68 results about "Endothelin receptor antagonist" patented technology

The present invention provides methods for treating a variety of urogenital disorders, such as, for example, vaginismus, dyspareunia, vulvodynia (including vulvar vestibulitis), interstitial cystitis, nonspecific urethriris (i.e., nonspecific pain and/or burning of the urinary tract) and sexual dysfunctions, such as, for example, female sexual arousal disorders and female sexual orgasmic disorders, using a variety of compounds, including, but not limited to, NO donors, calcium channel blockers, cholinergic modulators, α-adrenergic receptor antagonists, β-adrenergic receptor agonists, phosphodiesterase inhibitors, cAMP-dependent protein kinase activators (e.g., cAMP mimetics), superoxide scavengers, potassium channel activators, estrogen-like compounds, testosterone-like compounds, benzodiazepines, adrenergic nerve inhibitors, antidiarrheal agents, HMG-CoA reductase inhibitors, smooth muscle relaxants, adenosine receptor modulators, adenylyl cyclase activators, endothelin receptor antagonists, bisphosphonates and cGMP-dependent protein kinase activators (e.g., cGMP mimetics).

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating pulmonary arterial hypertension. More particularly, aspects of the present invention are related to using a combination of iloprost and at least one additional agent, selected from the group consisting of an endothelin receptor antagonist and a PDE inhibitor.

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT_2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

The invention relates generally to combination therapies comprising an endothelin A receptor (ET_A) antagonist and a phosphodiesterase 5 (PDE5) inhibitor, pharmaceutical compositions comprising ET_A antagonist and PDE5 inhibitor and methods of treating various disorders comprising administering an ET_A antagonist and a PDE5 inhibitor. In particular, the combination therapies and pharmaceutical compositions are useful for the treatment and/or prevention of cardiac disorders such as pulmonary arterial hypertension (PAH).

Provided are devices and methods for treating or preventing smooth muscle cell proliferation caused by endothelin-mediated conditions. In particular, a medical device comprising a structure which is implantable within a body lumen and means on or within the structure for releasing an endothelin (A) receptor antagonist at a rate effective to inhibit smooth muscle cell proliferation. The device can be, for example, an expansible stent or a graft, and the means can include a matrix coating, wherein the endothelin (A) receptor antagonist can be dispersed within the coating or disposed directly on the structure and under the matrix. The methods and devices of this invention can be used to decrease the incidence of restenosis as well as other thromboembolic complications resulting from implantation of medical devices.

Methods of administering and pharmaceutical compositions of a biphenyl sulfonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.

A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the 10 method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a 13 receptor blocker; an imidazoline receptor antagonist; a centrally acting tx receptor antagonist; a peripherally acting ct receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduce SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Aliquots of extracts from ethnopharmacological plants that have activity against the effects of sarafotoxins present in snake venom are isolated and identified as antagonists of endothelin using a fluorescence-based assay. A process is provided for the identification of an antagonist of an endothelin selected from the group consisting of endothelin-1, endothelin-2, endothelin-3 and mixtures thereof. The process comprises extraction of ethnopharmacological plants with a solvent followed by evaporation of the solvent to form an aliquot containing at least one component of the extract, optionally purifying and isolating one or more component by chromatography, and subjecting the aliquot or purified component to a competitive fluorescent binding assay using biotinylated endothelin-1, wherein the plants having activity against the effects of one or more sarafotoxins present in snake venom.

Disclosed are methods and compositions containing endothelin receptor antagonists for emergency contraception.

Methods for identifying cancer patients eligible to receive endothelin receptor antagonist therapy and for monitoring patient response to endothelin receptor antagonist therapy comprise assessment of the expression levels of at least one of PAI-1, uPA, TGFbeta2, IL-6, IL-8 and OPG in a patient tissue sample. The methods of the invention allow more effective identification of patients to receive endothelin receptor antagonist therapy and of determination of patient response to the therapy.

The invention provides a system and method of collecting, storing and managing laboratory test results of patients. In one embodiment the invention is directed towards collecting, storing and managing laboratory test results of patients taking an endothelin receptor antagonist (ERA). The system provides a way of securely collecting and tracking information from a plurality of patients, a plurality of laboratories, and a plurality of health care providers by use of a database. The method comprises receiving patient information from health care providers, receiving a laboratory test schedule for each patient, and laboratory tests needed for each patient. This data is entered into a central processing computer. The patients then go to any laboratory to have the monthly testing done due to the ERA prescription. The laboratory test data collected is sent to the central processing computer. The central processing computer can generate an automated report on the laboratory results and supply the results to the health care provider. Additionally, if no laboratory test data for the patient is entered into the central processing computer in accordance with the laboratory test schedule for the patient, the central processing computer will notify a call center which will call the patient, laboratory or health care provider informing them of the overdue laboratory test data.

Methods for treating conditions or disorders which can be alleviated by reducing food intake are disclosed which comprise administration of an effective amount of an endothelin or an endothelin agonist, alone or in conjunction with other compounds or compositions that affect satiety. The methods are useful for treating conditions or disorders, including obesity, Type II diabetes, eating disorders, and insulin-resistance syndrome. Pharmaceutical compositions for use in the methods of the invention are also disclosed.

The present invention relates to therapeutic protocols and pharmaceutical compositions designed to treat and prevent cancer. More specifically, the present invention relates to a novel method of treating cancer using antagonists to the endothelin B receptor (ETB) or inactive mimic forms of endothelin-1. The pharmaceutical compositions of the invention are capable of selectively inhibiting the early events associated with the development of cancer. The present invention further relates to screening assays to identify compounds which inhibit ETB activation.

This invention relates to novel endothelin receptor antagonists that selectively inhibit the interaction between Endothelin-1 (ET-1) and endothelin type-A receptors, their derivatives, acceptable acid addition salts. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by endothelin receptor antagonists, particularly those diseases and conditions that are beneficially treated by selective inhibitors of endothelin type-A receptors.

The disclosure relates to an endothelin receptor antagonist for use in the prevention or treatment of brain metastases in combination with a cytotoxic chemotherapy agent, radiotherapy or both. The endothelin receptor antagonist may for example be bosentan, macitentan or a mixture of bosentan and macitentan.

This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by compounds that block the endothelin signaling pathway that leads to vasoconstriction and in particular those diseases or conditions beneficially treated by endothelin receptor antagonists.

The present invention relates to improved processes for the preparation of Endothelin receptor antagonists, their salts and intermediates.

The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.

The invention relates to a splitting method of 2-hydracrylic acid racemic mixture. The method comprises the following steps of: carrying out optical active alkali reaction on 2-hydracrylic acid racemic mixture and L-prolinamide, separating a single isomer L-prolinamide salt of 2-hydroxyl acrylic acid compound; and taking the single isomer of the 2-hydroxyl acrylic acid compound as important intermediate for synthetizing endothelin receptor antagonist for treating cardiovascular disease. Therefore, the single isomer with high optical purity is separated by the splitting method which is simple to operate and is provided by the invention; and the method is cheap in required material and reagent, and suitable for industrial production, and has good economic benefit.