Compositions And Methods Of Bdnf Activation

Patent No. US12036261 (titled "Compositions And Methods Of Bdnf Activation") was filed by Vdf Futureceuticals Inc on Jul 15, 2021.

What is this patent about?

’261 is related to the field of compositions and methods for increasing the level of endogenous Brain-Derived Neurotrophic Factor (BDNF) in the blood of mammals, particularly humans. BDNF is a protein crucial for neuronal survival, differentiation, and synaptic plasticity, playing a key role in learning, memory, and mood regulation. Reduced BDNF levels have been linked to various neurological and psychiatric disorders, creating a need for interventions that can safely and effectively boost BDNF production.

The underlying idea behind ’261 is that extracts from the whole coffee fruit, specifically those with a low caffeine content and enriched with procyanidins , can significantly increase BDNF levels in the blood when administered orally. This effect is more pronounced for BDNF found within exosomes, which are small vesicles that can cross the blood-brain barrier, potentially delivering BDNF directly to the brain. The inventors discovered that this increase in BDNF is not simply due to caffeine or general polyphenol content, but rather a specific property of the whole coffee fruit extract.

The claims of ’261 focus on methods of improving cognition, learning, memory, and alertness in mammals, particularly humans, by administering a composition containing a preparation of coffee fruit. This preparation is an extract from the whole coffee fruit, including the pulp, husk, hull, and/or mucilage, with a caffeine content of less than 2%. The claims specify that the extract should have a total procyanidin concentration of at least 5 μg/g and be administered at a dosage sufficient to acutely increase exosomal BDNF levels in the blood.

In practice, the invention involves orally administering a relatively small dose (5-500mg) of the whole coffee fruit extract. The extract's procyanidins are believed to stimulate the production and release of BDNF, particularly in its exosomal form. The exosomes then act as delivery vehicles, transporting BDNF across the blood-brain barrier and into the brain, where it can exert its neurotrophic effects, leading to improved cognitive function, enhanced learning and memory, and increased alertness.

Prior approaches to increasing BDNF levels, such as exercise or caffeine consumption, have shown only moderate effects. ’261 differentiates itself by utilizing a specific composition – whole coffee fruit extract with low caffeine and high procyanidin content – to achieve a substantial increase in exosomal BDNF. This targeted approach, leveraging the exosome-mediated delivery system , offers a potentially more effective and direct way to enhance BDNF levels in the brain compared to previous methods.

How does this patent fit in bigger picture?

Technical landscape at the time

In the early 2010s when ’261 was filed, compositions for oral administration were typically formulated using well-established methods for achieving desired release profiles and bioavailability, at a time when hardware or software constraints made precise control over exosomal BDNF levels non-trivial, and when systems commonly relied on traditional extraction techniques rather than more advanced purification methods.

Novelty and Inventive Step

The claims were rejected in a non-final office action, and the applicant filed arguments. The claims were again rejected in a final office action. The prosecution record does not describe the technical reasoning or specific claim changes that led to allowance.

Claims

This patent contains 17 claims, with independent claims 1, 8, and 14. The independent claims are directed to methods of improving cognition, learning, memory, and/or alertness in mammals or humans by administering a composition containing a coffee fruit preparation. The dependent claims generally specify details and limitations to the methods described in the independent claims.

Key Claim Terms New

Definitions of key terms used in the patent claims.

Term (Source)Support for SpecificationInterpretation
Caffeine content of less than 2%
(Claim 1, Claim 8, Claim 14)
“The inventors have now surprisingly discovered that various compositions comprising a preparation of whole coffee fruit (e.g., whole coffee fruit extract) or a procyanidin-enriched preparation of a fruit or vegetable are highly effective in stimulating BDNF in a mammal to levels typically exceeding 50, more typically 100, and in some cases even exceeding 150% of levels above baseline ordinarily observed without administration of the composition.”The preparation of coffee fruit contains less than 2% caffeine.
Extract from whole coffee fruit
(Claim 1, Claim 8, Claim 14)
“In preferred compositions, the preparation of the coffee fruit is a whole coffee fruit extract or a whole coffee fruit powder (exemplary compositions are commercially available as N580 and N286, respectively, from VDF FutureCeuticals, Inc. 2692 N. State Route 1 17—Momence, IL 60954, USA).”A substance extracted from the entire coffee fruit, including pulp, husk, hull, and/or mucilage.
Preparation of a coffee fruit
(Claim 1, Claim 8, Claim 14)
“Therefore, in one aspect of the inventive subject matter, the inventor contemplate a method of increasing endogenous BDNF in blood of a mammal in which a composition that increases a BDNF level in the blood is administered to the mammal, wherein the composition comprises a preparation of a coffee fruit or a procyanidin-enriched preparation of a fruit or vegetable, wherein the composition is formulated and administered at a dosage to increase the BDNF level in the blood in an amount of at least 25%.”A substance derived from coffee fruit, including extracts and powders.
Total procyanidin concentration
(Claim 1, Claim 8, Claim 14)
“Therefore, in one aspect of the inventive subject matter, the inventor contemplate a method of increasing endogenous BDNF in blood of a mammal in which a composition that increases a BDNF level in the blood is administered to the mammal, wherein the composition comprises a preparation of a coffee fruit or a procyanidin-enriched preparation of a fruit or vegetable, wherein the composition is formulated and administered at a dosage to increase the BDNF level in the blood in an amount of at least 25%.”The concentration of procyanidins in the preparation.
Whole coffee fruit powder
(Claim 1)
“In preferred compositions, the preparation of the coffee fruit is a whole coffee fruit extract or a whole coffee fruit powder (exemplary compositions are commercially available as N580 and N286, respectively, from VDF FutureCeuticals, Inc. 2692 N. State Route 1 17—Momence, IL 60954, USA).”A powdered substance derived from the entire coffee fruit.

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US12036261

VDF FUTURECEUTICALS INC
Application Number
US17377286
Filing Date
Jul 15, 2021
Status
Granted
Expiry Date
Aug 18, 2034
External Links
Slate, USPTO, Google Patents