JP2017521387A5 - - Google Patents
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- Publication number
- JP2017521387A5 JP2017521387A5 JP2016572520A JP2016572520A JP2017521387A5 JP 2017521387 A5 JP2017521387 A5 JP 2017521387A5 JP 2016572520 A JP2016572520 A JP 2016572520A JP 2016572520 A JP2016572520 A JP 2016572520A JP 2017521387 A5 JP2017521387 A5 JP 2017521387A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- compound
- heterocyclyl
- halogen
- groups
- 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 40
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000002619 bicyclic group Chemical group 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 8
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- -1 pyrrolopyridinyl Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 208000004051 Chronic Traumatic Encephalopathy Diseases 0.000 claims 3
- 208000017004 dementia pugilistica Diseases 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 2
- 208000024571 Pick disease Diseases 0.000 claims 2
- 206010044688 Trisomy 21 Diseases 0.000 claims 2
- 238000004220 aggregation Methods 0.000 claims 2
- 230000002776 aggregation Effects 0.000 claims 2
- 210000004227 basal ganglia Anatomy 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 230000001054 cortical effect Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 230000008021 deposition Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000025688 early-onset autosomal dominant Alzheimer disease Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 208000015756 familial Alzheimer disease Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000004612 furopyridinyl group Chemical group O1C(=CC2=C1C=CC=N2)* 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000003384 imaging method Methods 0.000 claims 2
- 125000002346 iodo group Chemical group I* 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 208000014644 Brain disease Diseases 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 208000032274 Encephalopathy Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 208000034799 Tauopathies Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 238000000376 autoradiography Methods 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000001514 detection method Methods 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000002595 magnetic resonance imaging Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 238000002600 positron emission tomography Methods 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000000472 traumatic effect Effects 0.000 claims 1
- KAXAUWZJVWGFDO-UHFFFAOYSA-N Nc(c1c(cc2)cnc(-[n](cc3)c4c3ccnc4)c1)c2F Chemical compound Nc(c1c(cc2)cnc(-[n](cc3)c4c3ccnc4)c1)c2F KAXAUWZJVWGFDO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/079834 | 2014-06-13 | ||
| PCT/CN2014/079834 WO2015188368A1 (en) | 2014-06-13 | 2014-06-13 | Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles |
| PCT/US2015/034794 WO2015191506A2 (en) | 2014-06-13 | 2015-06-09 | Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017521387A JP2017521387A (ja) | 2017-08-03 |
| JP2017521387A5 true JP2017521387A5 (enExample) | 2018-03-15 |
| JP6513107B2 JP6513107B2 (ja) | 2019-05-15 |
Family
ID=54832744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016572520A Active JP6513107B2 (ja) | 2014-06-13 | 2015-06-09 | 神経原線維濃縮体のイメージング剤としてのピロロ［２，３−ｃ］ピリジン |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9808542B2 (enExample) |
| EP (1) | EP3154970B1 (enExample) |
| JP (1) | JP6513107B2 (enExample) |
| KR (1) | KR102478430B1 (enExample) |
| CN (1) | CN106661018B (enExample) |
| AU (1) | AU2015274843B2 (enExample) |
| BR (1) | BR112016028345B1 (enExample) |
| CA (1) | CA2948528C (enExample) |
| DK (1) | DK3154970T3 (enExample) |
| ES (1) | ES2763095T3 (enExample) |
| HU (1) | HUE048395T2 (enExample) |
| MX (1) | MX375282B (enExample) |
| PL (1) | PL3154970T3 (enExample) |
| RU (1) | RU2695373C2 (enExample) |
| WO (2) | WO2015188368A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5422782B1 (ja) | 2012-12-21 | 2014-02-19 | 独立行政法人放射線医学総合研究所 | 脳内に蓄積したタウタンパク質をイメージングするための新規化合物 |
| WO2018015549A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| EP3487545A1 (en) * | 2016-07-22 | 2019-05-29 | AC Immune S.A. | Compounds for imaging tau protein aggregates |
| US11541033B2 (en) | 2017-06-02 | 2023-01-03 | Fujifilm Toyama Chemical Co., Ltd. | Agent for preventing or treating Alzheimer's disease |
| RU2728717C1 (ru) | 2017-06-02 | 2020-07-30 | ФУДЖИФИЛМ Тояма Кемикал Ко., Лтд. | Средство для профилактики или лечения спиноцеребеллярной атаксии |
| CN110691594A (zh) * | 2017-06-02 | 2020-01-14 | 富士胶片富山化学株式会社 | Tau蛋白病预防或治疗剂 |
| JP7282028B2 (ja) | 2017-06-02 | 2023-05-26 | 富士フイルム富山化学株式会社 | 脳萎縮予防または治療剤 |
| KR20200003102A (ko) | 2017-06-02 | 2020-01-08 | 후지필름 도야마 케미컬 가부시키가이샤 | 아밀로이드 β 단백질량 감소제 |
| JP7227914B2 (ja) | 2017-10-30 | 2023-02-22 | 富士フイルム富山化学株式会社 | エモパミル結合タンパク質結合剤およびその利用 |
| EP3743426A1 (en) | 2018-01-24 | 2020-12-02 | AC Immune SA | Azacarboline compounds for the detection of tau aggregates |
| WO2019145291A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Gamma-carboline compounds for the detection of tau aggregates |
| CN111770924B (zh) * | 2018-04-04 | 2023-05-09 | 深圳福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
| KR102017324B1 (ko) * | 2018-04-30 | 2019-09-02 | 경북대학교 산학협력단 | 신규한 asm 활성 직접 억제 화합물 2-아미노-2-(1,2,3-트리아졸-4-일)프로판-1,3-디올 유도체 및 이의 용도 |
| CN112384517B (zh) * | 2018-05-09 | 2023-07-14 | 新旭生技股份有限公司 | 杂芳基化合物及其用途 |
| JP7478142B2 (ja) | 2018-06-07 | 2024-05-02 | ディスアーム セラピューティクス， インコーポレイテッド | Ｓａｒｍ１阻害剤 |
| CN108676007B (zh) * | 2018-06-22 | 2020-06-26 | 厦门大学 | 放射性核素标记的苯并蝶啶类衍生物及其制备方法和应用 |
| CA3123215C (en) | 2018-12-19 | 2024-04-02 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| CA3161455A1 (en) | 2019-11-13 | 2021-05-20 | Aprinoia Therapeutics Limited | Compounds for degrading tau protein aggregates and uses thereof |
| US20220008563A1 (en) * | 2020-07-10 | 2022-01-13 | The Regents Of The University Of California | Radiolabelled and nonradiolabelled pegylated compounds and uses thereof |
| BR112023002139A2 (pt) * | 2020-08-06 | 2023-04-18 | Chdi Foundation Inc | Compostos de heterobiarila e agentes de imageamento para proteína huntingtina |
| CN112939753B (zh) * | 2020-09-15 | 2022-04-05 | 浙江大学 | 一种1-茚酮类化合物的合成方法 |
| KR102240400B1 (ko) * | 2020-11-19 | 2021-04-15 | 한국원자력연구원 | 베타-아밀로이드 검출용 수용성 화합물 |
| CN112745299B (zh) * | 2021-01-07 | 2022-01-25 | 温州大学 | 4-氰基-7,8-二氢异喹啉衍生物及其制备方法和应用 |
| TWI782769B (zh) * | 2021-10-28 | 2022-11-01 | 行政院原子能委員會核能研究所 | 一種新穎神經纖維糾結微管相關蛋白質Tau造影化合物、其製備方法及用途 |
| CN114149425A (zh) * | 2021-11-16 | 2022-03-08 | 上海应用技术大学 | 5-氟甲基吡啶衍生物和18-f同位素标记的5-氟甲基吡啶衍生物及其制备与应用 |
| CN114276259B (zh) * | 2022-01-04 | 2022-12-06 | 济川(上海)医学科技有限公司 | 一种马来酸二甲茚定关键中间体的制备方法 |
| CN115417816B (zh) * | 2022-09-05 | 2024-01-26 | 江苏南大光电材料股份有限公司 | 一种3,6-二溴-1-氯-异喹啉的制备方法 |
| WO2025230262A1 (ko) * | 2024-04-29 | 2025-11-06 | 심플렉스 주식회사 | 신규한 헤테로아릴 유도체 및 이의 aak1 억제 용도 |
| WO2026153567A1 (zh) * | 2025-01-20 | 2026-07-23 | 天津恒瑞医药有限公司 | 一种吡咯并[2,3-c]吡啶类衍生物及其制备方法和用途 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5451566A (en) | 1993-11-17 | 1995-09-19 | Zeneca Limited | Herbicidal pyrrolopyridine compounds |
| AU2005336513B2 (en) * | 2004-10-07 | 2012-08-09 | Merck Sharp & Dohme Llc | Thiazolyl mGluR5 antagonists and methods for their use |
| US20080027044A1 (en) * | 2006-06-13 | 2008-01-31 | Kim Lewis | Prodrug antibiotic screens |
| WO2008103615A1 (en) | 2007-02-21 | 2008-08-28 | Kalypsys, Inc. | Isoquinolines useful as inducible nitric oxide synthase inhibitors |
| TW200902499A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| EP2296474A1 (en) * | 2008-05-30 | 2011-03-23 | Merck Sharp & Dohme Corp. | Novel substituted indoles |
| JP5789252B2 (ja) | 2009-05-07 | 2015-10-07 | インテリカイン， エルエルシー | 複素環式化合物およびその使用 |
| GB201004311D0 (en) * | 2010-03-15 | 2010-04-28 | Proximagen Ltd | New enzyme inhibitor compounds |
| WO2012064973A2 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| USRE47009E1 (en) | 2011-02-01 | 2018-08-28 | The Children's Hospital Of Philadelphia | HDAC inhibitors and therapeutic methods using the same |
| US8684313B2 (en) | 2011-02-02 | 2014-04-01 | Ocean Rodeo Sports Inc. | Inflatable kite with leading edge swept forwards at wingtip |
| US20140348748A1 (en) * | 2011-09-16 | 2014-11-27 | Lisheng Cai | Beta-amyloid imaging agents, methods of manufacture, and methods of use thereof |
| US20150336948A1 (en) * | 2012-05-29 | 2015-11-26 | Merck Sharp & Dohme Corp. | Isotopically Labeled Biaryl Urea Compounds |
| CN103450152B (zh) * | 2012-06-04 | 2015-11-18 | 济南海乐医药技术开发有限公司 | 基于吲唑、吲哚或氮杂吲唑、氮杂吲哚的双芳基脲类结构抗肿瘤药物 |
| GB201304526D0 (en) * | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
| GB201404498D0 (en) * | 2014-03-13 | 2014-04-30 | Proximagen Ltd | New compounds |
-
2014
- 2014-06-13 WO PCT/CN2014/079834 patent/WO2015188368A1/en not_active Ceased
-
2015
- 2015-06-09 BR BR112016028345-7A patent/BR112016028345B1/pt active IP Right Grant
- 2015-06-09 PL PL15806980T patent/PL3154970T3/pl unknown
- 2015-06-09 CA CA2948528A patent/CA2948528C/en active Active
- 2015-06-09 DK DK15806980.7T patent/DK3154970T3/da active
- 2015-06-09 WO PCT/US2015/034794 patent/WO2015191506A2/en not_active Ceased
- 2015-06-09 MX MX2016016384A patent/MX375282B/es active IP Right Grant
- 2015-06-09 HU HUE15806980A patent/HUE048395T2/hu unknown
- 2015-06-09 JP JP2016572520A patent/JP6513107B2/ja active Active
- 2015-06-09 EP EP15806980.7A patent/EP3154970B1/en active Active
- 2015-06-09 ES ES15806980T patent/ES2763095T3/es active Active
- 2015-06-09 AU AU2015274843A patent/AU2015274843B2/en active Active
- 2015-06-09 RU RU2016150404A patent/RU2695373C2/ru active
- 2015-06-09 US US15/317,333 patent/US9808542B2/en active Active
- 2015-06-09 KR KR1020177000709A patent/KR102478430B1/ko active Active
- 2015-06-09 CN CN201580031335.2A patent/CN106661018B/zh active Active
-
2017
- 2017-10-04 US US15/724,402 patent/US10022461B2/en active Active