AU2016214537B2 - 9H-pyrrolo-dipyridine derivatives - Google Patents
9H-pyrrolo-dipyridine derivatives Download PDFInfo
- Publication number
- AU2016214537B2 AU2016214537B2 AU2016214537A AU2016214537A AU2016214537B2 AU 2016214537 B2 AU2016214537 B2 AU 2016214537B2 AU 2016214537 A AU2016214537 A AU 2016214537A AU 2016214537 A AU2016214537 A AU 2016214537A AU 2016214537 B2 AU2016214537 B2 AU 2016214537B2
- Authority
- AU
- Australia
- Prior art keywords
- pyrrolo
- optionally substituted
- methyl
- dipyridine
- halogens
- 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 Cc(cc1*)nc(*)c1-c1ccc(c2cnccc2[n]2)c2n1 Chemical compound Cc(cc1*)nc(*)c1-c1ccc(c2cnccc2[n]2)c2n1 0.000 description 9
- YJFDJTNGFPHWAM-UHFFFAOYSA-N CC1(C)OB(c2n[nH]c(C)c2)OC1(C)C Chemical compound CC1(C)OB(c2n[nH]c(C)c2)OC1(C)C YJFDJTNGFPHWAM-UHFFFAOYSA-N 0.000 description 1
- DINGZOCGMDSQHE-UHFFFAOYSA-N CNC(c(cc1)ncc1-c1ccc(c2cnccc2[nH]2)c2n1)=O Chemical compound CNC(c(cc1)ncc1-c1ccc(c2cnccc2[nH]2)c2n1)=O DINGZOCGMDSQHE-UHFFFAOYSA-N 0.000 description 1
- JHFJFJHQZAIQLE-UHFFFAOYSA-N CNC(c(cn1)ccc1Br)=O Chemical compound CNC(c(cn1)ccc1Br)=O JHFJFJHQZAIQLE-UHFFFAOYSA-N 0.000 description 1
- BQJQGNUGTXEDOF-UHFFFAOYSA-N CNC(c(cn1)ccc1[Sn](C)(C)C)=O Chemical compound CNC(c(cn1)ccc1[Sn](C)(C)C)=O BQJQGNUGTXEDOF-UHFFFAOYSA-N 0.000 description 1
- MFKBDJBBFKJRDS-UHFFFAOYSA-N CNC(c1ccc(-c2ccc(c(c([nH]3)c4)cnc4OC)c3n2)nc1)=O Chemical compound CNC(c1ccc(-c2ccc(c(c([nH]3)c4)cnc4OC)c3n2)nc1)=O MFKBDJBBFKJRDS-UHFFFAOYSA-N 0.000 description 1
- NCFMDIJKEYGCRD-UHFFFAOYSA-N COc1c[nH]nc1 Chemical compound COc1c[nH]nc1 NCFMDIJKEYGCRD-UHFFFAOYSA-N 0.000 description 1
- DZCDYZWUSHIPHQ-UHFFFAOYSA-N COc1c[n](-c(cc2)nc3c2c(ccnc2)c2[nH]3)nc1 Chemical compound COc1c[n](-c(cc2)nc3c2c(ccnc2)c2[nH]3)nc1 DZCDYZWUSHIPHQ-UHFFFAOYSA-N 0.000 description 1
- ZYIUFBZANBZCOW-UHFFFAOYSA-N C[Sn](C)(C)c(nc1)ccc1C(N)=O Chemical compound C[Sn](C)(C)c(nc1)ccc1C(N)=O ZYIUFBZANBZCOW-UHFFFAOYSA-N 0.000 description 1
- SBWXKXXPHSUKRY-UHFFFAOYSA-N ClC1=NC2C=Cc3ccncc3C2C=C1 Chemical compound ClC1=NC2C=Cc3ccncc3C2C=C1 SBWXKXXPHSUKRY-UHFFFAOYSA-N 0.000 description 1
- QCTHDAPPTWLTGR-UHFFFAOYSA-N Clc(cc1)nc2c1c(cncc1)c1[nH]2 Chemical compound Clc(cc1)nc2c1c(cncc1)c1[nH]2 QCTHDAPPTWLTGR-UHFFFAOYSA-N 0.000 description 1
- VZRAAQURGGLCMY-UHFFFAOYSA-N Clc1ccc(c(ccnc2)c2[nH]2)c2n1 Chemical compound Clc1ccc(c(ccnc2)c2[nH]2)c2n1 VZRAAQURGGLCMY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
- 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
- A61K51/0463—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- 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
-
- 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
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15153448.4 | 2015-02-02 | ||
| EP15153448 | 2015-02-02 | ||
| PCT/EP2016/051993 WO2016124508A1 (en) | 2015-02-02 | 2016-01-29 | 9h-pyrrolo-dipyridine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2016214537A1 AU2016214537A1 (en) | 2017-08-03 |
| AU2016214537B2 true AU2016214537B2 (en) | 2018-05-10 |
Family
ID=52477553
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016214537A Active AU2016214537B2 (en) | 2015-02-02 | 2016-01-29 | 9H-pyrrolo-dipyridine derivatives |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US20180022748A1 (enExample) |
| EP (1) | EP3253762B1 (enExample) |
| JP (1) | JP6579670B2 (enExample) |
| KR (1) | KR102621513B1 (enExample) |
| CN (1) | CN107207508B (enExample) |
| AU (1) | AU2016214537B2 (enExample) |
| BR (1) | BR112017016311A2 (enExample) |
| CA (1) | CA2973648C (enExample) |
| CL (1) | CL2017001923A1 (enExample) |
| DK (1) | DK3253762T3 (enExample) |
| EA (1) | EA036518B1 (enExample) |
| ES (1) | ES2875734T3 (enExample) |
| IL (1) | IL253381B (enExample) |
| MX (1) | MX378155B (enExample) |
| MY (1) | MY191590A (enExample) |
| SG (1) | SG11201705727TA (enExample) |
| WO (1) | WO2016124508A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009102498A1 (en) | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel imaging agents for detecting neurological dysfunction |
| WO2016124508A1 (en) * | 2015-02-02 | 2016-08-11 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| 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 |
| SG11201811311VA (en) | 2016-07-22 | 2019-01-30 | Ac Immune Sa | Compounds for imaging tau protein aggregates |
| ES2847903T3 (es) * | 2016-09-09 | 2021-08-04 | Hoffmann La Roche | Procedimiento para la preparación de 2-(6-nitropiridin-3-il)-9H-dipirido[2,3-b;3',4'-d]pirrol |
| AU2017367872B2 (en) * | 2016-11-01 | 2022-03-31 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| JPWO2018221728A1 (ja) | 2017-06-02 | 2020-04-02 | 富士フイルム富山化学株式会社 | アルツハイマー型認知症予防または治療剤 |
| CN110691595A (zh) | 2017-06-02 | 2020-01-14 | 富士胶片富山化学株式会社 | β-淀粉样蛋白量减少剂 |
| JP7133547B2 (ja) | 2017-06-02 | 2022-09-08 | 富士フイルム富山化学株式会社 | 脊髄小脳変性症予防または治療剤 |
| JP7370859B2 (ja) * | 2017-06-02 | 2023-10-30 | 富士フイルム富山化学株式会社 | タウオパチー予防または治療剤 |
| CN116473962A (zh) | 2017-06-02 | 2023-07-25 | 富士胶片富山化学株式会社 | 脑萎缩预防或治疗剂 |
| WO2019088083A1 (ja) | 2017-10-30 | 2019-05-09 | 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 |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| US20210041447A1 (en) * | 2018-01-24 | 2021-02-11 | Ac Immune Sa | Azacarboline compounds for the detection of tau aggregates |
| CN111868062B (zh) * | 2018-01-24 | 2023-07-07 | Ac免疫有限公司 | 制备显像化合物的方法 |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009102498A1 (en) * | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel imaging agents for detecting neurological dysfunction |
| WO2015052105A1 (en) * | 2013-10-08 | 2015-04-16 | F. Hoffmann-La Roche Ag | Diazacarbazole derivatives as tau-pet-ligands |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1268771A (en) | 1968-03-15 | 1972-03-29 | Glaxo Lab Ltd | Azacarbazoles |
| WO2008132454A1 (en) * | 2007-04-26 | 2008-11-06 | Ge Healthcare Limited | Carbolines and their use as imaging agents |
| CN102325752B (zh) * | 2008-12-19 | 2015-02-04 | 百时美施贵宝公司 | 咔唑和咔啉激酶抑制剂 |
| CA2873963C (en) * | 2012-05-22 | 2017-04-11 | Eli Lilly And Company | Carboline and carbazole based imaging agents for detecting neurological dysfunction |
| US20160115162A1 (en) | 2013-05-31 | 2016-04-28 | The General Hospital Corporation | Radiosynthesis of Tau Radiopharmaceuticals |
| WO2015010263A1 (en) * | 2013-07-24 | 2015-01-29 | Telefonaktiebolaget L M Ericsson(Publ) | Method and apparautus relating to reception of radio signals |
| US10662193B2 (en) * | 2014-01-21 | 2020-05-26 | Ac Immune Sa | Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins |
| WO2016124508A1 (en) * | 2015-02-02 | 2016-08-11 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
-
2016
- 2016-01-29 WO PCT/EP2016/051993 patent/WO2016124508A1/en not_active Ceased
- 2016-01-29 MX MX2017009505A patent/MX378155B/es unknown
- 2016-01-29 ES ES16702121T patent/ES2875734T3/es active Active
- 2016-01-29 CA CA2973648A patent/CA2973648C/en active Active
- 2016-01-29 US US15/547,980 patent/US20180022748A1/en not_active Abandoned
- 2016-01-29 DK DK16702121.1T patent/DK3253762T3/da active
- 2016-01-29 EP EP16702121.1A patent/EP3253762B1/en active Active
- 2016-01-29 BR BR112017016311A patent/BR112017016311A2/pt not_active Application Discontinuation
- 2016-01-29 KR KR1020177024371A patent/KR102621513B1/ko active Active
- 2016-01-29 JP JP2017540724A patent/JP6579670B2/ja active Active
- 2016-01-29 AU AU2016214537A patent/AU2016214537B2/en active Active
- 2016-01-29 EA EA201791733A patent/EA036518B1/ru not_active IP Right Cessation
- 2016-01-29 MY MYPI2017702668A patent/MY191590A/en unknown
- 2016-01-29 CN CN201680008314.3A patent/CN107207508B/zh active Active
- 2016-01-29 SG SG11201705727TA patent/SG11201705727TA/en unknown
-
2017
- 2017-07-10 IL IL253381A patent/IL253381B/en active IP Right Grant
- 2017-07-27 CL CL2017001923A patent/CL2017001923A1/es unknown
-
2020
- 2020-01-22 US US16/749,537 patent/US11312716B2/en active Active
-
2022
- 2022-03-21 US US17/700,075 patent/US12006316B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009102498A1 (en) * | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel imaging agents for detecting neurological dysfunction |
| WO2015052105A1 (en) * | 2013-10-08 | 2015-04-16 | F. Hoffmann-La Roche Ag | Diazacarbazole derivatives as tau-pet-ligands |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018503673A (ja) | 2018-02-08 |
| US20210047326A1 (en) | 2021-02-18 |
| MY191590A (en) | 2022-06-30 |
| IL253381A0 (en) | 2017-09-28 |
| MX378155B (es) | 2025-03-10 |
| ES2875734T3 (es) | 2021-11-11 |
| JP6579670B2 (ja) | 2019-09-25 |
| EP3253762B1 (en) | 2021-05-05 |
| KR102621513B1 (ko) | 2024-01-04 |
| IL253381B (en) | 2020-10-29 |
| EA036518B1 (ru) | 2020-11-18 |
| CA2973648C (en) | 2023-09-26 |
| CN107207508B (zh) | 2020-02-28 |
| AU2016214537A1 (en) | 2017-08-03 |
| DK3253762T3 (da) | 2021-07-19 |
| BR112017016311A2 (pt) | 2018-03-27 |
| CL2017001923A1 (es) | 2018-02-16 |
| US20220213103A1 (en) | 2022-07-07 |
| KR20170113607A (ko) | 2017-10-12 |
| EP3253762A1 (en) | 2017-12-13 |
| WO2016124508A1 (en) | 2016-08-11 |
| EA201791733A1 (ru) | 2018-01-31 |
| US12006316B2 (en) | 2024-06-11 |
| US11312716B2 (en) | 2022-04-26 |
| MX2017009505A (es) | 2017-11-02 |
| US20180022748A1 (en) | 2018-01-25 |
| SG11201705727TA (en) | 2017-08-30 |
| CN107207508A (zh) | 2017-09-26 |
| CA2973648A1 (en) | 2016-08-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |