BioTech IP Review

Patent Title: GPR52 Modulators and Methods of Use
Patent Number: US 12421193 B2
Filing Date: April 21, 2021
Patent Issue Date: September 23, 2025
Assignee: Neurocrine Biosciences, Inc. (San Diego, CA, USA)

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What This Patent Covers

This patent protects novel small‑molecule compounds that modulate the activity of the G‑protein coupled receptor‑52 (GPR52), along with related pharmaceutical compositions and therapeutic methods.

Key elements of the invention include:

• GPR52 Modulators: The compounds of Formula (I) and pharmaceutically acceptable salts thereof are designed to bind to GPR52 — an orphan G‑protein coupled receptor expressed primarily in the central nervous system — and modulate its activity.
• Pharmaceutical Compositions: The patent includes compositions (e.g., formulations, dosage forms) comprising these GPR52 modulators together with acceptable excipients for therapeutic administration.
• Methods of Use: The claims cover methods of treating neurological and psychiatric disorders associated with abnormal GPR52 signaling by administering an effective amount of a modulator to a subject in need. Conditions potentially addressed include schizophrenia, cognitive impairment, Parkinson’s disease, Alzheimer’s disease, mood disorders, movement disorders, dystonia, Tourette’s, Huntington’s chorea, addiction and others.

By modulating a receptor implicated in central nervous system function, these compounds could influence signaling pathways critical for a wide range of neuropsychiatric and neurological disorders.

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Why This Patent Is Important

1) Aligns With High‑Value Therapeutic Areas
Neurocrine is focused on neurological and psychiatric diseases, which represent large, high‑need markets globally (e.g., schizophrenia, movement disorders, cognitive impairments). A class of molecules that modulates a novel CNS target such as GPR52 could support multiple drug candidates across indications.

2) Broad Clinical Applicability
The patent’s claims cover not only individual compounds but also methods of treating a wide spectrum of CNS disorders. If effective, therapies built on these modulators could tap into multi‑billion‑dollar markets spanning neuropsychiatry and movement disorders.

3) Strong Patent Protection Into the Future
Although originally filed in 2021, the patent issued in late 2025, giving Neurocrine exclusive rights to these compositions and uses for many years going forward — providing a competitive moat against generic or alternative therapies targeting the same biological pathways.