HRP20192032T1 - Supstituirani 2-azabicikli i njihova upotreba kao modulatora receptora oreksina - Google Patents

Supstituirani 2-azabicikli i njihova upotreba kao modulatora receptora oreksina Download PDF

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HRP20192032T1
HRP20192032T1 HRP20192032TT HRP20192032T HRP20192032T1 HR P20192032 T1 HRP20192032 T1 HR P20192032T1 HR P20192032T T HRP20192032T T HR P20192032TT HR P20192032 T HRP20192032 T HR P20192032T HR P20192032 T1 HRP20192032 T1 HR P20192032T1
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disorder
pharmaceutical composition
disease
pharmaceutically acceptable
sleep
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HRP20192032TT
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Christine F. GELIN
Terry P. LEBOLD
Brock T. Shireman
Jeannie M. ZIFF
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Janssen Pharmaceutica Nv
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
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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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
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    • 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
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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  • Chemical & Material Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Claims (19)

1. (3-fluoro-2-(pirimidin-2-il)fenil)((1S,4R,6R)-6-((5-(trifluorometil)piridin-2-il)oksi)-2 azabiciklo[2.2.1]heptan-2-il)metanon ili njegova farmaceutski prihvatljiva sol ili solvat za upotrebu u terapiji.
2. Farmaceutski sastav koji sadrži terapeutski efikasnu količinu (3-fluoro-2-(pirimidin-2-il)fenil)((1S,4R,6R)-6-((5-(trifluorometil)piridin-2-il)oksi)-2-azabiciklo[2.2.1]heptan-2-il)metanona ili njegove farmaceutski prihvatljive soli ili solvata i bar jednu farmaceutski prihvatljivu pomoćnu tvar za upotrebu u terapiji.
3. Farmaceutski sastav koja sadrži terapeutski efikasnu količinu (3-fluoro-2-(pirimidin-2-il)fenil)((1S,4R,6R)-6-((5-(trifluorometil)piridin-2-il)oksi)-2-azabiciklo[2.2.1]heptan-2-il)metanona ili njegove farmaceutski prihvatljive soli ili solvata i bar jednu farmaceutski prihvatljivu pomoćnu tvar, za upotrebu u liječenju bolesti, poremećaja ili medicinskog stanja, gdje je bolest, poremećaj ili medicinsko stanje poremećaj spavanja, metabolički poremećaj, neurološki poremećaj, aritmije, akutni zastoj srca, čirevi, sindrom iritabilnog crijeva, proljev, gastroezofagealna refluksna bolest, poremećaj raspoloženja, posttraumatski stresni poremećaj , panični poremećaj, poremećaj nedostatka pozornosti, kognitivni nedostaci ili zloupotreba opojnih sredstava..
4. Farmaceutski sastav za upotrebu prema zahtjevu 3, gdje je bolest, poremećaj ili medicinsko stanje poremećaj raspoloženja, posttraumatski stresni poremećaj, panični poremećaj , poremećaj nedostatka pozornosti, kognitivni nedostaci, ili zloupotreba opojnih sredstava.
5. Farmaceutski sastav za upotrebu prema zahtjevu 3, gdje je bolest, poremećaj ili medicinsko stanje poremećaj spavanja.
6. Farmaceutski sastav za upotrebu prema zahtjevu 5, gdje je poremećaj spavanja poremećaj prelaska iz stanja sna u stanje budnosti, nesanica, sindrom nemirnih nogu, „jet-lag“, poremećeno spavanje, i sekundarni poremećaj spavanja u vezi s neurološkim poremećajima.
7. Farmaceutski sastav za upotrebu prema zahtjevu 3, gdje je bolest, poremećaj ili medicinsko stanje metabolički poremećaj .
8. Farmaceutski sastav za upotrebu prema zahtjevu 7, gdje je metabolički poremećaj prekomjerna težina, pretilost, inzulinska rezistencija, dijabetes tipa II, hiperlipidemija, žučni kamenci, angina, hipertenzija, dispneja, tahikardija, neplodnost, apneja u snu, bol u leđima i zglobovima, proširene vene ili osteoartritis.
9. Farmaceutski sastav za upotrebu prema zahtjevu 3, gdje je bolest, poremećaj ili medicinsko stanje, neurološki poremećaj.
10. Farmaceutski sastav za upotrebu prema zahtjevu 9, gdje je neurološki poremećaj Parkinsonova bolest, Alzheimerova bolest, Touretteov sindrom, katatonija, anksioznost, delirij ili demencija.
11. Farmaceutski sastav koji sadrži terapeutski efikasnu količinu (3-fluoro-2-(pirimidin-2-il)fenil)((1S,4R,6R)-6-((5-(trifluorometil)piridin-2-il)oksi)-2-azabiciklo[2.2.1]heptan-2-il)metanona ili njegove farmaceutski prihvatljive soli ili solvata i bar jednu farmaceutski prihvatljivu pomoćnu tvar za oralno davanje.
12. Farmaceutski sastav prema zahtjevu 11 u obliku tablete, kapsule, otopine, emulzije ili suspenzije.
13. Farmaceutski sastav prema zahtjevu 11 u obliku tablete.
14. Farmaceutski sastav prema zahtjevu 13, gdje su pomoćne tvari izabrane između inertnih razblaživača, sredstava za dezintegraciju, vezivnih sredstava, maziva, zaslađivača, pojačivača okusa , bojila i konzervansa.
15. Farmaceutski sastav prema zahtjevu 14, gdje su inertna sredstva za punjenje izabrana između natrijevog i kalcijevog karbonata, natrijevog i kalcijevog fosfata, laktoze, škroba, šećera, glukoze, metil celuloze, magnezijevog stearata, manitola i sorbitola .
16. Farmaceutski sastav prema zahtjevu 14, gdje su sredstva za raspadanje izabrana između škroba, polivinilpirolidona (PVP), natrijev škrob glikolata, mikrokristalične celuloze i alginske kiseline.
17. Farmaceutski sastav prema zahtjevu 14, gdje su vezivna sredstva izabrana između škroba i želatine.
18. Farmaceutski sastav prema zahtjevu 14, gdje su maziva sredstva izabrana između magnezijevog stearata, stearinske kiseline i talka.
19. Farmaceutski sastav prema zahtjevu 11 u obliku kapsule.
HRP20192032TT 2013-03-13 2019-11-08 Supstituirani 2-azabicikli i njihova upotreba kao modulatora receptora oreksina HRP20192032T1 (hr)

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US201361780378P 2013-03-13 2013-03-13
EP17206491.7A EP3363438B1 (en) 2013-03-13 2014-03-12 Substituted 2-azabicycles and their use as orexin receptor modulators

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HRP20230633TT HRP20230633T1 (hr) 2013-03-13 2014-03-12 Supstituirani 2-azabicikli i njihova uporaba kao modulatora receptora oreksina
HRP20180303TT HRP20180303T1 (hr) 2013-03-13 2018-02-20 Supstituirani 2-azabicikli i njihova uporaba kao modulatora receptora oreksina
HRP20192032TT HRP20192032T1 (hr) 2013-03-13 2019-11-08 Supstituirani 2-azabicikli i njihova upotreba kao modulatora receptora oreksina

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HRP20180303TT HRP20180303T1 (hr) 2013-03-13 2018-02-20 Supstituirani 2-azabicikli i njihova uporaba kao modulatora receptora oreksina

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JP (1) JP6275815B2 (hr)
KR (1) KR102209424B1 (hr)
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AR (1) AR095423A1 (hr)
AU (2) AU2014248680B2 (hr)
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