ES2867814T3 - Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes - Google Patents

Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes Download PDF

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Publication number
ES2867814T3
ES2867814T3 ES15725253T ES15725253T ES2867814T3 ES 2867814 T3 ES2867814 T3 ES 2867814T3 ES 15725253 T ES15725253 T ES 15725253T ES 15725253 T ES15725253 T ES 15725253T ES 2867814 T3 ES2867814 T3 ES 2867814T3
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compound
pharmaceutically acceptable
acceptable salt
individual
deuterated
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ES15725253T
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English (en)
Spanish (es)
Inventor
Jan Marik
Joseph P Lyssikatos
Simon Williams
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F Hoffmann La Roche AG
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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
    • 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
    • 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
    • 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)
  • 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)
ES15725253T 2014-05-13 2015-05-12 Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes Active ES2867814T3 (es)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
ES2867814T3 true ES2867814T3 (es) 2021-10-20

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
ES15725253T Active ES2867814T3 (es) 2014-05-13 2015-05-12 Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes

Country Status (21)

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US (4) US10076581B2 (enExample)
EP (2) EP3901145A1 (enExample)
JP (2) JP6529986B2 (enExample)
KR (2) KR102530129B1 (enExample)
CN (2) CN110483522B (enExample)
AU (2) AU2015261008B2 (enExample)
CA (1) CA2948721C (enExample)
DK (1) DK3143011T3 (enExample)
ES (1) ES2867814T3 (enExample)
HR (1) HRP20210641T1 (enExample)
HU (1) HUE053939T2 (enExample)
IL (3) IL280791B2 (enExample)
LT (1) LT3143011T (enExample)
MX (2) MX384604B (enExample)
PL (1) PL3143011T3 (enExample)
PT (1) PT3143011T (enExample)
RS (1) RS61810B1 (enExample)
RU (1) RU2696492C2 (enExample)
SG (2) SG10201805628TA (enExample)
SI (1) SI3143011T1 (enExample)
WO (1) WO2015173225A1 (enExample)

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CA2948721C (en) * 2014-05-13 2023-03-28 F. Hoffmann-La Roche Ag Deuterated compounds and uses thereof
JP7197476B2 (ja) 2016-07-22 2022-12-27 エーシー・イミューン・エス・アー タウタンパク質凝集体を画像化するための化合物
JP7059270B2 (ja) 2016-07-22 2022-04-25 エーシー・イミューン・エス・アー タウタンパク質凝集体を画像化するための化合物
JP7286539B2 (ja) * 2016-11-01 2023-06-05 アルビナス・オペレーションズ・インコーポレイテッド タウタンパク質標的化protac、および関連使用方法
CA3072362A1 (en) 2017-10-06 2019-04-11 Forma Therapeutics, Inc. Inhibiting ubiquitin specific peptidase 30
WO2019145292A1 (en) 2018-01-24 2019-08-01 Ac Immune Sa Azacarboline compounds for the detection of tau aggregates
US11306089B2 (en) 2018-01-24 2022-04-19 Life Molecular Imaging Limited Gamma-carboline compounds for the detection of Tau aggregates
US11623927B2 (en) 2018-03-02 2023-04-11 The Trustees Of The University Of Pennsylvania Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules
SG11202011299PA (en) 2018-05-17 2020-12-30 Forma Therapeutics Inc Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
WO2020041331A1 (en) 2018-08-20 2020-02-27 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
RS65335B1 (sr) 2018-10-05 2024-04-30 Annapurna Bio Inc Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj
MY209034A (en) 2018-10-05 2025-06-17 Forma Therapeutics Inc Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
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
CN114423763B (zh) * 2019-05-09 2025-01-21 豪夫迈·罗氏有限公司 咪唑并[1,2-a]嘧啶的区域选择性合成
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
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
CA3228359A1 (en) 2021-08-27 2023-03-02 Genentech, Inc. Methods of treating tau pathologies
EP4536358A1 (en) 2022-06-13 2025-04-16 Genentech Inc. Methods of delaying or preventing the onset of alzheimer's disease using crenezumab
WO2025155625A1 (en) * 2024-01-16 2025-07-24 Eli Lilly And Company Novel compounds for tau imaging
CN118957609B (zh) * 2024-07-23 2025-09-09 无锡绿能电合科技有限公司 一种氟代芳环的氘代方法

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DE76515C (de) F. MORA in Mailand Verfahren zur Herstellung imitirter Ledertapete aus Baumwollstoff
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EP1340759A1 (en) * 2002-02-28 2003-09-03 Sanofi-Synthelabo 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-(pyrimidin-4-yl)-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
US6875784B2 (en) 2002-10-09 2005-04-05 Pharmacia & Upjohn Company Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives
HUE032660T2 (en) * 2006-03-30 2017-10-30 Univ Pennsylvania Styrylpyridine derivatives and their use for binding and imaging amyloid plaques
JP5647519B2 (ja) 2007-09-13 2014-12-24 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化カテコールおよびベンゾ[d][1,3]ジオキソールおよびその誘導体の合成
SI2247558T2 (sl) 2008-02-14 2024-10-30 Eli Lilly And Company Nova kontrastna sredstva za zaznavanje nevroloških disfunkcij
US8932557B2 (en) 2008-02-14 2015-01-13 Eli Lilly And Company Imaging agents for detecting neurological dysfunction
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US8691187B2 (en) * 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
US8491869B2 (en) 2009-03-23 2013-07-23 Eli Lilly And Company Imaging agents for detecting neurological disorders
EP2450332A1 (en) 2010-10-22 2012-05-09 Bayer Pharma Aktiengesellschaft Compounds for use in Imaging, diagnosing and/or treatment of diseases of the central nervous system (F-D2-Deprenyl)
NZ610315A (en) * 2010-11-15 2015-08-28 Univ Leuven Kath Antiviral condensed heterocyclic compounds
WO2013176698A1 (en) * 2012-05-22 2013-11-28 Eli Lilly And Company Carboline and carbazole based imaging agents for detecting neurological dysfunction
CN105358558B (zh) * 2013-10-08 2017-09-26 豪夫迈·罗氏有限公司 作为tau‑pet‑配体的二氮杂咔唑衍生物
CA2948721C (en) 2014-05-13 2023-03-28 F. Hoffmann-La Roche Ag Deuterated compounds and uses thereof

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Publication number Publication date
AU2019203369B2 (en) 2020-06-04
IL271631B (en) 2021-05-31
JP6681498B2 (ja) 2020-04-15
NZ764181A (en) 2023-11-24
US20230218782A1 (en) 2023-07-13
JP2019147825A (ja) 2019-09-05
US10675367B2 (en) 2020-06-09
CN110483522B (zh) 2022-05-03
PT3143011T (pt) 2021-04-26
AU2015261008B2 (en) 2019-02-14
MX2016014615A (es) 2017-03-06
US11504440B2 (en) 2022-11-22
RS61810B1 (sr) 2021-06-30
US20160250358A1 (en) 2016-09-01
DK3143011T3 (da) 2021-05-03
LT3143011T (lt) 2021-05-10
US20200297875A1 (en) 2020-09-24
MX384604B (es) 2025-03-14
KR20230035445A (ko) 2023-03-13
IL280791B2 (en) 2024-03-01
WO2015173225A1 (en) 2015-11-19
US12214058B2 (en) 2025-02-04
KR20170002639A (ko) 2017-01-06
RU2016147742A3 (enExample) 2018-10-08
JP6529986B2 (ja) 2019-06-12
US20190201561A1 (en) 2019-07-04
NZ726208A (en) 2023-11-24
CN110483522A (zh) 2019-11-22
BR112016026443A2 (pt) 2017-08-15
IL248692A0 (en) 2017-01-31
EP3901145A1 (en) 2021-10-27
PL3143011T3 (pl) 2021-07-19
CN106459059B (zh) 2019-09-24
MX376163B (es) 2025-03-07
SG11201609281UA (en) 2016-12-29
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
CA2948721C (en) 2023-03-28
CN106459059A (zh) 2017-02-22
EP3143011A1 (en) 2017-03-22
EP3143011B1 (en) 2021-03-03
BR112016026443A8 (pt) 2021-07-06
IL280791A (en) 2021-04-29
KR102618139B1 (ko) 2023-12-27
HUE053939T2 (hu) 2021-08-30
IL271631A (en) 2020-02-27
AU2015261008A1 (en) 2016-11-17
IL280791B1 (en) 2023-11-01
SI3143011T1 (sl) 2021-08-31
US10076581B2 (en) 2018-09-18
AU2019203369A1 (en) 2019-06-06
IL248692B (en) 2020-01-30
MX2020010847A (es) 2021-07-16
CA2948721A1 (en) 2015-11-19
RU2016147742A (ru) 2018-06-18
HRP20210641T1 (hr) 2021-05-28
JP2017515856A (ja) 2017-06-15
KR102530129B1 (ko) 2023-05-10

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