Heteroaryl-substituted 2-Pyridinylmethylamine Derivatives

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

This patent discloses a new class of chemical compounds, specifically heteroaryl-substituted 2-pyridinylmethylamine derivatives, that act as selective modulators (mostly agonists) of the serotonin 5-HT1A receptor. These compounds have shown strong and selective activity at this receptor and are intended for use in pharmaceutical compositions for the treatment and/or prevention of various diseases that involve serotonin signaling dysfunction, particularly those affecting the central nervous system.

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

• Treatment of chronic pain (including neuropathic and nociceptive pain, trigeminal neuralgia, postoperative pain, migraine)
• Prevention and treatment of various forms of depression (major depression, depressive phases of bipolar disorder, somatogenic and psychogenic depressions)
• Treatment of anxiety disorders (generalized anxiety, panic disorder, social phobia, post-traumatic stress disorders)
• Management of compulsive and aggressive disorders
• Treatment of psychotic diseases such as schizophrenia, manic phases in bipolar disorder, and drug-induced psychoses
• Treatment of movement disorders (Parkinson’s disease and related conditions)
• Treatment of addiction (e.g., cocaine, alcohol, opiates, nicotine)
• Treatment of sexual dysfunction
• Improvement of amnesic and cognitive disorders (potential cognitive enhancers)
• Support in autism-related disorders
• Therapy of stroke and neurodegenerative diseases (Alzheimer's, ALS, Huntington's disease, etc.)
• Treatment of urinary incontinence

BenefitsContent extracted from patent full text and abstract with AI.

• High selectivity for the 5-HT1A receptor, reducing off-target side effects seen in less selective compounds
• Demonstrated potent agonist (activation) activity at the 5-HT1A receptor, leading to strong therapeutic effects
• Potential for neuroprotection, possibly delaying or preventing neurodegeneration
• Broad therapeutic applicability across multiple CNS disorders and symptoms (pain, mood, cognition, motor function)
• Oral and injectable formulations possible (pharmaceutically flexible)
• Structurally diverse set of compounds allows for fine-tuning of pharmacokinetic profiles, dosing, and side effect profiles
• Potential use in novel or treatment-resistant cases, including patients who do not benefit from or tolerate existing drugs
• Ability to use compounds as stand-alone therapy or part of combination treatments

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present disclosure relates to compounds having the general formula (I) wherein Q represents a five membered heteroaryl group. The compoungs are selective 5-HT1 a modulators and are useful for treating several diseases.