crystallized acid addition salt of losartan and purification method of losartan
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The present invention provides a crystalline or crystallized acid addition salt of Losartan useful for obtaining highly pure 2-n-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan), and a purification method of Losartan that includes production of the crystalline or crystallized acid addition salt.
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- INSULIN SENSITIVITY WITH ANGIOTENSIN II RECEPTOR BLOCKING IMIDAZOLES
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This invention relates to a novel method of using an Angiotensin II antagonist for the improvement of insulin sensitivity alone or in conjunction with the treatment of hypertension. Angiotensin II antagonists such as the class of substituted imidazoles represented by formula I: STR1 and specifically by Losartan, 2-butyl-4-chloro-1-[(2'-tetrazol-5-yl)biphenyl-4-yl]methyl]-5-(hydroxymethyl)imidazole potassium salt.
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- Polymorphs of losartan and the process for the preparation of form II of losartan
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Polymorphic forms of Losartan (Formula I) STR1 and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.
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- Treatment of atherosclerosis with angiotensin II receptor blocking imidazoles
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A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II antagonist. This method of treatment can be used in conjunction with the treatment of hypertension. Substituted imidazoles such as STR1 are useful as angiotensin II receptor antagonists for this method of treatment. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor. A method of treatment for atherosclerosis and/or reducing cholesterol using an angiotensin II receptor antagonist in combination with an HMG-Co A reductase inhibitor and an angiotensin converting enzyme inhibitor. Also within the scope of this invention are pharmaceutical compositions for this method of use.
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- Chemical process for making angiotesin II antagonist compounds
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The invention provides a novel chemical process for the manufacture of quinoline, pyridine and imidazole derivatives of the formula IV wherein Q, Y 1 and Y 2 have the various meanings defined herein, and their non-toxic salts, which are angiotensin II inhibitors. The process involves the removal of an electron-deficient phenyl group or a pyridyl or pyrimidyl group from a compound of the formula VI as defined herein.
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