AP460A - Naphthyl derivative for treatment method. - Google Patents
Naphthyl derivative for treatment method. Download PDFInfo
- Publication number
- AP460A AP460A APAP/P/1994/000656A AP9400656A AP460A AP 460 A AP460 A AP 460A AP 9400656 A AP9400656 A AP 9400656A AP 460 A AP460 A AP 460A
- Authority
- AP
- ARIPO
- Prior art keywords
- nabumetone
- medicament
- 6mna
- dementia
- use according
- Prior art date
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
- A61K31/12—Ketones
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The use of nabumetone or 6MNA in the manufacture of a medicament for the treatment and/or prevention of dementia.
Description
NAPHTHYL DERIVATIVE FOR TREATMENT METHOD
The present invention relates to a method for the treatment of cognitive disorders such as alzheimers disease and to a compound for use in such method.
U.S. Patent 4420639 describes 4-(6'-methoxy-2'-naphthyl)butan-2-one (nabumetone) and its use in the treatment of rheumatic and arthritic conditions. It is known that the active metabolite of nabumetone is 6-methoxynaphthyl acetic acid or 6MNA. It should be appreciated that the term 6MNA also includes pharmaceutically acceptable salts thereof.
US Patent 5,192,753 (McGeer) describes the use of NS AID'S to treat dementia, however, there is no mention of nabumetone in this patent.
It has now been discovered that nabumetone has potential therapeutic utility for treating and/or prevention of dementia such as alzheimers disease.
Accordingly, the present invention provides a method for treating and/or preventing dementia such as alzheimers disease in human or non-human animals, which comprises administering an effective, non-toxic amount of nabumetone or 6MNA, to human or non-human animals in need thereof.
The present invention also provides the use of nabumetone or 6MNA in the manufacture of a medicament for use in the treatment and/or prevention of dementia such as alzheimers disease.
A nabumetone or 6MNA medicament, for use in the treatment and/or prevention of dementia such as alzheimers disease may be prepared by admixture of nabumetone or 6MNA with an appropriate carrier, which may contain a diluent, binder, filler, disintegrant, flavouring agent, colouring agent, lubricant or preservative in conventional manner.
Preferably, the medicament is in unit dosage form and in a form adapted for use in the medical or veterinarial fields. For example, such preparations may be in a pack form accompanied by written or printed instructions for use as an agent in the treatment and/or prevention of dementia such as alzheimers disease.
The suitable dosage range for nabumetone or 6MNA depends on the severity of the dementia such as alzheimers disease and on the condition of the patient. It will also depend, inter alia, upon the relation of potency to absorbability and the frequency and route of administration.
Nabumetone or 6MNA may be formulated for administration by any route, and examples are oral, rectal, topical, parenteral, intravenous or intramuscular administration. Preparations may, if desired, be designed to give slow release of nabumetone.
The medicaments may, for example, be in the form of tablets, dispersible - 1 BAD ORIGINAL Λ
P30704 tablets, capsules, sachets, vials, powders, granules, lozenges, reconstitutable powders, or liquid preparations, for example solutions or suspensions, or suppositories.
The medicaments, for example those suitable for oral administration, may 5 contain conventional excipients such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone; fillers, for example lactose, sugar, maize-starch, calcium phosphate, sorbitol or glycerine; tabletting lubricants, for example magnesium stearate; disintegrants, for example starch, polyvinylpyrrolidone, sodium starch glycollate or microcrystalline cellulose; or pharmaceutically acceptable setting agents such as sodium lauryl sulphate.
Solid medicaments may be obtained by conventional methods of blending, filling, tabletting or the like. Repeated blending operations may be used to distribute nabumetone throughout those medicaments employing large quantities of fillers. When the medicament is in the form of a tablet, powder, or lozenge, any carrier suitable for formulating solid pharmaceutical compositions may be used, examples being magnesium stearate, starch, glucose, lactose, sucrose, rice flour and chalk. Tablets may be coated according to methods well known in normal pharmaceutical practice, in particular with an enteric coating. The medicament may also be in the form of an ingestible capsule, for example of gelatin containing nabumetone if desired with a carrier or other excipients.
Medicaments for oral administration as liquids may be in the form of, for example, emulsions, syrups, or elixirs, or may be presented as a dry product for reconstitution with water or other suitable vehicle before use. Such liquid medicaments may contain conventional additives such as suspending agents, for example sorbitol, syrup, methyl cellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminium stearate gel, hydrogenated edible fats; emulsifying agents, for example lecithin, sorbitan monooleate, or acacia; aqueous or non-aqueous vehicles, which include edible oils, for example almond oil, fractionated coconut oil, oily esters, for example esters of glycerine, or propylene glycol, or ethyl alcohol, glycerine, water or normal saline; preservatives, for example methyl or propyl p-hydroxybenzoate or sorbic acid; and if desired conventional flavouring or colouring agents.
Nabumetone or 6MNA may also be administered by a non-oral route. In accordance with routine pharmaceutical procedure, the medicaments may be formulated, for example for rectal administration as a suppository. They may also be formulated for presentation in an injectable form in an aqueous or non-aqueous solution, suspension or emulsion in a pharmaceutically acceptable liquid, e.g. sterile pyrogen-free water or a parenterally acceptable oil or a mixture of liquids.
AP/P/9 4 / 0 0 6 56
BAD ORIGINAL
P30704
The liquid may contain bacteriostatic agents, anti-oxidants or other preservatives, buffers or solutes to render the solution isotonic with the blood, thickening agents, suspending agents or other pharmaceutically acceptable additives. Such forms will be presented in unit dose form such as ampoules or disposable injection devices or in multi- dose forms such as a bottle from which the appropriate dose may be withdrawn or a solid form or concentrate which can be used to prepare an injectable formulation.
As mentioned hereinbefore, the effective dose of nabumetone or 6MNA depends on the severity of the alzheimers disease the condition of the patient and on the frequency and route of administration. A unit dose will generally contain from 20 to 2000 mg and preferably will contain from 30 to 1000 mg, in particular 50,
100, 150, 200, 250, 300, 350, 400,450,500,750, 800 or 1000 mg. The composition may be administered once or more times a day for example 2, 3 or 4 times daily, and the total daily dose for a 70 kg adult will normally be in the range
100 to 3000 mg. Alternatively the unit dose will contain from 2 to 20 mg of nabumetone and be administered in multiples, if desired, to give the preceding daily dose.
Most preferably nabumetone compositions are in the form of 500 mg or 1000 mg swallow tablets.
The present invention further provides a pharmaceutical composition for use in the treatment and/or prevention of dementia such as alzheimers disease which comprises an effective amount of nabumetone or 6MNA and a pharmaceutically acceptable carrier. Such compositions may be prepared in the manner as hereinbefore described.
The invention may be illustrated by carrying out clinical investigations conventional in the field of assessing dementia drugs such as these mentioned in US Patent 5,192,753.
Claims (5)
1. The use of nabumetone or 6MNA in the manufacture of a medicament for the treatment and/or prevention of dementia.
2. A use according to claim 1 wherein the dementia is alzheimer's disease.
3. A use according to claim 1 or 2 wherein the medicament is adapted for oral administration.
4. A use according to any one of claims 1 to 3 wherein the medicament is adapted for parenteral administration.
5. A use according to any one of claims 1 to 4 wherein the medicament is 15 adapted for topical administration.
6. A use according to any one of claims 1 to 5 wherein the medicament is in unit dose form and contains from 20 to 2000 mg of nabumetone or 6MNA.
20 7. A use according to claims 1, 2 or 3 wherein the medicament is in the form of a swallow tablet containing 500 mg or 1000 mg of nabumetone or 6MNA.
AP/P/9 4 / 0 0 656
BAD ORIGINAL
P30704
Abstract
NAPHTHYL DERIVATIVE FOR TREATMENT METHOD
5 The use of nabumetone or 6MNA in the manufacture of a medicament for the treatment and/or prevention of dementia.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB939314693A GB9314693D0 (en) | 1993-07-15 | 1993-07-15 | Naphthyl derivatives for treatment method |
Publications (2)
Publication Number | Publication Date |
---|---|
AP9400656A0 AP9400656A0 (en) | 1994-07-31 |
AP460A true AP460A (en) | 1996-02-16 |
Family
ID=10738900
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
APAP/P/1994/000656A AP460A (en) | 1993-07-15 | 1994-07-14 | Naphthyl derivative for treatment method. |
Country Status (10)
Country | Link |
---|---|
US (1) | US5695774A (en) |
EP (1) | EP0708641A1 (en) |
JP (1) | JPH09500121A (en) |
AP (1) | AP460A (en) |
AU (1) | AU7188194A (en) |
GB (1) | GB9314693D0 (en) |
IL (1) | IL110303A0 (en) |
MX (1) | MX9405371A (en) |
WO (1) | WO1995002399A1 (en) |
ZA (1) | ZA945083B (en) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU7485900A (en) * | 1999-09-14 | 2001-04-17 | Copley Pharmaceutical Inc. | Delayed release nabumetone formulation |
US6552078B2 (en) | 1999-10-27 | 2003-04-22 | Nobex Corp | 6-methoxy-2-naphthylacetic acid prodrugs |
TWI262791B (en) | 1999-10-27 | 2006-10-01 | Nobex Corp | 6-methoxy-2-naphthylacetic acid prodrugs |
US6436990B1 (en) | 1999-10-27 | 2002-08-20 | Nobex Corporation | 6-methoxy-2-naphthylacetic acid prodrugs |
US20060004086A1 (en) * | 2000-04-13 | 2006-01-05 | Mayo Foundation For Medical Education And Research | Method of reducing Abeta42 and treating diseases |
CA2406383A1 (en) * | 2000-04-13 | 2001-10-25 | Mayo Foundation For Medical Education And Research | A.beta.42 lowering agents |
CA2499599A1 (en) * | 2002-09-17 | 2004-04-01 | New York University | Methods of treating age associated memory impairment (aami), mild cognitive impairment (mci), and dementias with cell cycle inhibitors |
US20090155903A1 (en) * | 2004-03-19 | 2009-06-18 | Myriad Genetics, Incorporated | Pharmaceutical composition and method |
EP2046119A2 (en) * | 2006-07-07 | 2009-04-15 | Myriad Genetics, Inc. | Treatment of psychiatric disorders |
WO2015155544A1 (en) * | 2014-04-10 | 2015-10-15 | Patrick Crowley | Delivery of non-steroidal antiinflammatory agents to the brain via the nasal tract to treat neurological disorders |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4420639A (en) * | 1973-09-11 | 1983-12-13 | Beecham Group Limited | Aromatic compounds |
US5192753A (en) * | 1991-04-23 | 1993-03-09 | Mcgeer Patrick L | Anti-rheumatoid arthritic drugs in the treatment of dementia |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA960689A (en) * | 1967-01-13 | 1975-01-07 | Syntex Corporation | 2-naphthyl acetic acid derivatives and compositions |
US4061779A (en) * | 1973-09-11 | 1977-12-06 | Beecham Group Limited | Naphthalene derivatives having anti-inflammatory activity |
GB9019413D0 (en) * | 1990-09-05 | 1990-10-17 | Beecham Group Plc | Topical treatment and composition |
-
1993
- 1993-07-15 GB GB939314693A patent/GB9314693D0/en active Pending
-
1994
- 1994-07-11 WO PCT/EP1994/002300 patent/WO1995002399A1/en not_active Application Discontinuation
- 1994-07-11 JP JP7504342A patent/JPH09500121A/en active Pending
- 1994-07-11 US US08/578,586 patent/US5695774A/en not_active Expired - Fee Related
- 1994-07-11 AU AU71881/94A patent/AU7188194A/en not_active Abandoned
- 1994-07-11 EP EP94920985A patent/EP0708641A1/en not_active Withdrawn
- 1994-07-13 ZA ZA945083A patent/ZA945083B/en unknown
- 1994-07-13 IL IL11030394A patent/IL110303A0/en unknown
- 1994-07-14 AP APAP/P/1994/000656A patent/AP460A/en active
- 1994-07-14 MX MX9405371A patent/MX9405371A/en not_active Application Discontinuation
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4420639A (en) * | 1973-09-11 | 1983-12-13 | Beecham Group Limited | Aromatic compounds |
US4420639C1 (en) * | 1973-09-11 | 2001-08-21 | Beecham Group Ltd | Aromatic compounds |
US5192753A (en) * | 1991-04-23 | 1993-03-09 | Mcgeer Patrick L | Anti-rheumatoid arthritic drugs in the treatment of dementia |
Also Published As
Publication number | Publication date |
---|---|
AU7188194A (en) | 1995-02-13 |
WO1995002399A1 (en) | 1995-01-26 |
MX9405371A (en) | 1995-01-31 |
JPH09500121A (en) | 1997-01-07 |
US5695774A (en) | 1997-12-09 |
IL110303A0 (en) | 1994-10-21 |
GB9314693D0 (en) | 1993-08-25 |
EP0708641A1 (en) | 1996-05-01 |
AP9400656A0 (en) | 1994-07-31 |
ZA945083B (en) | 1995-05-26 |
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