MX376163B - Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. - Google Patents
Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes.Info
- Publication number
- MX376163B MX376163B MX2016014615A MX2016014615A MX376163B MX 376163 B MX376163 B MX 376163B MX 2016014615 A MX2016014615 A MX 2016014615A MX 2016014615 A MX2016014615 A MX 2016014615A MX 376163 B MX376163 B MX 376163B
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- sub
- imaging agents
- salts
- heterocyclic compounds
- Prior art date
Links
- 239000012216 imaging agent Substances 0.000 title abstract 2
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 3
- 208000037259 Amyloid Plaque Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002285 radioactive effect Effects 0.000 abstract 1
- 102000013498 tau Proteins Human genes 0.000 abstract 1
- 108010026424 tau Proteins Proteins 0.000 abstract 1
Classifications
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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
- 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
- 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
Landscapes
- 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)
Abstract
La presente invención se refiere a compuestos deuterados y etiquetados detectables opcionalmente de la fórmula (I): R1-A-R2 y de la fórmula (V) y las sales de los mismos, en donde R1, R2, A y X10-X19 tienen cualquiera de los valores definidos en la especificación. También se incluyen las composiciones farmacéuticas que comprenden tales compuestos y las sales, y los métodos de uso de tales compuestos y las sales como agentes formadores de imágenes, en particular en la medición de la señal radioactiva del compuesto asociado con los depósitos amiloides y/o los agregados de la proteína tau.
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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2016014615A MX2016014615A (es) | 2017-03-06 |
| MX376163B true MX376163B (es) | 2025-03-07 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020010847A MX384604B (es) | 2014-05-13 | 2015-05-12 | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
| MX2016014615A MX376163B (es) | 2014-05-13 | 2015-05-12 | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020010847A MX384604B (es) | 2014-05-13 | 2015-05-12 | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US10076581B2 (es) |
| EP (2) | EP3143011B1 (es) |
| JP (2) | JP6529986B2 (es) |
| KR (2) | KR102618139B1 (es) |
| CN (2) | CN106459059B (es) |
| AU (2) | AU2015261008B2 (es) |
| CA (1) | CA2948721C (es) |
| DK (1) | DK3143011T3 (es) |
| ES (1) | ES2867814T3 (es) |
| HR (1) | HRP20210641T1 (es) |
| HU (1) | HUE053939T2 (es) |
| IL (3) | IL280791B2 (es) |
| LT (1) | LT3143011T (es) |
| MX (2) | MX384604B (es) |
| PL (1) | PL3143011T3 (es) |
| PT (1) | PT3143011T (es) |
| RS (1) | RS61810B1 (es) |
| RU (1) | RU2696492C2 (es) |
| SG (2) | SG11201609281UA (es) |
| SI (1) | SI3143011T1 (es) |
| WO (1) | WO2015173225A1 (es) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX384604B (es) | 2014-05-13 | 2025-03-14 | Hoffmann La Roche | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
| 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 |
| SG11201811311VA (en) | 2016-07-22 | 2019-01-30 | Ac Immune Sa | 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 |
| WO2019071073A1 (en) | 2017-10-06 | 2019-04-11 | Forma Therapeutics, Inc. | INHIBITION OF THE SPECIFIC PEPTIDASE OF UBIQUITIN |
| US20210041447A1 (en) | 2018-01-24 | 2021-02-11 | 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 |
| ES2988920T3 (es) | 2018-05-17 | 2024-11-22 | Forma Therapeutics Inc | Compuestos bicíclicos fusionados útiles como inhibidores de la peptidasa 30 específica de ubiquitina |
| 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 |
| CN112996795B (zh) | 2018-09-18 | 2024-11-12 | 尼坎治疗公司 | 作为src同源-2磷酸酶抑制剂的稠合的三环衍生物 |
| HUE066335T2 (hu) | 2018-10-05 | 2024-07-28 | Annapurna Bio Inc | Vegyületek és készítmények APJ receptor aktivitáshoz kapcsolódó állapotok kezelésére |
| AU2019356011B2 (en) | 2018-10-05 | 2025-02-06 | 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 |
| WO2020227575A1 (en) * | 2019-05-09 | 2020-11-12 | Genentech, Inc. | Synthesis of labeled imidazo[1,2-a]pyrimidines |
| 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 |
| MX2024002295A (es) | 2021-08-27 | 2024-03-07 | Genentech Inc | Metodos para tratar las patologias de tau. |
| 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 |
|---|---|---|---|---|
| DD76515A (es) * | ||||
| 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 |
| UA97802C2 (uk) | 2006-03-30 | 2012-03-26 | Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания | Стирилпіридинові похідні і їх застосування для зв'язування і візуалізації амілоїдних бляшок |
| AU2008299921B2 (en) * | 2007-09-13 | 2012-03-01 | Concert Pharmaceuticals, Inc. | Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof |
| WO2009102498A1 (en) | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel 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 |
| US8691187B2 (en) * | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| CA2756137C (en) | 2009-03-23 | 2015-11-24 | 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) |
| NZ610315A (en) * | 2010-11-15 | 2015-08-28 | Univ Leuven Kath | Antiviral condensed heterocyclic compounds |
| CA2873963C (en) * | 2012-05-22 | 2017-04-11 | Eli Lilly And Company | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
| PT3055308T (pt) * | 2013-10-08 | 2018-01-18 | Hoffmann La Roche | Resumo |
| MX384604B (es) | 2014-05-13 | 2025-03-14 | Hoffmann La Roche | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
-
2015
- 2015-05-12 MX MX2020010847A patent/MX384604B/es unknown
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active Active
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es 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
- 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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Legal Events
| Date | Code | Title | Description |
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| FG | Grant or registration |