Abstract
Recent advancements in psychedelic therapeutics, tryptamine derivatives, neuroplastic modulators, and AI-powered machine-learning platforms mark a new frontier in precision medicine. These innovations address critical challenges in neurological and psychiatric disorders, chronic pain management, and computational accessibility. By harnessing the principles of receptor modulation, targeted delivery systems, and simplified AI integration, these breakthroughs promise transformative solutions for patient care and technological development.
Important Compound Classes
Title
Formulations Containing Tryptamine Derivatives and Uses Thereof; Movement Disorders; Machine-Learning Based Artificial Intelligence Capability; and Neuroplastigen Modulators for the Treatment of Pain, Itch and Nerve Injury.
Patent Publication Number
WO 2024/243488 A2 (URL: https://patents.google.com/patent/WO2024243488A2/en?oq=WO+2024%2f243488+A2); WO 2024/238035 A1 (URL: https://patents.google.com/patent/WO2024238035A1/en?oq=WO+2024%2f238035+A1); WO 2024/249611 A1 (URL: https://patents.google.com/patent/WO2024249611A1/en?oq=WO+2024%2f249611+A1); and WO 2024/249820 A2 (URL: https://patents.google.com/patent/WO2024249820A2/en?oq=WO+2024%2f249820+A2)
Publication Date
November 28, 2024; November 21, 2024; December 5, 2024
Priority Application
US 63/504,034; US 18/197,892; US 18/203,568; US 63/470,061
Priority Date
May 24, 2023; May 16, 2023; May 30, 2023; May 31, 2023
Inventors
Salm, J. L.; Witowski, C. G. (WO 2024/243488 A2); Barrow, R.; Karlin, D. R.; Smagin, G. N. (WO 2024/238035 A1); Yalamanchi, U. B.; Akshat, F.; Ramanathan, P.; Jagarlapudi, A.; Zhang, Y.; Banerjee, A.; Ballingam, V.; et al. (WO 2024/249611 A1); and Roberson, D.; Roberson, K.; Perni, R. B. (WO 2024/249820 A2).
Assignee Company
Psilera Inc. [US/US]; 3201 W, Hillsborough Ave., Tampa, Florida 33614, United States (WO 2024/243488 A2); Mind Medicine, Inc. [US/US]; One World Trade Center, Suite 8500, New York, New York 10007, United States (WO 2024/238035 A1); Oracle International Corporation [US/US]; 500 Oracle Parkway, Mail Stop 50P7, Redwood Shoes, California 94065, United States (WO 2024/249611 A1); Cacti, Inc. [US/US]; 2801 Justin Rd, Bldg 200 Suite 210, Flower Mound, TX 75028, United States (WO 2024/249820 A2).
Disease Area
Psychiatric disorder
Biological Target
5-HT2A
Summary
The intersection of neuroscience and technology has brought forth groundbreaking innovations targeting the most challenging aspects of healthcare and computational modeling. Disorders involving maladaptive plasticity, chronic pain, movement impairments, and complex neurological pathways have historically been challenging to treat. Advances detailed in four recent patents exemplify the potential to revolutionize this landscape.
The therapeutic applications of psychedelics, encapsulated in the first patent (WO 2024/238035), emphasize their ability to modulate 5-HT2A receptors, fostering neuroplasticity and enhanced CNS connectivity. These effects are auspicious for addressing movement disorders such as Parkinson’s disease and essential tremors. Similarly, innovations in tryptamine derivative formulations (WO 2024/243488 A2) tackle the delivery challenges associated with these compounds, enabling improved stability and bioavailability for treating mood and neurodegenerative disorders.
Neuroplastic modulators (WO 2024/249820 A1) complement these chemical therapies and provide a new approach to managing chronic pain and neuropathic itch. Their ability to selectively target peripheral pathways while avoiding systemic effects offers a precision treatment model. Finally, the application of artificial intelligence in healthcare, presented in the fourth patent (WO 2024/249611 A1), underscores the importance of accessible, scalable platforms for machine learning. These innovations illustrate a cohesive movement toward a more effective and tailored medical treatment and operational efficiency approach.
Therapeutic Innovations: The use of psychedelics in movement disorders highlights their dual ability to address both the psychological and neurobiological dimensions of these conditions. Acting through serotonin receptor agonism, these compounds promote symptom relief, and the underlying plasticity needed for functional improvement. This innovation extends beyond tremors, including stress-related and neurodegenerative etiologies, supported by versatile administration methods like oral and sublingual routes.
Meanwhile, the tryptamine derivatives extend this progress by resolving critical issues in drug delivery. Through sophisticated formulations, including transdermal patches, intranasal sprays, and extended-release capsules, these derivatives achieve targeted action for conditions such as depression, PTSD, and Alzheimer’s disease. Structural modifications, such as 2-bromo or 2-chloro substitutions, enhance receptor affinity and provide additional therapeutic opportunities.
Neuroplastic modulators fundamentally redefine pain and itch management. Unlike traditional painkillers, these compounds address maladaptive neural plasticity at its source, leveraging serotonin receptor pathways and ion channels like TRPV1 and TRPA1. Their selective targeting ensures minimal off-target effects, providing relief without systemic or cognitive side effects.
The AI-driven machine learning platform complements these biochemical advancements by simplifying the development of custom models for clinical and industrial applications. This no-code system allows nontechnical users to train, deploy, and manage machine-learned solutions within secure cloud environments. This platform bridges the gap between technical innovation and real-world applications, from personalized diagnostics to inventory optimization in healthcare.
Integrating these cutting-edge approaches heralds a new era of precision medicine. The healthcare landscape may overcome long-standing challenges by leveraging advancements in neuroplasticity, receptor modulation, and AI-driven solutions. These innovations promise improved therapeutic outcomes and create a foundation for more accessible and personalized care, driving a paradigm shift in medicine and technology.
Key Structures
Biological Assay
ELISA, behavioral and functional assays, PK, bioavailability
Biological Data
The table below shows in vitro radioligand
binding assays of various serotonergic receptors - Ki (nM)
Recent Review Articles
The author declares no competing financial interest.
Special Issue
Published as part of ACS Medicinal Chemistry Lettersspecial issue “Psychedelics and Entactogens”.
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