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Publication Number
US-12760058-B2
Publication Date
2026-10-13
Expiration Date
Abstract
The present application relates to novel compounds that are prodrugs of brexanolone, ganaxolone and zuranolone, pharmaceutical compositions comprising one or more compounds disclosed herein and salts thereof, and a pharmaceutically acceptable excipient, and use of the compounds disclosed herein and salts thereof for treating diseases or conditions related to GABAA receptor function, such as major depression disorder (MDD) and postpartum depression (PPD), in mammals and especially in humans.
Core Innovation
The disclosure relates to steroid-derived compounds, including brexanolone C3 derivatives, cyclopenta[a]phenanthrene steroid derivatives, and prodrugs capable of releasing brexanolone, ganaxolone, or zuranolone to modulate GABA_A receptors. These compounds encompass Formula (I) and related subfamilies bearing ester, carbonate, or carbamate substituents, as well as their pharmaceutically acceptable salts. The independent claim covers a compound having a depicted structure or a pharmaceutically acceptable salt thereof, alongside associated pharmaceutical compositions containing pharmaceutically acceptable excipients.
The disclosure reports categorical plasma and liver S9 stability screening results for exemplary compounds, showing plasma half-lives exceeding 200 minutes and liver S9 half-lives below 50 minutes. Synthesis and characterization of steroidal derivatives are described; [procedural detail omitted for safety]. Because background sections are omitted from the supplied content, the specific technical problem being solved is not explicitly described in patent.
Claims Coverage
The claims comprise one independent claim and two dependent claims, defining three inventive features.
Compound having a depicted structure
The independent claim covers a compound having the depicted structure, or a pharmaceutically acceptable salt thereof.
Pharmaceutical composition with an excipient
A dependent claim covers a pharmaceutical composition comprising the claimed compound or salt and at least one pharmaceutically acceptable excipient.
Further specified compound structure
A dependent claim further specifies the compound by a depicted structure, or a pharmaceutically acceptable salt thereof.
The claims cover the depicted compound or its pharmaceutically acceptable salt, a pharmaceutical composition comprising the compound or salt with an excipient, and a further depicted structural form.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment of GABA_A receptor-related conditions and neurological disorders, including major depression and postpartum depression.
A pharmaceutical composition comprising the claimed compound or pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient.
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