3-substituted Xanthine Derivatives as Mrgprx4 Receptor Modulators

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

This invention is about a new class of chemical compounds—specifically, 3-substituted xanthine derivatives—that function as modulators (agonists or antagonists) of the human MRGPRX4 receptor, a protein involved in sensory perception in humans. Modulating this receptor can have significant therapeutic effects, especially in the management of conditions such as chronic pain, chronic itch, and wounds. The patent covers the compounds themselves, their chemical synthesis, and their pharmaceutical use, particularly for promoting wound healing and controlling pain and itch.

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

• Topical or local pharmaceutical treatments to promote wound healing (including incisions, lacerations, abrasions, punctures, and crash injuries)
• Medications to manage and reduce chronic pain, neuropathic pain, or other persistent painful states
• Therapies to relieve chronic itch (pruritus) associated with skin disorders or systemic diseases
• Combination therapy with other agents (e.g., anti-inflammatories, antibiotics) for enhanced wound care
• Potential use in dermatological creams, gels, or patches for targeted delivery to skin or injured tissue
• Possible research tools to study the MRGPRX4 receptor function and biology in sensory neurons

BenefitsContent extracted from patent full text and abstract with AI.

• Offers a novel, targeted approach to pain and itch relief by acting directly on a human-specific sensory receptor (MRGPRX4)
• Potential for faster and improved wound healing through activation of keratinocytes
• Reduces reliance on systemic pain medications, possibly resulting in fewer side effects
• Compounds can be formulated for topical or local administration, allowing direct application to the affected area and minimizing systemic exposure
• Applicable to both acute injuries (wounds) and chronic conditions (pain, itch)
• Human specificity (not expressed in rodents), increasing translational relevance for human therapy
• Versatile chemical structures allow for fine-tuning of pharmacological properties for different medical needs

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to MRGPRX4 receptor agonists and antagonists useful for treating, alleviating and/or preventing diseases and disorders related to MRGPRX4 receptor function as well as pharmaceutical compositions comprising such compounds and methods for preparing such compounds. The invention is further directed to the use of these compounds, alone or in combination with other therapeutic agents, for alleviating, preventing and/or treating diseases and disorders, especially the use as wound healing medicaments and for the treatment of chronic pain and itch.