Substituted Vicinal Diamine Compounds and Their Use in the Treatment, Amelioration or Prevention of Pain

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

This patent relates to a new class of substituted vicinal diamine compounds designed to act as modulators of opioid receptors — especially the µ-opioid receptor — with a functional selectivity favoring G-protein signaling over β-arrestin recruitment. These compounds aim to offer effective pain relief and treatment of various disorders, including opioid overdose, addictions, neuropsychiatric, gastrointestinal, and skin conditions, with a reduced risk of common opioid side effects such as respiratory depression and constipation. The invention also covers pharmaceutical compositions using these compounds and describes their synthesis, pharmacological properties, and potential routes of administration.

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

• Treatment of acute and chronic pain, including pain associated with disease, injury, or surgical procedures
• Management of opioid overdose (e.g., reversing respiratory depression from drugs like fentanyl, heroin, or morphine)
• Treatment of opioid, nicotine, alcohol, or behavioral addictions
• Relief of neuropsychiatric disorders (such as depression, anxiety, obsessive-compulsive disorder, Tourette’s syndrome, eating and sleep disorders, and schizophrenia)
• Therapy for Prader-Willi Syndrome
• Managing gastrointestinal disorders (like constipation, diarrhea, irritable bowel syndrome, and Crohn’s disease)
• Treatment of skin disorders, including chronic itching and urticaria
• Relief of dyspnea (shortness of breath)
• Treatment of headaches and temporomandibular joint (TMJ) dysfunction
• Use in combination therapies, potentially replacing or supplementing existing opioids with a safer alternative

BenefitsContent extracted from patent full text and abstract with AI.

• Reduced side effects compared to traditional opioids (notably lower risk of respiratory depression and constipation) due to functional selectivity at opioid receptors
• Potential for improved safety in the treatment of pain and overdose scenarios
• Broad applicability across diverse medical conditions beyond pain, including addictions and neuropsychiatric disorders
• Favorable pharmacokinetic properties, such as metabolic stability and ability to cross the blood-brain barrier, making them effective for central nervous system indications
• Structure allows for formulation in various pharmaceutical forms enabling oral, parenteral, transdermal, and topical delivery
• May reduce the risk of addiction while treating pain, supporting use in populations at risk for opioid dependency
• Potential to improve the quality of life for patients suffering from chronic pain, addiction, or neuropsychiatric diseases by providing more targeted and safer pharmacotherapy

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to a compound of the following formula (I) or (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof:The invention furthermore relates to a pharmaceutical composition comprising the compound having formula (I) or (II) and optionally one or more pharmaceutically acceptable excipient(s) and/or carrier(s), as well as to these compounds for use in the treatment, amelioration or prevention of pain, opioid overdose, addictions, neuropsychiatric disorders, Prader-Willi Syndrome, gastrointestinal disorders, skin disorders, dyspnea, headache and/or temporomandibular joint dysfunction, including methods of treating, ameliorating or preventing pain involving administering to a patient in need thereof an effective amount of the compound having formula (I) or (II).