AU2015261008B2 - Deuterated heterocyclic compounds and their use as imaging agents - Google Patents
Deuterated heterocyclic compounds and their use as imaging agents Download PDFInfo
- Publication number
- AU2015261008B2 AU2015261008B2 AU2015261008A AU2015261008A AU2015261008B2 AU 2015261008 B2 AU2015261008 B2 AU 2015261008B2 AU 2015261008 A AU2015261008 A AU 2015261008A AU 2015261008 A AU2015261008 A AU 2015261008A AU 2015261008 B2 AU2015261008 B2 AU 2015261008B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- pharmaceutically acceptable
- animal
- acceptable salt
- deuterated
- 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.)
- Active
Links
- 0 *c1c(*=C(**=*)*=*)cccc1 Chemical compound *c1c(*=C(**=*)*=*)cccc1 0.000 description 3
- QCEIHUNQJSTPKS-UHFFFAOYSA-N C1C(C2)C1CN2c1nc2nc3ccccc3[n]2cc1 Chemical compound C1C(C2)C1CN2c1nc2nc3ccccc3[n]2cc1 QCEIHUNQJSTPKS-UHFFFAOYSA-N 0.000 description 1
- FCZFPMKLLXTSNP-UHFFFAOYSA-N CCOC(C=N)=O Chemical compound CCOC(C=N)=O FCZFPMKLLXTSNP-UHFFFAOYSA-N 0.000 description 1
- FTHNMBUFXOTCDE-VBVNFKHJSA-N C[C@@](C1)(C2CN1OC(c1ccccc1)=O)[C@H]2C=O Chemical compound C[C@@](C1)(C2CN1OC(c1ccccc1)=O)[C@H]2C=O FTHNMBUFXOTCDE-VBVNFKHJSA-N 0.000 description 1
- PWOZUTBCKUVKFF-UHFFFAOYSA-N OCCC(CC1)CCN1c1nc2nc(cccc3)c3[n]2cc1 Chemical compound OCCC(CC1)CCN1c1nc2nc(cccc3)c3[n]2cc1 PWOZUTBCKUVKFF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Optics & Photonics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physics & Mathematics (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2019203369A AU2019203369B2 (en) | 2014-05-13 | 2019-05-14 | Deuterated heterocyclic compounds and their use as imaging agents |
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 |
|---|---|---|---|
| AU2019203369A Division AU2019203369B2 (en) | 2014-05-13 | 2019-05-14 | Deuterated heterocyclic compounds and their use as imaging agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2015261008A1 AU2015261008A1 (en) | 2016-11-17 |
| AU2015261008B2 true AU2015261008B2 (en) | 2019-02-14 |
Family
ID=53269446
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2015261008A Active AU2015261008B2 (en) | 2014-05-13 | 2015-05-12 | Deuterated heterocyclic compounds and their use as imaging agents |
| AU2019203369A Active AU2019203369B2 (en) | 2014-05-13 | 2019-05-14 | Deuterated heterocyclic compounds and their use as imaging agents |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2019203369A Active AU2019203369B2 (en) | 2014-05-13 | 2019-05-14 | Deuterated heterocyclic compounds and their use as imaging agents |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US10076581B2 (enExample) |
| EP (2) | EP3901145A1 (enExample) |
| JP (2) | JP6529986B2 (enExample) |
| KR (2) | KR102530129B1 (enExample) |
| CN (2) | CN110483522B (enExample) |
| AU (2) | AU2015261008B2 (enExample) |
| CA (1) | CA2948721C (enExample) |
| DK (1) | DK3143011T3 (enExample) |
| ES (1) | ES2867814T3 (enExample) |
| HR (1) | HRP20210641T1 (enExample) |
| HU (1) | HUE053939T2 (enExample) |
| IL (3) | IL280791B2 (enExample) |
| LT (1) | LT3143011T (enExample) |
| MX (2) | MX384604B (enExample) |
| PL (1) | PL3143011T3 (enExample) |
| PT (1) | PT3143011T (enExample) |
| RS (1) | RS61810B1 (enExample) |
| RU (1) | RU2696492C2 (enExample) |
| SG (2) | SG10201805628TA (enExample) |
| SI (1) | SI3143011T1 (enExample) |
| WO (1) | WO2015173225A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2948721C (en) * | 2014-05-13 | 2023-03-28 | F. Hoffmann-La Roche Ag | Deuterated compounds and uses thereof |
| JP7197476B2 (ja) | 2016-07-22 | 2022-12-27 | エーシー・イミューン・エス・アー | タウタンパク質凝集体を画像化するための化合物 |
| JP7059270B2 (ja) | 2016-07-22 | 2022-04-25 | エーシー・イミューン・エス・アー | タウタンパク質凝集体を画像化するための化合物 |
| JP7286539B2 (ja) * | 2016-11-01 | 2023-06-05 | 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ｐｒｏｔａｃ、および関連使用方法 |
| CA3072362A1 (en) | 2017-10-06 | 2019-04-11 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 30 |
| WO2019145292A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Azacarboline compounds for the detection of tau aggregates |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| US11623927B2 (en) | 2018-03-02 | 2023-04-11 | The Trustees Of The University Of Pennsylvania | Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules |
| SG11202011299PA (en) | 2018-05-17 | 2020-12-30 | Forma Therapeutics Inc | Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors |
| 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 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| RS65335B1 (sr) | 2018-10-05 | 2024-04-30 | Annapurna Bio Inc | Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj |
| MY209034A (en) | 2018-10-05 | 2025-06-17 | Forma Therapeutics Inc | Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors |
| 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 |
| CN114423763B (zh) * | 2019-05-09 | 2025-01-21 | 豪夫迈·罗氏有限公司 | 咪唑并[1,2-a]嘧啶的区域选择性合成 |
| US11912699B2 (en) | 2019-07-17 | 2024-02-27 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated |
| 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 |
| CA3228359A1 (en) | 2021-08-27 | 2023-03-02 | Genentech, Inc. | Methods of treating tau pathologies |
| EP4536358A1 (en) | 2022-06-13 | 2025-04-16 | Genentech Inc. | Methods of delaying or preventing the onset of alzheimer's disease using crenezumab |
| 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110182812A1 (en) * | 2009-03-23 | 2011-07-28 | Siemens Medical Solutions Usa, Inc. | Imaging Agents for Detecting Neurological Disorders |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE76515C (de) | F. MORA in Mailand | Verfahren zur Herstellung imitirter Ledertapete aus Baumwollstoff | ||
| DD76515A (enExample) * | ||||
| 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 |
| HUE032660T2 (en) * | 2006-03-30 | 2017-10-30 | Univ Pennsylvania | Styrylpyridine derivatives and their use for binding and imaging amyloid plaques |
| JP5647519B2 (ja) | 2007-09-13 | 2014-12-24 | コンサート ファーマシューティカルズ インコーポレイテッド | 重水素化カテコールおよびベンゾ［ｄ］［１，３］ジオキソールおよびその誘導体の合成 |
| SI2247558T2 (sl) | 2008-02-14 | 2024-10-30 | Eli Lilly And Company | Nova kontrastna sredstva za zaznavanje nevroloških disfunkcij |
| US8932557B2 (en) | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| US20100144657A1 (en) | 2008-12-09 | 2010-06-10 | Auspex Pharmaceuticals, Inc. | PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS |
| US8491869B2 (en) | 2009-03-23 | 2013-07-23 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| 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) |
| NZ610315A (en) * | 2010-11-15 | 2015-08-28 | Univ Leuven Kath | Antiviral condensed heterocyclic compounds |
| WO2013176698A1 (en) * | 2012-05-22 | 2013-11-28 | Eli Lilly And Company | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
| CN105358558B (zh) * | 2013-10-08 | 2017-09-26 | 豪夫迈·罗氏有限公司 | 作为tau‑pet‑配体的二氮杂咔唑衍生物 |
| CA2948721C (en) | 2014-05-13 | 2023-03-28 | F. Hoffmann-La Roche Ag | Deuterated compounds and uses thereof |
-
2015
- 2015-05-12 CA CA2948721A patent/CA2948721C/en active Active
- 2015-05-12 HR HRP20210641TT patent/HRP20210641T1/hr unknown
- 2015-05-12 SG SG10201805628TA patent/SG10201805628TA/en unknown
- 2015-05-12 JP JP2016567651A patent/JP6529986B2/ja active Active
- 2015-05-12 EP EP21155891.1A patent/EP3901145A1/en active Pending
- 2015-05-12 MX MX2020010847A patent/MX384604B/es unknown
- 2015-05-12 MX MX2016014615A patent/MX376163B/es active IP Right Grant
- 2015-05-12 RU RU2016147742A patent/RU2696492C2/ru active
- 2015-05-12 PT PT157252537T patent/PT3143011T/pt unknown
- 2015-05-12 PL PL15725253T patent/PL3143011T3/pl unknown
- 2015-05-12 RS RS20210532A patent/RS61810B1/sr unknown
- 2015-05-12 HU HUE15725253A patent/HUE053939T2/hu unknown
- 2015-05-12 WO PCT/EP2015/060447 patent/WO2015173225A1/en not_active Ceased
- 2015-05-12 KR KR1020167034871A patent/KR102530129B1/ko active Active
- 2015-05-12 LT LTEP15725253.7T patent/LT3143011T/lt unknown
- 2015-05-12 SG SG11201609281UA patent/SG11201609281UA/en unknown
- 2015-05-12 CN CN201910795177.8A patent/CN110483522B/zh active Active
- 2015-05-12 CN CN201580025219.XA patent/CN106459059B/zh active Active
- 2015-05-12 SI SI201531590T patent/SI3143011T1/sl unknown
- 2015-05-12 DK DK15725253.7T patent/DK3143011T3/da active
- 2015-05-12 KR KR1020237006997A patent/KR102618139B1/ko active Active
- 2015-05-12 EP EP15725253.7A patent/EP3143011B1/en active Active
- 2015-05-12 ES ES15725253T patent/ES2867814T3/es active Active
- 2015-05-12 AU AU2015261008A patent/AU2015261008B2/en active Active
- 2015-05-12 IL IL280791A patent/IL280791B2/en unknown
-
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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110182812A1 (en) * | 2009-03-23 | 2011-07-28 | Siemens Medical Solutions Usa, Inc. | Imaging Agents for Detecting Neurological Disorders |
Non-Patent Citations (1)
| Title |
|---|
| Zhang, W. et al., Journal of Alzheimer's Disease, 2012, 31(3), pp. 601-612. * |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |