GPR139 Antagonist Patent for Depression and Neurological Disorders

ChangeBridge: Patent Grants - Organic Chemistry (C07D)

Published March 31st, 2026

Detected March 31st, 2026

Summary

USPTO granted Takeda Pharmaceutical Company Limited Patent US12590086B2 for GPR139 antagonist compounds (3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives) used in methods of treating depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and ADHD. The patent contains 27 claims and includes tablet formulations.

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What changed

USPTO granted Patent US12590086B2 to Takeda Pharmaceutical Company Limited for GPR139 antagonist compounds. The patent covers 3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds for therapeutic use. The 27 claims encompass methods of treating depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder.

This patent grant establishes Takeda's intellectual property rights over the specified GPR139 antagonist compounds and their medical applications. Competitors developing similar GPR139 antagonists should conduct freedom-to-operate analyses. Potential licensees seeking access to the technology should contact Takeda Pharmaceutical. The filing date was May 20, 2021, with application number 17999514.

What to do next

Conduct freedom-to-operate analysis if developing competing GPR139 antagonist compounds
Review patent claims for potential licensing opportunities if developing treatments for listed conditions
Monitor patent expiry timeline for strategic planning (patents typically expire 20 years from filing)

Source document (simplified)

← USPTO Patent Grants

3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds as GPR139 antagonists for use in a method of treatment of e.g. depression

Grant US12590086B2 Kind: B2 Mar 31, 2026

Assignee

Takeda Pharmaceutical Company Limited

Inventors

Tomoaki Hasui, Satoshi Mikami, Toru Yamashita, Shinji Nakamura, Shinji Morimoto, Toshihiro Imaeda, Kazuaki Takami, Masaki Daini, Hiroyuki Kakei, Minoru Nakamura, Fumie Yamaguchi, Chunxiang Wang, Sachie Takashima, Makoto Kamata, Yuya Oguro, Shuhei Ikeda

Abstract

The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease, schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder. Exemplary compounds are e.g. 3-((1H-pyrazol-4-yl)methyl)-6′-(phenyl)-2H-(1,2′-bipyridin)-2-one derivatives and related compounds. The present description discloses the synthesis and characterisation of exemplary compounds, pharmacological data thereof, as well as exemplary tablet formulations comprising the compounds of the invention (e.g. page 83 to page 110; examples 1 to 33; reference example 1; test examples 1 and 2; tables 1 to 4).

CPC Classifications

C07D 413/14 C07D 401/14 C07D 405/14

Filing Date

2021-05-20

Application No.

17999514

Claims

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Named provisions

GPR139 Antagonists for Depression Treatment GPR139 Antagonists for Alzheimer's Disease GPR139 Antagonists for Schizophrenia GPR139 Antagonists for Drug Addiction GPR139 Antagonists for Sleep Disorders GPR139 Antagonists for Pain GPR139 Antagonists for ADHD Tablet Formulations