Beta-2 Selective Adrenergic Receptor Agonists

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes a new class of chemical compounds that act as highly selective beta-2 adrenergic receptor (β2AR) agonists, distinguishing themselves from standard beta-adrenergic agonists by their targeted action and reduced side effects. The compounds are conformationally constrained analogs of traditional catecholamines (like adrenaline or isoprenaline) engineered to preferentially activate β2AR over β1AR. These new agonists are proposed for use as bronchodilators in respiratory diseases (e.g., asthma, COPD), for managing preterm labor, and in other therapeutic settings where selective β2AR activation is beneficial. Methods of making, using, and delivering these drugs (including inhalers, nebulizers, and injections) are also disclosed.

Use CasesContent extracted from patent full text and abstract with AI.

• Treatment of asthma, bronchial asthma attacks, and chronic obstructive pulmonary disease (COPD) as bronchodilators to relieve airway constriction.
• Acute rescue therapy for asthma attacks via inhaled formulations.
• Prevention and management of preterm labor in pregnant individuals by relaxing uterine smooth muscle.
• Adjunct or alternative treatment for heart failure where β2AR signaling is beneficial.
• Reduction of side effects in patients sensitive to or at risk from non-selective beta-agonists, such as those with cardiovascular issues.
• Potential use in veterinary medicine for respiratory or uterine conditions in animals.
• Research tools for studying β2AR function in cells and tissues due to their selectivity and signaling bias.

BenefitsContent extracted from patent full text and abstract with AI.

• Increased selectivity for β2AR over β1AR, dramatically reducing cardiovascular side effects such as elevated blood pressure, arrhythmia, and tachycardia common in non-selective β-agonists.
• Potential for improved safety and tolerability for patients with underlying heart conditions or who are sensitive to β1AR stimulation.
• Effective bronchodilation for respiratory diseases (asthma, COPD) due to potent and selective β2AR activation.
• Applications in preterm labor management by specifically targeting uterine relaxation with fewer off-target effects.
• Availability in multiple delivery formats, including inhalers and nebulizers for direct lung delivery, and injections (autoinjectors) for emergency use.
• Compositions can be tailored for short- or long-acting therapeutic needs.
• May allow lower effective dosing due to enhanced receptor match and potency, further minimizing side effects.

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Inventors & Applicants

Patent Abstract

Aspects of the present disclosure include conformationally restricted analogs of catecholamine type compounds (e.g., isoprenaline, adrenaline, noradrenaline) which activate β2AR with high selectivity over β1AR. The subject beta-2 selective adrenergic receptor agonist compounds may serve as bronchiodilators and find use in the treatment of a variety of bronchoconstrictive diseases and conditions. Also provided are compositions and methods for treating preterm labor. A method of treating acute asthma including administration of a subject compound to a subject in need thereof is provided. The subject method can provide for reduced undesirable side effects associated with non-selective β-adrenergic receptor agonism, such as inotropic and chronotropic effects that leads to elevated blood pressure. The compounds can also be used to prevent or treat heart failure. Kits and compositions for practicing the subject methods are also provided.