EP2442808A2 - Composition for transporting orotic acid across the blood-brain barrier - Google Patents
Composition for transporting orotic acid across the blood-brain barrierInfo
- Publication number
- EP2442808A2 EP2442808A2 EP10763117A EP10763117A EP2442808A2 EP 2442808 A2 EP2442808 A2 EP 2442808A2 EP 10763117 A EP10763117 A EP 10763117A EP 10763117 A EP10763117 A EP 10763117A EP 2442808 A2 EP2442808 A2 EP 2442808A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- disease
- compound
- orotic acid
- composition
- carrier substance
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Definitions
- composition for the transport of orotic acid across the blood-brain barrier Composition for the transport of orotic acid across the blood-brain barrier
- the invention relates to a composition for the transport of orotic acid across the blood-brain barrier.
- Some brain diseases such as Alzheimer's disease, are accompanied by a decrease in the learning and memory of the brain.
- a variety of drugs has been developed, with which the reduction of the memory performance is at least delayed.
- the problem to be overcome in the application of such pharmaceuticals to be effective in the brain is that they must be transported across the blood-brain barrier into the brain.
- a direct application through, for example, injection is indicated only in extreme emergency.
- such pharmaceuticals must be taken regularly, so that an oral or intravenous administration is indicated.
- the blood-brain barrier is the protective barrier of the brain. In its function, it ensures the supply of nutrients to the brain as well as the removal of metabolic products from the brain. Water-soluble nutrients and peptides essentially cross the blood-brain barrier through specific transporters or specific channels in the cell membrane. Most other soluble compounds, if any, pass through this barrier through passive diffusion.
- Orotic acid is a precursor for pyrimidine nucleotides and ribonucleic acids, which are indispensable for brain performance and development.
- a lack of orotate creates a bottleneck in brain metabolism that can negatively affect memory and learning.
- the ability of the brain to create memory is called piasticity of neural systems.
- the dose was 100 mg / kg in an intraperitoneal administration.
- magnesium orotate is above the value of pure orotsa ⁇ re. Magnesium orotate is also used to increase brain function, especially learning and alertness. It is offered commercially in tablet form.
- the object of the invention is to provide a composition with which the learning and Merkfahmaschine the brain can be maintained or increased and which is to be administered orally or intravenously.
- the object is achieved in that a composition for the transport of Orotsaure across the blood-brain barrier comprising a compound of Orotsaure with a Camersubstanz, the compound of Orotsaure and Camersubstanz has a high water solubility, is given.
- the carrier substance is a substance or compound which is able to pass through the blood-brain barrier and which is bound to or conjugated with the orotic acid.
- the carrier substance is able to transport the orotic acid across the blood-brain barrier.
- the orotic acid is released from the carrier, so that the carrier substance and the orotic acid are present in free form.
- the dissolution of the compound can be carried out enzymatically by cleavage of the compound or on the basis of subsequent chemical reactions or equilibrium conditions.
- the carrier substance is a substance selected from the group "minocycline, cefriaxone, disodium-3, 5-H 2 O, cefotaxime, doxycycline, thiamine, thiamine hydrochloride HCl, nicotinamide, pyridoxine, riboflavin, dexpanthenol, cyanocobalamin, biotin, folic acid, ⁇ - Lipoic acid, fluoxetine HCl, venlaflaxin HCl, 5-hydroxytryptophan, L-tryptophan, melatonin, lecithin, choline, dehydro-Epj-adrosterone, glycine,
- Phosphatidylserine or a salt or a derivative of one of the carrier substances selected from the group.
- the compound of orotic acid with a vitamin of the vitamin B group is preferably, the compound of orotic acid with a vitamin of the vitamin B group.
- vitamins of the vitamin B group is that they also have a positive effect on the regeneration and maintenance of nerve tissue, so that in addition to the function as a carrier at the same time a supply of the brain with supplements takes place.
- the Lyme disease is associated with damage to the nerve tracts.
- both antibiotic treatment of the Borrelia-affected region and supplementation of the cerebral tissue with orotic acid can then occur.
- the administration of orotic acid to a carrier of the group of pharmaceuticals acting on the receptors of the central nervous system can include simultaneous treatment of nervous system dysfunction.
- Parkinson's disease is six times more likely to develop dementia than healthy individuals of the same age.
- the frequency of dementia increases with the duration of Parkinson's disease and the age of the patients.
- a large-scale investigation in Germany showed that of the more than 75-year-old Parkinson's patients about two-thirds suffer from dementia.
- Activation of the affected areas of the brain can be achieved by simultaneous acupuncture treatment of the acupuncture points indicated for Parkinson's disease, triggering and challenging regenerative processes in the affected brain areas.
- the chemical structure of the compound of orotic acid with a Camersubstanz may be an ester compound, a conjugate, a complex and / or a salt compound, in particular an orotate salt.
- the orotic acid is chemically equimolar connected to the Camersubstanz.
- composition for the transport of orotic acid across the blood-brain barrier may contain, in addition to the compound of orotic acid with the Camersubstanz other substances and compounds.
- Such substances may be, for example, adjuvants for the galenic preparation of the desired administration form.
- the compound of orotic acid with the cameral substance in the composition may be combined with other active ingredients to a Kombmatonspraparat.
- the composition can be prepared in the form of a single-dose solid dosage form, in particular as a tablet, globules, capsule and / or powder.
- these dosage forms are prepared for oral administration.
- the composition must be prepared as a suppository.
- the composition is prepared as an injectable liquid dosage form.
- the invention also relates to the use of the composition comprising a compound of orotic acid with the Camersubstanz with the said characteristics as food supplement.
- the invention also relates to the use of the composition comprising a compound of orotic acid with the Camersubstanz with the said characteristics as a medicament.
- composition containing a compound of orotic acid with the cameral substance of the compound of orotic acid can be used to produce a nootropic agent for maintaining and / or increasing brain plastidity.
- nootropics are drugs,
- a disease is insbensodere a disease selected from the group "Alzheimer's disease, Parkinson's disease, Lewy body disease, lobar atrophy, Huntington's disease, Korsakoff syndrome".
- composition can be used for the treatment of degenerative diseases of the cerebral tissue.
- degenerative disease is Lyme disease.
- the invention also relates to the use of a composition comprising a compound of orotic acid with the carrier substance for the preparation of a medicament or dietary supplement.
- the medicine or dietary supplement is used to treat brain diseases associated with temporary or permanent dementia, such as Alzheimer's disease, Parkinson's disease, Lewy body disorder, lobar atrophy, Huntington's disease and / or Korsakoff's syndrome. Also can be treated with the drug or dietary supplement degenerative diseases of the cerebral tissue such as Lyme disease.
- FIG. 1 shows:
- reaction of orotic acid and vitamin B ⁇ , 1 shows the simplified esterification reaction of orotic acid 1 and vitamin B ⁇ 2, also called pyridoxine, in which the orotic acid is bound via an ester bond 3 to the vitamin B6.
- the compound has good water solubility.
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
Abstract
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102009025549A DE102009025549A1 (en) | 2009-06-15 | 2009-06-15 | Composition for the transport of orotic acid across the blood-brain barrier |
PCT/DE2010/000676 WO2010145644A2 (en) | 2009-06-15 | 2010-06-14 | Composition for transporting orotic acid across the blood-brain barrier |
Publications (1)
Publication Number | Publication Date |
---|---|
EP2442808A2 true EP2442808A2 (en) | 2012-04-25 |
Family
ID=43069889
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP10763117A Withdrawn EP2442808A2 (en) | 2009-06-15 | 2010-06-14 | Composition for transporting orotic acid across the blood-brain barrier |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP2442808A2 (en) |
DE (1) | DE102009025549A1 (en) |
WO (1) | WO2010145644A2 (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3981407A1 (en) * | 2020-10-07 | 2022-04-13 | WÖRWAG Pharma GmbH & Co.KG | Biofactors for the treatment and prophylaxis of dementia |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2131946A1 (en) * | 1971-06-26 | 1972-12-28 | Storto Martin Dipl Chem Dr | Orotic acid salts with amino alcohols - useful as geriatric medicaments |
DD116036A1 (en) * | 1973-12-27 | 1975-11-05 | ||
DE2443979A1 (en) * | 1974-09-12 | 1976-04-29 | Josef Dipl Chem Dr Rer N Klosa | THIAMINE DISULFIDE OROTATE |
DE3112479A1 (en) * | 1981-03-26 | 1982-11-25 | Josef Dipl.-Chem. Dr.Rer.Nat. 1000 Berlin Klosa | Nicotinamide orotate |
DE19629802A1 (en) * | 1996-07-24 | 1998-01-29 | Woerwag Pharma Gmbh | Medicines used to treat neuropathies |
US7807654B2 (en) * | 1998-08-31 | 2010-10-05 | Wellstat Therapeutics Corporation | Compositions and methods for treatment of mitochondrial diseases |
-
2009
- 2009-06-15 DE DE102009025549A patent/DE102009025549A1/en not_active Withdrawn
-
2010
- 2010-06-14 WO PCT/DE2010/000676 patent/WO2010145644A2/en active Application Filing
- 2010-06-14 EP EP10763117A patent/EP2442808A2/en not_active Withdrawn
Non-Patent Citations (1)
Title |
---|
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 22 July 2005 (2005-07-22), "4-Pyrimidinecarboxylic acid, 1,2,3,6-tetrahydro-2,6-dioxo-, 4,5-bis(hydroxymethyl)-2-methyl-3-pyridinyl ester (CA INDEX NAME)", Database accession no. 856573-85-8 * |
Also Published As
Publication number | Publication date |
---|---|
WO2010145644A2 (en) | 2010-12-23 |
WO2010145644A3 (en) | 2011-03-03 |
DE102009025549A1 (en) | 2010-12-16 |
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Legal Events
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RAP1 | Party data changed (applicant data changed or rights of an application transferred) |
Owner name: CENTRO DE MEDICINA NEURO-REGENERATIVA, S. L. |
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DAX | Request for extension of the european patent (deleted) | ||
17Q | First examination report despatched |
Effective date: 20160223 |
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Owner name: WERTH, ULRICH |
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Owner name: FOREVER NEEDLE S.L. |
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