IP Library Granted Patent US 12,667,574
Granted Patent B2
US 12,667,574 · App. 17/965,754 · Granted Jun 30, 2026

Paraxanthine-based bioactive composition and method of use thereof

Inventors: Shawn Wells (Frisco, TX); Ralf Jager (Milwaukee, WI); Kylin Liao (Plano, TX); Martin Purpura (Spring, TX)
Assignee: PX ING, LLC
A61K31/522A23L33/10A61K31/685A61K45/06A61P25/28
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Quick Facts
Patent No.
US 12,667,574
App. No.
17/965,754
Granted
Jun 30, 2026
Kind
B2
Abstract

The disclosed compositions and methods relate to compositions for human consumption comprising paraxanthine and a cholinergic agent and/or theanine. The disclosed compositions are useful for promoting cognitive function, energy, athletic performance and providing neuroprotective anti-oxidative effects.

Claims (16)

1 . A method for improving physical performance in a subject, comprising: providing the subject with a composition comprising about 50 mg to about 800 mg of paraxanthine and an effective amount of alpha-GPC (L-alpha glycerylphosphorylcholine).

2 . The method of claim 1 , wherein paraxanthine is present in the composition in an amount from about 50 mg to about 400 mg.

3 . The method of claim 2 , wherein the alpha-GPC is present in the composition in an amount from about 50 mg to about 400 mg.

4 . The method of claim 2 , wherein the composition is substantially free of caffeine.

5 . The method of claim 2 , wherein administration of the composition to a subject produces a synergistic increase in physical performance relative to the administration of a comparable dose of paraxanthine or alpha-GPC.

6 . The method of claim 1 further comprising a paraxanthine congener or paraxanthine analog selected from the group consisting of caffeine, methyl caffeine, theobromine, theophylline, liberine, methylliberine, theacrine and combinations thereof.

7 . The method of claim 6 , wherein the paraxanthine congener or paraxanthine analog is caffeine.

8 . A method of improving cognitive function in a subject comprising administering to the subject a composition comprising about 50 mg to about 800 mg of paraxanthine and an effective amount of alpha-GPC.

9 . The method of claim 8 , wherein administration of the composition increases one or more of attention, information acquisition, information processing, working memory, short-term memory, long-term memory, anterograde memory, retrograde memory, memory retrieval, discrimination learning, decision-making, inhibitory response control, attentional set-shifting, delayed reinforcement learning, reversal learning, the temporal integration of voluntary behavior, speed of processing, reasoning, problem solving and/or social cognition.

10 . The method of claim 9 , wherein administration of the composition enhances dopaminergic tone, cholinergic tone, and/or brain BDNF levels.

11 . The method of claim 8 , wherein administration of the composition is neuroprotective against oxidative stress.

12 . The method of claim 8 further comprising a paraxanthine congener or paraxanthine analog selected from the group consisting of caffeine, methyl caffeine, theobromine, theophylline, liberine, methylliberine, theacrine and combinations thereof.

13 . The method of claim 8 , wherein the alpha-GPC is present in the composition in an amount from about 50 mg to about 400 mg.

14 . The method of claim 8 , wherein the composition is substantially free of caffeine.

15 . The method of claim 8 , wherein administration of the composition to a subject produces a synergistic increase in cognitive function relative to the administration of a comparable dose of paraxanthine or alpha-GPC.

16 . A method for enhancing energy in a subject comprising administering to the subject a composition comprising about 50 mg to about 800 mg of paraxanthine and an effective amount of alpha-GPC.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 20, 2023
From: INGENIOUS INGREDIENTS, LP
To: PX ING, LLC
Reel/Frame 063998/0456 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 18, 2023
From: JAGER, RALF; PURPURA, MARTIN; WELLS, SHAWN; LIAO, KYLIN
To: INGENIOUS INGREDIENTS, LP
Reel/Frame 063687/0950 →
Continuity (3)
Provisional Application 63255327 · Oct 13, 2021
Provisional Application 63255309 · Oct 13, 2021
Related Publication 20230115966A1 · Apr 13, 2023
References Cited (66)
US 20080220129A1 · Cossette et al. · 2008 [cited by applicant]
US 20090110674A1 · Loizou · 2009 [cited by applicant]
US 20090325984A1 · Cosentin et al. · 2009 [cited by applicant]
US 20140080847A1 · Geissler · 2014 [cited by applicant]
US 20160038552A1 · Bredesen et al. · 2016 [cited by applicant]
US 20160143920A1 · Notelovitz · 2016 [cited by applicant]
US 20160339078A1 · Hamill · 2016 [cited by applicant]
US 20180105498A1 · Zemel et al. · 2018 [cited by applicant]
US 20180236016A1 · Gamay · 2018 [cited by applicant]
US 20190038640A1 · Notelovitz · 2019 [cited by examiner]
US 20200077689A1 · Lee · 2020 [cited by examiner]
US 20210068429A1 · Sippy · 2021 [cited by applicant]
US 20210121469A1 · Bhargava · 2021 [cited by applicant]
US 20210169891A1 · Lelah · 2021 [cited by applicant]
US 20220331327A1 · Jager et al. · 2022 [cited by applicant]
US 20220331328A1 · Jager et al. · 2022 [cited by applicant]
US 20230072854A1 · Purpura et al. · 2023 [cited by applicant]
CN 112979651A · 2021 [cited by applicant]
WO 2006024545A1 · 2006 [cited by applicant]
WO 2010076112A2 · 2010 [cited by applicant]
WO 2012072670A2 · 2012 [cited by applicant]
WO 2012073025A1 · 2012 [cited by applicant]
WO 2013173265A1 · 2013 [cited by applicant]
WO 2014078459A1 · 2014 [cited by applicant]
WO WO2014065446A1 · 2014 [cited by applicant]
WO 2014172568A2 · 2014 [cited by applicant]
WO 2015131152A1 · 2015 [cited by applicant]
WO 2020252302A1 · 2020 [cited by applicant]
WO 2021151094A1 · 2021 [cited by applicant]
WO 2022204598A1 · 2022 [cited by applicant]
Damann et al., “Effects of consumption of sucromalt, a slowly digestible carbohydrate, on mental and physical energy questionnaire responses”, 2013, Nutritional Neuroscience, 16, pp. 83-95 (Year: 2013). [cited by examiner]
Decker, “Esports enthusiasts target dietary supplements to up their game”, 2020, Nutritional Outlook, 23, pp. 66-70 (Year: 2020). [cited by examiner]
Guerreiro et al., “Paraxanthine, the Primary Metabolite of Caffeine, Provides Protection against Dopaminergic Cell Death via Stimulation of Ryanodine Receptor Channels”, 2008, Molecular Pharmacology, 74, Abstract Only (… [cited by examiner]
Hoffman et al., “The effects of acute and prolonged CRAM supplementation on reaction time and subjective measures of focus and alertness in healthy college students”, 2010, Journal of the International Society of Sports… [cited by examiner]
Guerreiro et al., “Paraxanthine, the Primary Metabolite of Caffeine, Provides Protection against Dopaminergic Cell Death via Stimulation of Ryanodine Receptor Channels”, 2008, Molecular Pharmacology, 74, pp. 980-989 (Ye… [cited by examiner]
Orrú et al., “Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humans”, 2013, Neuropharmacology, 67, pp. 476-484 (Year: 2013). [cited by examiner]
Bryan, “Psychological effects of dietary components of tea: caffeine and L-theanine”, 2008, Nutrition Reviews, 66, pp. 82-90 (Year: 2008). [cited by examiner]
Bryan, Janet , “Psychological effects of dietary components of tea: caffeine and L-theanine”, Nutrition Reviews, vol. 66, 2008, 82-90. [cited by applicant]
Cornelis, Marilyn C., et al., “Genome-wide association study caffeine metabolites provides new insights to caffeine metabolism and dietary caffeine-consumption behavior”, Human Molecular Genetics, vol. 25, No. 4, Oct. 3… [cited by applicant]
Dammann, Kristen W., et al., “Effects of consumption of sucromalt, a slowly digestable carbohydrate, on mental and physical energy questionnaire responses”, Nutritional Neuroscience, vol. 16, No. 2, 2013, 83-95. [cited by applicant]
Decker, Kimberly , “Leveling Up: Esports enthusiasts target deitary supplements to up their game”, Nutritional Outlook, Apr. 1, 2020, 66-70. [cited by applicant]
Dulloo, A.G. , et al., “Paraxanthine (metabolic of caffeine) mimics caffeine's interaction with sympathetic control of thermogenesis”, The American Journal of Physiology, vol. 267, No. 5, 11/1/1194, E801-E804. [cited by applicant]
Ferre, Sergi , et al., “Paraxanthine: Connecting Caffeine to Nitric Oxide Neurotransmission”, Journal of Caffeine Research, vol. 3, Nov. 2, 2013. [cited by applicant]
Grgic, Jozo , et al., “CYP1A2 genotype and acute effects of caffeine on resistance of exercise, jumping, and sprinting performance”, Journal of the International Society of Sports Nutrition, vol. 17, No. 21, Apr. 15, 20… [cited by applicant]
Guerreiro , et al., “Paraxanthine, the Primary Metabolite of Caffeine, Provides Protection Against Dopaminergic Cell Death via Stiulation of Ryanodine Receptor Channels”, Molecular Pharmacology, vol. 74, 2008, 980-989. [cited by applicant]
Hoffman , et al., “The effects of acute and prolonged CRAM supplementation on reaction time and subjective measures of focus and alertness in healthy college students”, Journal of the International Society of Sports Nut… [cited by applicant]
Karami, Zohreh , et al., “Bioactive food derviced peptides: a review on correlation between structure of bioactive peptides and their functional properties”, Journal of Food Science Technology, vol. 56 No. 2, Mar. 20, 2… [cited by applicant]
Konopelniuk, Victoria , et al., “The correction of the metabolic parameters of msg-induced obestity in rats by 2-[4-(benzyloxy) phenoxy] acetic acid”, Journal of Nutrition & Intermediary Metabolism, vol. 13, Sep. 1, 201… [cited by applicant]
Lao-Peregrin, Cristina , et al., “Caffeine-mediated BDNF release regulates long-term synaptic plasticity through activation of IRS2 signaling”, Addiction Biology, vol. 22, No. 6, Jul. 25, 2016, 1706-1718. [cited by applicant]
Monterio, Joao , et al., “Pharmacological potential of methylxanthines: Retrospective analysis and future expectations”, Critical Reviews in Food and Science Nutrition, vol. 59, No. 16, May 15, 2018, 2597-2625. [cited by applicant]
Orru, Marco , et al., “Psychostimulant pharmacological profile of paraxanthine, the main metabolite of caffeine in humans”, Neuropharmacology, vol. 67, 2013, 476-484. [cited by applicant]
Rothwell, Joseph A., et al., “Biomarkers of intake for coffee, tea, and sweetened beverages”, Genes and Nutrition, vol. 13, No. 15, Jul. 4, 2018, 1-18. [cited by applicant]
Ryu, Sungpil , et al., “Caffeine as a Lipolytic Food Component Increase Endurance Performance in Rats and Athletes”, Journal of Nutritional Science Vitaminol, vol. 47, 2001, 139-146. [cited by applicant]
Soares, Rogerio Nogueira, et al., “The influence of CYP1A2 genotype in the blood pressure response to caffeine ingestion is affected by physical status and caffeine consumption level”, Vascular Pharmacology, vol. 106, M… [cited by applicant]
Song, Jae-Kyung , et al., “Effect of Paraxanthine on Body Fat Reduction and Insulin Sensitivity in Monosodiun Glutamate-Obsse Rats”, Journal of Yeungnam Medical Science, vol. 24, No. 2, Dec. 1, 2007, 481-492. [cited by applicant]
Tartar et al. , “A Prospective Study Evaluation the Effects of a Nutritional Supplement Intervention on Cognition, Mood States, and Mental Performance in Video Gamers”, Oct. 1, 2019. [cited by applicant]
Thida, Khine , “Does Caffeine Consumption before High-Intensity Intermittent Exercise Enhance Immunity?”, Aukland University of Technology, 2016, 8-14, 48-54. [cited by applicant]
Vitale, Kenneth , et al., “Nutrition and Supplement Update for the Endurance Athlete: Review and Recommendations”, Nutrients, Jun. 11, 2019. [cited by applicant]
Yoo et al. , “Acute Paraxanthine Ingestion Improves Cognition and Short-Term Memory and Helps Sustain Attention in a Double-Blind, Placebo-Controlled, Crossover Trial”, Nov. 9, 2021. [cited by applicant]
“Are you a slow or fast metabolizer?”, Green Plantation, 2023. [cited by applicant]
Carswell, Alexander T., et al., “The effect of caffeine on cognitive performance is influenced by CYP1A2 but not ADORA2A genotype, yet neither genotype affects exercise performance in healthy adults”, European Journal o… [cited by applicant]
Mandal, Ananya , “Caffeine Pharmacology”, News Medical, Jun. 19, 2023. [cited by applicant]
Muller, Christa , et al., “Xanthines as Adenosine Receptor Antagonists”, Handb Exp Pharmacol, NIH, 2011, 1-59. [cited by applicant]
Nair, Anroop B., et al., “A simple practice guide for dose conversion between animals and humans”, Journal of Basic and Clinical Pharmacy, 2016. [cited by applicant]
Schuster, Julius , et al., “More than just caffeine: psychopharmacology of methylxanthine interactions with plant-derived phytochemicals”, Progress in Neuropsychopharmacology & Biological Psychiatry, vol. 89, 2019, 263-… [cited by applicant]
St. Pierre, Brian , “All about coffee: Is it good for us?”, Precise Nutrition, 2012. [cited by applicant]