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
  • A61K31/66—Phosphorus compounds
• • 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
  • A61K31/66—Phosphorus compounds
  • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
• • 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
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
  • A61K31/7032—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyldiacylglycerides, lactobionic acid, gangliosides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/02—Nutrients, e.g. vitamins, minerals

Definitions

• the invention relates to the use of compatible Soulten, in particular ectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-
• cDPG Diphosphoglycerate
• DGP 1, 1-diglycerol phosphate
• Firoin ß-mannosylglyceramide
• Firoin-A ß-mannosylglyceramide
• proline betaine proline betaine and / or their derivatives and combinations for the preparation of an agent for prevention
• the invention further relates to compositions containing the aforementioned compatible solutes producing or accumulating microorganisms.
• the living world includes a wide variety of habitats. This includes biotopes that are at first glance hostile and yet animated. These include, for example, salt lakes, hot springs, cold deserts, geysers or other extreme locations. What all these habitats have in common is that they provide living conditions that biological macromolecules and structures can not withstand unprotected.
• microorganisms in these habitats in particular have developed a series of protective measures that enable them to survive. These microorganisms are called extremophilic microorganisms.
• compatible solutes This class of substances is very heterogeneous, it can be found in addition to carbohydrate derivatives and cyclic amino acids, organic phosphorus compounds and similar substances typical compatible solutes of extremophilic microorganisms include ectoine (2-methyl-4-carboxy-3,4,5,6-tetrathydropyrimidine), hydroxyectoine (2-methyl-4-carboxy-5-hydroxy-3,4,5,6-tetratrahydropyrimidine ), Firoin (mannosylglycerate), firoin-A (mannosylglyceramide), DGP (di-glycerol phosphate), cDPG (cyclic diphosphoglycerate), proline, proline betaine and DIP (di-myo-inositol phosphate).
• Compatible solutes are low molecular weight, hydrophilic compounds that are very polar and therefore very soluble in water.
• Compatible solutes of extremophilic microorganisms made by the Applicant include:
• DGP diglycerophosphate
• compatible solute derives from the high compatibility with the intracellular metabolism of microorganisms and the associated very high compatibility. The compatibility is also given at very high concentrations in the molar range. The function of compatible solutes lies in the protection of biological structures from destructive influences.
• compatible solutes are used as skin protection agents (eg EP 1 315 473 A or DE 100 44 985 A).
• compatible solutes stabilize the protein structure, protect proteins from degradation reactions and stabilize solutions of proteins (for example in EP 0 671 161 A, US 2003157040 A or also EP 1 127 141 A, see also Göller & Galinski, J. Molec Catalysis B: 1999 , 7, 37-45).
• a variety of synthetic and semi-synthetic components, as well as microbiological fermentation products and microbial products are used as a means of oral supplementation. Some examples are:
• Ectoine may result in significantly better absorption of ectoine as well as direct protection of the digestive tract cells.
• the invention relates to the use of compatible solutes in profilaxe and therapy as well as nutritional supplementation.
• an object of the invention is the use mentioned of compatible solutes for the prevention and treatment of diseases of the gastrointestinal tract and amyloid diseases.
• Another object of the invention are agents which contain the above-mentioned compatible solutes together with vitamins, minerals and / or conventional adjuvants.
• Another subject is foods having a corresponding content of compatible solute.
• the subject of the invention is an agent containing compatible solutes producing or accumulating microorganisms.
• compatible solutes are understood in particular to be the species mentioned at the outset. Preference is given to using compatible solute ectoine and hydroxyectoine according to the invention.
• Amyloid fibrils consist of anti-parallel folded beta-sheet structures and are hallmarks of major diseases such as Alzheimer's disease, Type II diabetes, Parkinson's disease, AA amyloidosis, AL amyloidosis and ATTR amyloidosis, iatrogenic insulin amyloidosis and many more protein deposition diseases.
• an oral dosage form to be administered in which compatible solutes, in particular ectoine and hydroxyectoine, or preparations of microorganisms which contain compatible solutes, in particular:
• the dosage form may, without limiting the invention thereby, due to the physicochemical properties of the compatible solutes, e.g. a powdered mixture, a tablet, a paste or a concentrated solution, either in the form of extracts of microorganisms, living or killed microorganisms, mixtures or as a pure substance.
• the compatible solutes e.g. a powdered mixture, a tablet, a paste or a concentrated solution, either in the form of extracts of microorganisms, living or killed microorganisms, mixtures or as a pure substance.
• compatible solutes or preparations of microorganisms containing compatible solutes may be included with extracts of herbs and fruits such as Icelandic moss, devil's claw, cinnamon, yarrow, star anise, sage, rosemary, Allspice, peppermint, oregano, carnation, dandelion, lovage, lavender, raspberry, ginger, chamomile, cardamom, coriander, cumin, turmeric, basil, savory can be combined.
• compatible solute-containing agents for oral use may be combined with natural oils such as evening primrose oil, salmon oil and other fish oils.
• Other substances that can be combined with the compatible solutes or preparations that contain compatible solutes are minerals (zinc, sodium, potassium, calcium, magnesium, selenium, chromium, iron, cobalt, copper, manganese, silicon, zinc), vitamins (Vitamin A, vitamin D, vitamin E, vitamin K, vitamin I B1, vitamin B2, niacin, vitamin B6, pantothenic acid, biotin, folic acid, vitamin B12, vitamin C), L-carnitine and isoflavones.
• the compatible solutes can also be combined with solid foods. This is especially true, e.g. when the solutes are mixed as a highly concentrated aqueous solution and then dried. Because of the i5 thermal stability it is also possible to use it in pastry.
• the concentration of compatible solutes is in the range of 0.01-50%.
• the daily dose is usually 1 to 2000 mg / kg body weight and may vary widely depending on the application.
• compositions containing compatible solutes may include tablets, dragees, capsules, powders, granules, lozenges, aqueous solutions, liquid ampoules and
• the remedies can also contain microorganisms, as well as extracts and
• the remedies may also contain extracts from food, as well
• the amount of compatible solute is at least 100 mg of active substance per dosage unit (administration unit), advantageously 200 to 500 mg.
• Mannosylglycerate mannosylglyceramide, di-glycerol phosphate, cyclic
• diphosphoglycerta, proline, proline betaine and di-myo-inositol phosphate can be obtained from microorganisms and other biological sources be won.
• the microorganisms may be members of the genus Brevibacterium, Vibrio, Bacillus, Halomonas, Planococcus, Sporosarcina and Marinococcus. Particularly preferred is the use of microorganisms which synthesize ectoine and hydroxyectoine and are found in foods such as Brevibacterium linens, Brevibacterium casei, Vibrio costicola, Halomonas elongata.
• the substances can be obtained by treating the cells with a washing solution, which consists of water, volatiles and / or substances stabilizing cells.
• the agent for oral use can either be prepared from washed, dried cells or isolated from the cells by osmotic shock.
• the compatible solutes can be generated by chemical synthesis.
• the compatible solutes and preparations of extremophilic microorganisms containing compatible solutes may be used as dietary supplements, in dietetic foods or supplemented balanced diets and in the prevention and treatment of diseases, especially diseases of the gastrointestinal tract, e.g. Crohn's disease, find.
• the invention is based on the fact that the compatible solutes, as defined above, are suitable as active substances numerous

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
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• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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• Neurology (AREA)
• Biomedical Technology (AREA)
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• Nutrition Science (AREA)
• Rheumatology (AREA)
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• Pain & Pain Management (AREA)
• Diabetes (AREA)
• Hematology (AREA)
• Obesity (AREA)
• Psychiatry (AREA)
• Hospice & Palliative Care (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)

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Citations (15)

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• 2006
  • 2006-03-13 WO PCT/EP2006/002286 patent/WO2006097263A2/de not_active Ceased
  • 2006-03-13 EP EP06723388A patent/EP1858519B1/de active Active
  • 2006-03-13 JP JP2008501213A patent/JP2008537734A/ja active Pending
  • 2006-03-13 US US11/885,687 patent/US9089568B2/en active Active

Patent Citations (15)

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