JP6529986B2 - 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 - Google Patents
重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 Download PDFInfo
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- JP6529986B2 JP6529986B2 JP2016567651A JP2016567651A JP6529986B2 JP 6529986 B2 JP6529986 B2 JP 6529986B2 JP 2016567651 A JP2016567651 A JP 2016567651A JP 2016567651 A JP2016567651 A JP 2016567651A JP 6529986 B2 JP6529986 B2 JP 6529986B2
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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
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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
-
- 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)
- 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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| 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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019091813A Division JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017515856A JP2017515856A (ja) | 2017-06-15 |
| JP2017515856A5 JP2017515856A5 (enExample) | 2018-06-14 |
| JP6529986B2 true JP6529986B2 (ja) | 2019-06-12 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567651A Active JP6529986B2 (ja) | 2014-05-13 | 2015-05-12 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
| JP2019091813A Active JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019091813A Active JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US10076581B2 (enExample) |
| EP (2) | EP3901145A1 (enExample) |
| JP (2) | JP6529986B2 (enExample) |
| KR (2) | KR102530129B1 (enExample) |
| CN (2) | CN106459059B (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) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3143011T (pt) * | 2014-05-13 | 2021-04-26 | Hoffmann La Roche | Compostos heterocíclicos deuterados e a sua utilização como agentes de imagiologia |
| MX386900B (es) | 2016-07-22 | 2025-03-19 | Ac Immune S A Star | Compuestos para formacion de imagenes de agregados de proteinas tau. |
| WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| AU2017367872B2 (en) * | 2016-11-01 | 2022-03-31 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| AU2018346597B2 (en) | 2017-10-06 | 2023-07-13 | Forma Therapeutics, Inc. | Inhibiting Ubiquitin Specific Peptidase 30 |
| EP3743423A1 (en) | 2018-01-24 | 2020-12-02 | 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 |
| EP3758696A4 (en) | 2018-03-02 | 2021-12-08 | The Trustees of the University of Pennsylvania | [1,2,4] TRIAZOLO [1,5-A] PYRIMIDINE COMPOUNDS AND USE THEREOF TO STABILIZE MICROTUBULES |
| ES2988920T3 (es) | 2018-05-17 | 2024-11-22 | Forma Therapeutics Inc | Compuestos bicíclicos fusionados útiles como inhibidores de la peptidasa 30 específica de ubiquitina |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| HRP20230409T1 (hr) | 2018-10-05 | 2023-07-07 | Forma Therapeutics, Inc. | Fuzionirani pirolini koji djeluju kao inhibitori ubikvitin specifične proteaze 30 (usp30) |
| ES2976515T3 (es) | 2018-10-05 | 2024-08-02 | Annapurna Bio Inc | Compuestos y composiciones para tratar afecciones asociadas con la actividad del 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 |
| TWI804079B (zh) | 2019-05-09 | 2023-06-01 | 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 |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 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 |
| 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 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE76515C (de) | F. MORA in Mailand | Verfahren zur Herstellung imitirter Ledertapete aus Baumwollstoff | ||
| DD76515A (enExample) * | ||||
| 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 |
| BRPI0710225B1 (pt) | 2006-03-30 | 2021-07-13 | The Trustees Of The University Of Pennsylvania | Derivados e composições de estirilpiridina compreendendo os mesmos |
| CN101855218A (zh) | 2007-09-13 | 2010-10-06 | 康塞特医药品有限公司 | 氘化的儿茶酚和苯并[d][1,3]间二氧杂环戊烯及其衍生物的合成 |
| KR20100135235A (ko) | 2008-02-14 | 2010-12-24 | 지멘스 메디컬 솔루션즈 유에스에이, 인크. | 신경학적 기능이상을 검출하기 위한 조영제 |
| 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 |
| US8691187B2 (en) | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| CN102438660A (zh) | 2009-03-23 | 2012-05-02 | 美国西门子医疗解决公司 | 用于检测神经障碍的显像剂 |
| 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) |
| MX2013005478A (es) * | 2010-11-15 | 2013-08-29 | Univ Leuven Kath | Compuestos heterociclicos condensados antivirales. |
| KR101609504B1 (ko) * | 2012-05-22 | 2016-04-05 | 일라이 릴리 앤드 캄파니 | 신경계 기능장애를 검출하기 위한 카르볼린계 및 카르바졸계 영상화제 |
| NO3055308T3 (enExample) * | 2013-10-08 | 2018-04-21 | ||
| PT3143011T (pt) | 2014-05-13 | 2021-04-26 | Hoffmann La Roche | Compostos heterocíclicos deuterados e a sua utilização como agentes de imagiologia |
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2015
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 MX MX2020010847A patent/MX384604B/es unknown
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active Active
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
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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
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