JP2015517572A5 - - Google Patents
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- Publication number
- JP2015517572A5 JP2015517572A5 JP2015513993A JP2015513993A JP2015517572A5 JP 2015517572 A5 JP2015517572 A5 JP 2015517572A5 JP 2015513993 A JP2015513993 A JP 2015513993A JP 2015513993 A JP2015513993 A JP 2015513993A JP 2015517572 A5 JP2015517572 A5 JP 2015517572A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrido
- indole
- compound
- ethoxy
- fluoroethoxy
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 7
- 241000124008 Mammalia Species 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 206010001897 Alzheimer's disease Diseases 0.000 claims 2
- 210000004556 Brain Anatomy 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 210000001519 tissues Anatomy 0.000 claims 2
- HNEGJTWNOOWEMH-UHFFFAOYSA-N 1-fluoropropane Chemical group [CH2]CCF HNEGJTWNOOWEMH-UHFFFAOYSA-N 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- -1 3-fluoro-propoxy Chemical group 0.000 claims 1
- WYTGDRQOERRVOD-UHFFFAOYSA-N 7-(2-nitroethyl)-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(CC[N+](=O)[O-])C=C3NC2=C1 WYTGDRQOERRVOD-UHFFFAOYSA-N 0.000 claims 1
- LTQKXJQXVGFYEJ-UHFFFAOYSA-N 7-(3-fluoropropyl)-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(CCCF)C=C3NC2=C1 LTQKXJQXVGFYEJ-UHFFFAOYSA-N 0.000 claims 1
- SLACXXPWBNDWSW-UHFFFAOYSA-N 7-(3-nitropropyl)-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(CCC[N+](=O)[O-])C=C3NC2=C1 SLACXXPWBNDWSW-UHFFFAOYSA-N 0.000 claims 1
- HCOLWFHEOAJVJC-UHFFFAOYSA-N 7-[2-(2-fluoroethoxy)ethoxy]-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(OCCOCCF)C=C3NC2=C1 HCOLWFHEOAJVJC-UHFFFAOYSA-N 0.000 claims 1
- PGQPLORRJVHERS-UHFFFAOYSA-N 7-[2-(2-fluoroethoxy)ethoxymethyl]-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(COCCOCCF)C=C3NC2=C1 PGQPLORRJVHERS-UHFFFAOYSA-N 0.000 claims 1
- NEKSMXSTDNEBFB-UHFFFAOYSA-N 7-[2-[2-(2-fluoroethoxy)ethoxy]ethoxy]-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(OCCOCCOCCF)C=C3NC2=C1 NEKSMXSTDNEBFB-UHFFFAOYSA-N 0.000 claims 1
- BTZWEODKMIMOLZ-UHFFFAOYSA-N 7-[2-[2-(2-fluoroethoxy)ethoxy]ethyl]-5H-pyrido[4,3-b]indole Chemical compound C1=NC=C2C3=CC=C(CCOCCOCCF)C=C3NC2=C1 BTZWEODKMIMOLZ-UHFFFAOYSA-N 0.000 claims 1
- 239000000032 diagnostic agent Substances 0.000 claims 1
- 238000003384 imaging method Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
Claims (5)
- 7−(3−フルオロプロポキシ)−5H−ピリド[4,3−b]インドール;
7−(2−(2−(2−フルオロエトキシ)エトキシ)エトキシ)−5H−ピリド[4,3−b]インドール;
7−(2−(2−フルオロエトキシ)エトキシ)−5H−ピリド[4,3−b]インドール;
7−((2−(2−フルオロエトキシ)エトキシ)メチル)−5H−ピリド[4,3−b]インドール;
7−(3−フルオロプロピル)−5H−ピリド[4,3−b]インドール;
7−(2−フルオロエチル)−5H−ピリド[4,3−b]インドール;
7−(2−(2−(2−フルオロエトキシ)エトキシ)エチル)−5H−ピリド[4,3−b]インドール;および
7−(3−フルオロプロピル)−5H−ピリド[4,3−b]インドール
からなる群から選択される化合物またはその製薬上許容される塩であって、
フルオロが、所望により放射性核種で置換されている、化合物またはその製薬上許容される塩。 - フルオロが18Fである、請求項1記載の化合物。
- 7−(2−ニトロエチル)−5H−ピリド[4,3−b]インドール;および
7−(3−ニトロプロピル)−5H−ピリド[4,3−b]インドール
からなる群から選択される化合物またはその製薬上許容される塩。 - 哺乳動物においてアルツハイマー病またはその素因を診断するための医薬組成物であって、a)前記哺乳動物に診断上有効量の請求項2記載の放射性標識化合物を投与すること;b)前記化合物を脳組織に分布させること;およびc)前記脳組織を画像化することを特徴とする、組成物。
- 哺乳動物におけるアルツハイマー病またはその素因を診断するための診断薬の製造における請求項1〜3のいずれか記載の化合物の使用。
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 |
US13/477,095 | 2012-05-22 | ||
PCT/US2012/061912 WO2013176698A1 (en) | 2012-05-22 | 2012-10-25 | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015517572A JP2015517572A (ja) | 2015-06-22 |
JP2015517572A5 true JP2015517572A5 (ja) | 2015-10-15 |
JP5976206B2 JP5976206B2 (ja) | 2016-08-23 |
Family
ID=47146722
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015513993A Active JP5976206B2 (ja) | 2012-05-22 | 2012-10-25 | 神経機能障害を検出するための造影剤 |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP2852572B1 (ja) |
JP (1) | JP5976206B2 (ja) |
KR (1) | KR101609504B1 (ja) |
CN (2) | CN107011342A (ja) |
AU (1) | AU2012381042B2 (ja) |
CA (1) | CA2873963C (ja) |
CO (1) | CO7131359A2 (ja) |
ES (1) | ES2792830T3 (ja) |
WO (1) | WO2013176698A1 (ja) |
Families Citing this family (21)
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 |
ES2788977T3 (es) | 2014-04-22 | 2020-10-23 | Univ Montreal | Compuestos y uso de los mismos en la expansión de células madre hematopoyéticas y/o células progenitoras hematopoyéticas |
PL3143011T3 (pl) * | 2014-05-13 | 2021-07-19 | F. Hoffmann-La Roche Ag | Deuterowane związki heterocykliczne i ich zastosowanie jako środki obrazujące |
MX2017009505A (es) * | 2015-02-02 | 2017-11-02 | Ucb Biopharma Sprl | Derivados de 9h-pirrolo-dipiridina. |
EP3266778A4 (en) * | 2015-03-04 | 2018-11-14 | Kyoto University | RADIOACTIVE IODINE LABELED PYRIDO[1,2-a]BENZOIMIDAZOLE DERIVATIVE COMPOUND |
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 |
EP3374358B1 (en) | 2015-11-13 | 2021-02-17 | Eli Lilly and Company | Azetidine derivatives for tau imaging |
WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
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 |
WO2018024643A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
WO2018024642A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
WO2018102067A2 (en) * | 2016-11-01 | 2018-06-07 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
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 |
WO2019145292A1 (en) | 2018-01-24 | 2019-08-01 | 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 |
WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
KR102215255B1 (ko) * | 2019-06-12 | 2021-02-15 | 한국과학기술연구원 | 타우 응집체에 선택적으로 결합하는 형광 탐침자로서 유효한 신규 화합물 및 이의 제조 방법 |
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 |
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 |
US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006005063A2 (en) * | 2004-06-30 | 2006-01-12 | Smithkline Beecham Corporation | Methods and compositions |
FR2885905A1 (fr) * | 2005-05-23 | 2006-11-24 | Trophos Sa | Nouveaux composes chimiques et leurs utilisations comme medicament |
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 |
CA2731738A1 (en) * | 2008-07-24 | 2010-01-28 | Siemens Medical Solutions Usa, Inc. | Imaging agents useful for identifying ad pathology |
JP2012051804A (ja) * | 2008-12-26 | 2012-03-15 | Kyoto Univ | Eg5阻害剤 |
US8691187B2 (en) | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
WO2010111303A2 (en) * | 2009-03-23 | 2010-09-30 | Siemens Medical Solutions Usa, Inc. | Imaging agents for detecting neurological disorders |
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 WO PCT/US2012/061912 patent/WO2013176698A1/en active Application Filing
- 2012-10-25 AU AU2012381042A patent/AU2012381042B2/en active Active
- 2012-10-25 KR KR1020147032388A patent/KR101609504B1/ko active IP Right Grant
- 2012-10-25 CN CN201611136351.0A patent/CN107011342A/zh active Pending
- 2012-10-25 CN CN201280073373.0A patent/CN104781234A/zh active Pending
- 2012-10-25 CA CA2873963A patent/CA2873963C/en active Active
- 2012-10-25 JP JP2015513993A patent/JP5976206B2/ja active Active
- 2012-10-25 EP EP12783780.5A patent/EP2852572B1/en active Active
- 2012-10-25 ES ES12783780T patent/ES2792830T3/es active Active
-
2014
- 2014-11-20 CO CO14255692A patent/CO7131359A2/es unknown
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