DK2357183T3 - Morphinanforbindelser - Google Patents

Morphinanforbindelser Download PDF

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DK2357183T3
DK2357183T3 DK11000764.8T DK11000764T DK2357183T3 DK 2357183 T3 DK2357183 T3 DK 2357183T3 DK 11000764 T DK11000764 T DK 11000764T DK 2357183 T3 DK2357183 T3 DK 2357183T3
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disorders
compound
pain
diseases
formula
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DK11000764.8T
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Roger Tung
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Concert Pharmaceuticals Inc
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Priority claimed from EP08747238A external-priority patent/EP2152709B1/en
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    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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    • C12Q1/28—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving oxidoreductase involving peroxidase
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    • 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
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/49—Cinchonan derivatives, e.g. quinine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • C07D221/28—Morphinans
    • 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
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    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/483—Physical analysis of biological material
    • G01N33/487—Physical analysis of biological material of liquid biological material
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    • G01N33/491—Blood by separating the blood components
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/483—Physical analysis of biological material
    • G01N33/487—Physical analysis of biological material of liquid biological material
    • G01N33/493—Physical analysis of biological material of liquid biological material urine

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Claims (22)

  1. MORPHINANFORBINDELSER
    1. Forbindelse med formlen I:
    eller et farmaceutisk acceptabelt salt deraf, hvor: R1 er CD3 og R2 er CH3, til anvendelse ved behandling af en patient, der lider af eller er modtagelig for en sygdom eller tilstand, udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrrelser; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte i forbindelse med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmeforstyrrelser på grund af ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer.
  2. 2. Forbindelse eller farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor ethvert atom, der ikke er specificeret som deuterium, er til stede ved dets naturlige isotophyppighed.
  3. 3. Pyrogenfri sammensætning omfattende: forbindelsen eller det farmaceutisk acceptable salt deraf ifølge et hvilket som helst af de foregående krav; til anvendelse ved behandling af en patient, der lider af eller er modtagelig for en sygdom eller tilstand, udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrrelser; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte i forbindelse med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmeforstyrrelser på grund af ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer; og en acceptabel bærer.
  4. 4. Sammensætning ifølge krav 3, der er formuleret til farmaceutisk administration, og hvor bæreren er en farmaceutisk acceptabel bærer.
  5. 5. Forbindelse, farmaceutisk acceptabelt salt deraf eller sammensætning ifølge krav 4, til anvendelse ved behandling af neuropatisk smerte eller pseudobulbær affekt.
  6. 6. Forbindelse, farmaceutisk acceptabelt salt deraf eller sammensætning ifølge krav 5, til anvendelse ved behandling af pseudobulbær affekt.
  7. 7. Sammensætning ifølge et hvilket som helst af kravene 3-6, der endvidere omfatter et andet terapeutisk middel, der er anvendeligt i behandling eller forebyggelse af en sygdom eller tilstand, der er udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrrelser; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser, der er forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser, der er forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte, der er forbundet med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmelidelser grundet ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer.
  8. 8. Sammensætning ifølge krav 7, hvor det andet terapeutiske middel er udvalgt fra quinidin, quinidinsulfat, oxycodon og gabapentin.
  9. 9. Separate doseringsformer af: (i) en forbindelse, et farmaceutisk acceptabelt salt deraf eller en sammensætning ifølge et hvilket som helst af kravene 1-4; og (ii) et andet terapeutisk middel, der er anvendeligt i behandling eller forebyggelse af en sygdom eller tilstand, der er udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrrelser; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser, der er forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser, der er forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte, der er forbundet med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmelidelser, der er forårsaget af ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer, hvor forbindelsen, det farmaceutisk acceptable salt deraf eller sammensætningen og det andet terapeutiske middel er forbundet med hinanden.
  10. 10. Separate doseringsformer ifølge krav 9, hvor det andet terapeutiske middel er udvalgt fra quinidin, quinidinsulfat, oxycodon og gabapentin.
  11. 11. Pakning, der omfatter separate doseringsformer ifølge krav 9 eller 10.
  12. 12. Separate doseringsformer eller pakning ifølge et hvilket som helst af kravene 9-11, hvor det andet middel er til simultan administration.
  13. 13. Separate doseringsformer eller pakning ifølge et hvilket som helst af kravene 9-11, hvor det andet middel er til separat administration.
  14. 14. Sammensætning, separat doseringsform eller pakning ifølge et hvilket som helst af kravene 7-13, til anvendelse ved behandling af en patient, der lider af eller er modtagelig for diabetisk neuropati, hvor det andet terapeutiske middel er quinidinsulfat.
  15. 15. Sammensætning, separate doseringsformer eller pakning ifølge et hvilket som helst af kravene 7-14, der omfatter 10-60 mg af forbindelsen med formlen I eller et farmaceutisk acceptabelt salt deraf og 2,5-30 mg quinidin.
  16. 16. Anvendelse af en forbindelse med formlen I:
    eller et farmaceutisk acceptabelt salt deraf, hvor: R1 er CD3 og R2 er CH3, til fremstilling af et lægemiddel til behandling af en patient, der lider af eller er modtagelig for en sygdom eller tilstand, udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrrelser; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser, der er forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte i forbindelse med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmeforstyrrelser på grund af ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer.
  17. 17. Anvendelse ifølge krav 16, hvor ethvert atom, der ikke er specificeret som deuterium, er til stede ved dets naturlige isotophyppighed.
  18. 18. Anvendelse ifølge krav 16 eller 17, hvor sygdommen eller tilstanden er neuropatisk smerte eller pseudobulbær affekt.
  19. 19. Anvendelse ifølge krav 18, hvor sygdommen eller tilstanden er pseudobulbær affekt.
  20. 20. Anvendelse ifølge et hvilket som helst af kravene 16-19, sammen med et andet terapeutisk middel, der er anvendeligt til behandling eller forebyggelse af en sygdom eller tilstand, der er udvalgt fra emotionel labilitet; pseudobulbær affekt; autisme; neurologiske forstyrreler; neurodegenerative sygdomme; hjerneskade; forstyrrelser af bevidsthedslidelser; kardiovaskulære sygdomme; glaukom; tardiv dyskinesi; diabetisk neuropati; retinopatiske sygdomme; sygdomme eller forstyrrelser, der er forårsaget af homocystein-induceret apoptose; sygdomme eller forstyrrelser, der er forårsaget af forhøjede niveauer af homocystein; kronisk smerte; vanskeligt behandlelig smerte; neuropatisk smerte; sympatetisk medieret smerte; smerte, der er forbundet med gastrointestinal dysfunktion; epileptiske anfald; tinnitus; seksuel dysfunktion; vanskeligt behandlelig hoste; dermatitis; afhængighedsforstyrrelser; Retts syndrom (RTT); stemmeforstyrrelser på grund af ukontrollerede laryngalmuskelspasmer; methotrexat neurotoksicitet og træthed forårsaget af cancer.
  21. 21. Anvendelse ifølge krav 20, hvor det andet terapeutiske middel er udvalgt fra quinidin, quinidinsulfat, oxycodon og gabapentin.
  22. 22. Anvendelse ifølge krav 20 eller 21, hvor det andet middel er quinidin, og hvor doseringsmængden af forbindelsen med formlen I eller det farmaceutisk acceptable salt deraf er 10-60 mg, og doseringsmængden af quinidin er 2,5-30 mg.
DK11000764.8T 2007-05-01 2008-04-30 Morphinanforbindelser DK2357183T3 (da)

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Application Number Priority Date Filing Date Title
US91513007P 2007-05-01 2007-05-01
US91666207P 2007-05-08 2007-05-08
US97604407P 2007-09-28 2007-09-28
EP08747238A EP2152709B1 (en) 2007-05-01 2008-04-30 Morphinan compounds

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DK12176544.0T DK2522668T3 (da) 2007-05-01 2008-04-30 Morphinanforbindelser
DK14173190.1T DK2792662T3 (da) 2007-05-01 2008-04-30 Morphinanforbindelser
DK20200633.4T DK3825306T3 (da) 2007-05-01 2008-04-30 Morphinanforbindelser
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DK12176544.0T DK2522668T3 (da) 2007-05-01 2008-04-30 Morphinanforbindelser
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DK20200633.4T DK3825306T3 (da) 2007-05-01 2008-04-30 Morphinanforbindelser

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US (6) US9314440B2 (da)
EP (5) EP3357923B1 (da)
BR (1) BRPI0811478B8 (da)
CA (3) CA3208128A1 (da)
CY (1) CY1117826T1 (da)
DK (4) DK2522668T3 (da)
ES (5) ES2577477T3 (da)
FI (1) FI3825306T3 (da)
HK (5) HK1155442A1 (da)
HR (5) HRP20230745T3 (da)
HU (3) HUE063526T2 (da)
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PL (3) PL2792662T3 (da)
PT (5) PT3825306T (da)
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WO2017020014A1 (en) * 2015-07-30 2017-02-02 Concert Pharmaceuticals, Inc. Deuterated morphinan compounds for use in treating agitation
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