CN110483522B - 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 PDFInfo
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- CN110483522B CN110483522B CN201910795177.8A CN201910795177A CN110483522B CN 110483522 B CN110483522 B CN 110483522B CN 201910795177 A CN201910795177 A CN 201910795177A CN 110483522 B CN110483522 B CN 110483522B
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- 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
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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
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- 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
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- 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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- 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
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- 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
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- 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
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- 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
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- 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)
- 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)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
| CN201580025219.XA CN106459059B (zh) | 2014-05-13 | 2015-05-12 | 氘化杂环化合物和其作为成像剂的用途 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580025219.XA Division CN106459059B (zh) | 2014-05-13 | 2015-05-12 | 氘化杂环化合物和其作为成像剂的用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110483522A CN110483522A (zh) | 2019-11-22 |
| CN110483522B true CN110483522B (zh) | 2022-05-03 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910795177.8A Active CN110483522B (zh) | 2014-05-13 | 2015-05-12 | 氘化杂环化合物和其作为成像剂的用途 |
| CN201580025219.XA Active CN106459059B (zh) | 2014-05-13 | 2015-05-12 | 氘化杂环化合物和其作为成像剂的用途 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580025219.XA Active CN106459059B (zh) | 2014-05-13 | 2015-05-12 | 氘化杂环化合物和其作为成像剂的用途 |
Country Status (21)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110483522B (zh) | 2014-05-13 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 氘化杂环化合物和其作为成像剂的用途 |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110182812A1 (en) * | 2009-03-23 | 2011-07-28 | Siemens Medical Solutions Usa, Inc. | 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) |
| WO2012065963A2 (en) * | 2010-11-15 | 2012-05-24 | Katholieke Universiteit Leuven | Novel antiviral compounds |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD76515A (cg-RX-API-DMAC7.html) * | ||||
| DE76515C (de) | F. MORA in Mailand | Verfahren zur Herstellung imitirter Ledertapete aus Baumwollstoff | ||
| 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 |
| 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 |
| AU2008299921B2 (en) * | 2007-09-13 | 2012-03-01 | Concert Pharmaceuticals, Inc. | Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof |
| CA2715390A1 (en) | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Imaging agents for detecting neurological dysfunction |
| US8932557B2 (en) | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| US20100144657A1 (en) * | 2008-12-09 | 2010-06-10 | Auspex Pharmaceuticals, Inc. | PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS |
| KR101316982B1 (ko) | 2009-03-23 | 2013-10-15 | 일라이 릴리 앤드 캄파니 | 신경계 장애를 검출하기 위한 조영제 |
| KR101609504B1 (ko) * | 2012-05-22 | 2016-04-05 | 일라이 릴리 앤드 캄파니 | 신경계 기능장애를 검출하기 위한 카르볼린계 및 카르바졸계 영상화제 |
| SI3055308T1 (en) * | 2013-10-08 | 2018-03-30 | F. Hoffmann-La Roche Ag | Diazacarbazole derivatives as tau-pet-ligands |
| CN110483522B (zh) | 2014-05-13 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 氘化杂环化合物和其作为成像剂的用途 |
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2015
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
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- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
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- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
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- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
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- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
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2016
- 2016-01-26 US US15/006,997 patent/US10076581B2/en active Active
- 2016-11-01 IL IL248692A patent/IL248692B/en active IP Right Grant
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2018
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- 2019-05-14 AU AU2019203369A patent/AU2019203369B2/en active Active
- 2019-05-15 JP JP2019091813A patent/JP6681498B2/ja active Active
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2020
- 2020-06-08 US US16/895,352 patent/US11504440B2/en active Active
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2022
- 2022-11-18 US US18/056,856 patent/US12214058B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110182812A1 (en) * | 2009-03-23 | 2011-07-28 | Siemens Medical Solutions Usa, Inc. | 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) |
| WO2012065963A2 (en) * | 2010-11-15 | 2012-05-24 | Katholieke Universiteit Leuven | Novel antiviral compounds |
Non-Patent Citations (3)
| Title |
|---|
| Development of a novel fluorine-18 labeled deuterated fluororasagiline ([18F]fluororasagiline-D2) radioligand for PET studies of monoamino oxidase B (MAO-B);S. Nag等;《Bioorganic & Medicinal Chemistry》;20130815;第21卷(第22期);全文 * |
| Evaluation of Deuterated 18F- and 11C-Labeled Choline Analogs for Cancer Detection by Positron Emission Tomography;Timothy H. Witney等;《Clin Cancer Res》;20120110;第18卷(第4期);1-7 * |
| 氘代作用在药物研究中的应用;江文峰等;《齐鲁药事》;20101231;第29卷(第11期);全文 * |
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