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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (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)
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) | EP3901145A1 (es) |
| JP (2) | JP6529986B2 (es) |
| KR (2) | KR102618139B1 (es) |
| CN (2) | CN110483522B (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) | SG11201609281UA (es) |
| SI (1) | SI3143011T1 (es) |
| WO (1) | WO2015173225A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2016014615A (es) | 2014-05-13 | 2017-03-06 | Hoffmann La Roche | Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes. |
| WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| SG11201811311VA (en) | 2016-07-22 | 2019-01-30 | 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 |
| WO2019071073A1 (en) | 2017-10-06 | 2019-04-11 | Forma Therapeutics, Inc. | INHIBITION OF THE SPECIFIC PEPTIDASE OF UBIQUITIN |
| EP3743423A1 (en) | 2018-01-24 | 2020-12-02 | AC Immune SA | 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 |
| 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 |
| MX2021003158A (es) | 2018-09-18 | 2021-07-16 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2. |
| DK3860989T3 (da) | 2018-10-05 | 2023-05-01 | Forma Therapeutics Inc | Kondenserede pyrroliner der fungerer som inhibitorer af ubiquitin-specifik protease 30 (usp30) |
| KR20210125471A (ko) | 2018-10-05 | 2021-10-18 | 안나푸르나 바이오, 인코포레이티드 | Apj 수용체 활성과 관련된 병태를 치료하기 위한 화합물 및 조성물 |
| 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 |
| JP7369208B2 (ja) * | 2019-05-09 | 2023-10-25 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 標識されたイミダゾ［１，２－ａ］ピリミジンの合成 |
| 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 |
| TW202328177A (zh) | 2021-08-27 | 2023-07-16 | 美商建南德克公司 | 治療ｔａｕ病理學之方法 |
| 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 |
|---|---|---|---|---|
| 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 |
| SI1999109T1 (sl) | 2006-03-30 | 2012-04-30 | Univ Pennsylvania | Derivati stirilpiridina in njihova uporaba za vezavo in prikazovanje amiloidnih plakov |
| EP2200997B9 (en) * | 2007-09-13 | 2016-01-13 | Concert Pharmaceuticals Inc. | Synthesis of deuterated benzodioxoles |
| US8318132B2 (en) | 2008-02-14 | 2012-11-27 | 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 |
| US8691187B2 (en) | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| JP2012521988A (ja) | 2009-03-23 | 2012-09-20 | シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド | 神経学的障害を検知するためのイメージング剤 |
| 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) |
| AU2011331301A1 (en) * | 2010-11-15 | 2013-05-23 | Katholieke Universiteit Leuven | 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 |
| PE20160159A1 (es) * | 2013-10-08 | 2016-03-18 | Hoffmann La Roche | Derivados de diazacarbazol como ligandos de tau para pet |
| MX2016014615A (es) | 2014-05-13 | 2017-03-06 | Hoffmann La Roche | Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes. |
-
2015
- 2015-05-12 MX MX2016014615A patent/MX2016014615A/es active IP Right Grant
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active IP Right Grant
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 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 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en active Application Filing
- 2015-05-12 MX MX2020010847A patent/MX2020010847A/es unknown
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh 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
-
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 |