FI112868B - Spiro[1-azabicyclo[2.2.2]oktan- eller -[2.2.1]heptan-3,5'-oxazolidin]-2'-onföreningar användbara i terapi och förfarande för framställning av desamma samt mellanprodukter - Google Patents

Spiro[1-azabicyclo[2.2.2]oktan- eller -[2.2.1]heptan-3,5'-oxazolidin]-2'-onföreningar användbara i terapi och förfarande för framställning av desamma samt mellanprodukter Download PDF

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Publication number
FI112868B
FI112868B FI970762A FI970762A FI112868B FI 112868 B FI112868 B FI 112868B FI 970762 A FI970762 A FI 970762A FI 970762 A FI970762 A FI 970762A FI 112868 B FI112868 B FI 112868B
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Finland
Prior art keywords
enantiomer
compound
formula
pharmaceutically acceptable
azabicyclo
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FI970762A
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English (en)
Finnish (fi)
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FI970762A (sv
FI970762A0 (sv
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Ronald Conrad Griffith
Robert John Murray
Michael Balestra
John Charles Gordon
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Astra Ab
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Priority claimed from GB9417084A external-priority patent/GB9417084D0/en
Priority claimed from GBGB9504627.2A external-priority patent/GB9504627D0/en
Application filed by Astra Ab filed Critical Astra Ab
Publication of FI970762A publication Critical patent/FI970762A/sv
Publication of FI970762A0 publication Critical patent/FI970762A0/sv
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Publication of FI112868B publication Critical patent/FI112868B/sv

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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

Claims (11)

1. Spiro[1-azabicyclo[2.2.2]oktan- eller -[2.2.1]heptan-3,5'-oxazolidin]-2'-onförening med formel I 5 <£«»>. •Φ, vari R är väte eller metyl; och 10 n är 1 eller 2; eller ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav.
2. Förening enligt patentkrav 1, kännetecknad av att R är ' ’· 15 väte, eller ett farmaceutiskt acceptabelt syraadditionssalt ; : eller enantiomer därav. . 3. Spiro[1-azabicyclo[2.2.2]oktan-3,5'-oxazolidin]-2'-on ; eller ett farmaceutiskt acceptabelt syraadditionssalt eller 20 enantiomer därav. 4. (+)-spiro[1-azabicyclo[2.2.2]oktan-3,5'-oxazolidin]-2'-on eller ett farmaceutiskt acceptabelt syraadditionssalt därav. 25 5. (-)-spiro[1-azabicyclo[2.2.2]oktan-3,5'-oxazolidin]-2'-on eller ett farmaceutiskt acceptabelt syraadditionssalt därav. 1 Spiro[1-azabicyclo[2.2.1]heptan-3,5'-oxazolidin-2'-on], eller ett farmaceutiskt acceptabelt syraadditionssalt eller 30 enantiomer därav. 112868 7 . 3'-metyl-spiro[1-azabicyclo[2.2.2]oktan-3,5'-oxazolidin- 2'-on], eller ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav.
8. Farmaceutisk formulering, kännetecknad av att den inne- fattar en förening enligt nägot av patentkraven 1-7, eller ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav, i blandning med ett farmaceutiskt acceptabelt utspädningsmedel eller bärare. 10
9. Förening enligt nägot av patentkraven 1-7, eller ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav, för användning som ett läkemedel.
10. Användning av en förening enligt nägot av patentkraven 1- 7, eller ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav, vid framställning av ett läkemedel för behandling eller profylax av psykotiska sjukdomar eller sjukdomar med intellektuell försvagning. 20 ,·, ; 11. Användning enligt patentkrav 10, kännetecknad av att sjukdomen är schizofreni, Alzheimer's sjukdom, inlärnings-störning, kognitionsförsvagning, eller uppmärksamhetsbrist-hyperaktivitetsrubbning. 25 • " 12. Användning av en förening enligt nägot av patentkraven 1- ·’ 7, eller ett f armaceutiskt acceptabelt syraadditionssalt eller enantiomer därav, vid framställning av ett läkemedel för behandling eller profylax av ängest. ; 3 0
13. Förfarande för framställning av en förening med formel I enligt patentkrav 1, eller ett farmaceutiskt acceptabelt syraadditionsalt eller enantiomer därav, kännetecknat av att: 35 (a) man framställer en förening med formel I, väri R är väte, genom cyklisering av en motsvarande förening med formel II 112868 «en,». Jy Ηύ\ N - C - O väri n är säsom definierats i patentkrav 1; 5 (b) man framställer en förening med formel I genom omsättning av en motsvarande förening med formel III IM. db NHR 10 ; : väri n och R är säsom definierats i patentkrav 1, med en karbonyldonerande förening; 15 (c) man framställer en förening med formel I, väri R är metyl, genom alkylering av en motsvarande förening med formel I väri R är väte; eller (d) man framställer en enantiomer av en förening med formel I 20 genom upplösning av den ena enantiomeren frän en blandning av enantiomerer; och om sä önskas eller om nödvändigt, överförs den erhällna föreningen med formel I, eller ett farmaceutiskt acceptabelt 25 syraadditionssalt eller enantiomer därav, tili ett farmaceutiskt acceptabelt syraadditionssalt eller enantiomer därav, eller vice versa. 112368 14. 3-hydroxi-1-azabicyklo[2.2.2]okt- eller -[2.2.1]hept-3 -ylättiksyra-hydrazid med formel IV <cm. ^fS iv 5 väri n är säsom definierats i patentkrav 1, eller ett salt eller enantiomer därav. 10 15. 3-hydroxi-1-azabicyklo[2.2.2]okt- eller - [2.2.1] hept - 3 -ylmetylaminometyl med formel III (CH.), v; . HO'i NHR « · ; ’’ 15 ’väri n är säsom definierats i patentkrav 1, och R är metyl, ’ eller ett salt eller enantiomer därav.
FI970762A 1994-08-24 1997-02-24 Spiro[1-azabicyclo[2.2.2]oktan- eller -[2.2.1]heptan-3,5'-oxazolidin]-2'-onföreningar användbara i terapi och förfarande för framställning av desamma samt mellanprodukter FI112868B (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB9417084 1994-08-24
GB9417084A GB9417084D0 (en) 1994-08-24 1994-08-24 Compounds useful in therapy
GBGB9504627.2A GB9504627D0 (en) 1995-03-08 1995-03-08 Compounds for use in therapy
GB9504627 1995-03-08
SE9500937 1995-08-22
PCT/SE1995/000937 WO1996006098A1 (en) 1994-08-24 1995-08-22 Spiro-azabicyclic compounds useful in therapy

Publications (3)

Publication Number Publication Date
FI970762A FI970762A (sv) 1997-02-24
FI970762A0 FI970762A0 (sv) 1997-02-24
FI112868B true FI112868B (sv) 2004-01-30

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FI970762A FI112868B (sv) 1994-08-24 1997-02-24 Spiro[1-azabicyclo[2.2.2]oktan- eller -[2.2.1]heptan-3,5'-oxazolidin]-2'-onföreningar användbara i terapi och förfarande för framställning av desamma samt mellanprodukter

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EP (1) EP0777671B1 (sv)
JP (1) JP3708962B2 (sv)
KR (1) KR100366331B1 (sv)
CN (2) CN1056846C (sv)
AR (1) AR031828A2 (sv)
AT (1) ATE192157T1 (sv)
AU (1) AU690735B2 (sv)
BR (1) BR9508751A (sv)
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DK (1) DK0777671T3 (sv)
EE (1) EE03399B1 (sv)
EG (1) EG24222A (sv)
ES (1) ES2145922T3 (sv)
FI (1) FI112868B (sv)
GR (1) GR3033878T3 (sv)
HK (1) HK1010370A1 (sv)
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ES2145922T3 (es) 2000-07-16
IL115039A0 (en) 1995-12-08
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PL183933B1 (pl) 2002-08-30
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NO307707B1 (no) 2000-05-15
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