Fused polycyclic substituted 5-carboxylic acid thienopyrimidinedione compounds and uses thereof
Novel GnRH receptor antagonists with a fused polycyclic structure address the limitations of current endometriosis treatments by providing effective inhibition of endometriotic lesions and favorable pharmacokinetic properties for oral use.
Patent Information
- Application Number
- JP2023574747
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2022-02-10
- Filing Date
- 2022-02-21
- Publication Date
- 2026-01-26
- Estimated Expiration
- 2042-02-21
AI Technical Summary
Current clinical treatments for endometriosis, such as nonsteroidal anti-inflammatory drugs, oral contraceptives, aromatase inhibitors, and gonadotropin-releasing hormone agonists, suffer from drawbacks like side effects, inconvenient administration, and limited efficacy, necessitating the development of more effective small molecule GnRH receptor antagonists.
Development of novel GnRH receptor antagonists with a fused polycyclic structure, which have significant inhibitory activity against the GnRH receptor, offering potential oral administration with high plasma exposure, low clearance, and long half-life.
The compounds exhibit excellent inhibitory effects on human gonadotropin-releasing hormone receptors, significantly reducing endometriotic lesion volume in mice, with favorable pharmacokinetic properties suitable for oral administration.