US 20090176740A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/017674.0 A1 Phillips, II (43) Pub. Date: Jul. 9, 2009

(54) TREATMENT OF NEUROLOGICAL Publication Classification CONDITIONS BY THE (51) Int. Cl. CO-ADMINISTRATION OF ANIRACETAM A6II 3/66 (2006.01) ANDL-ALPHA GLYCERYLPHOSPHORYLCHOLINE (52) U.S. Cl...... 514/75 (57) ABSTRACT (76) Inventor: Dauglas James Phillips, II, Jupiter, Aniracetam (1-(4-methoxybenzoyl)-2-pyrrolidinone) is co FL (US) administered with the acetylcholine precursor 1-alpha glyc erylphosphorylcholine (Alpha GPC, choline alfoscerate, Correspondence Address: choline alphoscerate) to potentiate cognition enhancing Douglas J. Phillips II effects in healthy Subjects and patients suffering from neuro 1100 Sioux Street logical conditions including Alzheimer's Disease (AD), Jupiter, FL 33458 (US) attention deficit disorder (ADD), Parkinson's Disease, Schizophrenia, Vascular dementia, post stroke aphasia, anxi ety disorders, cerebral atrophy, chronic alcoholism, Down (21) Appl. No.: 12/315,255 syndrome, dyslexia, and various other neurodegenerative conditions. The co-administration of aniracetam (and other (22) Filed: Dec. 1, 2008 racetam derivatives including oxiracetam) with the acetyl choline precursor 1-alpha glycerylphosphorylcholine decreases negative side-effects such as severe headaches Related U.S. Application Data while increasing the synthesis and release of the neurotrans (60) Provisional application No. 60/991.278, filed on Nov. mitters acetylcholine and glutamate to facilitate proper brain 30, 2007. functioning. US 2009/0176740 A1 Jul. 9, 2009

TREATMENT OF NEUROLOGICAL of chemical compounds with wide-ranging neurological ben CONDITIONS BY THE efits and minimal side-effects. CO-ADMINISTRATION OF ANIRACETAM 0006 Aniracetam and 1-alpha glycerylphosphocholine ANDL-ALPHA work synergistically with one another to help counter the GLYCERYLPHOSPHORYLCHOLINE deleterious effects of acetylcholine depletion and neurode geration often associated with age-related neurological con ditions. The combination of aniracetam and 1-alpha glycer 0001. This application claims priority to my earlier filed ylphosphocholine is more efficacious in the treatment of provisional application Ser. No. 60/991,278 filed on Nov.30, neurological disorders when taken together than if either 2007. were administered alone. 0007 Aniracetam and 1-alpha glycerylphosphocholine may be co-administered orally Such as in capsule, tablet, BACKGROUND OF THE INVENTION powdered, or liquid form. A ratio of aniracetam to 1-alpha 0002 Aniracetam falls into a category of neurological glycerylphospocholine appropriate and efficacious for cogni agents called racetams that are analogs of piracetam. Pirac tive enhancement and neurological treatment is 4:3. A cap etam was first discovered and synthesized by a team of Sule containing 400 mg of aniracetam and 300 mg of 1-alpha researchers led by Dr Corneliu E. Giurgea in 1964 and has glycerylphosphorylcholine administered orally is one Such been used extensively throughout the world as a cognitive form and method of co-administration. enhancer and to treat neurological conditions such as Alzhe What is claimed is: imer's Disease and senile dementia Since the original discov 1. The reduction of undesirable side effects such as head ery of piracetam, analogs such as aniracetam and oxiracetam aches associated with administration of aniracetam can be have been synthesized that are significantly more potent than alleviated in human subjects by the co-administration with the original piracetam. Aniracetam is one Such racetam ana 1-alpha glycerylphosphorylcholine. Co-administration of log that is claimed to be four to ten times stronger than aniracetam and 1-alpha glycerylphosphorylcholine restores piracetam. proper acetylcholine and glutamate neurotransmitter levels 0003. Aniracetam is often considered a member of the for proper brain functioning. ampakine class of neurological compounds that interact with 2. The process of treating neurological conditions includ the glutamatergic AMPA receptor of the brain to increase ing Alzheimer's Disease (AD), attention deficit disorder memory functions, facilitate learning activities, and help (ADD), memory impairment, Parkinson's Disease, schizo modulate neurological conditions. Such neurobiological phrenia, Vascular dementia, post stroke aphasia, anxiety dis activity increases the release of the neurotransmitter orders, cerebral atrophy, chronic alcoholism, Down Syn glutamate that assists with neurological functions critical to drome, dyslexia, and other neurodegenerative conditions normal and healthy brain operations. using the combination of aniracetam and 1-alpha glycer 0004 L-alpha glycerylphosporylcholine (Alpha GPC, ylphosphorylcholine. choline alfoscerate, choline alphoscerate, glycerylphosporyl 3. The process of enhancing or improving memory and choline) is an acetylcholine precursor derived from Soy leci brain functions associated with the acetylcholine neurotrans thin used to enhance memory and treat neurological disorders mitter system in healthy human adults by the co-administra associated with neurodegeneration. L-alpha glycerylphos tion of aniracetam with 1-alpha glycerylphosphorylcholine. porylcholine readily crosses the blood brain barrier (BBB) 4. The method of claim 1 wherein the mode of administra and is considered one of the most efficacious of all the ace tion is oral. tylcholine precursors in synthesizing the neurotransmitter 5. The process of claim 2 wherein the mode of administra acetylcholine. L-alpha glycerylphosporylcholine is the most tion is oral. bioavailable form of choline currently known. Further, L-al 6. The process of claim 3 wherein the mode of administra pha glycerylphosporylcholine has also been shown to be tion is oral. involved with the secretion of human growth hormone in the 7. The method of claim 1 wherein the mode of administra hypothalamus region of the brain where memory functions tion is intravenous. take place. Several neurological conditions, including Alzhe 8. The process of claim 2 wherein the mode of administra imer's Disease, have been correlated with decreased levels of tion is intravenous. acetylcholine and hypothalamus degeneration. 9. The process of claim 3 wherein the mode of administra tion is intravenous. SUMMARY OF THE INVENTION 10. The method of claim 1 wherein a racetam analog simi lar to aniracetam Such as oxiracetam, pramiracetam, phe 0005. This invention is based on the discovery that mem nylpiracetam, etiracetam, levetiracetam, nefiracetam, bers of the racetam family (including piracetam, aniracetam, rolziracetam, nebracetam, fasoracetam, coluracetam, bri and oxiracetam) lead to undesirable side effects when taken varacetam, or seletracetam is combined with an acetylcholine without an acetylcholine precursor Such as 1-alpha glycer precursor similar to 1-alpha glycerylphosphorylcholine ylphosphorylcholine (Alpha GPC). Such side effects include including DMAE, cholinebitartrate, choline citrate, cytidine severe headaches and pain associated with acetylcholine diphosphate choline, centrophenoXine, or lecithin. depletion. When aniracetam is co-administered with 1-alpha 11. The process of claim 2 wherein a racetam analog simi glycerylphosphorylcholine, headaches and cerebral pain can lar to aniracetam Such as oxiracetam, pramiracetam, phe be significantly avoided while maintaining neurological effi nylpiracetam, etiracetam, levetiracetam, nefiracetam, cacy. The combination of derivatives of piracetam (including rolziracetam, nebracetam, fasoracetam, coluracetam, bri aniracetam and oxiracetam) with the acetylcholine precursor varacetam, or seletracetam is combined with an acetylcholine 1-alpha glycerylphosphorylcholine represents a novel class precursor similar to 1-alpha glycerylphosphorylcholine US 2009/0176740 A1 Jul. 9, 2009

including DMAE, cholinebitartrate, choline citrate, cytidine varacetam, or seletracetam is combined with an acetylcholine diphosphate choline, centrophenoXine, or lecithin. precursor similar to 1-alpha glycerylphosphorylcholine 12. The process of claim3 wherein a racetam analog simi including DMAE, cholinebitartrate, choline citrate, cytidine lar to aniracetam Such as oxiracetam, pramiracetam, phe diphosphate choline, centrophenoXine, or lecithin. nylpiracetam, etiracetam, levetiracetam, nefiracetam, rolziracetam, nebracetam, fasoracetam, coluracetam, bri c c c c c