HRP20210641T1 - Deuterirani heterociklični spojevi i njihova uporaba kao sredstva za kontrastiranje - Google Patents

Deuterirani heterociklični spojevi i njihova uporaba kao sredstva za kontrastiranje Download PDF

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HRP20210641T1
HRP20210641T1 HRP20210641TT HRP20210641T HRP20210641T1 HR P20210641 T1 HRP20210641 T1 HR P20210641T1 HR P20210641T T HRP20210641T T HR P20210641TT HR P20210641 T HRP20210641 T HR P20210641T HR P20210641 T1 HRP20210641 T1 HR P20210641T1
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compound
pharmaceutically acceptable
acceptable salt
individual
deuterated
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HRP20210641TT
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Jan Marik
Joseph P. Lyssikatos
Simon Williams
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F. Hoffmann - La Roche Ag
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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
    • C07D487/04Ortho-condensed 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • A61P25/28Drugs 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
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (18)

1. Deuterirani spoj s izotopom za kontrastiranje, naznačen time, da spoj ima formulu (Ie): [image] i naznačen time, da ugljik označen zvjezdicom * ima faktor izotopskog obogaćenja deuterija od najmanje 3500.
2. Deuterirani spoj s izotopom za kontrastiranje, naznačen time, da ima formulu (Ie): [image] ili njegova sol.
3. Deuterirani spoj s izotopom za kontrastiranje, naznačen time, da se spoj bira između: [image] [image] [image] [image] i njihovih soli.
4. Farmaceutski pripravak, naznačen time da sadrži deuterirani spoj prema bilo kojem patentnom zahtjevu od 1 do 3 ili njegovu farmaceutski prihvatljivu sol te farmaceutski prihvatljivo otapalo ili nosač.
5. Postupak za otkrivanje neurofibrilarnih čvorova i/ili senilnih plakova kod pojedinca, naznačen time, da obuhvaća - davanje pojedincu deuteriranog spoja s izotopom za kontrastiranje, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegove farmaceutski prihvatljive soli, - i mjerenje radioaktivnog signala spoja.
6. Postupak prema patentnom zahtjevu 5, naznačen time, da se mjerenje vrši putem gama scintigrafije.
7. Postupak otkrivanja neurološkog poremećaja povezanog s amiloidnim plakom i/ili nakupljanjem tau proteina kod pojedinca, naznačen time, da obuhvaća - davanje pojedincu deuteriranog spoja s izotopom za kontrastiranje, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegove farmaceutski prihvatljive soli, u količini koju je moguće detektirati, - i mjerenje radioaktivnog signala spoja povezanog s amiloidnim naslagama i/ili agregatima tau proteina.
8. Postupak otkrivanja Alzheimerove bolesti kod pojedinca, naznačen time, da obuhvaća - davanje pojedincu deuteriranog spoja s izotopom za kontrastiranje, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3 ili njegove farmaceutski prihvatljive soli, u količini koju je moguće detektirati, i - nakon što se spoj poveže s amiloidnim naslagama i/ili tau proteinima, mjerenje radioaktivnog signala spoja povezanog s amiloidnim naslagama i/ili agregatima tau proteina.
9. Postupak otkrivanja Alzheimerove bolesti, naznačen time, da obuhvaća - davanje pojedincu deuteriranog spoja prema bilo kojem od patentnih zahtjeva od 1 do 3 ili njegove farmaceutski prihvatljive soli, u količini koju je moguće detektirati, i - nakon što se kod pojedinca spoj poveže s agregatima tau proteina, mjerenje radioaktivnog signala spoja povezanog s agregatima tau proteina.
10. Deuterirani spoj, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegova farmaceutski prihvatljiva sol za primjenu u medicinskoj dijagnostici neuroloških poremećaja.
11. Deuterirani spoj, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegova farmaceutski prihvatljiva sol za primjenu u otkrivanju neurofibrilarnih čvorova i/ili senilnih plakova u dijagnostici neuroloških poremećaja.
12. Deuterirani spoj, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegova farmaceutski prihvatljiva sol za primjenu u dijagnostici neurološkog poremećaja.
13. Deuterirani spoj, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegova farmaceutski prihvatljiva sol za primjenu u dijagnostici Alzheimerove bolesti.
14. Uporaba deuteriranog spoja, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegove farmaceutski prihvatljive soli, za pripremu medikamenta za otkrivanje neurofibrilarnih čvorova i/ili senilnih plakova kod pojedinca.
15. Uporaba deuteriranog spoja, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegove farmaceutski prihvatljive soli, za pripremu medikamenta za otkrivanje neurološkog poremećaja kod pojedinca.
16. Uporaba deuteriranog spoja, kako je opisan u bilo kojem od patentnih zahtjeva od 1 do 3, ili njegove farmaceutski prihvatljive soli, za pripremu medikamenta za otkrivanje Alzheimerove bolesti kod pojedinca.
17. Postupak otkrivanja progresivne supranuklearne paralize kod pojedinca, naznačen time, da obuhvaća - davanje pojedincu deuteriranog spoja prema bilo kojem od patentnih zahtjeva od 1 do 3 ili njegove farmaceutski prihvatljive soli, u količini koju je moguće detektirati, i - nakon što se spoj veže za amiloidni plak i/ili agregate tau proteina, mjerenje radioaktivnog signala spoja povezanog s amiloidnim naslagama i/ili agregatima tau proteina.
18. Postupak otkrivanja progresivne supranuklearne paralize, naznačen time da obuhvaća - davanje deuteriranog spoja prema bilo kojem od patentnih zahtjeva od 1 do 3 ili njegove farmaceutski prihvatljive soli, u količini koju je moguće detektirati, i - nakon što se spoj veže za agregate tau proteina, mjerenje radioaktivnog signala spoja povezanog s agregatima tau proteina.
HRP20210641TT 2014-05-13 2021-04-22 Deuterirani heterociklični spojevi i njihova uporaba kao sredstva za kontrastiranje HRP20210641T1 (hr)

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Application Number Priority Date Filing Date Title
US201461992717P 2014-05-13 2014-05-13
EP15725253.7A EP3143011B1 (en) 2014-05-13 2015-05-12 Deuterated heterocyclic compounds and their use as imaging agents
PCT/EP2015/060447 WO2015173225A1 (en) 2014-05-13 2015-05-12 Deuterated heterocyclic compounds and their use as imaging agents

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EP (2) EP3901145A1 (hr)
JP (2) JP6529986B2 (hr)
KR (2) KR102530129B1 (hr)
CN (2) CN110483522B (hr)
AU (2) AU2015261008B2 (hr)
CA (1) CA2948721C (hr)
DK (1) DK3143011T3 (hr)
ES (1) ES2867814T3 (hr)
HR (1) HRP20210641T1 (hr)
HU (1) HUE053939T2 (hr)
IL (3) IL280791B2 (hr)
LT (1) LT3143011T (hr)
MX (2) MX2016014615A (hr)
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KR20170002639A (ko) 2017-01-06
AU2019203369A1 (en) 2019-06-06
AU2019203369B2 (en) 2020-06-04
EP3901145A1 (en) 2021-10-27
RU2016147742A (ru) 2018-06-18
SI3143011T1 (sl) 2021-08-31
AU2015261008A1 (en) 2016-11-17
NZ764181A (en) 2023-11-24
MX2020010847A (es) 2021-07-16
US20200297875A1 (en) 2020-09-24
IL248692A0 (en) 2017-01-31
BR112016026443A8 (pt) 2021-07-06
KR102618139B1 (ko) 2023-12-27
US11504440B2 (en) 2022-11-22
JP6529986B2 (ja) 2019-06-12
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
EP3143011B1 (en) 2021-03-03
KR20230035445A (ko) 2023-03-13
DK3143011T3 (da) 2021-05-03
BR112016026443A2 (pt) 2017-08-15
PT3143011T (pt) 2021-04-26
PL3143011T3 (pl) 2021-07-19
RS61810B1 (sr) 2021-06-30
JP6681498B2 (ja) 2020-04-15
CN106459059B (zh) 2019-09-24
US20230218782A1 (en) 2023-07-13
AU2015261008B2 (en) 2019-02-14
CA2948721A1 (en) 2015-11-19
IL280791B2 (en) 2024-03-01
IL248692B (en) 2020-01-30
WO2015173225A1 (en) 2015-11-19
MX2016014615A (es) 2017-03-06
CN110483522A (zh) 2019-11-22
IL271631A (en) 2020-02-27
US10675367B2 (en) 2020-06-09
LT3143011T (lt) 2021-05-10
RU2016147742A3 (hr) 2018-10-08
US20190201561A1 (en) 2019-07-04
IL280791A (en) 2021-04-29
KR102530129B1 (ko) 2023-05-10
EP3143011A1 (en) 2017-03-22
US20160250358A1 (en) 2016-09-01
CN106459059A (zh) 2017-02-22
ES2867814T3 (es) 2021-10-20
JP2019147825A (ja) 2019-09-05
IL271631B (en) 2021-05-31
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HUE053939T2 (hu) 2021-08-30
US10076581B2 (en) 2018-09-18
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SG11201609281UA (en) 2016-12-29
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