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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (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)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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

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Family Applications (1)

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ES15725253T Active ES2867814T3 (es) 2014-05-13 2015-05-12 Compuestos heterocíclicos deuterados y su uso como agentes de formación de imágenes

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US (4) US10076581B2 (cg-RX-API-DMAC7.html)
EP (2) EP3143011B1 (cg-RX-API-DMAC7.html)
JP (2) JP6529986B2 (cg-RX-API-DMAC7.html)
KR (2) KR102618139B1 (cg-RX-API-DMAC7.html)
CN (2) CN110483522B (cg-RX-API-DMAC7.html)
AU (2) AU2015261008B2 (cg-RX-API-DMAC7.html)
CA (1) CA2948721C (cg-RX-API-DMAC7.html)
DK (1) DK3143011T3 (cg-RX-API-DMAC7.html)
ES (1) ES2867814T3 (cg-RX-API-DMAC7.html)
HR (1) HRP20210641T1 (cg-RX-API-DMAC7.html)
HU (1) HUE053939T2 (cg-RX-API-DMAC7.html)
IL (3) IL280791B2 (cg-RX-API-DMAC7.html)
LT (1) LT3143011T (cg-RX-API-DMAC7.html)
MX (2) MX384604B (cg-RX-API-DMAC7.html)
PL (1) PL3143011T3 (cg-RX-API-DMAC7.html)
PT (1) PT3143011T (cg-RX-API-DMAC7.html)
RS (1) RS61810B1 (cg-RX-API-DMAC7.html)
RU (1) RU2696492C2 (cg-RX-API-DMAC7.html)
SG (2) SG10201805628TA (cg-RX-API-DMAC7.html)
SI (1) SI3143011T1 (cg-RX-API-DMAC7.html)
WO (1) WO2015173225A1 (cg-RX-API-DMAC7.html)

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WO2018015549A1 (en) 2016-07-22 2018-01-25 Ac Immune S.A. Compounds for imaging tau protein aggregates
US10865207B2 (en) 2016-07-22 2020-12-15 Ac Immune S.A. Compounds for imaging Tau protein aggregates
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
KR102717600B1 (ko) 2017-10-06 2024-10-15 포르마 세라퓨틱스 인크. 유비퀴틴 특이적 펩티다제 30의 억제
WO2019145291A1 (en) 2018-01-24 2019-08-01 Ac Immune Sa Gamma-carboline compounds for the detection of tau aggregates
EP3743426A1 (en) 2018-01-24 2020-12-02 AC Immune SA Azacarboline 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
CA3098628A1 (en) 2018-05-17 2019-11-21 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
WO2020061101A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
PT3860989T (pt) 2018-10-05 2023-06-30 Forma Therapeutics Inc Pirrolinas fundidas que atuam como inibidores da protease 30 específica da ubiquitina (usp30)
BR112021006488A2 (pt) 2018-10-05 2021-07-06 Annapurna Bio Inc compostos e composições para o tratamento de condições associadas com atividade do receptor apj
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
CA3138873C (en) * 2019-05-09 2024-01-09 Kyle Bradley Pascual CLAGG Synthesis of labeled imidazo[1,2-a]pyrimidines
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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US6875784B2 (en) 2002-10-09 2005-04-05 Pharmacia & Upjohn Company Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives
SI2363392T1 (sl) 2006-03-30 2017-09-29 The Trustees Of The University Of Pennsylvania Center For Technology Transfer Derivati stirilpiridina in njihova uporaba za vezavo in prikazovanje amiloidnih plakov
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MX2020010847A (es) 2021-07-16
KR102530129B1 (ko) 2023-05-10
US10076581B2 (en) 2018-09-18
LT3143011T (lt) 2021-05-10
HUE053939T2 (hu) 2021-08-30
IL271631A (en) 2020-02-27
RU2016147742A (ru) 2018-06-18
HRP20210641T1 (hr) 2021-05-28
CN106459059A (zh) 2017-02-22
CA2948721C (en) 2023-03-28
RU2016147742A3 (cg-RX-API-DMAC7.html) 2018-10-08
AU2019203369A1 (en) 2019-06-06
CA2948721A1 (en) 2015-11-19
US20200297875A1 (en) 2020-09-24
IL280791A (en) 2021-04-29
KR102618139B1 (ko) 2023-12-27
WO2015173225A1 (en) 2015-11-19
IL280791B1 (en) 2023-11-01
IL248692A0 (en) 2017-01-31
US20160250358A1 (en) 2016-09-01
JP6681498B2 (ja) 2020-04-15
AU2015261008A1 (en) 2016-11-17
RU2696492C2 (ru) 2019-08-02
SG10201805628TA (en) 2018-08-30
PT3143011T (pt) 2021-04-26
PL3143011T3 (pl) 2021-07-19
MX376163B (es) 2025-03-07
AU2015261008B2 (en) 2019-02-14
SG11201609281UA (en) 2016-12-29
US10675367B2 (en) 2020-06-09
US11504440B2 (en) 2022-11-22
BR112016026443A2 (pt) 2017-08-15
NZ764181A (en) 2023-11-24
US20230218782A1 (en) 2023-07-13
US12214058B2 (en) 2025-02-04
MX2016014615A (es) 2017-03-06
AU2019203369B2 (en) 2020-06-04
JP2019147825A (ja) 2019-09-05
CN110483522B (zh) 2022-05-03
DK3143011T3 (da) 2021-05-03
IL248692B (en) 2020-01-30
US20190201561A1 (en) 2019-07-04
BR112016026443A8 (pt) 2021-07-06
JP6529986B2 (ja) 2019-06-12
IL280791B2 (en) 2024-03-01
MX384604B (es) 2025-03-14
CN110483522A (zh) 2019-11-22
RS61810B1 (sr) 2021-06-30
EP3143011A1 (en) 2017-03-22
CN106459059B (zh) 2019-09-24
SI3143011T1 (sl) 2021-08-31
EP3901145A1 (en) 2021-10-27
EP3143011B1 (en) 2021-03-03
KR20230035445A (ko) 2023-03-13
KR20170002639A (ko) 2017-01-06
IL271631B (en) 2021-05-31
NZ726208A (en) 2023-11-24
JP2017515856A (ja) 2017-06-15

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