81 results about "Losartan" patented technology

The invention relates to a formula of a sartan compound or a pharmaceutically acceptable salt thereof and a calcium channel blocker or a pharmaceutically acceptable salt, which belong to the technical field of medicine. The formula comprises the following components by weight proportion: 5-200 parts of [(2-n-propyl-4-methyl-1H-benzimidazole)-6-carboxamide-1-radical] methyl biphenyl tetrazolium and a carboxylic acid compound and salt thereof and 0.5-60 parts of a calcium ion retarder; the preferable scheme is 20-100 parts of the [(2-n-propyl-4-methyl-1H-benzimidazole)-6-carboxamide-1-radical] methyl biphenyl tetrazolium and the carboxylic acid compound and the salt thereof and 1-30 parts of the calcium ion retarder; the administration forms can be one of the following forms such as oral administration, inhalation, subcutaneous administration, sublingual administration, intramuscular administration, intravenous administration, transdermal administration, local administration or rectal administration. In the formula of the invention, an antihypertensive I and the calcium channel blocker or the pharmaceutically acceptable salt are studied; thus a preparation with a new formula for treating hypertension is provided. The preparation is characterized by low dosage, obvious blood pressure lowering effect and little adverse reaction.

One or more embodiments of the invention provide various novel formulations, and tablet dosage forms, comprising losartan that are non-crystalline, stable, and/or otherwise improvements over known losartan formulations. One or more embodiments of the invention further provide methods for preparing the formulation, methods for preparing the tablet dosage form, and to methods of administering the tablet dosage and/or formulation comprising losartan. The losartan-containing formulations may be administered to a user to treat hypertension, and related conditions.

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.

The invention provides a method for preparing losartan shown in a formula (I). The method comprises the following steps: reacting 2-butyl-4-chlorine-5-(hydroxymethyl)-1-{[(2'- cyano-group) xenyl-4-group]methyl} imidazole and natrium azide and triethylamine hydrochloride shown in a formula (II) in toluol; regulating the obtained reaction liquid by alkali to separate organic layers; adding a reducing agent into the collected liquid; regulating the obtained reaction liquid by acid to obtain losartan solid; and if required, refining the losartan solid by isopropyl alcohol. The method has the advantages of high yield, high purity of the losartan, low cost, little environmental pollution and suitability for industrialized production.

The invention discloses a medicinal composition for treating hypertension, and belongs to the field of medicaments. The antihypertensive medicinal composition comprises a pharmaceutically effective dose of levoamlodipine or a pharmaceutically acceptable salt thereof and losartanpotassium, wherein the levoamlodipine is weighed in free alkali; the losartan is weighed in free acid; and the weight ratio of the levoamlodipine to the losartan is 1 to 11-19. The medicinal composition does not damage the target organ while reducing the blood pressure so as to enhance the therapeutic effect and reduce the risk for therapy of a patient.

The invention relates to amlodipine series salt, generally comprising camphor sulfonic acid salt, L-aminobutanedioic acid salt, maleic acid salt and methanesulfonic acid salt and sartan compound or pharmaceutical composition of pharmaceutically acceptable thereof and preparation method of same, and kit for drug combination containing amlodipine serious salt and sartan compound composition. The composition or kit can be applied to treat patient suffering angina pectoris, atherosclerosis, and/or hypertension complicated with hyperlipemia and patient having risk of heart diseases (including human).

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.

The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds of formulas (I), (IIa), (IIIb) in hydrophilic or lipophilic form, which are useful as angiotensin II AT1 receptor antagonists with sympathetic suppressant properties. In particular, the invention provides pharmaceutical compositions containing the pharmacophoric groups of Losartan and Clonidine as well compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases through Renin Angiotensin System (RAS) and Sympathetic System (SS). Alkylated histamine based double action Saltans are lipophilic and can act transdermally.

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.

The invention discloses a medicine that cures muscle atrophy after spinal cord injury and its application method: the medicine that cures muscle atrophy after spinal cord injury is losartan. The application method is that losartan activates a signal pathway of IGF1/Akt/mTOR and inhibits an expression of MuRF-1; A receptor blocking pharmacon of angiotensin II takes effect through activating the pathway of IGF-1/Art/mTOR and inhibiting a ubiquotin-proteasomes system. The receptor blocking pharmacon of angiotensin II can improve the skeletal muscle atrophy after spinal cord injury of rats and may take effect through activating the pathway of IGF-1/Akt/mTOR and inhibiting the ubiquitin-proteasomes system, which provides a part of basis for later clinical application and combined therapy.

The invention provides a method for preparing a losartan derivative 5-losartan carbonate from 2-butyl-4-chloro-5-formoxyl-1-{[2'-2(1-H-tetrazole-5-yl)-biphenyl-4]-methyl} imidazole. According to the invention, the total yield of 5-losartan carbonate is 75.6%; and on the existing technology basis, the yield is further improved, cost is reduced, product purity is improved, maneuverability is increased. Thus, the method provided by the invention is suitable for industrial production.

The present invention discloses preparation process of 5-losartan carboxylate. In polar solvent, such as DMF, pyridine, acetone, the mixed solvent with water, etc, losartan or its ammonium salt, alkali metal salt, hydrochloride, sulfate, formate, etc and the organic salt or inorganic salt of permanganic acid react to produce 5-losartan carboxylate or its ammonium salt, alkali metal salt, hydrochloride, sulfate, formate, etc. The preparation process is direct, economic, efficient and suitable for industrial production.

The invention relates to a preparation method of losartan, which comprises the following steps: triphenylmethyl losartan (structure III) is dissolved in a long chain liquid alcohol over C12, inorganic acid (hydrochloride, sulfate, phosphate) aqueous solution is added as a catalyst and the losartan (structure II) is finally obtained after 24 hours -36 hours of reaction at room temperature. By the improvement of the reaction conditions, no side reaction occurs during the reaction process, thereby ensuring the quality of the final products.

The invention provides a glioma-targeting composite nanometer preparation, a preparation method and applications thereof, wherein the glioma-targeting composite nanometer preparation is a nasal nanometer complex assembled by coating a coated material hepatoma-derived growth factor delivery shRNA with a coating material losartan-chitosan-polyethyleneimine vector copolymer, and the particle size is50-250 nm. The preparation method comprises: carrying out an oxidation reaction on chitosan and potassium periodate to obtain oxidized chitosan; carrying out a reaction on the oxidized chitosan and polyethyleneimine to obtain a chitosan-polyethyleneimine copolymer; carrying out a Schiff base reaction on the chitosan-polyethyleneimine copolymer and carboxylated losartan to obtain a losartan-chitosan-polyethyleneimine vector copolymer; and assembling the losartan-chitosan-polyethyleneimine vector copolymer and shHDGF to obtain the nasal nanometer complex. According to the present invention, after the nasal cavity product is prepared from the glioma-targeting composite nanometer preparation, the good brain glioma targeting property can be provided.

The invention relates to a method for preparing losartan. The method comprises the following steps of: removing a protective group of triphenylmethyl from 2-butyl-4-chloro-5-formyl-l-[(2'-(1-triphenylmethyl-tetrazole-5-yl)-biphenyl-4-)methyl] imidazole in the presence of a strong acid to give an intermediate of 2-butyl-4-chloro-5-formyl-1-[(2'-(1-H-tetrazole-5-)-biphenyl-4-)methyl] imidazole; producing 2-butyl-4-chloro-5-(hydroxymethyl)-1[(2'-(1-H-tetrazole-5-yl)-biphenyl-4-) methyl] imidazole in the presence of a reducer.

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.

The invention discloses a method for removing trityl from 1-trityl-5-(1,1'-biphenyl-2yl)-1H-tetrazole compound (I). The method is characterized by adding acyl halide in low-grade alcohol at low moisture condition to remove the trityl. The method has the advantages of rapid reaction speed, greatly shortened reaction time, higher product purity, and being fit for industrialized production. The method can be used for preparing related candesartan (VIII), losartan (X), irbesartan (XII), valsartan (XIV), olmesartan medoxomil (XVI) or olmesartan (XVIII).