78 results about "Vasopressin Antagonists" patented technology

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 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.

A compound of the formula (I); wherein the variables X1 to X10, R1 to R7 including R3′, E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.

A compound of the formula I: (I) wherein the variables are as described herein, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixture thereof, formulations and methods of use thereof are disclosed.

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.

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 present invention relates to 4′-[(1R)-1-[[(6,7-dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin- 4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid and its pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

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.

Combinations of ACE inhibitors and vasopressin antagonists are useful to slow and reverse the process of ventricular dilation, and CHF in mammals.

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.