RU2016112547A - Имидазо[1,2-а]пиридин-7-амины в качестве средств визуализации - Google Patents
Имидазо[1,2-а]пиридин-7-амины в качестве средств визуализации Download PDFInfo
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- RU2016112547A RU2016112547A RU2016112547A RU2016112547A RU2016112547A RU 2016112547 A RU2016112547 A RU 2016112547A RU 2016112547 A RU2016112547 A RU 2016112547A RU 2016112547 A RU2016112547 A RU 2016112547A RU 2016112547 A RU2016112547 A RU 2016112547A
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- imidazo
- pyridin
- amine
- tau protein
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
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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
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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
- A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/52—Use of compounds or compositions for colorimetric, spectrophotometric or fluorometric investigation, e.g. use of reagent paper and including single- and multilayer analytical elements
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Physics & Mathematics (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biochemistry (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Microbiology (AREA)
- Cell Biology (AREA)
- Food Science & Technology (AREA)
- Biotechnology (AREA)
- Analytical Chemistry (AREA)
- Optics & Photonics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (27)
1. Соединение формулы
где R1 представляет собой низший алкил или низший алкил, замещенный галогеном;
R2, R3 представляет собой водород или тритий;
или его фармацевтически приемлемая кислотно-аддитивная соль.
2. Соединение формулы I по п. 1, где R1 представляет собой низший алкил, a R2 и R3 являются такими, как определено в п. 1.
3. Соединение формулы I по п. 1, где R1 представляет собой низший алкил, замещенный галогеном, a R2 и R3 являются такими, как определено в п. 1.
4. Соединение формулы I по п. 1, где R2 и R3 представляют собой тритий, а R1 является таким, как определено в п. 1.
5. Соединение, выбранное из:
2-(4-метоксифенил)имидазо[1,2-а]пиридин-7-амин
[3Н]-2-(4-метоксифенил)имидазо[1,2-а]пиридин-7-амин
2-(4-(фторметокси)фенил)имидазо[1,2-а]пиридин-7-амин
2-[4-(3-фторпропокси)фенил]имидазо[1,2-а]пиридин-7-амин
2-[4-(2-фторэтокси)фенил]имидазо[1,2-а]пиридин-7-амин
[3Н]-2-[4-(2-фторэтокси)фенил]имидазо[1,2-а]пиридин-7-амин
[3Н]-2-(4-метоксифенил)имидазо[1,2-а]пиридин-7-амин
[3Н]-2-[4-(2-фторэтокси)фенил]имидазо[1,2-а]пиридин-7-амин.
6. Соединение по любому из пп. 1-5 для применения для связывания и визуализации агрегатов белка tau, агрегатов бета-амилоида или агрегатов альфа-синуклеина.
7. Соединение по любому из пп. 1-5 для применения для связывания и визуализации агрегатов белка tau у пациентов с болезнью Альцгеймера.
8. Соединение по любому из пп. 1-5 для применения в исследованиях, включающих связывание белка tau.
9. Соединение по любому из пп. 1-5 для применения в диагностической визуализации агрегатов белка tau в мозге млекопитающих.
10. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-5 и фармацевтически приемлемый носитель.
11. Способ визуализации отложений агрегатов белка tau, содержащий
- введение млекопитающему детектируемого количества композиции по п. 10;
- выдержку в течение времени, достаточного для связывания соединения формулы I с отложениями агрегатов белка tau, и
- детекцию соединения, связанного с одним или более отложениями агрегатов белка tau.
12. Применение соединения по любому из пп. 1-5 для диагностической визуализации отложений агрегатов белка tau в мозге млекопитающих.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13186074.4 | 2013-09-26 | ||
| EP13186074 | 2013-09-26 | ||
| PCT/EP2014/070162 WO2015044095A1 (en) | 2013-09-26 | 2014-09-23 | Imidazo[1,2-a]pyridin-7-amines as imaging tools |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016112547A true RU2016112547A (ru) | 2017-10-31 |
| RU2016112547A3 RU2016112547A3 (ru) | 2018-05-25 |
| RU2671506C2 RU2671506C2 (ru) | 2018-11-01 |
Family
ID=49230646
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016112547A RU2671506C2 (ru) | 2013-09-26 | 2014-09-23 | Имидазо[1,2-а]пиридин-7-амины в качестве средств визуализации |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9957266B2 (ru) |
| EP (1) | EP3049411B1 (ru) |
| JP (1) | JP6182668B2 (ru) |
| KR (1) | KR101770532B1 (ru) |
| CN (1) | CN105579453B (ru) |
| AR (1) | AR097739A1 (ru) |
| CA (1) | CA2920068A1 (ru) |
| HK (1) | HK1220201A1 (ru) |
| MX (1) | MX2016003422A (ru) |
| RU (1) | RU2671506C2 (ru) |
| TW (1) | TWI518087B (ru) |
| WO (1) | WO2015044095A1 (ru) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2991983T3 (pl) * | 2013-04-29 | 2017-07-31 | F.Hoffmann-La Roche Ag | Pochodne 2-fenylo lub 2-hetaryloimidazolo[1,2-a]pirydyny |
| SI3197277T1 (sl) | 2014-08-29 | 2022-04-29 | Chdi Foundation, Inc. | Sonde za slikanje proteina huntingtina |
| CN109475648B (zh) | 2016-07-22 | 2023-03-14 | Ac免疫有限公司 | 用于成像tau蛋白聚集体的化合物 |
| US10865207B2 (en) | 2016-07-22 | 2020-12-15 | Ac Immune S.A. | Compounds for imaging Tau protein aggregates |
| JP7260521B2 (ja) * | 2017-07-12 | 2023-04-18 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | タウタンパク質分解の化合物 |
| 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 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA62972C2 (en) * | 1997-07-03 | 2004-01-15 | Application of imidazopyrimidins and imidazopyridins for the treatment of neural disorders | |
| GB9927687D0 (en) * | 1999-11-23 | 2000-01-19 | Merck Sharp & Dohme | Therapeutic agents |
| ES2536449T3 (es) | 2000-08-24 | 2015-05-25 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Derivados de tioflavina para uso en diagnosis de la enfermedad de Alzheimer |
| CN100422180C (zh) * | 2001-04-23 | 2008-10-01 | 宾夕法尼亚州大学理事会 | 淀粉样斑块聚集抑制剂和诊断成像剂 |
| ES2435070T3 (es) | 2001-08-27 | 2013-12-18 | The Trustees Of The University Of Pennsylvania | Derivados de estilbeno y su uso para unión y formación de imágenes de placas amiloides |
| CN102532055B (zh) * | 2003-03-14 | 2016-05-11 | 匹兹堡大学联邦制高等教育 | 苯并噻唑衍生物化合物、组合物及用途 |
| CA2438032C (en) * | 2003-03-14 | 2013-05-07 | University Of Pittsburgh | Benzothiazole derivative compounds, compositions and uses |
| AU2006261917A1 (en) * | 2005-06-24 | 2007-01-04 | The Trustees Of The University Of Pennsylvania | Radiolabeled-pegylation of ligands for use as imaging agents |
| JP4738419B2 (ja) | 2005-11-30 | 2011-08-03 | 富士フイルムＲｉファーマ株式会社 | アミロイドの凝集及び／又は沈着に起因する疾患の診断薬及び治療薬 |
| EP2023919A4 (en) * | 2006-05-08 | 2010-12-22 | Molecular Neuroimaging Llc | COMPOUNDS AND AMYLOID PROBES FOR THERAPY AND IMAGING USES |
| BRPI0806621A2 (pt) * | 2007-01-22 | 2011-09-13 | Astrazeneca Ab | composto, uso de um composto, composição farmacêutica, e, método in vivo para medir depósitos amilóides em um indivìduo |
| US20100272642A1 (en) * | 2007-07-04 | 2010-10-28 | Tohoku University | Pet probe having an alkoxy group substituted by fluorine and hydroxy group |
| US20100267952A1 (en) * | 2007-10-30 | 2010-10-21 | Nihon Medi-Physics Co., Ltd. | Use of novel compound having affinity for amyloid, and process for production of the same |
| RU2518892C2 (ru) * | 2008-09-23 | 2014-06-10 | Виста Лабораториз Лтд. | Лиганды для агрегированных молекул тау-белка |
| US8691187B2 (en) * | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| JP5629322B2 (ja) * | 2009-09-24 | 2014-11-19 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ホスホジエステラーゼ１０ａ阻害剤としてのイミダゾピリジンまたはイミダゾピリミジン誘導体 |
| US8410117B2 (en) * | 2010-03-26 | 2013-04-02 | Hoffmann-La Roche Inc. | Imidazopyrimidine derivatives |
| PL2991983T3 (pl) | 2013-04-29 | 2017-07-31 | F.Hoffmann-La Roche Ag | Pochodne 2-fenylo lub 2-hetaryloimidazolo[1,2-a]pirydyny |
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2014
- 2014-09-23 EP EP14771582.5A patent/EP3049411B1/en active Active
- 2014-09-23 RU RU2016112547A patent/RU2671506C2/ru not_active IP Right Cessation
- 2014-09-23 CA CA2920068A patent/CA2920068A1/en not_active Abandoned
- 2014-09-23 JP JP2016517347A patent/JP6182668B2/ja active Active
- 2014-09-23 WO PCT/EP2014/070162 patent/WO2015044095A1/en active Application Filing
- 2014-09-23 KR KR1020167008021A patent/KR101770532B1/ko active IP Right Grant
- 2014-09-23 CN CN201480053175.7A patent/CN105579453B/zh active Active
- 2014-09-23 MX MX2016003422A patent/MX2016003422A/es unknown
- 2014-09-24 AR ARP140103520A patent/AR097739A1/es unknown
- 2014-09-25 TW TW103133334A patent/TWI518087B/zh not_active IP Right Cessation
-
2016
- 2016-03-25 US US15/081,002 patent/US9957266B2/en active Active
- 2016-07-15 HK HK16108347.5A patent/HK1220201A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20160207919A1 (en) | 2016-07-21 |
| HK1220201A1 (zh) | 2017-04-28 |
| JP6182668B2 (ja) | 2017-08-16 |
| EP3049411A1 (en) | 2016-08-03 |
| RU2016112547A3 (ru) | 2018-05-25 |
| CN105579453B (zh) | 2017-12-22 |
| TWI518087B (zh) | 2016-01-21 |
| JP2016533334A (ja) | 2016-10-27 |
| TW201516046A (zh) | 2015-05-01 |
| KR20160048166A (ko) | 2016-05-03 |
| CN105579453A (zh) | 2016-05-11 |
| CA2920068A1 (en) | 2015-04-02 |
| KR101770532B1 (ko) | 2017-08-22 |
| MX2016003422A (es) | 2016-06-28 |
| RU2671506C2 (ru) | 2018-11-01 |
| EP3049411B1 (en) | 2017-04-26 |
| WO2015044095A1 (en) | 2015-04-02 |
| AR097739A1 (es) | 2016-04-13 |
| US9957266B2 (en) | 2018-05-01 |
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