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
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
• • 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
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
• • 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
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
  • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

Definitions

• the present invention relates to the use of a powder preparation containing hydroxypyridones for the treatment of lower leg ulcers (UIcus cruris) and pressure ulcers (decubital ulcers).
• UIcus cruris lower leg ulcers
• pressure ulcers decubital ulcers
• UIcus cruris therapy consists of a double strategy of local wound treatment and the elimination of the causes of ulceration. This can include compression therapy for an ulcer caused by chronic venous hypertension, as well as the rehabilitation of the arterial flow path in an arterial ulcer.
• composition of local therapeutic agents should therefore be as simple as possible and the number of substances used should be kept as low as possible.
• the phase-adapted wound healing corresponds to the conventional, traditional therapy, has to be changed constantly and is complex, but inexpensive.
• the cross-phase therapy which uses modern wound dressings, which can be used in the same way during all 3 phases, is much easier to use, but also much more expensive. Both therapeutic methods are comparable in their therapeutic effect.
• phase-adapted wound treatment intervenes in the 3 wound healing phases as follows:
• the aim of cleaning is to create a clean wound bed.
• ointment residues and crusts must first be removed and any necrosis that may be present 3 be removed. The latter is best done with a sharp spoon and with tweezers and scissors.
• enzymatic ointments that preferentially break down denatured protein. They contain substances such as trypsin, chymotrypsin, collagenase, fibrolysin, streptokinase etc.
• the ulcer environment should always be protected by applying hard zinc paste.
• regular disinfection takes place, for example with potassium permanganate or Rivanol * baths.
• epithelization In the epithelization phase, the sensitive newly formed tissue is to be protected and the epithelization is to be promoted. Epithelization begins when the granulation tissue has reached the upper skin level.
• epithelization-promoting wound dressings e.g. Hydrogels, hydrocolloids, foam compresses and gauze grids.
• Split skin transplants can also be performed.
• Dry wound dressings and gels xerodressing and xerogel
• hydrocolloidal wound dressings hydrocolloid dressings
• Prolonged pressure on the skin with a disturbance in the microcirculation is the most important factor that leads to pressure ulcers (National Pressure Ulcer Advisory Panel (1989)).
• Shear forces, which act on the skin and the underlying tissue, as well as friction and moisture also play an important role.
• the local treatment of decubital ulcers is basically carried out in the same way as that of lower leg ulcers.
• the invention therefore relates to the use of powder and at least one compound of the formula I. (I),
• R 1 , R 2 and R 3 which are identical or different, denote hydrogen atom or alkyl having 1-4 carbon atoms, and R 4 represents a saturated hydrocarbon radical having 6 to 9 carbon atoms or a radical of the formula II,
• X means S or O
• Y represents hydrogen atom or up to 2 halogen atoms such as chlorine and / or bromine
• Z is a single bond or the divalent radicals O, S, -CR 2 -, in which
• R represents hydrogen atom or dC -alkyl, or other divalent radicals with 2-10 chain-linked C and optionally O and / or S atoms, where - if the radicals contain 2 or more O and / or S atoms - the latter must be separated from one another by at least 2 C atoms and where 2 adjacent C atoms can also be linked to one another by a double bond and the free valences of the C atoms are saturated by H and / or d- C 4 alkyl groups,
• Ar is an aromatic ring system with up to two rings, which can be substituted by up to three radicals from the group fluorine, chlorine, bromine, methoxy, C 1 -C 4 -alkyl, trifluoromethyl and trifluoromethoxy, 6 for the manufacture of a medicament for the treatment of lower leg ulcers and / or decubital ulcers.
• saturated hydrocarbon radical means that the radical can be straight-chain, branched or cyclic and does not contain any aliphatic multiple bonds.
• examples of the radical R 4 are hexyl, heptyl, octyl, cyclohexyl or cycloheptyl.
• R 4 is preferably a (C 6 -C 8 ) alkyl or cyclohexyl, which can also be bonded to the pyridone ring via a methylene or ethylene group or contain an endomethyl group.
• R 4 can also represent an aromatic radical, which, however, is preferably bonded to the pyridone radical via at least one aliphatic carbon atom.
• the C chain links are preferably CH 2 groups. If the CH 2 groups are substituted by (-CC 4 ) alkyl groups, CH 3 and C 2 H 5 are preferred substituents.
• the remainder "S” means sulfur atom, the remainder “O” means oxygen atom.
• the term “Ar” means phenyl and condensed systems such as naphthyl, tetrahydronaphthyl and indenyl, as well as isolated systems such as those derived from biphenyl, diphenylalkanes, diphenyl ethers and diphenyl thioethers.
• alkyl having 1 to 4 carbon atoms stands for radicals such as methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl or tertiary-butyl.
• Cyclohexyl radical can also each carry a methyl radical
• the active compounds of the compound of the formula I to be used in the preparations can be prepared, for example, by processes according to US 2,540,218 or US 4,797,409. 8th
• Powder preparations are particularly suitable for the use of the compounds mentioned according to the invention.
• the active ingredient is incorporated into the preparations according to the invention in amounts which are usually between about 0.05 and about 5%, preferably between 0.1 and 1%.
• Native substances such as sucrose, lactose, gelatin, pectin, carrageenan, agar, tragacanth and alginates, semi-synthetic powder bases such as cellulose ethers, starch, dextran and pectin derivatives as well as fully synthetic substances such as polyvinylpyrrolidones can be used as the powder base.
• Modified starch types are particularly suitable. They are used in amounts of 95.0 to 99.4 parts by weight per 100 parts by weight of the end product.
• highly disperse silicon dioxide is suitable for improving the flowability and scatterability.
• the preparations are prepared in a manner known per se by mixing the individual components and, if necessary, further processing adapted to the particular preparation.
• a preparation according to the invention has the following composition:
• a preparation according to the invention has the following composition:
• a preparation according to the invention has the following composition:

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Medicinal Chemistry (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Dermatology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Biochemistry (AREA)
• Inorganic Chemistry (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Molecular Biology (AREA)
• Hematology (AREA)
• Communicable Diseases (AREA)
• Diabetes (AREA)
• Oncology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Pyridine Compounds (AREA)
• Medicinal Preparation (AREA)
• Medicines Containing Plant Substances (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Priority Applications (18)

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Publications (1)

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Cited By (3)

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Citations (3)

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• 1998
  • 1998-01-24 DE DE19802708A patent/DE19802708A1/de not_active Withdrawn
• 1999
  • 1999-01-11 TR TR2000/02118T patent/TR200002118T2/xx unknown
  • 1999-01-11 BR BR9907734-5A patent/BR9907734A/pt not_active Application Discontinuation
  • 1999-01-11 HR HR20000496A patent/HRP20000496A2/hr not_active Application Discontinuation
  • 1999-01-11 EP EP99902528A patent/EP1049468B1/de not_active Expired - Lifetime
  • 1999-01-11 PT PT99902528T patent/PT1049468E/pt unknown
  • 1999-01-11 ES ES99902528T patent/ES2285829T3/es not_active Expired - Lifetime
  • 1999-01-11 AT AT99902528T patent/ATE360418T1/de active
  • 1999-01-11 RS YUP-437/00A patent/RS50903B/sr unknown
  • 1999-01-11 SI SI9930962T patent/SI1049468T1/sl unknown
  • 1999-01-11 KR KR1020007008050A patent/KR100597332B1/ko not_active Expired - Lifetime
  • 1999-01-11 US US09/600,903 patent/US6534528B1/en not_active Expired - Lifetime
  • 1999-01-11 ME MEP-559/08A patent/MEP55908A/xx unknown
  • 1999-01-11 RU RU2000122313/14A patent/RU2212239C2/ru active
  • 1999-01-11 SK SK1089-2000A patent/SK285350B6/sk not_active IP Right Cessation
  • 1999-01-11 HU HU0200851A patent/HU228824B1/hu unknown
  • 1999-01-11 DE DE59914312T patent/DE59914312D1/de not_active Expired - Lifetime
  • 1999-01-11 CA CA002319359A patent/CA2319359C/en not_active Expired - Lifetime
  • 1999-01-11 NZ NZ505898A patent/NZ505898A/en not_active IP Right Cessation
  • 1999-01-11 IL IL13745399A patent/IL137453A/xx not_active IP Right Cessation
  • 1999-01-11 DK DK99902528T patent/DK1049468T3/da active
  • 1999-01-11 AU AU22787/99A patent/AU752406B2/en not_active Expired
  • 1999-01-11 JP JP2000528282A patent/JP5127091B2/ja not_active Expired - Lifetime
  • 1999-01-11 CN CN99802327A patent/CN1128619C/zh not_active Expired - Lifetime
  • 1999-01-11 PL PL342055A patent/PL192550B1/pl unknown
  • 1999-01-11 WO PCT/EP1999/000105 patent/WO1999037300A1/de not_active Ceased
  • 1999-01-21 AR ARP990100243A patent/AR016445A1/es unknown
• 2007
  • 2007-06-28 CY CY20071100855T patent/CY1106684T1/el unknown

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