82 results about "Adrenergic receptor agonists" patented technology

Disclosed in certain embodiments is a method of treating a drug overdose comprising administering to a patient in need thereof a therapeutically effective amount of a respiratory stimulant, wherein the overdosed drug comprises an α2 adrenergic receptor agonist.

A method for preparing an intermediate of an adrenergic receptor agonist. The method comprises the following steps: cyclizing the compound of formula E1 or the compound of formula E2 and the compound of formula F0 to obtain the compound of formula C, wherein R1 is methyl, ethyl, isopropyl, propyl, tert-butyl, or butyl; R3 is H, Cl, F or Br; and L1 and L2 are each individually a leaving group. The method uses easily available raw materials, avoids the use of toxic and harmful reagents, is mild in terms of reaction conditions, is simple to operate, achieves a substantial improvement in yield and reduction in cost, and is more favorable for commercial production.

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.

Disclosed herein are methods for treating a fatigue disorder in a subject in need thereof. The method may include administering to the subject by a therapeutically effective amount of a composition comprising an alpha-2 adrenergic agonist, such as guanfacine. Also disclosed herein are methods of diagnosing a fatigue disorder in a subject.

The present invention provides a beta-3 adrenergic receptor agonist, along with its pharmaceutical composition, for use in the treatment and / or prevention of pulmonary fibrosis, preferably pulmonary fibrosis associated with bronchopulmonary dysplasia (BPD).

Respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) are commonly treated with β2-adrenergic receptor agonists that activate intracellular signaling pathways to induce airway relaxation. However, current therapies are limited by progressive receptor desensitization, or tachyphylaxis, largely attributed to β-arrestin recruitment. This desensitization reduces therapeutic efficacy over time and complicates long-term disease management, resulting in suboptimal outcomes for patients who rely on bronchodilators for daily symptom control. Disclosed herein are pharmaceutical compositions comprising biased agonists and their methods of use, which minimally activate recruitment of beta-arrestin2.

There is herein provided a pharmaceutical formulation comprising one or more compounds that are β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and β3-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and optionally one or more pharmaceutically acceptable excipient, for use in the treatment or prophylaxis of obesity and other medical uses.

The present disclosure relates to compositions, formulations, and associated methods for treating neurodegenerative diseases, wherein the compositions include an alpha-1 adrenergic agonist, such as midodrine, and an alpha-2A adrenergic agonist, such as dexmedetomidine. Upon administering to a human subject, the alpha-2A adrenergic agonist crosses the subject's blood-brain barrier thereby acting upon the subject's central nervous system, whereas the alpha-1 adrenergic agonist does not cross the subject's blood-brain barrier. The alpha-1 adrenergic agonist minimizes or eliminates the systemic vascular effects induced by the alpha-2A adrenergic agonist that causes the negative cerebral autoregulatory response, thereby enabling the alpha-2A adrenergic agonist to increase glymphatic flow in the subject's brain.

The invention relates to an ophthalmic spray combined preparation for relieving blepharoptosis or relieving red eyes from blepharoptosis. The ophthalmic spray combined preparation is characterized by comprising the following components in percentage by mass: 0.01-1.15% of an alpha-adrenergic receptor agonist, 0.01-1.15% of an emulsifier, 0.01-1.15% of an emulsifier and the balance of water. 0.1% to 0.3% of sodium hyaluronate; 0.01%-2% of an osmotic pressure regulator; the liquid medicine further comprises a pH buffering agent, wherein the concentration of the pH buffering agent is 0.002 M to 0.16 M; the thickening agent is one or a combination of more of hydroxyethyl cellulose, polyvinyl alcohol and povidone, and the mass percent of the vitamin A derivative and the vitamin E derivative is 0.01%-0.2%. The spray preparation comprises a spraying device, and the spray particle size ranges from 5 mu m to 500 mu m, preferably ranges from 5 mu m to 100 mu m, and more preferably ranges from 10 mu m to 30 mu m.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

Disclosed is a pharmaceutical composition in dry powder form for intranasal administration, comprising an anti-anaphylactic adrenergic receptor agonist in the form of dry powder for intranasal administration, the composition comprising solid particles of the active agent in combination with at least one functional additive, and solid particles of an inert carrier.

The present disclosure provides for fixed-dose combination formulations comprising flavoxate or a pharmaceutically acceptable salt thereof and at least one β3-adrenergic receptor agonist, along with methods of making and using the same to treat symptoms associated with prostate, bladder, urinary tract, and pelvic conditions.

Provided are methods for treating trigeminal nerve pain in a subject in need thereof. The method may include administering to the subject by perineural injection of the trigeminal nerve a therapeutically effective amount of a composition comprising an alpha-2 adrenergic agonist, such as guanfacine. The composition may further comprise lidocaine.

There is herein provided a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment or prophylaxis of a disease or disorder characterised by muscle wasting.

The application discloses a refining method of a selective beta3-adrenergic receptor agonist, which comprises the following steps: (1) dissolving the crude selective beta3-adrenergic receptor agonist in an anhydrous ethanol / purified water system, the mass ratio of the anhydrous ethanol and the purified water being 0.5-0.65:1, to obtain a solution with a concentration of 0.01-0.3 g / ml; (2) adding a selective beta3-adrenergic receptor agonist crystal seed at 55-70 DEG C, and then gradually cooling to 0-10 DEG C to stir and crystallize; and (3) filtering, washing and drying to obtain the selective beta3-adrenergic receptor agonist. The refining method of the selective beta3-adrenergic receptor agonist has high yield, and the obtained selective beta3-adrenergic receptor agonist has high purity and low acetylated impurity content.

The present invention discloses a class of 4-(1H)-imidazole derivatives represented by the following formula (I), their pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomers and tautomers, as well as pharmaceutical compositions containing them, and their use as α2-adrenergic receptor agonists, especially as α 2A -agonists and their methods of use. Compared with the prior art, the compounds of the present invention show more potent agonist activity and higher selectivity for α 2A -AR, superior to the positive drug dexmedetomidine; and at the same time have a potent in vivo sedative effect. #imgabs0#

To provide a composition or the like for treating agitation or signs of agitation.SOLUTION: The present invention discloses a method of treating agitation or signs of agitation in a subject comprising sublingual administration of an effective amount of an alpha-2 adrenergic agent, more particularly dexmedetomidine or a pharmaceutically acceptable salt thereof. The method is particularly suitable for the treatment of agitation associated with neurodegenerative diseases and / or neuropsychiatric diseases. The present invention also discloses sublingual administration of an alpha-2 adrenergic agent, more specifically dexmedetomidine or a pharmaceutically acceptable salt thereof, at a dose that is effective to treat agitation or the symptoms of agitation but does not cause significant sedation in the subject.SELECTED DRAWING: Figure 1A

There is provided herein a method of treatment comprising: (i) a first treatment cycle comprising administration of a therapeutically effective amount of a therapeutic agent, or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the therapeutic agent directly or indirectly induces muscle wasting; and (ii) a second treatment cycle following the discontinuation of the first treatment cycle, wherein the second treatment cycle comprises administration of a therapeutically effective amount of a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, to the subject, wherein the first and second treatment cycles are within the same therapeutic intervention.

Provided are methods for treating trigeminal nerve pain in a subject in need thereof. The method may include administering to the subject by perineural injection of the trigeminal nerve a therapeutically effective amount of a composition comprising an alpha-2 adrenergic agonist, such as guanfacine. The composition may further comprise lidocaine.

The present invention provides ophthalmic formulations comprising long-acting beta-adrenergic receptor agonist (LABA) compounds, long-acting muscarinic antagonists (LAMA), and combinations thereof. Also provided are methods of treating visual impairment with LABA, LAMA, and combinations thereof.

This specification provides a β2-adrenergic receptor agonist or a pharmaceutically acceptable salt thereof for use in the treatment and / or prophylactic care of hyperglycemia or a disorder characterized by hyperglycemia, wherein the treatment and / or prophylactic care further comprises the administration of (a) insulin or a therapeutic insulin derivative, or (b) a therapeutic agent that stimulates the release of insulin.

Provided herein are methods, compositions, kits, and systems for treating depression and / or producing an electroencephalogram (EEG) profile using a combination of anesthetics. The combination of anesthetics may include a NMDA-type glutamatergic receptor antagonist anesthetic, a GABAergic anesthetic, or a α2-adrenergic receptor agonist anesthetic.

The present disclosure relates to novel alpha-2 adrenergic receptor (α2AR) agonists and uses thereof. In particular, the present disclosure relates to imidazole containing compounds, in particular, of formula (I-A), formula (I-B), formula (I-C), formula (I-D), or formula (II). These compounds can be useful as peripherally selective α2AR agonists for the treatment or prevention of disease thereof, either used alone or in combination with a second therapeutical agent.

The compounds and methods of the present disclosure exhibit induce Ucp1 transcription, enhance of mitochondrial respiration, activate protein kinase A, increase lipolysis, and increase p38 MAPK phosphorylation in cells, particularly brown adipocytes and white adipocytes. They also protect primary cardiomyocytes against hypertrophy induced by adrenergic agonists. Such compounds and methods are useful in the treatment and prevention of conditions such as obesity and associated complex metabolic, endocrine, and hemodynamic changes, as well as related conditions as dyslipidemias, cardiovascular disease, and type 2 diabetes.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

Described are compositions, combinations, and methods of using the compositions and combinations for use in treating depression. The compositions and combinations comprise a GABA B receptor agonist and an alpha-2 adrenergic receptor agonist.

In some embodiments, the present invention discloses a method for treating drug overdose, comprising administering a therapeutically effective amount of a respiratory stimulant to a patient in need, wherein the overdose drug comprises an α2-adrenergic receptor agonist.

The present disclosure relates to compositions, formulations, and associated methods for treating neurodegenerative diseases, wherein the compositions include an alpha-1 adrenergic agonist, such as midodrine, and an alpha-2A adrenergic agonist, such as dexmedetomidine. Upon administering to a human subject, the alpha-2A adrenergic agonist crosses the subject's blood-brain barrier thereby acting upon the subject's central nervous system, whereas the alpha-1 adrenergic agonist does not cross the subject's blood-brain barrier. The alpha-1 adrenergic agonist minimizes or eliminates the systemic vascular effects induced by the alpha-2A adrenergic agonist that causes the negative cerebral autoregulatory response, thereby enabling the alpha-2A adrenergic agonist to increase glymphatic flow in the subject's brain.

To provide a non-surgical alternative to blepharoplasty for treatment and cosmetic applications.SOLUTION: To provide cosmetic and therapeutic compositions of alpha-adrenergic agents. The compositions of the disclosure may be used for topical, transdermal or parenteral administration to the eye or eyelid. The compositions of the present disclosure may be used cosmetically to improve the appearance of the eye or therapeutically to treat ptosis.SELECTED DRAWING: None

Disclosed herein are compositions for supporting bladder health and / or treating, ameliorating, preventing or ameliorating overactive bladder or a symptom associated therewith. The compositions disclosed herein comprise a beta-adrenergic receptor agonist and at least one muscarinic receptor antagonist. Also described herein are methods of using the above compositions.