33 results about "Adrenergic antagonist" patented technology

The present invention relates to combinatorial therapies for treating anxiety, depression or psychotic conditions using a lithium salt and a psychoactive drug selected from the group consisting of serotonin reuptake inhibitor, a 5HT2 receptor antagonist, an anticonvulsant, a norepinephrine reuptake inhibitor, an α-adrenoreceptor antagonist, an NK-3 antagonist, an NK-1 receptor antagonist, a PDE4 inhibitor, an Neuropeptide Y5 Receptor Antagonists, a D4 receptor antagonist, a 5HT1A receptor antagonist, a 5HT1D receptor antagonist, a CRF antagonist, a monoamine oxidase inhibitor, a sedative-hypnotic drug, and an atypical antipsychotic.

Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, β-adrenergic agonists, cAMP-dependent protein kinase activators, α1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.

The present invention discloses a novel compound and method for the treatment of inflammatory autoimmune diseases, for example, rheumatoid arthritis, using α-adrenergic antagonists and β-adrenergic agonists in combination. Treatment of animals, namely humans, with an α-adrenergic antagonist, preferably, phentolamine, and a β-adrenergic agonist, preferably terbutaline, in combination can significantly suppress the joint destruction and inflammation due to disease in these animals.

The invention describes novel nitrosated and / or nitrosylated compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and / or nitrosylated compound, and, optionally, at least one nitric oxide donor and / or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one compound of the invention, that is optionally nitrosated and / or nitrosylated, and, optionally, at least one nitric oxide donor compound and / or at least one therapeutic agent. The invention also provides methods for treating ophthalmic disorders. The nitrosated and / or nitrosylated compounds are preferably nitrosated and / or nitrosylated (3-adrenergic antagonists and nitrosated and / or nitrosylated angiotensin-converting enzyme (ACE) inhibitors.

This invention relates to methods for treatment, diagnosis and prevention of bone disease and comprises methods including measurement and modulation of sympathetic tone and leptin activity. Alteration of sympathetic tone in bone disease can be accomplished by decreasing or increasing leptin synthesis, leptin receptor synthesis, leptin binding to the leptin receptor, and leptin receptor activity. Alteration of sympathetic tone in bone disease can also be accomplished in the foregoing manner, in combination with traditional sympathetic nervous system agonists and / or antagonists, such as, but not limited to, a dopamine β hydroxylase antagonist or a β adrenergic antagonist for treatment or prevention of osteoporosis.

The invention provides methods for (a) prolonging time to hospitalization for heart failure; (b) prolonging time to first hospitalization for heart failure; (c) reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); (d) reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays (i.e., two or more hospital stays); (e) reducing the number of hospital admissions for heart failure; (f) reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and / or the number of hospital visits); (g) increasing the left ventricular ejection fraction in a heart failure patient; (h) treating a sexual dysfunction (e.g., erectile dysfunction and female sexual dysfunction) (j) treating a headache in a heart failure patient by administering a non-steroidal antiinflammatory compound (i.e., NSAIDs); (k) treating a heart failure patient who has a history of hypertension (but who is not currently diagnosed with hypertension); (l) improving the quality of life in a heart failure patient based on the Minnesota Living with heart failure questionnaire; (m) decreasing the levels of B-type natriuretic peptide; (n) treating hypertension in a heart failure patient; (o) lowering blood pressure in a heart failure patient; (p) treating labile hypertension; (q) treating idiopathic hypertension; (r) increasing patient compliance with medication dosing in a heart failure patient; (s) treating hypertension in a patient with a dilated heart; (t) treating ischemic disease and / or coronary artery disease; and (u) reducing cardiomegaly in a patient in need thereof comprising administering to the patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and / or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), and diuretic compounds.

The invention provides methods for (a) prolonging time to hospitalization for heart failure; (b) prolonging time to first hospitalization for heart failure; (c) reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); (d) reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays; (e) reducing the number of hospital admissions for heart failure; and (f) reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and / or the number of hospital visits) in a patient in need thereof comprising administering to the patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and / or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), and diuretic compounds.

The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a β-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and / or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and / or growth in a mammal by administering a composition comprising a β2-selective antagonist or agonist.

The invention relates to the field of cosmetics, and provides a skin care product for skin whitening and a preparation method thereof. The skin care product for skin whitening provided by the invention comprises oil-phase raw materials, water-phase raw materials and third-phase raw materials, wherein the oil-phase raw materials comprise an emulsifying agent, an emollient and succinate dimethoxy-methyl-nor-aporphine; the water-phase raw materials comprise a skin humectant, a metal chelating agent and reverse osmosis water; and the third-phase raw materials comprise a preservative and perfume. The calcium current principle is adopted to impede the activation of tyrosinase for the skin care product for skin whitening and preparation method thereof provided by the invention, thus the effects of skin whitening and color spot fading are achieved. The skin care product for skin whitening provided by the invention is added with nor-aporphine derivatives, thus the skin care product can interfere the inflow and outflow of the calcium current in cells; and the activation of protein kinase C is inhibited by an adrenergic antagonist which locks the calcium exchange, thereby impeding the activation of tyrosinase, achieving the effects of skin whitening and color spot fading.

The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and / or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably β-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds. The heterocyclic nitric oxide donor groups are preferably furoxans, sydnonimines, oxatriazole-5-ones and / or oxatriazole-5-imines.

A method of treating inflammation and joint deterioration in mammals includes administering a therapeutically effective dose of alpha 1A receptor antagonists alone or in combination with a beta 2 adrenergic antagonists or beta 2 adrenergic antagonists and beta 2 adrenergic agonists.

This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I):wherein R', R'', R1, R2, m, n, and A are as defined in the specification, or acceptable prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Provided are methods for treating a mammal undergoing sepsis, or at risk for sepsis. Also provided are methods of preventing or treating a physiological effect of sepsis in a mammal. Additionally provided are methods of inhibiting an inflammatory response in a mammal. Further provided is the use of an α2A-adrenergic antagonist for the manufacture of a medicament for preventing or treating a physiologic effect of sepsis in a mammal, and the use of an α2A-adrenergic antagonist for the treatment of a mammal having sepsis or at risk for sepsis.

Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

The present disclosure provides for improved methods for treating pain, including pain associated with chronic inflammatory diseases, neuropathic pain and cancer by using α-adrenergic antagonists and β-adrenergic agonists (particularly β2-adrenergic agonists) alone or in combination.

Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2-) scavengers, beta-adrenergic agonists, cAMP-dependent protein kinase activators, alpha1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.

The present disclosure provides for improved methods for treating pain, including pain associated with chronic inflammatory diseases, neuropathic pain and cancer by using α-adrenergic antagonists and β-adrenergic agonists (particularly β2-adrenergic agonists) alone or in combination.

The present invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are alpha-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are alpha-1 antagonist compositions and a method for antagonizing alpha-1 adrenoreceptors and treating BPH.

A pharmaceutical composition including active ingredients of (R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl-2-methoxybenzene-1-sulfonamide and (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid (3R)-quinuclidin-3-yl ester, or their pharmaceutically acceptable salts, provides improvement of lower urinary tract symptoms associated with prostatic hypertrophy. The active ingredients may be administered either simultaneously or at a time interval. The pharmaceutical composition also provides significant improvement of lower urinary tract symptoms associated with benign prostatic hyperplasia having a substantial storage component.

The present invention discloses a novel compound and method for the treatment of inflammatory autoimmune diseases, for example, rheumatoid arthritis, using α-adrenergic antagonists and β-adrenergic agonists in combination. Treatment of animals, namely humans, with an α-adrenergic antagonist, preferably, phentolamine, and a β-adrenergic agonist, preferably terbutaline, in combination can significantly suppress the joint destruction and inflammation due to disease in these animals.

Pharmaceutical compositions are provided including therapeutically effective amounts of an α1 adrenergic receptor antagonist, together with one or more of (1) a mu (or opioid receptor subtype) antagonist or agonist, (2) a vasopressor, (3) an anticholinergic agent and / or cholinergic agents. (4) a combined alpha-1 adrenergic antagonist and anticholinergic (e.g. droperidol), (5) a paralytic or muscle relaxant, (6) a respiratory accelerant, (7) a GABA complex antagonist, (8) an anti-seizure / membrane stabilizer agent, (9) an α1 adrenergic receptor agonist, and / or (10) an α2 adrenergic receptor agonist; and a pharmaceutically acceptable carrier. Also provided are methods of preventing or reversing effects in a subject (including muscle and chest wall rigidity, laryngospasm, WCS, and / or respiratory depression) arising from intentional or accidental opioid or opiate exposure, involving administering to the subject such a pharmaceutical composition. Methods of providing analgesia with a modified side effect profile to reduce risk of WCS or respiratory effects are also provided.

The invention provides methods, compositions, and kits containing an alpha-adrenergic antagonist, such as phentol amine, for use in mono-therapy or as part of a combination therapy to treat patients suffering from presbyopia, mydriasis, and / or other ocular disorders.

The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a beta-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and / or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and / or growth in a mammal by administering a composition comprising a beta2-selective antagonist or agonist.

A method for healing a hard-to-heal wound including the steps of: topically administering a wound healing composition to a wounded area, wherein the wound healing composition includes, at least one of: (a) a medicament characterized as a calcium channel blocker or pharmaceutically acceptable salts or solvates thereof; (b) a medicament characterized as an alpha-adrenergic antagonist or pharmaceutically acceptable salts or solvates thereof; (c) a medicament characterized as a direct vasodilator or pharmaceutically acceptable salts or solvates thereof; and (d) a medicament characterized as a phosphodiesterase type five inhibitor or pharmaceutically acceptable salts or solvates thereof; and (e) a hemorrheologic agent or pharmaceutically acceptable salts or solvates thereof; (f) a primary dermal penetrating agent or pharmaceutically acceptable salts or solvates thereof: and (g) a topical stimulating agent or pharmaceutically acceptable salts or solvates thereof.

The invention provides methods for (a) prolonging time to hospitalization for heart failure; (b) prolonging time to first hospitalization for heart failure; (c) reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); (d) reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays; (e) reducing the number of hospital admissions for heart failure; and (f) reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and / or the number of hospital visits) in a patient in need thereof comprising administering to the patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and / or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), and diuretic compounds.

The invention provides methods for reducing the total number of days a patient with heart failure spends in the hospital for heart failure for a single hospital stay (i.e., reducing the duration of a single hospital stay for a patient with heart failure); reducing the total number of days a patient spends in the hospital for heart failure for multiple hospital stays (i.e., two or more hospital stays); reducing the number of hospital admissions for heart failure; and reducing mortality and reducing hospitalizations for heart failure (e.g., the total number of days in the hospital and / or the number of hospital visits); by administering to a patient a therapeutically effective amount of (i) a hydralazine compound or pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and / or isosorbide mononitrate, and (iii) optionally at least one angiotensin converting enzyme inhibitors, β-adrenergic antagonists, angiotensin II antagonists, aldosterone antagonists, cardiac glucosides (digitalis), or diuretic compounds.

Pharmaceutical compositions are provided including therapeutically effective amounts of an α1 adrenergic receptor antagonist, together with one or more of (1) a mu (or opioid receptor subtype) antagonist or agonist, (2) a vasopressor, (3) an anti-cholinergic agent and / or cholinergic agents, (4) a combined alpha-1 adrenergic antagonist and anticholinergic (e.g. droperidol), (5) a paralytic or muscle relaxant, (6) a respiratory accelerant, (7) a GABA complex antagonist, (8) an anti-seizure / membrane stabilizer agent, (9) an α1 adrenergic receptor agonist, and / or (10) an α2 adrenergic receptor agonist; and a pharmaceutically acceptable carrier. Also provided are methods of preventing or reversing effects in a subject (including muscle and chest wall rigidity, laryngospasm, WCS, and / or respiratory depression) arising from intentional or accidental opioid or opiate exposure, involving administering to the subject such a pharmaceutical composition. Methods of providing analgesia with a modified side effect profile to reduce risk of WCS or respiratory effects are also provided.

Methods, compositions and kits comprising alpha-adrenergic antagonists, such as phentolamine, for the treatment of glaucoma, ocular hypertension, and / or other ocular disorders, such as non-arteritic anterior ischemic optic neuropathy or keratoconus, are provided. Said methods, compositions and kits may further comprise additional therapeutic agents, including prostaglandin analogues such as latanoprost, beta-adrenergic antagonists, alpha-adrenergic agonists, carbonic anhydrase inhibitors, cholinergic agonists, NMDA receptor antagonist, adenosine receptor antagonists, 5-HT2a receptor agonists, or Rho kinase inhibitors.

Provided are methods for treating a mammal undergoing sepsis, or at risk for sepsis. Also provided are methods of preventing or treating a physiological effect of sepsis in a mammal. Additionally provided are methods of inhibiting an inflammatory response in a mammal. Further provided is the use of an α2A-adrenergic antagonist for the manufacture of a medicament for preventing or treating a physiologic effect of sepsis in a mammal, and the use of an α2A-adrenergic antagonist for the treatment of a mammal having sepsis or at risk for sepsis.