81 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.

A pharmaceutical composition for preventing or treating visual function disorders caused by ocular circulatory disorders (for example, ocular hypertension and glaucoma) and visual function disorders based on ciliary tension (for example, myopia) whose active component is a vasopressin antagonist.

Various compounds such as those having the formula I and XIV where the variables have the values described herein antagonize the vitamin D receptor and are useful in treating conditions such as asthma and in preparing medicaments for use in antagonizing the vitamin D receptor or treating conditions such as asthma

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 is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

The present invention is directed to compositions useful in treating or preventing ileus in a patient. The compositions of the invention include a pituitary adenylate cyclase activating peptide (PACAP) receptor antagonist and / or a vasoactive intestinal peptide (VIP) receptor antagonist in an amount sufficient to treat or prevent ileus in a patient. In one embodiment both a PACAP and VIP receptor antagonists are present, preferably in a combination that blocks vasoactive pituitary cyclase 1 (VPAC1), VPAC2 and pituitary adenylate cyclase 1 (PAC1) receptors. Methods of using such composition to treat or prevent ileus in a patient are also encompassed by the invention.

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, R3′, 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.

The present invention features compositions for intranasal administration comprising an opioid receptor antagonist. The invention also features methods of using such compositions in the treatment of various diseases and disorders, such as the treatment of alcoholism. In certain embodiments, the opioid receptor antagonist is naltrexone or a pharmaceutically acceptable salt thereof.

Disclosed are compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, whereinR1 isR is —C(O)—N(R27)(R28) orand the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

A compound of formula:wherein X is a C2-10 spacer, and R is a substituted or unsubstituted C6-30 aryl, a substituted or unsubstituted C5-30 heteroaryl, orWhere R′ and R″ are independently a substituted or unsubstituted aryl or a substituted or unsubstituted alkyl, wherein said compound is a vitamin D receptor (VDR) antagonist, a compound comprising same, and a method of treating a patient for a disease that can be treated prophylactically or therapeutically by administration of a VDR antagonist, which method comprises administering an effective amount of aforementioned compound or composition, whereupon the patient is treated prophylactically or therapeutically for the disease.

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 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.

The present invention concerns compounds according to general formula 1a . Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of primary dysmenorrhoea.

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 present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. [Formula should be inserted here] The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.; Such conditions include, but are not limited to, Parkinsons disease, restless leg syndrome, Alzheimers disease, neurodegenerative disorder, inflammation, wound healing, dermal fibrosis, nocturnal myoclonus, cerebral ischaemia, myocardial ischemia, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease or other disorders of basal ganglia which results in dyskinesias, post traumatic stress disorder, hepatic cirrhosis, sepsis, spinal cord injury, retinopathy, hypertension, social memory impairment, depression, neuroprotection, narcolepsy or other sleep related disorders, attention deficit hyperactivity disorder, drug addiction, post traumatic stress disorder and vascular injury and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

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.

Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred vasopressin antagonists have the formulawherein R and R5 are hydrogen or lower alkyl;R1, R2, and R3 are hydrogen, halo, alkyl, alkoxy, and amino; andR4 is hydrogen or phenyl, and a pharmaceutically acceptable salt thereof.

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, R3′, p, y, and z are as defined in the claims.

Disclosed herein are methods of treating disorders of the retina (e.g., macular degeneration, retinitis pigmentosa, etc.) comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound (for example, an antipsychotic drug) that blocks or diminishes agonist-mediated responses upon binding to either dopamine D2-like receptors or serotonin 5-HT2 receptors.

Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and / or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.