78 results about "Vasopressin Antagonists" patented technology

Disclosed are A₁adenosine receptor antagonists, useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.

The present invention relates to a method for reducing infarction comprising administering to a patient ion need thereof a therapeutically effective amount of a composition comprising as an active ingredient a vasopressin antagonist compound and to a composition useful therefor. The present invention also relates to a method for reducing infarction comprising administering to a patient in need thereof a therapeutically effective amount of a combination of a vasopressin antagonist compound and a beta-blocker and to combinations useful therefor. The methods, compositions and combinations of the present invention can be used for reducing infarction in the heart (myocardial infarction) and the brain (stroke). The methods, compositions and combinations of the present invention can also be used for the treatment and/or prevention of hypertension, edema, ascites, heart failure, renal function disorder, vasopressin inappropriate secretion syndrome (SIADH), hepatocirrhosis, hyponatremia, hypokalemia, polycystic kidney disease, diabetes, or circulation disorder.

Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists.

Processes of their preparation are also described in the disclosure.

The invention discloses a new application of 1 type receptor antagonist of angiotensin II in treating tumour. Angiotensin II (Ang II) is the foremost effector of rennin-angiotensin system (RAS), the 1 type receptor of the Ang II plays an important role in propagation, migration and infiltration of tumour cells as well as in tumour angiogenesis. The 1 type receptor antagonist of the Ang II can effectively inhibit propagation and migration of tumour cells of various solid tumours such as prostate cancer, pancreatic cancer, liver cancer, gastric cancer, renal cancer and the like as well as tumour angiogenesis.

Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein j, k, l, m, n, q, r, Ar, Ar<1>, R<1>, R<2>, R<3>, R<4>, R<5>, R<6 >and X are as defined in the description. The compounds of the invention have an affinity for the BB1 receptor and some of them also have affinity for the BB2 receptor. Accordingly they may be useful for the diagnosis, prevention, or treatment of male and female sexual dysfunction. They can also be used in the diagnosis, prevention or treatment of anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders or pruritus.

The present invention relates to compounds of formulae (I) and (II) useful as opioid receptor antagonists for the treatment of obesity, wherein p is 0, 1, or 2; y is 0, 1, or 2; and z is 0, 1, or 2; X₁ is CH₂, CH, or N; to form a indolinyl, indolyl, or benzimidazole ring respectively and including applicable double bonds and/or hydrogen atoms; X₂ is CH or N; R¹ to R⁷, R^3′, p, y, and z are as defined in the claims.

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1 )antagonist; and a pharmaceuticalcomposition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.

The present invention relates to methods of reducing cardiotoxicity and/or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration.

A compound of formula:

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 discloses an aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and a preparation method thereof. The aerosol contains a propulsive agent, long-acting beta 2 receptor stimulant particles, and long-acting muscarine antagonist particles; in LABA particles, by volume, the geometric particle size of 90% particles is smaller than 10<mu>m, and the geometric particle size of 50% particles is smaller than 4<mu>m or even smaller; the middle particle size of LAMA particles ranges from 500nm to 10<mu>m; the LAMA particles are particles composed of LAMA, calcium chloride, and a surfactant; or the LAMA particles are particles composed of LAMA and an excipient. 1 to 100<mu>g of the aerosol is sprayed in each time of pressing of a MDI (metered dose inhaler), and the amount of LABA or LAMA in the aerosol ranges from 0.02 to 2mg/mL. The advantages of the aerosol are that: delivery efficiency is relatively high, and the delivery dosage is stable in long term of storing.

The invention relates to a benzazepines compounds serving as vasopressin receptor antagonism, in particular to a benzazepines compound shown in formula (I) or pharmaceutically acceptable salt thereof and a preparation method thereof, and a medicinal composition containing a compound containing curative dose of the compound or the pharmaceutically acceptable salt thereof, and application in preparing medicament for treating diseases related to the vasopressin thereof.

The present invention is directed to a compound of Formula (I) or a form thereof:

wherein U, V, W and Ring A are as defined herein, useful as vasopressin receptor antagonists.