52 results about "Angiotensin Receptor Antagonists" patented technology

A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and / or heart failure. ARB includes S—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate.

The invention discloses an imidazole-5-carboxylic acids derivative and the manufacturing method. It is the angiotensin II acceptor antagon. It has strong angiotensin II antagonize activity and high blood pressure proofing activity. And it could be used as therapeutic agent to cure high blood pressure.

The present invention discloses a novel crystalline form of an angiotensin receptor antagonist and neutral endopeptidase inhibitor supramolecular complex. The novel crystalline form of the supramolecular complex has high water solubility and good stability. Experiments show that the moisture absorption and intrinsic dissolution extent and speed are superior to those of a conventional crystalline supramolecular complex.

The invention provides a pharmaceutical composition which comprises calcium channel blockers of a medicinal dose, angiotensin II receptor antagonists of a medicinal dose, one or more of B vitamins of a medicinal dose and pharmaceutically acceptable carriers, wherein the calcium channel blockers are selected from amlodipine, felodipine, israbipine, nicardipine, nifedipine, nisoldipine, nitrendipine, lacidipine, diltiazem or verapamil; the angiotensin II receptor antagonists are selected from candesartan, telmisartan, losartan, valsartan, irbesartan, eprosartan, tasosartan or olmesartan; and the B vitamins are selected from one or more of vitamin B6, vitamin B12, folic acid and calcium leucovorin. The pharmaceutical composition of the invention can improve the curative effect of the hypotensor, enhance the target organ protecting action of the hypotensor, and reduce the morbidity of complications of angina, myocardial infarction and the like.

A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.

A novel non-peptide angiotonin II receptor antagon kind of medicines, and their preparing process and application are disclosed.

A 4,6-dihydrofurano[3,4-d] imidazole-6-ketone derivative, its pharmacological receptible salt, and the preparing process of said derivatives are disclosed. Said compound can be used as the intermediate for synthesizing the antagon of angiotensin II receptor.

The present invention provides a an angiotensin receptor antagonist and creatine phosphate sodium complex and uses thereof, wherein the complex comprises an angiotensin receptor antagonist and creatine phosphate sodium, a molar ratio of the angiotensin receptor antagonist to the creatine phosphate sodium is 1:1-2, and the angiotensin receptor antagonist is selected from valsartan, losartan, irbesartan, telmisartan, eprosartan, candesartan, olmesartan, saprisartan, tasosartan, and elisartan. According to the present invention, the complex is formed by compounding the angiotensin receptor antagonist and the creatine phosphate sodium, and provides the unexpected double effect and the synergistic effect for treatment of heart failure and high blood pressure, the cocrystallization salt hydrate formed by linking the hydrogen bond has the stable characteristic, the pharmacokinetic property is significantly provided, and the positive application prospects are provided in the fields of anti-high blood pressure treatment and anti-heart failure treatment.

The invention relates to a sustained release preparation of a novel prescription for treating hypertension and the preparing method thereof. The novel prescription comprises a heart selective Beta1 receptor blocker metoprolol and an angiotensin II receptor antagonist (sartan drugs). The sustained release preparation consists of delayed release part and rapid release part, wherein the heart selective Beta1 receptor blocker metoprolol is the delayed release part, with first hour releasing 25-45%, fourth hour releasing 40-75% and eighth hour releasing over 75%; the angiotensin II receptor antagonist (sartan drugs) is the rapid release part, with 45 minutes dissolution over 75%. The composition has both rapid and prolonged action. The invention discloses in vitro drug release characteristics and preparation method thereof.

Solid oral dosage forms, especially tablets, of a pharmaceutical composition comprising a supramolecular complex can be formed from a direct compression process or a compaction process such as roller compaction. Such solid oral dosage forms feature an immediate release profile that allows for fast release of the therapeutic agent. A particularly useful supramolecular complex is trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate]hemipentahydrate.

The invention provides an angiotensin receptor antagonist and milrinone compound and a use thereof. The compound comprises an angiotensin receptor antagonist and milrinone, the angiotensin receptor antagonist and milrinone can be directly mixed, or can be indirectly connected through hydrogen bonds, and cocrystallized sodium hydrate formed by using the hydrogen bonds have stable properties and substantially improved pharmacokinetic properties. The action mechanisms of the angiotensin receptor antagonist and milrinone are different, but the compound formed by the angiotensin receptor antagonist and milrinone have unexpected synergism, so the compound has positive application prospect in the anti-heart failure and anti-hypertension field.

The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.

In one aspect, the present invention relates to use of an ACE inhibitor and / or angiotensin II receptor antagonist for the preparation of a medicament for the treatment of a dermatological disorder, particularly by topical application of said ACE inhibitor and / or angiotensin II receptor antagonist. The present invention also provides cosmetic methods for improving and / or maintaining the skin tone of an individual suffering from, or at risk of suffering from, a dermatological disorder, said method comprising contacting the skin of said individual with an ACE inhibitor and / or angiotensin II receptor antagonist.

The invention provides a compound prepared from an angiotensin receptor antagonist and an enkephalinase inhibitor and application of the compound. The compound is prepared from the angiotensin receptor antagonist and the enkephalinase inhibitor, the angiotensin receptor antagonist and the enkephalinase inhibitor can be directly mixed or indirectly connected through hydrogen bonds, and a co-crystallized sodium hydrate prepared through hydrogen bond connection is more stable in property and significant in pharmacokinetic property; although the action mechanism of the angiotensin receptor antagonist and the action mechanism of the enkephalinase inhibitor are different, the compound prepared from the angiotensin receptor antagonist and the enkephalinase inhibitor has an unexpected synergistic effect and has a positive application prospect in the anti-heart-failure and anti-hypertension treatment field.

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 relates to a drug combination of applying jointly angiotensin II receptor antagonist / diuretic / folacin and the purpose. The combination includes: officinal dose of angiotensin II receptor antagonist, officinal dose of diuretic, officinal does of folic acid compound and pharmacy-acceptable carrier. The invention provides the purpose of the combination in preparing the medicine used for preventing, treating or delaying hypertension, target organ damage caused by hypertension or hypertension-related diseases; the invention also provides the purpose of the drug combination in preparing the medicine used for reducing the danger of cardiovascular and cerebrovascular events caused by hypertension. The implementation of the invention, which provides the patient with the drug combination, can improve the curative effect, increase the compliance of the patient, convenience the drug administration and reduce the medical expenses.

The invention provides a compound of an angiotensin receptor blocker and levosimendan and use of the compound. The compound is composed of the angiotensin receptor blocker and levosimendan, which can be mixed directly or be connected indirectly through a hydrogen bond, wherein a co-crystallized sodium hydrate formed by connection through hydrogen bond is more stable in property; and the pharmacokinetic properties are improved significantly; the action mechanisms of the angiotensin receptor blocker and the levosimendan are different, but the formed compound has an unexpected synergistic effect and has positive application prospects in the anti-heart failure and anti-hypertensive treatment field.

The invention provides a medicine composition for treating hypertension. The medicine composition is characterized in that the medicine composition comprises (1) angiotensin II receptor antagonists, (2) diuretic metolazone and (3) acceptable auxiliary materials on pharmaceutical science. The weight proportion of the angiotensin II receptor antagonists to the metolazone is 20-200:0.5-10; the angiotensin II receptor antagonists and the metolazone are combined to strengthen the collaboration antihypertensive effect; untoward effects are reduced; the compliance of patients is improved; the medication crowds are wide; and the medicine composition can be used by the patients with the seriously-damaged renal function. The medicine composition is suitable for treating mild and moderate primary hypertension, and is particularly suitable for treating secondary hypertension caused by kidney damage.

Provided a complex of formula is [3-((1S, 3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl) propionate-(S)-3′-methyl-2′-(pentanoyl {2″-(tetrazol-5-ylate) biphenyl-4′-ylmethyl}amino) butyrate]6.XCa2+.YNa+.ZH2O, wherein X=1-3, Y=12-16, Z=9-18, and 2X+Y=18, and represented by formula (I). Also disclosed are the method of preparing the complex and the method of treating chronic heart disease using a medicament comprising the complex.

The invention provides a compound of an angiotensin receptor inhibitor and an enkephalinase inhibitor and a usage thereof. The compound is formed by the angiotensin receptor inhibitor and the enkephalinase inhibitor. The compound can be directly blended, or indirectly connected by a hydrogen bond, and cocrystallization sodium hydrate formed by the hydrogen bond connection is more stable in property, and the pharmacokinetics property is remarkably improved. Although the action mechanisms of the angiotensin receptor inhibitor and the enkephalinase inhibitor are different, the compound formed bythe both parties has an unexpected synergistic effect, and has the positive application prospect in the field of anti-heart-failure and anti-hypertension treatments.

The present application belongs to the technical field of drug application, relates to a treatment method using a complex of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, and specifically relates to the dosage of the drug.

The invention relates to a new crystal form of a sartan drug as well as a preparation method and application thereof, and belongs to the field of pharmaceutical chemicals. The invention discloses a sacubitril valsartan trisodium trihydrate eutectic composed of an angiotensin receptor antagonist and an enkephalinase inhibitor for treating hypertension or heart failure and a preparation method of the sacubitril valsartan trisodium trihydrate eutectic. The obtained crystal is analyzed by an X-ray powder diffraction spectrogram, and the characteristic absorption peaks 2 theta are located at 4.2 + / -0.2 degrees, 5.0 + / -0.2 degrees, 5.4 + / -0.2 degrees, 9.7 + / -0.2 degrees, 12.6 + / -0.2 degrees, 17.0 + / -0.2 degrees, 18.1 + / -0.2 degrees, 19.4 + / -0.2 degrees, 21.3 + / -0.2 degrees and 23.0 + / -0.2 degrees. The new eutectic crystal form disclosed by the invention is simple in preparation method, the crystal is easy to separate, and experiments show that the hygroscopicity and the stability of the neweutectic crystal form are superior to those of the existing eutectic crystal form, so that the new eutectic crystal form is favorable for being prepared into an oral solid preparation and processing and producing the oral solid preparation, and can be used for treating hypertension or heart failure.

The invention discloses 6-pyridin benzimidazole indole derivatives and a preparation method thereof. The compounds are novel angiotensin II receptor antagonists and can be used for prevention and treatment of cardiovascular, cerebrovascular and renal-vascular diseases like hypertension, coronary heart disease and pulmonary arterial hypertension.

The invention relates to a pharmaceutical composition containing angiotensin II receptor antagonist, statin lipid-lowering drugs and folic acid compound. The pharmaceutical composition contains medicinal dose of angiotensin II receptor antagonist, medicinal dose of statin lipid-lowering drugs, medicinal dose of folic acid composite and a carrier acceptable in pharmaceutics. The invention also relates to an application of the pharmaceutical composition in preparing medicines for preventing and treating or retarding high blood pressure accompanied by dyslipidemia and the application thereof in preparing medicines for treating target organ damage caused by the high blood pressure accompanied by dyslipidemia; in addition, the invention further relates to the application of the pharmaceutical composition in preparing medicines for lowering risk of cardiovascular and cerebrovascular events caused by high blood pressure accompanied by dyslipidemia. The invention belongs to the pharmaceutical field. With the implementation of the invention, the pharmaceutical composition with special usage, provided to the patients, can improve compliance of the patients, bring convenience to the patients to take medicines and reduce medical expenses, thus enjoying good market prospect.

The invention belongs to the technical field of medicine application, and relates to a novel application of a compound of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, in particular to an application of the compound in preparation of a medicine for salt-sensitive hypertension.

The invention relates to application of combination of an angiotensin converting enzyme inhibitor and an angiotensin receptor antagonist in preparation of medicine for treating osteoarthritis, and further relates to a corresponding medicine composition.

The invention provides a compound of an angiotensin receptor blocker and levosimendan and use of the compound. The compound is composed of the angiotensin receptor blocker and levosimendan, which can be mixed directly or be connected indirectly through a hydrogen bond, wherein a co-crystallized sodium hydrate formed by connection through hydrogen bond is more stable in property; and the pharmacokinetic properties are improved significantly; the action mechanisms of the angiotensin receptor blocker and the levosimendan are different, but the formed compound has an unexpected synergistic effect and has positive application prospects in the anti-heart failure and anti-hypertensive treatment field.

The medicine composition consists of one of AT1 receptor antagonist, its active metabolism product, ester and salt in treating effective amount of 4-800 mg, one or several kinds one B family vitamins in treating effective amount of 0.1-50 mg, and pharmaceutically acceptable carrier. The medicine composition of the present invention has the beneficial effects of raising the treating effect of blood pressure lowering AT1 receptor antagonist, strengthening the protecting effect of blood pressure lowering AT1 receptor antagonist on target organ and reducing the incidence rate of hemorrhage of the ocular fundus, angina pectoris, myocardial infarction and other complications.

The invention relates to a new application of a compound of an angiotensin II receptor antagonist metabolite and an NEP inhibitor, which belongs to the technical field of pharmaceutical application, and specifically relates to the application of the compound in the preparation of medicines for salt-sensitive hypertension.