Beta-adrenergic Receptor Allosteric Modulators

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

This patent discloses a new class of chemical compounds that function as allosteric modulators of beta-adrenergic receptors, particularly beta-2 adrenergic receptors (β2AR). These modulators bind to an allosteric (non-orthosteric) site on the receptor, altering how the receptor responds to endogenous signaling molecules like adrenaline and noradrenaline. The compounds are designed to provide more selective and finely-tuned modulation of β2AR activity, which can minimize off-target effects. The patent identifies these compounds, details their synthesis, their specific binding mechanism elucidated by X-ray crystallography and molecular dynamics, and demonstrates their ability to modulate receptor signaling relevant to diseases such as asthma, cardiovascular conditions, and Parkinson’s disease.

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

• Development of new medications to treat asthma by modulating β2-adrenergic signaling more selectively.
• Treatment of cardiovascular diseases, such as hypertension and heart failure, by finely regulating β2AR activity.
• Design of therapies for neurodegenerative diseases including Parkinson's disease, based on β2-adrenergic receptor involvement.
• Adjunct therapies alongside existing β2AR antagonists or agonists, providing increased subtype selectivity and fewer side effects compared to traditional ligands.
• Potential research tools for dissecting GPCR allosteric signaling mechanisms in drug discovery.

BenefitsContent extracted from patent full text and abstract with AI.

• Greater receptor subtype selectivity compared to traditional orthosteric (active site) drugs, reducing risks of off-target effects.
• Ability to fine-tune receptor responses rather than fully activating or blocking them, leading to better safety profiles (e.g., less risk of overdose or excessive inhibition/activation).
• Novel mechanism of action by targeting an allosteric site, which may retain efficacy where resistance to orthosteric drugs develops.
• Versatility to be used in combination with other β2AR agents for additive or synergistic therapeutic effects.
• Potential to advance treatment options for a range of prevalent, complex diseases including asthma, heart disease, and certain neurodegenerative disorders.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

Provided herein are modulators of beta-adrenergic receptors.