SI3061760T1 - Devterirani derivati benzokinolizina kot inhibitorji vezikularnega monoaminskega transporterja 2 - Google Patents

Devterirani derivati benzokinolizina kot inhibitorji vezikularnega monoaminskega transporterja 2 Download PDF

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Publication number
SI3061760T1
SI3061760T1 SI200931797T SI200931797T SI3061760T1 SI 3061760 T1 SI3061760 T1 SI 3061760T1 SI 200931797 T SI200931797 T SI 200931797T SI 200931797 T SI200931797 T SI 200931797T SI 3061760 T1 SI3061760 T1 SI 3061760T1
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compound
use according
deuterium
enrichment
group
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SI200931797T
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Thomas G. Gant
Manoucherhr Shahbaz
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Auspex Pharmaceuticals, Inc.
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Application filed by Auspex Pharmaceuticals, Inc. filed Critical Auspex Pharmaceuticals, Inc.
Publication of SI3061760T1 publication Critical patent/SI3061760T1/sl

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D455/00Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C07D455/06Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Claims (13)

  1. Devterirani derivati benzokinolizina kot inhibitorji vezikulamega monoaminskega transporterja 2 Patentni zahtevki
    1. Spojina,
    ali njena sol za uporabo v zdravljenju kronične hiperkinetične motnje gibanja.
  2. 2. Spojina za uporabo po zahtevku 1, kjer je omenjena kronična hiperkinetična motnja gibanja Tourettov sindrom.
  3. 3. Spoj ina za uporabo po zahtevku 1, kjer je omenjena kronična hiperkinetična motnja gibanja tardivna diskinezija.
  4. 4. Spojina za uporabo po zahtevku 1, kjer je omenjena kronična hiperkinetična motnja gibanja tik.
  5. 5. Spojina za uporabo po zahtevku 1 v kombinaciji z dodatnim terapevtskim sredstvom.
  6. 6. Spojina za uporabo po zahtevku 5, kjer je omenjeno dodatno terapevtsko sredstvo izbrano iz skupine, ki vsebuje olanzapin in pimozid.
  7. 7. Spojina za uporabo po zahtevku 6, kjer je omenjeno dodatno terapevtsko sredstvo izbrano iz skupine, ki vsebuje benzodiazepine in antipsihotike.
  8. 8. Spojina za uporabo po zahtevku 7, kjer je omenjeni benzodiazepin izbran iz skupine, ki vsebuje alprazolam, adinazolam, bromazepam, kamazepam, klobazam, klonazepam, clotiazepam, kloksazolam, diazepam, etil loflazepat, estizolam, fludiazepam, flunitrazepam, halazepam, ketazolam, lorazepam, medazepam, dazolam, nitrazepam, nordazepam, oksazepam, kalijev klorazepat, pinazepam, prazepam, tofisopam, triazolam, temazepam in klordiazepoksid.
  9. 9. Spojina za uporabo po zahtevku 7, kjer je omenjeni antipsihotik izbran iz skupin, ki vsebuje klorpromazin, levomepromazin, promazi, acepromazin, triflupromazin, ciamemazin, klorproetazin, diksirazin, flufenazin, perfenazin, proklorperazin, tiopropazat, trifluoperazin, acetofenazin, tioproperazin, butaperazin, perazin, periciazin, tioridazin, mesoridazin, pipotiazin, haloperidol, trifluperidol, melperon, moperon, pipamperon, bromperidol, benperidol, droperidol, fluanison, oksipertin, molindon, sertindol, ziprazidon, flupentiksol, clopentiksol, klorprotiksen, tiotiksen, zuklopentiksol, fluspirilen, pimozid, penfluridol, loksapin, klozapin, olanzapin, kvetiapin, tetrabenazin, sulpirid, sultoprid, tiaprid, remoksiprid, amisulprid, veraliprid, levosulpirid, litij, protipendil, risperidon, klotiapin, mozapramin, zotepin, pripiprazol in paliperidon.
  10. 10. Spojina za uporabo po zahtevku 1, kjer ima vsak položaj, kije predstavljen kot D obogatitev z devterijem ne manj kot približno 10%.
  11. 11. Spojina za uporabo po zahtevku 1, kjer ima vsak položaj, kije predstavljen kot D obogatitev z devterijem ne manj kot približno 50%.
  12. 12. Spojina za uporabo po zahtevku 1, kjer ima vsak položaj, kije predstavljen kot D obogatitev z devterijem ne manj kot približno 90%.
  13. 13. Spojina za uporabo po zahtevku 1, kjer ima vsak položaj, kije predstavljen kot D obogatitev z devterijem ne manj kot približno 98%.
SI200931797T 2008-09-18 2009-09-18 Devterirani derivati benzokinolizina kot inhibitorji vezikularnega monoaminskega transporterja 2 SI3061760T1 (sl)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9789608P 2008-09-18 2008-09-18
EP15185548.3A EP3061760B1 (en) 2008-09-18 2009-09-18 Deuterated benzoquinolizine derivatives as inhibitors of vesicular monoamine transporter 2

Publications (1)

Publication Number Publication Date
SI3061760T1 true SI3061760T1 (sl) 2018-04-30

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SI200931797T SI3061760T1 (sl) 2008-09-18 2009-09-18 Devterirani derivati benzokinolizina kot inhibitorji vezikularnega monoaminskega transporterja 2

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US (15) US8524733B2 (sl)
EP (4) EP2326643B1 (sl)
JP (3) JP5616345B2 (sl)
CN (2) CN104311552A (sl)
AU (1) AU2009303758B8 (sl)
BR (1) BRPI0913457B8 (sl)
CA (2) CA2736409C (sl)
CY (1) CY1120060T1 (sl)
DK (2) DK3061760T3 (sl)
ES (4) ES2896678T3 (sl)
HK (3) HK1186728A1 (sl)
HR (1) HRP20180239T1 (sl)
HU (1) HUE038158T2 (sl)
LT (1) LT3061760T (sl)
NO (1) NO3061760T3 (sl)
NZ (1) NZ591615A (sl)
PL (1) PL3061760T3 (sl)
PT (1) PT3061760T (sl)
SI (1) SI3061760T1 (sl)
WO (1) WO2010044981A2 (sl)

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