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
  • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• • 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
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
• • 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
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
• • 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
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/36—Opioid-abuse

Definitions

• N-substituted azabicycloalkane derivatives for the treatment of diseases of the central nervous system
• N-substituted azabicycloalkane derivatives are already known as neuroleptics (WO 95/13279, WO 95/15327, WO 96/04272, US 5,475,105, US 5,521,209, US 5,616,705, US 5,753,690). It has now been found that these substances are also suitable for combating addiction disorders and other disorders of the central nervous system.
• the invention relates to the use of N-substituted 3-azabicycloalkane derivatives of the formula I.
• B is a 4-, 5- or 6-ring which can contain a double bond
• R 1 is a mono- or disubstituted phenyl, naphthyl or optionally substituted by halogen atoms, C 4 alkyl, trifluoromethyl, hydroxy, C 4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups Phenanthryl or thienyl group,
• n the number 0, 1, 2, 3 or 4 and
• R 2 denotes a naphthyl group which is optionally substituted by one or two halogen atoms or one of the following radicals: R3 0 R8 C R5 NR 6 CR 7 NR 6 - so 2 - (CJS
• R 3 represents a hydrogen atom, a hydroxyl group or a phenyl radical optionally substituted by a fluorine, chlorine or bromine atom,
• R 4 represents a hydrogen atom
• R 3 and R 4 together represent an oxygen atom
• R 5 is optionally mono- or disubstituted phenyl by fluorine, chlorine or bromine atoms or hydroxyl, nitro, amino, C ⁇ _ 4 -alkanoylamino, C ⁇ - 4 alkyl, amino, C ⁇ _ 4 alkyl or methoxy groups , Naphthyl or thienyl group means
• R 6 represents a hydrogen atom or a methyl group
• R 7 is a phenyl mono- or disubstituted by fluorine, chlorine or bromine atoms or by C 4 alkyl, hydroxyl, methoxy, nitro, cyano, trifluoromethyl, amino or di-C 4 alkylamino groups -, naphthyl, benzofuryl, benzothienyl, thienyl, indolyl, N-methylindolyl or indenyl group or a C 3 _ 7 -cycloalkyl group,
• R 8 is a hydrogen atom or a fluorine or chlorine atom or a C 4 alkyl, methoxy or amino group
• R 9 represents a hydrogen atom or a methyl group
• R 10 represents a hydrogen atom or a methyl group
• R 9 and R 10 together with the ring carbon atom represent a spirocyclopropane ring
• R 11 is a hydrogen atom, a hydroxy, -CC 4 alkyl or
• X and Y are carbon atoms, CH, CH 2 , NH or -CC alkyl-N groups or nitrogen atoms,
• Z is a direct bond, a CO group, CS group or one
• A is a hydrogen tom, a hydroxy, amino, mercapto,
• A denotes a C 3 -C 4 -alkylene group linked to Y, which may contain one or two non-cumulative double bonds and in which a CH or CH 2 group is replaced by a nitrogen or sulfur atom or an NH or N-CH 3 - Group can be replaced and the ring either by a fluorine or chlorine atom or a methyl, methoxy, nitro or amino group monosubstituted or in the case of a benzene ring this by fluorine or chlorine atoms or methyl, trifluoromethyl, nitro, hydroxyl, methoxy, amino, monomethyl or dimethylamino groups can be mono-, di- or tri-substituted,
• ring containing X, Y and Z on nitrogen atom No. 1 has a C ⁇ -C 4 -alkyl, allyl or benzyl group and can contain 1 to 3 non-cumulative double bonds,
• Addictive substances can be:
• Opioids such as morphine or heroin, nicotine, alcohol,
• Substances that interact with the benzodiazepine-receptor complex sedatives or tranquilizers, such as the benzodiazepines.
• cocaine or amphetamine and amphetamine-like substances are particularly suitable as addictive substances.
• the compounds of formula I can be used both in the form of their racemates and their optical isomers.
• the compounds can be administered orally or parenterally, intravenously or intramuscularly in the usual way.
• the dosage depends on the age, condition and weight of the patient and on the type of application.
• the daily dose of active substance is between approximately 1 and 100 mg / kg body weight when administered orally and between 0.1 and 10 mg / kg body weight when administered parenterally.
• the compounds can be used in common galenical application forms in solid or liquid form, for example as tablets, film tablets, capsules, powders, granules, dragees, suppositories, solutions, ointments, creams or sprays. These are produced in the usual way.
• the active ingredients can be processed with the usual pharmaceutical auxiliaries such as tablet binders, fillers, preservatives, tablet disintegrants, flow regulators, plasticizers, wetting agents, dispersants, emulsifiers, solvents, retardants, antioxidants 10 and / or propellants (see H. Sucker et al:
• the administration forms obtained in this way normally contain the active ingredient in an amount of 1 to 99% by weight.

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• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Neurosurgery (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Neurology (AREA)
• Engineering & Computer Science (AREA)
• Biomedical Technology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Psychiatry (AREA)
• Addiction (AREA)
• Epidemiology (AREA)
• Hospice & Palliative Care (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
• Indole Compounds (AREA)
• Plural Heterocyclic Compounds (AREA)
• Nitrogen Condensed Heterocyclic Rings (AREA)

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• 1998
  • 1998-11-24 DE DE19854147A patent/DE19854147A1/de not_active Withdrawn
• 1999
  • 1999-11-12 CN CN99813559A patent/CN1328455A/zh active Pending
  • 1999-11-12 PL PL99348758A patent/PL348758A1/xx not_active Application Discontinuation
  • 1999-11-12 TR TR2001/01476T patent/TR200101476T2/xx unknown
  • 1999-11-12 KR KR1020017006445A patent/KR20010080535A/ko not_active Application Discontinuation
  • 1999-11-12 SK SK711-2001A patent/SK7112001A3/sk unknown
  • 1999-11-12 WO PCT/EP1999/008734 patent/WO2000030639A1/de not_active Application Discontinuation
  • 1999-11-12 CA CA002352526A patent/CA2352526A1/en not_active Abandoned
  • 1999-11-12 HU HU0104416A patent/HUP0104416A3/hu unknown
  • 1999-11-12 IL IL14318199A patent/IL143181A0/xx unknown
  • 1999-11-12 BR BR9915589-3A patent/BR9915589A/pt not_active IP Right Cessation
  • 1999-11-12 CZ CZ20011796A patent/CZ20011796A3/cs unknown
  • 1999-11-12 JP JP2000583522A patent/JP2002530333A/ja active Pending
  • 1999-11-12 AU AU17753/00A patent/AU1775300A/en not_active Abandoned
  • 1999-11-12 EP EP99960974A patent/EP1133293A1/de not_active Withdrawn
  • 1999-11-24 AR ARP990105979A patent/AR021502A1/es unknown
• 2001
  • 2001-05-16 ZA ZA200103976A patent/ZA200103976B/en unknown
  • 2001-05-23 NO NO20012538A patent/NO20012538L/no not_active Application Discontinuation
  • 2001-05-30 BG BG105549A patent/BG105549A/xx unknown
  • 2001-06-21 HR HR20010472A patent/HRP20010472A2/hr not_active Application Discontinuation
• 2002
  • 2002-04-12 HK HK02102768.4A patent/HK1040933A1/zh unknown

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