CN106459059B - 氘化杂环化合物和其作为成像剂的用途 - Google Patents

氘化杂环化合物和其作为成像剂的用途 Download PDF

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Publication number
CN106459059B
CN106459059B CN201580025219.XA CN201580025219A CN106459059B CN 106459059 B CN106459059 B CN 106459059B CN 201580025219 A CN201580025219 A CN 201580025219A CN 106459059 B CN106459059 B CN 106459059B
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compound
certain embodiments
deuterated
compounds
imaging
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CN106459059A (zh
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扬·马里克
约瑟夫·P·利丝卡托斯
西蒙·威廉姆斯
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F Hoffmann La Roche AG
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
CN201580025219.XA 2014-05-13 2015-05-12 氘化杂环化合物和其作为成像剂的用途 Active CN106459059B (zh)

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US201461992717P 2014-05-13 2014-05-13
US61/992,717 2014-05-13
PCT/EP2015/060447 WO2015173225A1 (en) 2014-05-13 2015-05-12 Deuterated heterocyclic compounds and their use as imaging agents

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IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
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EP4218934B1 (en) 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
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JP7119978B2 (ja) * 2018-12-20 2022-08-17 オムロン株式会社 制御装置およびプログラム
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EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CN113526526A (zh) * 2021-07-12 2021-10-22 苏州大学 氘代氨制备方法及以其作为氘源参与的氘代反应
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BR112016026443A8 (pt) 2021-07-06
CA2948721A1 (en) 2015-11-19
CN110483522A (zh) 2019-11-22
IL248692A0 (en) 2017-01-31
MX2016014615A (es) 2017-03-06
IL280791A (en) 2021-04-29
LT3143011T (lt) 2021-05-10
IL280791B2 (en) 2024-03-01
JP2019147825A (ja) 2019-09-05
PT3143011T (pt) 2021-04-26
US20200297875A1 (en) 2020-09-24
JP2017515856A (ja) 2017-06-15
IL271631A (en) 2020-02-27
KR20170002639A (ko) 2017-01-06
HUE053939T2 (hu) 2021-08-30
MX376163B (es) 2025-03-07
ES2867814T3 (es) 2021-10-20
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
US20230218782A1 (en) 2023-07-13
NZ726208A (en) 2023-11-24
CN110483522B (zh) 2022-05-03
US10076581B2 (en) 2018-09-18
AU2019203369A1 (en) 2019-06-06
US20190201561A1 (en) 2019-07-04
RU2016147742A (ru) 2018-06-18
BR112016026443A2 (pt) 2017-08-15
MX2020010847A (es) 2021-07-16
PL3143011T3 (pl) 2021-07-19
AU2015261008A1 (en) 2016-11-17
MX384604B (es) 2025-03-14
HRP20210641T1 (hr) 2021-05-28
IL280791B1 (en) 2023-11-01
US12214058B2 (en) 2025-02-04
JP6681498B2 (ja) 2020-04-15
EP3143011A1 (en) 2017-03-22
IL248692B (en) 2020-01-30
RS61810B1 (sr) 2021-06-30
AU2019203369B2 (en) 2020-06-04
KR102530129B1 (ko) 2023-05-10
KR102618139B1 (ko) 2023-12-27
SG11201609281UA (en) 2016-12-29
US11504440B2 (en) 2022-11-22
CA2948721C (en) 2023-03-28
RU2016147742A3 (enExample) 2018-10-08
NZ764181A (en) 2023-11-24
JP6529986B2 (ja) 2019-06-12
WO2015173225A1 (en) 2015-11-19
KR20230035445A (ko) 2023-03-13
DK3143011T3 (da) 2021-05-03
EP3901145A1 (en) 2021-10-27
EP3143011B1 (en) 2021-03-03
US10675367B2 (en) 2020-06-09
AU2015261008B2 (en) 2019-02-14
CN106459059A (zh) 2017-02-22
SI3143011T1 (sl) 2021-08-31
US20160250358A1 (en) 2016-09-01
IL271631B (en) 2021-05-31

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