JP2017515856A5 - - Google Patents
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- Publication number
- JP2017515856A5 JP2017515856A5 JP2016567651A JP2016567651A JP2017515856A5 JP 2017515856 A5 JP2017515856 A5 JP 2017515856A5 JP 2016567651 A JP2016567651 A JP 2016567651A JP 2016567651 A JP2016567651 A JP 2016567651A JP 2017515856 A5 JP2017515856 A5 JP 2017515856A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocyclyl
- optionally substituted
- alkenyl
- 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 55
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 32
- 125000004452 carbocyclyl group Chemical group 0.000 claims 30
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 23
- 125000001475 halogen functional group Chemical group 0.000 claims 23
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 125000004043 oxo group Chemical group O=* 0.000 claims 18
- 238000003384 imaging method Methods 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 241001465754 Metazoa Species 0.000 claims 13
- 102000013498 tau Proteins Human genes 0.000 claims 10
- 108010026424 tau Proteins Proteins 0.000 claims 10
- 208000037259 Amyloid Plaque Diseases 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 238000001514 detection method Methods 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 230000002285 radioactive effect Effects 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 230000004845 protein aggregation Effects 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- -1 R ay Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 3
- 229910052805 deuterium Inorganic materials 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000000155 isotopic effect Effects 0.000 claims 2
- 210000002682 neurofibrillary tangle Anatomy 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 2
- 208000003808 Amyloid Neuropathies Diseases 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000012141 concentrate Substances 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- QCEIHUNQJSTPKS-UHFFFAOYSA-N C1C(C2)C1CN2c1nc2nc(cccc3)c3[n]2cc1 Chemical compound C1C(C2)C1CN2c1nc2nc(cccc3)c3[n]2cc1 QCEIHUNQJSTPKS-UHFFFAOYSA-N 0.000 description 1
- AUNIZHBGUCSRDA-UHFFFAOYSA-N C1C=CC=C2N=C3N=CC=CN3C12 Chemical compound C1C=CC=C2N=C3N=CC=CN3C12 AUNIZHBGUCSRDA-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461992717P | 2014-05-13 | 2014-05-13 | |
| US61/992,717 | 2014-05-13 | ||
| PCT/EP2015/060447 WO2015173225A1 (en) | 2014-05-13 | 2015-05-12 | Deuterated heterocyclic compounds and their use as imaging agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019091813A Division JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017515856A JP2017515856A (ja) | 2017-06-15 |
| JP2017515856A5 true JP2017515856A5 (https=) | 2018-06-14 |
| JP6529986B2 JP6529986B2 (ja) | 2019-06-12 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567651A Active JP6529986B2 (ja) | 2014-05-13 | 2015-05-12 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
| JP2019091813A Active JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019091813A Active JP6681498B2 (ja) | 2014-05-13 | 2019-05-15 | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US10076581B2 (https=) |
| EP (2) | EP3143011B1 (https=) |
| JP (2) | JP6529986B2 (https=) |
| KR (2) | KR102618139B1 (https=) |
| CN (2) | CN106459059B (https=) |
| AU (2) | AU2015261008B2 (https=) |
| CA (1) | CA2948721C (https=) |
| DK (1) | DK3143011T3 (https=) |
| ES (1) | ES2867814T3 (https=) |
| HR (1) | HRP20210641T1 (https=) |
| HU (1) | HUE053939T2 (https=) |
| IL (3) | IL280791B2 (https=) |
| LT (1) | LT3143011T (https=) |
| MX (2) | MX384604B (https=) |
| PL (1) | PL3143011T3 (https=) |
| PT (1) | PT3143011T (https=) |
| RS (1) | RS61810B1 (https=) |
| RU (1) | RU2696492C2 (https=) |
| SG (2) | SG11201609281UA (https=) |
| SI (1) | SI3143011T1 (https=) |
| WO (1) | WO2015173225A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS61810B1 (sr) | 2014-05-13 | 2021-06-30 | Hoffmann La Roche | Deuterisana heterociklična jedinjenja i njihova upotreba kao sredstva za snimanje |
| EP3487545A1 (en) | 2016-07-22 | 2019-05-29 | AC Immune S.A. | Compounds for imaging tau protein aggregates |
| KR102472003B1 (ko) | 2016-07-22 | 2022-11-29 | 에이씨 이뮨 에스에이 | 타우 단백질 응집체를 이미징하기 위한 화합물 |
| IL290809B2 (en) * | 2016-11-01 | 2024-01-01 | Arvinas Operations Inc | Tau-protein targeting protacs and associated methods of use |
| BR112020003725A2 (pt) | 2017-10-06 | 2020-11-03 | Forma Therapeutics, Inc. | inibição da peptidase 30 específica de ubiquitina |
| WO2019145292A1 (en) | 2018-01-24 | 2019-08-01 | 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 |
| EP3758696B1 (en) | 2018-03-02 | 2026-02-25 | The Trustees of the University of Pennsylvania | [1,2,4]triazolo[1,5-a]pyrimidine compounds and use in stabilizing microtubules |
| JP7449242B2 (ja) | 2018-05-17 | 2024-03-13 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的ペプチダーゼ３０（ｕｓｐ３０）阻害剤として有用な縮合二環化合物 |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| JP7542538B2 (ja) | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス， インコーポレイテッド | Ｓｒｃホモロジー－２ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| JP7640458B2 (ja) | 2018-10-05 | 2025-03-05 | アンナプルナ バイオ インコーポレイテッド | Ａｐｊ受容体活性に関連する状態を処置するための化合物および組成物 |
| LT3860989T (lt) | 2018-10-05 | 2023-06-12 | Forma Therapeutics, Inc. | Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai |
| 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 |
| WO2020227576A1 (en) | 2019-05-09 | 2020-11-12 | Genentech, Inc. | Regio-selective synthesis of imidazo[1,2-a]pyrimidines |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| 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 |
| IL310382A (en) | 2021-08-27 | 2024-03-01 | Genentech Inc | Methods for treating tau pathologies |
| CN120187452A (zh) | 2022-06-13 | 2025-06-20 | 基因泰克公司 | 使用克瑞尼珠单抗延迟或预防阿尔茨海默病的发作的方法 |
| WO2025155625A1 (en) * | 2024-01-16 | 2025-07-24 | Eli Lilly And Company | Novel compounds for tau imaging |
| CN118957609B (zh) * | 2024-07-23 | 2025-09-09 | 无锡绿能电合科技有限公司 | 一种氟代芳环的氘代方法 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD76515A (https=) * | ||||
| 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 |
| HRP20120135T1 (hr) * | 2006-03-30 | 2012-03-31 | The Trustees Of The University Of Pennsylvania | Derivati stirilpiridina i njihova upotreba kod vezanja na i vizualizacije amiloidnih plakova |
| CA2698808A1 (en) * | 2007-09-13 | 2009-03-19 | Concert Pharmaceuticals, Inc. | Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof |
| US8932557B2 (en) | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| US20110046378A1 (en) | 2008-02-14 | 2011-02-24 | Siemens Medical Solutions Usa, Inc. | Novel 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 |
| CN103739605B (zh) | 2009-03-23 | 2016-08-17 | 伊莱利利公司 | 用于检测神经障碍的显像剂 |
| 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) |
| JP2013542243A (ja) * | 2010-11-15 | 2013-11-21 | カトリーケ ウニヴェルシテイト ルーヴェン | 新規な抗ウイルス性化合物 |
| CN107011342A (zh) * | 2012-05-22 | 2017-08-04 | 伊莱利利公司 | 用于检测神经功能障碍的基于咔啉和咔唑的成像剂 |
| JP6194416B2 (ja) * | 2013-10-08 | 2017-09-06 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | タウ−ｐｅｔリガンドとしてのジアザカルバゾール誘導体 |
| RS61810B1 (sr) | 2014-05-13 | 2021-06-30 | Hoffmann La Roche | Deuterisana heterociklična jedinjenja i njihova upotreba kao sredstva za snimanje |
-
2015
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 MX MX2020010847A patent/MX384604B/es unknown
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active Active
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
-
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
-
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
-
2020
- 2020-06-08 US US16/895,352 patent/US11504440B2/en active Active
-
2022
- 2022-11-18 US US18/056,856 patent/US12214058B2/en active Active
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