36 results about "Telmisartan" patented technology

The invention discloses a telmisartan glucoside derivative, a microbial conversion preparation method thereof and application of the telmisartan glucoside derivative in preparation of a medicine for preventing or treating osteoporosis. The telmisartan glucoside derivative is characterized in that a telmisartan propyl side chain is connected with a glucosyl group. According to the invention, a microbial conversion technology is utilized, telmisartan is taken as a substrate, and glucosyl is introduced into a telmisartan propyl side chain in a regioselective manner, so that the telmisartan glucoside derivative with a novel structure is obtained. Experiments on the osteoblast proliferation promoting activity and the postmenopausal osteoporosis resisting effect of the telmisartan glucoside derivative by using an in-vitro osteoblast model and an ovariectomized induced osteoporosis mouse model prove that the telmisartan glucoside derivative has relatively good osteoblast proliferation promoting activity and postmenopausal osteoporosis resisting activity; the compound can be used as an active component of a medicine for treating osteoporosis, and has wide application.

The invention discloses a preparation method of a telmisartan intermediate 2-n-propyl-4-methyl-6-(1 '-methylbenzimidazole-2-yl) benzimidazole, and belongs to the field of medicine synthesis. The method comprises the following steps: carrying out amidation reaction on 2-n-propyl-4-methyl-6-carboxyl benzimidazole and N-methyl o-phenylenediamine hydrochloride in the presence of a triazine condensing agent under an alkaline condition; the preparation method comprises the following steps: mixing N-(2-methylaminophenyl)-2-n-propyl-4-methylbenzimidazole-6-formamide and 2-n-propyl-4-methyl-6-(1 '-methyl-benzimidazole-2-yl) benzimidazole to obtain a composition of N-(2-methylaminophenyl)-2-n-propyl-4-methylbenzimidazole-6-formamide and 2-n-propyl-4-methyl-6-(1'-methyl-benzimidazole-2-yl) benzimidazole; and then carrying out cyclization reaction under an acidic condition, so as to obtain the 2-n-propyl-4-methyl-6-(1 '-methyl-benzimidazole-2-yl) benzimidazole. The method is high in preparation yield, high in product purity and low in impurity risk; generated waste liquid and waste water are easy to treat; reaction conditions are mild, equipment requirements are low, operation is simple, comprehensive production cost is low, and large-scale industrial production is facilitated.

The invention provides a preparation method of telmisartan tablets, which is characterized by comprising the following steps: mixing telmisartan, a pH regulator, a solubilizer and povidone with water to prepare a solution, then freeze-drying the solution, mixing the freeze-dried material with a filler, then mixing with a lubricant, and tabletting to obtain the telmisartan tablets. Through the synergistic effect of the prescription and the preparation method, the material dried by the freeze-drying method can maintain the original chemical composition and physical property, and the prepared telmisartan tablet has the advantages of stable quality, good dissolution behavior, no influence of the raw material telmisartan crystal form, crystal lump and particle size on the process smoothness, high yield, long-term storage, and no toxic or side effect. The method is suitable for large-scale production.

Provided herein are pharmaceutical compositions useful for the treatment of hypertension comprising an angiotensin II receptor blocker, a diuretic and a calcium channel blocker. These compositions are administered at a dose of 40-80% of the lowest hypertensive therapeutic dose (LHTD) per agent. The present application also relates to a composition comprising telmisartan, a thiazine-like diuretic and a calcium channel blocker, administered at a dose of from 80 to 150% of the LHTD of each agent.

The application relates to a preparation method of telmisartan, and belongs to the field of medicine and chemical industry. The scheme comprises the following steps: reacting starting materials 1 and 2-cyano-4'-bromomethyl biphenyl to obtain compound 2, constructing an imidazole ring, reducing, hydrolyzing and finally obtaining telmisartan. The content of impurity B can be effectively reduced through the method, the content of impurity B can be effectively reduced through the preparation method, the purity of telmisartan is improved, the refining frequency is reduced, the reaction condition is mild, the post-treatment operation is simple, the total yield can reach more than 85%, and the method is more suitable for large-scale industrial production.

The invention discloses a preparation method of 2-methyl-4-(1-methyl-1H-benzo [d] imidazole-2-yl) aniline, and relates to a preparation method of 2-methyl-4-(1-methyl-1H-benzo [d] imidazole-2-yl) aniline. Specifically, the invention provides a preparation method of a compound 31, which comprises the following steps: in a solvent, in the presence of alkali, a compound 30 is subjected to an amino reaction as shown in the following formula to obtain the compound 31, and the alkali is alkali metal carbonate. According to the method, raw materials and reagents are low in cost and easy to obtain, and the telmisartan key intermediate can be prepared at high yield.

The invention belongs to the technical field of antigen-antibody detection, and relates to a monoclonal antibody of a non-biphenyl tetrazolsartan drug, a nucleic acid molecule, a detection kit and application thereof. The monoclonal antibody of the non-biphenyl tetrazolsartan medicine comprises a heavy chain variable region (VH) and a light chain variable region (VL), the heavy chain variable region comprises a VH-CDR1, a VH-CDR2 and a VH-CDR3, the light chain variable region comprises a VL-CDR1, a VL-CDR2 and a VL-CDR3, the sequence of the VH-CDR1 is as shown in SEQ ID NO.1, and the sequence of the VH-CDR2 is as shown in SEQ ID NO.2. The monoclonal antibody of the non-biphenyl tetrazolsartan medicine has the advantages that the monoclonal antibody of the non-biphenyl tetrazolsartan medicine can be used for preparing the non-biphenyl tetrazolsartan medicine; the monoclonal antibody capable of simultaneously recognizing azilsartan and telmisartan is successfully prepared by taking candesartan as an immunogen and azilsartan as a coating antigen, the azilsartan and telmisartan are specifically detected, and the problem that the two drugs cannot be covered by the existing immunodetection technology is solved.

The present invention relates to a pharmaceutical composition for preventing or treating metabolic abnormality-related fatty liver diseases containing empagliflozin and telmisartan. The pharmaceutical composition has no issues of drug-drug interaction and exhibits a synergistic effect in the prevention or treatment of metabolic dysfunction-related fatty liver disease, thereby allowing effective application to patients with metabolic dysfunction-related fatty liver disease.

The invention discloses a telmisartan and hydrochlorothiazide compound tablet which is characterized in that the telmisartan and hydrochlorothiazide compound tablet comprises a double-layer tablet A and a double-layer tablet B, and the layer A is prepared from telmisartan lipidosome, a diluent and a lubricant; and the layer B is prepared from hydrochlorothiazide, a diluent, a disintegrating agent, a lubricant and an antioxidant. The telmisartan liposome comprises lipid and telmisartan, the dosage ratio of the lipid to the telmisartan is (0.5-2.3): 1, the lipid comprises phospholipid and cholesterol, and in the lipid, the content of the cholesterol accounts for 20%-60% of the total amount of the lipid. The telmisartan liposome comprises lipid, telmisartan and a PH buffer solution, and the PH of the PH buffer solution is 5-7. According to the telmisartan and hydrochlorothiazide compound tablet prepared by the invention, the telmisartan dissolution is good, and the tablet is safe and stable.

The PH adjusting device comprises a box body and a box cover, a drainage cylinder is fixedly arranged in the box body, openings are formed in the top and the bottom of the drainage cylinder, a main stirring rod is rotatably arranged in the drainage cylinder, a plurality of first blades are fixedly arranged on the main stirring rod in an inclined mode, and a plurality of second blades are fixedly arranged on the main stirring rod. A supporting ring is fixedly arranged between the inner wall of the box body and the outer wall of the drainage cylinder, a plurality of rotatable auxiliary stirring rods are installed on the supporting ring in the circumferential direction, and a plurality of second blades are fixedly arranged on the auxiliary stirring rods. The telmisartan intermediate synthesis mixed liquid in the box body flows into the drainage barrel from the bottom opening of the drainage barrel and flows out of the top opening of the drainage barrel, the flowing-out circulating liquid downwards impacts the second blade, the second blade rotates automatically, the liquid is locally stirred, and the mixing efficiency is further improved.

The application discloses a benzimidazole compound and a preparation method thereof, and also discloses application of the benzimidazole compound in preparation of telmisartan. The benzimidazole compound can be used for preparing telmisartan, the preparation method has low raw material cost, simple operation, safety and controllability, high product purity, high total yield, and is suitable for industrial production.

The invention relates to a telmisartan amlodipine double-layer tablet and a preparation method thereof, the telmisartan amlodipine double-layer tablet comprises a telmisartan layer and an amlodipine layer, the telmisartan layer contains telmisartan and pharmaceutically acceptable auxiliary materials, and the auxiliary materials are selected from one or more of a filler, an alkaline reagent, a solubilizer, a crystal blocker, an adhesive, a disintegrating agent, a lubricant and a flow aid; the amlodipine layer contains amlodipine and pharmaceutically acceptable auxiliary materials, the auxiliary materials are selected from one or more of a flow aid, a filler, a disintegrating agent and a lubricant, the flow aid is silicon dioxide, the telmisartan layer adopts a fluidized bed granulation process, a filler lactose is used as a granulation substrate, and the telmisartan layer is prepared by a fluidized bed granulation process. The amlodipine layer is prepared by co-crushing amlodipine and silicon dioxide serving as a flow aid. According to the technical scheme, the telmisartan and amlodipine double-layer tablet which is not prone to moisture absorption, high in stability, good in content uniformity and good in dissolution rate is provided, the method for preparing the telmisartan and amlodipine double-layer tablet is provided, and the method is simple and convenient in process and low in cost.

The invention relates to the technical field of drug detection, and discloses a method for detecting two trace N-nitrosamine impurities in telmisartan, which comprises the following steps: mixing and dissolving a telmisartan sample with a preset weight and an alkaline aqueous solution with a first preset volume, and adding an extracting agent with a second preset volume to prepare a sample solution; adding N-nitrosodimethylamine with a first preset mass and N-nitrosodiethylamine with a second preset mass into an alkaline aqueous solution with a third preset volume, and mixing to prepare an impurity mixed stock solution; adding a fourth preset volume of an extracting agent into the impurity mixed stock solution to prepare a working solution of a standard curve; respectively carrying out gas chromatography separation and mass spectrometry detection on the sample solution and the working solution by virtue of a triple quadrupole gas chromatograph-mass spectrometer, and calculating the content of N-nitrosodimethylamine in the sample solution and the content of N-nitrosodiethylamine in the sample solution by combining a standard curve method.

The invention discloses a method for detecting related substances of telmisartan and hydrochlorothiazide double-layer tablets. According to the detection method disclosed by the invention, octyl silane bonded silica gel is used as a filling agent or a chromatographic column with equivalent efficiency, and an impurity trapping column is added; carrying out gradient elution by taking an ammonium dihydrogen phosphate solution as a mobile phase A and acetonitrile-methanol in a volume ratio of 1: 1 as a mobile phase B; dual wavelength detection is adopted, and the detection wavelengths are 268 nm to 272 nm and 296 nm to 300 nm. The detection method provided by the invention can realize effective separation and quantitative calculation of related substances of two active components (telmisartan and hydrochlorothiazide) in a telmisartan bulk drug, a hydrochlorothiazide bulk drug and a telmisartan and hydrochlorothiazide double-layer tablet, and has the characteristics of good sensitivity, specificity, accuracy, durability and the like; and meanwhile, the working efficiency is greatly simplified.

The invention provides a compound with a telmisartan tetravalent platinum structure as well as a preparation method and application of the compound. The compound with the telmisartan tetravalent platinum structure is shown as a general formula (I). Wherein the compound is selected from cis-platinum or oxaliplatin; l is hydroxyl or hydroxyl. The telmisartan tetravalent platinum structure compound disclosed by the invention has excellent tumor proliferation inhibition activity and shows a good treatment effect on metastatic malignant tumors; the compound can effectively inhibit the tumor epithelial-mesenchymal transition (EMT) process, can significantly activate tumor immune response, can be used for preparation of antitumor drugs, and provides a brand new direction for research and development of metastatic malignant tumor treatment drugs.

The invention belongs to the technical field of medicines, and particularly relates to application of BCAT2 as a target spot in preparation of a medicine for treating rheumatoid arthritis. Through metabonomics research, the inventor finds that the metabolic enzyme BCAT2 is remarkably highly expressed in synovial tissues of an active-stage RA patient and is relatively low in expression in synovial tissues of a remission-stage RA patient. The high expression of the metabolic enzyme BCAT2 is closely related to synovitis and bone destruction. The BCAT2 inhibitor (telmisartan) can significantly reduce joint inflammation score, reduce synovitis and bone destruction, and effectively reduce bone loss. The invention provides an innovative RA metabolism targeted treatment strategy which has high safety and strong targeting property.

The present invention discloses co-crystals of telmisartan (TM) and ascorbic acid (Asca). The present invention also discloses a process for the preparation of telmisartan and ascorbic acid co-crystals using microwave irradiation followed by slow evaporation of solvent under cooling conditions. The present invention also discloses pharmaceutical compositions comprising TM and Asca co-crystals for the treatment of JEV.

The present invention relates to compositions, systems, and methods for treating a subject with an eye condition (e.g., topically) using a composition comprising an ACE-2 receptor antagonist (also known as Angiotensin II Receptor Blocker or “ARB”) (e.g., losartan, telmisartan, valsartan, olmesartan, candesartan, irbesartan, eprosartan, azilsartan, or losartan metabolite EXP3174). In certain embodiments, the eye condition is selected from: i) a corneal scarring fibrosis, ii) a transforming growth factor beta-induced (TGFBI) corneal dystrophy, iii) a conjunctival fibrotic disease, iv) an intraocular fibrotic disease, and v) a conjunctival bleb scarring and / or shunt encapsulation (e.g., following glaucoma surgery).

The present invention concerns a composition for use in, or for the treatment of, Rett syndrome, which proposes a repositioning of an anti-inflammatory drug from the class of nonsteroidal anti-inflammatory drugs (NSAIDs).

This application discloses a telmisartan-amlodipine bilayer tablet. The telmisartan layer comprises telmisartan, an alkaline reagent, a binder, a filler, and a lubricant; the amlodipine layer comprises amlodipine besylate, a diluent, a disintegrant, a flow aid, a colorant, and a lubricant. The binder for the telmisartan layer is povidone, with a weight-average molecular weight of 3000–6000 kDa. The diluent for the amlodipine layer is microcrystalline cellulose, specifically a blend of two types. The weight ratio of microcrystalline cellulose PH-102 to PH-302 is 1–4:1–4. The povidone is one or both of povidone K-25 and K-29 / 32. The telmisartan-amlodipine bilayer tablet provided in this application exhibits high stability and dissolution performance similar to the reference tablet.

The invention belongs to the field of medicine, and discloses a telmisartan tablet which is prepared by the following steps: dissolving a pH regulator, a cosolvent, an adhesive and telmisartan in water to prepare a spray-dried solution, performing spray drying on the spray-dried solution to prepare spray-dried particles, mixing the spray-dried particles with a filler and a lubricant, performing dry granulation, and tabletting to obtain the telmisartan tablet. The preparation method comprises the following steps: preparing dry granulation particles, totally mixing the dry granulation particles with an adhesive and a lubricant to obtain totally mixed particles, and tabletting the totally mixed particles to obtain the telmisartan tablet. After the spray-dried particles are added with total mixed auxiliary materials, the obtained material is good in flowability and not prone to moisture absorption, and the layering phenomenon is not prone to occurring in the mixing process. The telmisartan tablet prepared by the invention has the same dissolution behavior as a reference preparation, and is completely dissolved out.

The present invention relates to a solid oral pharmaceutical composition of telmisartan sodium as an active ingredient and its preparation thereof. More specifically, the present invention provides a stable pharmaceutical composition of telmisartan sodium having minimal weight and reduced size.

To provide compositions for the treatment of hypertension. [Solution] This specification provides pharmaceutical compositions useful for the treatment of hypertension, comprising an angiotensin II receptor blocker, a diuretic, and a calcium channel blocker. These compositions are administered at 40% to 80% of the minimum hypertension therapeutic dose (LHTD) for each agent. This application also relates to compositions comprising telmisartan, a thiazide-like diuretic, and a calcium channel blocker, administered at 80% to 150% of the LHTD for each agent.

The present invention provides a trilayer tablet formulation containing telmisartan in an immediate release form, along with two additional antihypertensive agents in immediate or extended release forms, addresses the critical challenges of chemical incompatibility and dissolution interference. This advanced formulation strategy holds promise for improving the management of hypertension through more effective and stable combination therapies.

The application discloses a kind of solid dispersion nanoparticles and preparation method thereof, belong to medical technology field, using SAS process to obtain drug-carrier solution to further prepare telmisartan binary solid dispersion and telmisartan ternary solid dispersion.The application uses the above-mentioned one kind of solid dispersion nanoparticles and preparation method thereof, using SAS method successfully prepares telmisartan binary solid dispersion, ternary solid dispersion;And the construction of SAS method to telmisartan solid dispersion system, breaks through the limitation of traditional method, can accurately control particle size, stable formation amorphous drug to improve dissolution, can also protect the activity of heat-sensitive component and realize low solvent residue, with process flexibility and industrialization potential.

To provide a new therapeutic approach for the treatment of dogs against elevated UPC levels.SOLUTION: The present invention relates to telmisartan or a pharmaceutically acceptable salt thereof as a medicament for the treatment of elevated urinary protein-to-creatinine ratio (UPC) levels in dogs, wherein the therapeutically effective amount of telmisartan is administered in a daily dosage amount that is varied over a treatment period.SELECTED DRAWING: None

The present invention relates to telmisartan or a pharmaceutically acceptable salt thereof as a medicament for the treatment of hypertension in dogs, wherein the therapeutically effective amount of telmisartan is administered in a daily dosage amount that is varied over a treatment period.

The present invention relates to the use of a combination of one or more SGLT-2 inhibitors or pharmaceutically acceptable forms thereof and telmisartan or pharmaceutically acceptable forms thereof, in particular for the prevention and / or treatment of one or more kidney diseases and / or hypertension in non-human mammals / non-human mammalian patients, such as dogs or cats.

The present invention relates to the use of one or more SGLT-2 inhibitors or pharmaceutically acceptable forms thereof in combination with pimobendan and / or telmisartan or pharmaceutically acceptable forms thereof, in particular for the prevention and / or treatment of one or more cardiac diseases in non-human mammals / non-human mammalian patients, such as dogs or cats.

One embodiment provides a neurorestoration compound or composition implementing multiple neuroplasticity inducing mechanisms of action including a mixture of pharmacologically effective amounts of Cilostazol and Metformin and Telmisartan. A second embodiment provides a neurorestoration compound or composition implementing multiple neuroplasticity inducing mechanisms of action including a mixture of pharmacologically effective amounts of Cilostazol and Metformin and Duloxetine. The neurorestoration compound implementing multiple neuroplasticity inducing mechanisms of action is believed to be particularly well suited for stroke rehabilitation.