Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
  • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
  • C07D471/04—Ortho-condensed systems
• • 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]

Definitions

• alkyl' as a group or part of a group means a straight or branched chain alkyl group, for example a methyl, ethyl, n-propyl, i-propyl, n-butyl, s-butyl or t-butyl group.
• Compounds of the invention may also be useful for the treatment of cognitive disorders such as dementia, particularly degenerative dementia (including senile dementia, Alzheimer's disease, Pick's disease, Huntington's chorea,
• dementia particularly degenerative dementia (including senile dementia, Alzheimer's disease, Pick's disease, Huntington's chorea,
• a method of treating a human or animal subject suffering from an inflammatory disorder comprises administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative thereof.
• the compounds of formula (I) and their pharmaceutically acceptable derivatives may be formulated for administration in any suitable manner. They may, for example, be formulated for topical administration or administration by inhalation or, more preferably, for oral, transdermal or parenteral administration.
• the pharmaceutical composition may be in a form such that it can effect controlled release of the compounds of formula (I) and their pharmaceutically acceptable derivatives.
• the pharmaceutical composition may take the form of, for example, tablets (including sub-lingual tablets), capsules, powders, solutions, syrups or suspensions prepared by conventional means with acceptable excipients.
• a proposed daily dosage of a compound of formula (I) for the treatment of man is 0.01 mg/kg to 500 mg/kg, such as 0.05mg/kg to 100mg/kg, e.g. 0.1mg/kg to 50mg/kg, which may be conveniently administered in 1 to 4 doses.
• the precise dose employed will depend on the age and condition of the patient and on the route of administration. Thus, for example, a daily dose of 0.25mg/kg to 10mg/kg may be suitable for systemic administration.
• the oxidation is effected using a monopersulfate compound, such as potassium peroxymonosulfate (known as OxoneTM) and the reaction is carried out in a solvent, such as an aqueous alcohol, (e.g. aqueous methanol), and at between -78°C and ambient temperature.
• a monopersulfate compound such as potassium peroxymonosulfate (known as OxoneTM)
• OxoneTM potassium peroxymonosulfate
• a solvent such as an aqueous alcohol, (e.g. aqueous methanol), and at between -78°C and ambient temperature.
• Another process (D) for preparing compounds of formula (I) thus comprises deprotecting protected derivatives of compounds of formula (I).
• the solution may be packaged for injection, for example by filling and sealing in ampoules, vials or syringes.
• the ampoules, vials or syringes may be aseptically filled (e.g. the solution may be sterilised by filtration and filled into sterile ampoules under aseptic conditions) and/or terminally sterilised (e.g. by heating in an autoclave using one of the acceptable cycles).
• the solution may be packed under an inert atmosphere of nitrogen.
• the solution is filled into ampoules, sealed by fusion of the glass and terminally sterilised.

Landscapes

• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Health & Medical Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Pain & Pain Management (AREA)
• Pharmacology & Pharmacy (AREA)
• Rheumatology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Nitrogen Condensed Heterocyclic Rings (AREA)
• Plural Heterocyclic Compounds (AREA)

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• 1996
  • 1996-04-02 JP JP8529971A patent/JPH11501049A/ja active Pending
  • 1996-04-02 EP EP96909164A patent/EP0819127A1/en not_active Withdrawn
  • 1996-04-02 AU AU52766/96A patent/AU5276696A/en not_active Abandoned
  • 1996-04-02 KR KR1019970706963A patent/KR19980703559A/ko not_active Application Discontinuation
  • 1996-04-02 PL PL96322623A patent/PL322623A1/xx unknown
  • 1996-04-02 TR TR97/01105T patent/TR199701105T1/xx unknown
  • 1996-04-02 EA EA199700209A patent/EA199700209A1/ru unknown
  • 1996-04-02 WO PCT/EP1996/001438 patent/WO1996031509A1/en not_active Application Discontinuation
  • 1996-04-02 SK SK1332-97A patent/SK133297A3/sk unknown
  • 1996-04-02 CA CA002216809A patent/CA2216809A1/en not_active Abandoned
  • 1996-04-02 CZ CZ973133A patent/CZ313397A3/cs unknown
  • 1996-04-02 CN CN96194403A patent/CN1186492A/zh active Pending
  • 1996-04-02 NZ NZ304886A patent/NZ304886A/en unknown
  • 1996-04-02 HU HU9801602A patent/HUP9801602A3/hu unknown
• 1997
  • 1997-09-25 IS IS4570A patent/IS4570A/is unknown
  • 1997-09-30 BG BG101934A patent/BG101934A/xx unknown
  • 1997-10-03 NO NO974595A patent/NO974595L/no unknown

Non-Patent Citations (1)

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