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
-
- 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
-
- 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
-
- 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
- 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (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)
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)
| Country | Link |
|---|---|
| US (4) | US10076581B2 (enExample) |
| EP (2) | EP3143011B1 (enExample) |
| JP (2) | JP6529986B2 (enExample) |
| KR (2) | KR102618139B1 (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) | MX376163B (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) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3143011T (lt) | 2014-05-13 | 2021-05-10 | F. Hoffmann-La Roche Ag | Deuterinti heterocikliniai junginiai ir jų naudojimas kaip vaizdinimo agentų |
| WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| MY196981A (en) | 2016-07-22 | 2023-05-16 | Ac Immune Sa | Compounds for imaging tau protein aggregates |
| EP3535265A4 (en) * | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| BR112020003725A2 (pt) | 2017-10-06 | 2020-11-03 | Forma Therapeutics, Inc. | inibição da peptidase 30 específica de ubiquitina |
| WO2019145292A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Azacarboline compounds for the detection of tau aggregates |
| WO2019145291A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Gamma-carboline compounds for the detection of tau aggregates |
| WO2019169111A1 (en) | 2018-03-02 | 2019-09-06 | The Trustees Of The University Of Pennsylvania | [1,2,4]triazolo[1,5-a]pyrimidine compounds and use in stabilizing microtubules |
| CN112513036B (zh) | 2018-05-17 | 2024-05-24 | 福马治疗有限公司 | 用作泛素特异性肽酶30抑制剂的稠合双环化合物 |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| EP3853234B1 (en) | 2018-09-18 | 2025-04-23 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| CA3110113A1 (en) | 2018-10-05 | 2020-04-09 | Forma Therapeutics, Inc. | Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors |
| IL316875A (en) | 2018-10-05 | 2025-01-01 | Annapurna Bio Inc | Compounds and compositions for treating conditions associated with APJ receptor activity |
| 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 |
| TWI751548B (zh) * | 2019-05-09 | 2022-01-01 | 瑞士商赫孚孟拉羅股份公司 | 經標記之咪唑并[1,2-a]嘧啶之合成 |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| 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 |
| IL310382A (en) | 2021-08-27 | 2024-03-01 | Genentech Inc | Methods for treating tau pathologies |
| CN120187452A (zh) | 2022-06-13 | 2025-06-20 | 基因泰克公司 | 使用克瑞尼珠单抗延迟或预防阿尔茨海默病的发作的方法 |
| 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 (enExample) * | ||||
| 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 |
| CN101522624B (zh) * | 2006-03-30 | 2013-11-06 | 宾夕法尼亚大学理事会 | 苯乙烯基吡啶衍生物及其用于结合和成像淀粉样蛋白斑的用途 |
| EP2727915B1 (en) | 2007-09-13 | 2016-04-13 | Concert Pharmaceuticals Inc. | Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof |
| US8932557B2 (en) | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| LT2247558T (lt) | 2008-02-14 | 2022-04-11 | Eli Lilly And Company | Nauji vizualizavimo agentai neurologinės disfunkcijos aptikimui |
| US20100144657A1 (en) | 2008-12-09 | 2010-06-10 | Auspex Pharmaceuticals, Inc. | PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS |
| ES2797523T3 (es) | 2009-03-23 | 2020-12-02 | Lilly Co Eli | Agentes de obtención de imagen para detectar trastornos neurológicos |
| ES2792830T3 (es) * | 2012-05-22 | 2020-11-12 | Lilly Co Eli | Agentes para formación de imagen en base a carbolina y carbazol, para la detección de disfunción neurológica |
| 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 |
| LT3143011T (lt) | 2014-05-13 | 2021-05-10 | F. Hoffmann-La Roche Ag | Deuterinti heterocikliniai junginiai ir jų naudojimas kaip vaizdinimo agentų |
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2015
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active Active
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 MX MX2020010847A patent/MX384604B/es unknown
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru 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
- 2018-07-31 US US16/050,453 patent/US10675367B2/en active Active
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2019
- 2019-05-14 AU AU2019203369A patent/AU2019203369B2/en active Active
- 2019-05-15 JP JP2019091813A patent/JP6681498B2/ja active Active
- 2019-12-22 IL IL271631A patent/IL271631B/en active IP Right Grant
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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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