Medium chain fatty acid esters of beta-hydroxybutyrate and butanediol and compositions and methods for using same
Inventors
Verdin, Eric • Ulrich, Scott Michael • Newman, John C.
Assignees
J David Gladstone Institutes • University of California San Diego UCSD • Ithaca College
Publication Number
US-11608308-B2
Publication Date
2023-03-21
Expiration Date
2037-06-02
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Abstract
Aspects of the present disclosure include fatty acid β-hydroxyester compounds (e.g., fatty acid esters of β-hydroxybutyrate), fatty acid esters of butanediol, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions having one or more fatty acid β-hydroxyester compounds and/or one or more fatty acid esters of butanediol. Methods for treating a subject by administering one or more esters to the subject are also provided. Kits containing one or more of the subject esters are also described.
Core Innovation
The invention provides fatty acid β-hydroxyester compounds, such as fatty acid esters of β-hydroxybutyrate and butanediol, along with their pharmaceutical compositions and methods of administration. These compounds serve as alternative means to elevate ketone body levels in subjects, offering a practical substitute for ketogenic diets. The invention also encompasses kits containing these esters for therapeutic use.
A key aspect of the innovation is addressing the challenges of ketogenic diets, including poor palatability and side effects. By delivering specific fatty acid esters, the invention aims to efficiently increase ketone levels, thereby supporting the treatment of various neurological and systemic diseases, such as epilepsy and Alzheimer's disease, without the strict dietary restrictions.
Claims Coverage
The patent claims a method for reducing epileptiform activity and treating other diseases by administering specific fatty acid ester compounds, with additional claims detailing particular chemical structures and formulations.
Method of reducing epileptiform activity and treating diseases by administering specific fatty acid esters
Administering a therapeutically effective amount of a compound of formula II or related structures to reduce epileptiform activity in the brain of a subject and treat diseases including Alzheimer's, epilepsy, Parkinson's, heart failure, and others.
Use of specific fatty acid esters of defined alkyl groups
The compounds include specific alkyl substitutions: R4 as unsubstituted C(1-6) alkyl (e.g., methyl) and R5 and R6 as independently unsubstituted C(6-18) alkyl (e.g., hexyl or octyl).
Administration methods and formulations
The compounds can be administered orally in preparations that may include preservatives, flavoring agents, syrups, elixirs, suspensions, binders, and carriers.
Use of compounds in food supplemented with said compounds
Administering compounds as part of food supplements, optionally with additional components of a ketogenic diet.
The claims cover methods of using defined fatty acid ester compounds to reduce epileptiform activity and treat various diseases, including specific chemical structures, routes of administration, and formulations such as food supplements.
Stated Advantages
The compounds increase blood β-hydroxybutyrate levels similar to ketogenic diets or fasting but without the dietary restrictions.
They rapidly and consistently reduce epileptiform spikes in mouse models of Alzheimer's disease, with effects lasting for months.
Long-term use of these compounds improves cognition and survival in affected mice.
The compounds offer a more palatable and tolerable alternative to ketogenic diets for raising ketone levels.
Documented Applications
Treatment of Alzheimer's disease by reducing epileptiform activity and improving cognition.
Treatment of epilepsy via reduction of epileptiform spikes.
Treatment of neurological and systemic diseases, including Parkinson's disease, heart failure, traumatic brain injury, and stroke, by administering the described compounds.
Use in ketogenic diets or as food supplements to raise ketone levels for therapeutic purposes.
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