Glycine Derivatives with P2x4 Receptor-Blocking Activity as Diagnostics and for the Treatment of Pain, Inflammation, Cancer, and Other P2x4 Receptor-Related Diseases

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

This patent discloses a new class of glycine derivatives that function as potent and selective antagonists of the P2X4 receptor, a type of ATP-gated ion channel implicated in pain, inflammation, cancer, and other diseases. These compounds can block the P2X4 receptor's activity, providing a novel approach to treat chronic neuropathic and inflammatory pain, neurodegenerative diseases, and certain types of cancer. The patent also covers the use of these compounds as diagnostic tools and provides extensive synthetic methods for their preparation.

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

• Treatment of chronic neuropathic and inflammatory pain (e.g., diabetic neuropathy, trigeminal neuralgia, chronic pain syndromes)
• Therapy for neurodegenerative diseases such as Alzheimer's, Parkinson's, ALS, and multiple sclerosis
• Use in treating cancers such as colon, liver, prostate, gastric, breast cancer, and glioma
• Management of CNS disorders including epilepsy, stroke, and traumatic brain injury
• Intervention in inflammatory disorders like rheumatoid arthritis, colitis, allergic asthma, atherosclerosis, and obesity-related or liver inflammation
• Adjunct therapy in pain and depression comorbidity
• Diagnostic tools for diseases involving P2X4 receptor overactivity

BenefitsContent extracted from patent full text and abstract with AI.

• Selective blockade of the P2X4 receptor may provide pain relief without some of the drawbacks of current pain medications
• Potential for neuroprotection and modification of disease progression in neurodegenerative and CNS injury scenarios
• Applicability to a broad range of chronic and hard-to-treat pain conditions, including those refractory to traditional therapies
• Possible synergistic or adjunct effects in cancer therapy, particularly in tumor types where P2X4 signaling contributes to pathology or treatment resistance
• Reduced risk of side effects compared to less selective P2X family antagonists
• Novel diagnostic capabilities for identifying and monitoring P2X4-related disease states
• Versatility of administration (oral, injectable, topical, etc.), increasing treatment adaptability

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to glycine derivatives with P2X4 receptor-blocking activity for the treatment of pain, inflammation, cancer, and other P2X4 receptor-related diseases.