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236 results about "Adrenergic receptor" patented technology
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The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, β₂ agonists and α₂ agonists, which are used to treat high blood pressure and asthma, for example.
Stabilized extended release pharmaceutical compositions comprising a beta-adrenoreceptor antagonist
InactiveUS20070092573A1Well formedStrengthen matrixBiocideOrganic active ingredientsGreek letter betaAdrenergic receptor sites
The present invention is a new stable extended release drug composition particularly suitable for use as a beta-adrenoreceptor antagonist agent. The present invention is specifically a drug composition comprising a pharmaceutical, a methacrylic acid copolymer and a matrix forming agent, and a method for manufacturing same. When applied to highly soluble drugs like metoprolol succinate, the resulting drug composition is characterized by an extended-release profile.
Owner:ORBUS PHARMA INC
Arthroscopic irrigation solution and method for peripheral vasoconstriction and inhibition of pain and inflammation
InactiveUS20030087962A1Control inflammationPain controlBiocideKallidin/bradykinin ingredientsArteriolar VasoconstrictionInflammation Process
A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that demonstrates substantial agonist activity at alpha adrenergic receptors and that is selected for peripheral (local) vasoconstriction and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and / or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.
Owner:OMEROS CORP
Compounds and methods for the treatment of urogenital disorders
InactiveUS6987129B2Reduce painLess discomfortBiocidePeptide/protein ingredientsDiseaseFemale Sexual Arousal Disorder
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).
Owner:STREHKEHN INT LTD
4-(2-Methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2B agonist and methods of using the same
The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and / or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
Owner:ALLERGAN INC
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
The compound of the formulawherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and / or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
Owner:ALLERGAN INC
Compounds and methods for treating diabetes
ActiveUS20130190294A1Lower blood sugar levelsStabilize blood sugar levelsBiocideOrganic chemistryAntagonistDisease cause
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α2B; or the compounds are not antagonists of the adrenergic receptor α2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
Owner:MEDIVATION TECH INC
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and / or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and / or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and / or sedatory activity.
Owner:ALLERGAN INC
Novel methods and compositions for alleviating pain
The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic alpha-adrenergic receptor in the absence of alpha-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic alpha-adrenergic receptor can be, for example, the alpha-2B receptor.
Owner:ALLERGAN INC
Compounds and methods of treating diabetes
InactiveUS20140155384A1Lower blood sugar levelsIncreased insulin secretionBiocideOrganic chemistryDiseaseAdrenergic
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α2B; or the compounds are not antagonists of the adrenergic receptor α2β and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
Owner:MEDIVATION TECH INC
Method of therapeutic administration of dhe to enable rapid relief of migraine while minimizing side effect profile
Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (Cmax) and slightly delaying the peak such as to avoid activating the dopaminergic and adrenergic receptors, while achieving sufficient active binding to the serotonin receptors to provide relief from migraine symptoms within a timeframe that permits rapid resolution of migraine symptoms. Inhaler devices suitable for the methods are disclosed. Kits for practicing the methods of invention are disclosed.
Owner:MAP PHARMACEUTICAL INC
Compounds and methods of treating hypertension
InactiveUS20140303144A1Speed up the flowDecreasing sodium reabsorptionBiocideOrganic chemistryDiseaseBlood flow
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and / or (ii) promote renal blood flow and / or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
Owner:MEDIVATION TECH INC
Compounds and methods for the treatment of urogenital disorders
Owner:STREHKEHN INT LTD
Real-time polymerase chain reaction-based genotyping assay for beta2-adrenergic receptor single nucleotide polymorphism
InactiveUS20050153353A1Rapid and inexpensive and robust chain reactionGrowth inhibitionSugar derivativesMicrobiological testing/measurementGenotype AssayReal-Time PCRs
The present invention provides fluorescence-based real-time PCR assays for the rapid detection of β2-adrenergic receptor single nucleotide polymorphisms (SNPs). The genotyping assay can be used to detect SNPs of human β2-adrenergic receptor (β2-AR) single nucleotide polymorphisms A46G and C79G.
Owner:UNIV OF TENNESSEE RES FOUND
Compounds and methods for treatment of hypertension
InactiveUS20140296209A1Increase heart rateGood blood pressureBiocideOrganic chemistryNephropathyPyridine
Owner:MEDIVATION TECH INC
Methods and compositions for inhibition of beta2-adrenergic receptor degradation
The present invention generally relates to compositions and kits comprising a β2-AR agonist and a modulator of a β2-AR regulator gene, where the modulator of the β2-AR regulator gene inhibits the internalization and / or degradation of the β2-ad-renergic receptor (β2-AR). More specifically, the present invention relates to the use of an agonist of β2-adrenergic receptor (β2-AR) and an agent which inhibits agonist induced β2-adrenergic receptor (β2-AR) internalization and / or degradation in method for the treatment of a respiratory disorder in a subject.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE
Image-guided therapy of myocardial disease: composition, manufacturing and applications
InactiveUS8440168B2Ultrasonic/sonic/infrasonic diagnosticsOrganic active ingredientsEthylenediamineRadical radiotherapy
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST
Compounds and methods for treatment of hypertension
InactiveUS20130053366A1Increase heart rateGood blood pressureBiocideOrganic chemistryDiseaseTreatment hypertension
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and / or (ii) promote renal blood flow and / or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
Owner:MEDIVATION TECH INC
Antihypertensive therapy
InactiveUS20090221549A1Beneficial effect on renal functionLower blood pressureBiocideAnimal repellantsAmbulatoryAnti hypertensive treatment
A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and / or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.
Owner:ABBOTT GMBH & CO KG
Compounds and methods of treating diabetes
InactiveUS20130053367A1Increased insulin secretionLower blood sugar levelsBiocideOrganic chemistryDiseaseAdrenergic
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α2A. The compounds may also bind to and are an antagonist of the adrenergic receptor α2B; or the compounds are not antagonists of the adrenergic receptor α2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
Owner:MEDIVATION TECH INC
Beta3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with .beta.-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases. 1
Owner:PFIZER INC
Dihydroindolyl methanones as alpha 1a/1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms
InactiveUS20060183902A1Affects blood pressureEffective amountBiocideOrganic chemistryEccentric hypertrophyDisease
The present invention relates to new compounds of Formula (I): and pharmaceutically acceptable forms thereof, use of the compounds as α1a and / or α1d adrenoreceptor modulators, including use of a pharmaceutical composition, medicine or medicament comprising said compounds, a process to prepare said compounds and a method for treating an α1a and / or α1d adrenoreceptor mediated disorder.
Owner:JANSSEN PHARMA NV
Heterodimeric opioid G-protein coupled receptors
InactiveUS6855807B1Effective treatmentAccurate identificationBacteriaBiological material analysisMu Opiate ReceptorHigh-throughput screening
Opioid receptors form functional heterodimers with each other and with other G-protein coupled receptors, such as dopamine receptors, adrenergic receptors, or chemokine receptors. These receptors can be exploited for high throughput screening of compounds to identify heterodimer opioid receptor modulators (agonists and antagonists). The invention also relates to identification of novel heterodimer receptor ligands and synergistic compositions, which can provide strategies for analgesia, narcotic addiction, hypertension, HIV infection, and immune system function.
Owner:NEW YORK UNIV
4-(Substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4- (substituted cycloalkylmethyl) imidazol-2-ones and 4- (substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and / or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and / or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and / or sedatory activity.
Owner:ALLERGAN INC
Method for treating resistant hypertension
A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.
Owner:MYOGEN INC +1
4-(Heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
InactiveUS20060069143A1Antibacterial agentsOrganic active ingredientsDiseaseAlpha2 adrenergic agonist
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.
Owner:ALLERGAN INC
Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the β2 adrenergic receptor
A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH═CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.
Owner:ALMIRALL
Prevention and treatment of sarcopenia
ActiveUS20120095070A1Good effectHigh prevalenceOrganic active ingredientsBiocideAdrenergicSarcopenia
The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.
Owner:ACTIMED THERAPEUTICS LTD
4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists
InactiveUS20060069144A1Minimal cardiovascularMinimal sedatory activityBiocideSenses disorderDiseaseSide effect
Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and / or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and / or sedatory activity are useful for treating pain and other conditions with minimal side effects.
Owner:ALLERGAN INC
Derivatives of 4-(2-amino-1-hydroxiethyl)phenol as agonists of the b2 adrenergic receptor
Owner:ALMIRALL
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
InactiveUS20070072926A1Minimal activityReduce chronic painOrganic active ingredientsBiocideDiseaseAdrenergic
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and / or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and / or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and / or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and / or sedatory activity.
Owner:ALLERGAN INC
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