MX2016014615A - Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes. - Google Patents
Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes.Info
- Publication number
- MX2016014615A MX2016014615A MX2016014615A MX2016014615A MX2016014615A MX 2016014615 A MX2016014615 A MX 2016014615A MX 2016014615 A MX2016014615 A MX 2016014615A MX 2016014615 A MX2016014615 A MX 2016014615A MX 2016014615 A MX2016014615 A MX 2016014615A
- Authority
- MX
- Mexico
- Prior art keywords
- imaging agents
- heterocyclic compounds
- salts
- compounds
- deuterated
- 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
-
- 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
-
- 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)
- 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)
- 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 (1)
| Publication Number | Publication Date |
|---|---|
| MX2016014615A true MX2016014615A (es) | 2017-03-06 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016014615A MX2016014615A (es) | 2014-05-13 | 2015-05-12 | Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes. |
| MX2020010847A MX2020010847A (es) | 2014-05-13 | 2015-05-12 | Compuestos heterocíclicos deuterados y su uso como agentes formadores de imágenes. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020010847A MX2020010847A (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) | KR102530129B1 (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) | MX2016014615A (es) |
| PL (1) | PL3143011T3 (es) |
| PT (1) | PT3143011T (es) |
| RS (1) | RS61810B1 (es) |
| RU (1) | RU2696492C2 (es) |
| SG (2) | SG10201805628TA (es) |
| SI (1) | SI3143011T1 (es) |
| WO (1) | WO2015173225A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2696492C2 (ru) | 2014-05-13 | 2019-08-02 | Ф. Хоффманн-Ля Рош Аг | Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации |
| 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 |
| AU2017299219B2 (en) | 2016-07-22 | 2022-12-22 | Ac Immune Sa | Compounds for imaging Tau protein aggregates |
| IL290809B2 (en) | 2016-11-01 | 2024-01-01 | Arvinas Operations Inc | PROTACS Targeted Tau-Protein and Related Methods of Use |
| MX2020003671A (es) | 2017-10-06 | 2020-08-03 | Forma Therapeutics Inc | Inhibicion de peptidasa especifica de ubiquitina 30. |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| US20210041447A1 (en) | 2018-01-24 | 2021-02-11 | 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 OF THESE IN THE STABILIZATION OF MICROTUBULES |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| CA3113233A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| AU2019353144B2 (en) | 2018-10-05 | 2023-11-16 | Annapurna Bio, Inc. | Compounds and compositions for treating conditions associated with APJ receptor activity |
| LT3860989T (lt) | 2018-10-05 | 2023-06-12 | Forma Therapeutics, Inc. | Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai |
| 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 |
| EP3966216A1 (en) * | 2019-05-09 | 2022-03-16 | F. Hoffmann-La Roche AG | Regio-selective synthesis of imidazo[1,2-a]pyrimidines |
| JP2022540935A (ja) | 2019-07-17 | 2022-09-20 | 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化合物および関連する使用方法 |
| 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 |
| WO2023245008A1 (en) | 2022-06-13 | 2023-12-21 | Genentech, Inc. | Methods of delaying or preventing the onset of alzheimer's disease using crenezumab |
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 (es) * | ||||
| 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 |
| PL2363392T3 (pl) * | 2006-03-30 | 2017-10-31 | Univ Pennsylvania | Styrylopirydynowe pochodne i ich zastosowanie do wiązania i obrazowania płytek amyloidowych |
| 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 |
| EP2599763A1 (en) | 2008-02-14 | 2013-06-05 | Siemens Molecular Imaging, 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 |
| KR101316982B1 (ko) | 2009-03-23 | 2013-10-15 | 일라이 릴리 앤드 캄파니 | 신경계 장애를 검출하기 위한 조영제 |
| US8691187B2 (en) | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | 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) |
| US9132129B2 (en) * | 2010-11-15 | 2015-09-15 | Katholieke Universiteit Leuven | Antiviral compounds |
| WO2013176698A1 (en) * | 2012-05-22 | 2013-11-28 | Eli Lilly And Company | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
| SG11201602786UA (en) * | 2013-10-08 | 2016-05-30 | Hoffmann La Roche | Diazacarbazole derivatives as tau-pet-ligands |
| RU2696492C2 (ru) | 2014-05-13 | 2019-08-02 | Ф. Хоффманн-Ля Рош Аг | Дейтрированные гетероциклические соединения и их применение в качестве средств визуализации |
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2015
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en active Application Filing
- 2015-05-12 MX MX2016014615A patent/MX2016014615A/es active IP Right Grant
- 2015-05-12 MX MX2020010847A patent/MX2020010847A/es unknown
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active IP Right Grant
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active IP Right Grant
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt 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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2021
- 2021-04-22 HR HRP20210641TT patent/HRP20210641T1/hr unknown
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2022
- 2022-11-18 US US18/056,856 patent/US20230218782A1/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |