CN104781234A - 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 - Google Patents
用于检测神经功能障碍的基于咔啉和咔唑的成像剂 Download PDFInfo
- Publication number
- CN104781234A CN104781234A CN201280073373.0A CN201280073373A CN104781234A CN 104781234 A CN104781234 A CN 104781234A CN 201280073373 A CN201280073373 A CN 201280073373A CN 104781234 A CN104781234 A CN 104781234A
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- China
- Prior art keywords
- alkyl
- halogen
- optionally
- compound
- substitute
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 0 *CCCc1ccc(c2cnccc2[n]2)c2c1 Chemical compound *CCCc1ccc(c2cnccc2[n]2)c2c1 0.000 description 11
- UFFSCBWGJRYKSX-UHFFFAOYSA-N C[NH+](C(CC1)=CC=C1I)[O-] Chemical compound C[NH+](C(CC1)=CC=C1I)[O-] UFFSCBWGJRYKSX-UHFFFAOYSA-N 0.000 description 1
- KOZHNZIZUPCYIY-UHFFFAOYSA-N FCCc1ccc(c2cnccc2[nH]2)c2c1 Chemical compound FCCc1ccc(c2cnccc2[nH]2)c2c1 KOZHNZIZUPCYIY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
-
- 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
- A61K51/0446—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/06—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
- C07D311/08—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
- C07D311/18—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted otherwise than in position 3 or 7
-
- 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
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—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)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Optics & Photonics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Physics & Mathematics (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
- Indole Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611136351.0A CN107011342A (zh) | 2012-05-22 | 2012-10-25 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13/477,095 US8932557B2 (en) | 2008-02-14 | 2012-05-22 | Imaging agents for detecting neurological dysfunction |
| US13/477095 | 2012-05-22 | ||
| PCT/US2012/061912 WO2013176698A1 (en) | 2012-05-22 | 2012-10-25 | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611136351.0A Division CN107011342A (zh) | 2012-05-22 | 2012-10-25 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104781234A true CN104781234A (zh) | 2015-07-15 |
Family
ID=47146722
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280073373.0A Pending CN104781234A (zh) | 2012-05-22 | 2012-10-25 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
| CN201611136351.0A Pending CN107011342A (zh) | 2012-05-22 | 2012-10-25 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611136351.0A Pending CN107011342A (zh) | 2012-05-22 | 2012-10-25 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP2852572B1 (https=) |
| JP (1) | JP5976206B2 (https=) |
| KR (1) | KR101609504B1 (https=) |
| CN (2) | CN104781234A (https=) |
| AU (1) | AU2012381042B2 (https=) |
| CA (1) | CA2873963C (https=) |
| CO (1) | CO7131359A2 (https=) |
| ES (1) | ES2792830T3 (https=) |
| WO (1) | WO2013176698A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114539250A (zh) * | 2022-03-04 | 2022-05-27 | 上海裕兰生物科技有限公司 | 一种阿尔兹海默症PET-tau示踪剂的制备方法 |
| CN117050070A (zh) * | 2023-07-05 | 2023-11-14 | 湘潭大学 | 一种荧光探针及其制备方法和在Aβ检测中的应用 |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015110263A1 (en) * | 2014-01-21 | 2015-07-30 | Ac Immune Sa | Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyolid-like proteins |
| JP6762233B2 (ja) * | 2014-04-22 | 2020-09-30 | ウニヴェルシテ ド モントリオールＵｎｉｖｅｒｓｉｔｅ Ｄｅ Ｍｏｎｔｒｅａｌ | 化合物および造血幹細胞および／または造血前駆細胞の増大におけるその使用 |
| HUE053939T2 (hu) | 2014-05-13 | 2021-08-30 | Hoffmann La Roche | Deuterált heterociklikus vegyületek és képalkotó kontrasztanyagként való használatuk |
| EA036518B1 (ru) * | 2015-02-02 | 2020-11-18 | Юсб Байофарма Спрл | Производные 9h-пирролодипиридина |
| JP6609866B2 (ja) * | 2015-03-04 | 2019-11-27 | 国立大学法人京都大学 | 放射性ヨウ素標識ピリド［１，２−ａ］ベンゾイミダゾール誘導体化合物 |
| TW201707726A (zh) * | 2015-08-19 | 2017-03-01 | 國立大學法人京都大學 | 放射性鹵素標誌吡啶并［１，２－ａ］苯并咪唑衍生物化合物 |
| CA3003884C (en) | 2015-11-13 | 2020-04-21 | Eli Lilly And Company | Azetidine derivatives for tau imaging |
| KR102472003B1 (ko) | 2016-07-22 | 2022-11-29 | 에이씨 이뮨 에스에이 | 타우 단백질 응집체를 이미징하기 위한 화합물 |
| WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| WO2018024642A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| WO2018024643A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| MX2019005007A (es) * | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| CN109884194A (zh) * | 2017-12-06 | 2019-06-14 | 新疆维吾尔药业有限责任公司 | 一种药用植物的分离方法及其产品和应用 |
| US20210041447A1 (en) | 2018-01-24 | 2021-02-11 | Ac Immune Sa | Azacarboline compounds for the detection of tau aggregates |
| EP3743423A1 (en) | 2018-01-24 | 2020-12-02 | AC Immune SA | Gamma-carboline compounds for the detection of tau aggregates |
| CN108409634B (zh) * | 2018-05-10 | 2021-04-27 | 曲阜师范大学 | 咔唑类荧光胺类化合物标记试剂、合成和应用 |
| 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 |
| KR102215255B1 (ko) * | 2019-06-12 | 2021-02-15 | 한국과학기술연구원 | 타우 응집체에 선택적으로 결합하는 형광 탐침자로서 유효한 신규 화합물 및 이의 제조 방법 |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| US11319319B1 (en) | 2021-04-07 | 2022-05-03 | Ventus Therapeutics U.S., Inc. | Compounds for inhibiting NLRP3 and uses thereof |
| CN116003402B (zh) * | 2021-11-02 | 2025-08-29 | 上海如絮生物科技有限公司 | 一种三环类化合物、其中间体、制备方法和应用 |
| US12331048B2 (en) | 2022-10-31 | 2025-06-17 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors |
| KR20250137711A (ko) | 2023-02-02 | 2025-09-18 | 일라이 릴리 앤드 캄파니 | 타우 영상화를 위한 신규 화합물 |
| WO2025155625A1 (en) | 2024-01-16 | 2025-07-24 | Eli Lilly And Company | Novel compounds for tau imaging |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006125887A1 (fr) * | 2005-05-23 | 2006-11-30 | Trophos | Composes derives de 5h-pyrido[4,3-b]indole et leurs utilisations comme medicament pour traiter les maladies neurodegeneratives a polyglutamines |
| WO2010011964A2 (en) * | 2008-07-24 | 2010-01-28 | Siemens Medical Solutions Usa, Inc. | Imaging agents useful for identifying ad pathology |
| WO2011119565A1 (en) * | 2010-03-23 | 2011-09-29 | Siemens Medical Solutions Usa, Inc. | 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 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090170882A1 (en) * | 2004-06-30 | 2009-07-02 | Dashyant Dhanak | Methods and compositions |
| DE102006062203A1 (de) * | 2006-12-22 | 2008-06-26 | Curacyte Discovery Gmbh | Substituierte 5H-Pyrimido[5,4-b]indole als Induktoren der Apoptose bei B-CLL Zellen |
| WO2008132454A1 (en) * | 2007-04-26 | 2008-11-06 | Ge Healthcare Limited | Carbolines and their use as imaging agents |
| EP2247558B2 (en) * | 2008-02-14 | 2024-07-03 | Eli Lilly and Company | Novel imaging agents for detecting neurological dysfunction |
| JP2012051804A (ja) * | 2008-12-26 | 2012-03-15 | Kyoto Univ | Ｅｇ５阻害剤 |
| US10639608B2 (en) * | 2010-04-08 | 2020-05-05 | Siemens Medical Solutions Usa, Inc. | System, device and method for preparing tracers and transferring materials during radiosynthesis |
| JP5585382B2 (ja) * | 2010-10-22 | 2014-09-10 | コニカミノルタ株式会社 | 有機エレクトロルミネッセンス素子、照明装置及び表示装置 |
-
2012
- 2012-10-25 CN CN201280073373.0A patent/CN104781234A/zh active Pending
- 2012-10-25 CA CA2873963A patent/CA2873963C/en active Active
- 2012-10-25 ES ES12783780T patent/ES2792830T3/es active Active
- 2012-10-25 EP EP12783780.5A patent/EP2852572B1/en active Active
- 2012-10-25 CN CN201611136351.0A patent/CN107011342A/zh active Pending
- 2012-10-25 KR KR1020147032388A patent/KR101609504B1/ko active Active
- 2012-10-25 JP JP2015513993A patent/JP5976206B2/ja active Active
- 2012-10-25 WO PCT/US2012/061912 patent/WO2013176698A1/en not_active Ceased
- 2012-10-25 AU AU2012381042A patent/AU2012381042B2/en active Active
-
2014
- 2014-11-20 CO CO14255692A patent/CO7131359A2/es unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006125887A1 (fr) * | 2005-05-23 | 2006-11-30 | Trophos | Composes derives de 5h-pyrido[4,3-b]indole et leurs utilisations comme medicament pour traiter les maladies neurodegeneratives a polyglutamines |
| WO2010011964A2 (en) * | 2008-07-24 | 2010-01-28 | Siemens Medical Solutions Usa, Inc. | Imaging agents useful for identifying ad pathology |
| 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 |
| WO2011119565A1 (en) * | 2010-03-23 | 2011-09-29 | Siemens Medical Solutions Usa, Inc. | Imaging agents for detecting neurological disorders |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114539250A (zh) * | 2022-03-04 | 2022-05-27 | 上海裕兰生物科技有限公司 | 一种阿尔兹海默症PET-tau示踪剂的制备方法 |
| CN114539250B (zh) * | 2022-03-04 | 2023-08-29 | 上海裕兰生物科技有限公司 | 一种阿尔兹海默症PET-tau示踪剂的制备方法 |
| CN117050070A (zh) * | 2023-07-05 | 2023-11-14 | 湘潭大学 | 一种荧光探针及其制备方法和在Aβ检测中的应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2852572B1 (en) | 2020-04-01 |
| CA2873963A1 (en) | 2013-11-28 |
| KR20150002854A (ko) | 2015-01-07 |
| CO7131359A2 (es) | 2014-12-01 |
| AU2012381042B2 (en) | 2015-10-01 |
| CA2873963C (en) | 2017-04-11 |
| EP2852572A1 (en) | 2015-04-01 |
| KR101609504B1 (ko) | 2016-04-05 |
| CN107011342A (zh) | 2017-08-04 |
| JP2015517572A (ja) | 2015-06-22 |
| AU2012381042A1 (en) | 2014-11-20 |
| WO2013176698A1 (en) | 2013-11-28 |
| ES2792830T3 (es) | 2020-11-12 |
| JP5976206B2 (ja) | 2016-08-23 |
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Application publication date: 20150715 |