Use of Glycine Transporter 1 Antagonists as Central Nervous Analgesics

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This patent describes the use of Glycine Transporter 1 (GlyT1) antagonists, specifically compounds such as Bitopertin, as new central nervous system analgesics for treating chronic and/or neuropathic pain. These compounds act by inhibiting GlyT1 in the nervous system, thereby increasing glycine levels and enhancing pain inhibition pathways with fewer side effects compared to conventional treatments like opioids. The invention covers pharmaceutical compositions, dosing, routes of administration (oral, injectable), and potential co-administration with other painkillers or co-analgesics.

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

• Treatment of chronic pain conditions, such as those persisting after injury or disease healing
• Therapy for neuropathic pain resulting from nerve damage, diabetes, or chemotherapy
• Pain management in cancer patients suffering from persistent neuropathic pain
• Adjunctive therapy in combination with existing analgesics (e.g., opioids, NSAIDs, antidepressants, anticonvulsants) to enhance pain relief and reduce dosage requirements
• Use in animal health for chronic pain in pets or horses

BenefitsContent extracted from patent full text and abstract with AI.

• Provides new treatment option for chronic and neuropathic pain, where current therapies are often inadequate or have substantial side effects
• Demonstrates effective pain reduction without typical central nervous system side effects (e.g., dizziness, drowsiness, addiction potential) seen with traditional pain medications
• High oral bioavailability, enabling convenient dosing and potentially better patient compliance
• Reversible mechanism of action reduces risk of permanent receptor changes or tolerance
• Broad applicability, including use in humans and other mammals
• Potential to lower the required dose of other analgesics when used in combination, reducing related adverse events

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

Die Erfindung betrifft die Verwendung von Verbindungen der Formel (I) als Glycin-Transporter-1-Antagonisten zur Behandlung von chronischen und/oder neuropathischen Schmerzen.