UA116164C2 - Похідні діазокарбазолу як пет-ліганди білка tau - Google Patents
Похідні діазокарбазолу як пет-ліганди білка tauInfo
- Publication number
- UA116164C2 UA116164C2 UAA201604290A UAA201604290A UA116164C2 UA 116164 C2 UA116164 C2 UA 116164C2 UA A201604290 A UAA201604290 A UA A201604290A UA A201604290 A UAA201604290 A UA A201604290A UA 116164 C2 UA116164 C2 UA 116164C2
- Authority
- UA
- Ukraine
- Prior art keywords
- fluoro
- aggregates
- dipyrido
- pyridin
- pyrrole
- Prior art date
Links
- BZHCVCNZIJZMRN-UHFFFAOYSA-N 9h-pyridazino[3,4-b]indole Chemical class N1=CC=C2C3=CC=CC=C3NC2=N1 BZHCVCNZIJZMRN-UHFFFAOYSA-N 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- FDMOHTOITMTGNG-UHFFFAOYSA-N 11-(6-fluoropyridin-3-yl)-4,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene Chemical compound Fc1ccc(cn1)-c1ccc2c(n1)[nH]c1ccncc21 FDMOHTOITMTGNG-UHFFFAOYSA-N 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical group [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 102000003802 alpha-Synuclein Human genes 0.000 abstract 1
- 108090000185 alpha-Synuclein Proteins 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 238000003384 imaging method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052722 tritium Chemical group 0.000 abstract 1
Classifications
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- 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
- 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
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
- A61K49/10—Organic compounds
-
- 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
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- 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
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2800/00—Detection or diagnosis of diseases
- G01N2800/28—Neurological disorders
- G01N2800/2814—Dementia; Cognitive disorders
- G01N2800/2821—Alzheimer
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Physics & Mathematics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Optics & Photonics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biotechnology (AREA)
- Cell Biology (AREA)
- Microbiology (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Food Science & Technology (AREA)
- Radiology & Medical Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Даний винахід належать до сполуки загальної формули EMBED ISISServer , I де R означає водень або тритій; F означає фтор або 18фтор; або до її фармацевтично прийнятної кислотно-адитивної солі. Сполуки формули І включають: 2-(6-фтор-піридин-3-іл)-9Н-дипіридо[2,3-b;3',4'-d]пірол, 3Н-2-(6-фтор-піридин-3-іл)-9Н-дипіридо[2,3-b;3',4'-d]пірол і [18Р]-2-(6-фтор-піридин-3-іл)-9Н-дипіридо[2,3-b;3',4'-d]пірол. Зазначені сполуки можуть застосовуватися для зв'язування і візуалізації агрегатів білка tau і асоційованих бета-складчастих агрегатів, включаючи серед інших агрегати бета-амілоїду або агрегати альфа-синуклеїну
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13187764 | 2013-10-08 | ||
| PCT/EP2014/071283 WO2015052105A1 (en) | 2013-10-08 | 2014-10-06 | Diazacarbazole derivatives as tau-pet-ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA116164C2 true UA116164C2 (uk) | 2018-02-12 |
Family
ID=49301396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201604290A UA116164C2 (uk) | 2013-10-08 | 2014-10-06 | Похідні діазокарбазолу як пет-ліганди білка tau |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US10004817B2 (uk) |
| EP (1) | EP3055308B1 (uk) |
| JP (1) | JP6194416B2 (uk) |
| KR (1) | KR101770531B1 (uk) |
| CN (1) | CN105358558B (uk) |
| AR (1) | AR097931A1 (uk) |
| AU (1) | AU2014333996B2 (uk) |
| CA (1) | CA2917191C (uk) |
| CL (1) | CL2016000728A1 (uk) |
| CR (1) | CR20150663A (uk) |
| DK (1) | DK3055308T3 (uk) |
| EA (1) | EA028483B1 (uk) |
| ES (1) | ES2657121T3 (uk) |
| HR (1) | HRP20180049T1 (uk) |
| HU (1) | HUE035413T2 (uk) |
| IL (1) | IL243249A0 (uk) |
| LT (1) | LT3055308T (uk) |
| MA (1) | MA38935B1 (uk) |
| MX (1) | MX373153B (uk) |
| MY (1) | MY190196A (uk) |
| NO (1) | NO3055308T3 (uk) |
| PE (1) | PE20160159A1 (uk) |
| PH (1) | PH12016500249B1 (uk) |
| PL (1) | PL3055308T3 (uk) |
| PT (1) | PT3055308T (uk) |
| RS (1) | RS56777B1 (uk) |
| SG (1) | SG11201602786UA (uk) |
| SI (1) | SI3055308T1 (uk) |
| TW (1) | TWI513698B (uk) |
| UA (1) | UA116164C2 (uk) |
| WO (1) | WO2015052105A1 (uk) |
| ZA (1) | ZA201509013B (uk) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2247558T5 (pl) | 2008-02-14 | 2024-10-14 | Eli Lilly And Company | Nowe środki obrazujące do wykrywania czynnościowych zaburzeń neurologicznych |
| TWI513698B (zh) | 2013-10-08 | 2015-12-21 | Hoffmann La Roche | 做為ｔａｕ－ｐｅｔ－配位體之二氮雜咔唑衍生物 |
| EP3143011B1 (en) | 2014-05-13 | 2021-03-03 | F. Hoffmann-La Roche AG | Deuterated heterocyclic compounds and their use as imaging agents |
| DK3253762T3 (da) * | 2015-02-02 | 2021-07-19 | UCB Biopharma SRL | 9h-pyrrolo-dipyridinderivater. |
| US20180264146A1 (en) | 2015-07-15 | 2018-09-20 | Ac Immune S.A. | Novel imaging compounds |
| EP3118202A1 (en) | 2015-07-15 | 2017-01-18 | AC Immune S.A. | Dihydropyridopyrrole derivatives as tau-pet-ligands |
| US10865207B2 (en) | 2016-07-22 | 2020-12-15 | Ac Immune S.A. | Compounds for imaging Tau protein aggregates |
| CN115650982A (zh) | 2016-07-22 | 2023-01-31 | 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 |
| WO2018046428A1 (en) * | 2016-09-09 | 2018-03-15 | F. Hoffmann-La Roche Ag | Process for preparation of 2-(6-nitropyridin-3-yl)-9h-dipyrido[2,3-b;3',4'-d]pyrrole |
| 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 |
| CA3088232A1 (en) * | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Diagnostic compositions for pet imaging, a method for manufacturing the diagnostic composition and its use in diagnostics |
| AU2019212170B2 (en) | 2018-01-24 | 2022-12-22 | Ac Immune Sa | Novel method of preparing an imaging compound |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8932557B2 (en) * | 2008-02-14 | 2015-01-13 | Eli Lilly And Company | Imaging agents for detecting neurological dysfunction |
| PL2247558T5 (pl) * | 2008-02-14 | 2024-10-14 | Eli Lilly And Company | Nowe środki obrazujące do wykrywania czynnościowych zaburzeń neurologicznych |
| AU2009258115B2 (en) | 2008-06-11 | 2015-01-29 | Genentech, Inc. | Diazacarbazoles and methods of use |
| US8420052B2 (en) | 2008-07-24 | 2013-04-16 | Siemens Medical Solutions Usa, Inc. | Imaging agents useful for identifying AD pathology |
| CA2756137C (en) | 2009-03-23 | 2015-11-24 | Siemens Medical Solutions Usa, Inc. | Imaging agents for detecting neurological disorders |
| US8691187B2 (en) * | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| US20110183938A1 (en) | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
| US20150368244A1 (en) * | 2011-01-31 | 2015-12-24 | Genentech, Inc. | Diazacarbazoles and methods of use |
| TWI513698B (zh) | 2013-10-08 | 2015-12-21 | Hoffmann La Roche | 做為ｔａｕ－ｐｅｔ－配位體之二氮雜咔唑衍生物 |
-
2014
- 2014-10-06 TW TW103134795A patent/TWI513698B/zh active
- 2014-10-06 PT PT147811699T patent/PT3055308T/pt unknown
- 2014-10-06 WO PCT/EP2014/071283 patent/WO2015052105A1/en not_active Ceased
- 2014-10-06 HU HUE14781169A patent/HUE035413T2/en unknown
- 2014-10-06 HR HRP20180049TT patent/HRP20180049T1/hr unknown
- 2014-10-06 DK DK14781169.9T patent/DK3055308T3/en active
- 2014-10-06 KR KR1020167008013A patent/KR101770531B1/ko active Active
- 2014-10-06 CN CN201480037389.5A patent/CN105358558B/zh active Active
- 2014-10-06 PE PE2015002706A patent/PE20160159A1/es active IP Right Grant
- 2014-10-06 EA EA201690515A patent/EA028483B1/ru not_active IP Right Cessation
- 2014-10-06 MY MYPI2016000604A patent/MY190196A/en unknown
- 2014-10-06 CA CA2917191A patent/CA2917191C/en active Active
- 2014-10-06 LT LTEP14781169.9T patent/LT3055308T/lt unknown
- 2014-10-06 SG SG11201602786UA patent/SG11201602786UA/en unknown
- 2014-10-06 SI SI201430549T patent/SI3055308T1/en unknown
- 2014-10-06 MX MX2016002234A patent/MX373153B/es active IP Right Grant
- 2014-10-06 PL PL14781169T patent/PL3055308T3/pl unknown
- 2014-10-06 ES ES14781169.9T patent/ES2657121T3/es active Active
- 2014-10-06 EP EP14781169.9A patent/EP3055308B1/en active Active
- 2014-10-06 JP JP2016515518A patent/JP6194416B2/ja active Active
- 2014-10-06 AU AU2014333996A patent/AU2014333996B2/en active Active
- 2014-10-06 NO NO14781169A patent/NO3055308T3/no unknown
- 2014-10-06 AR ARP140103712A patent/AR097931A1/es active IP Right Grant
- 2014-10-06 RS RS20180058A patent/RS56777B1/sr unknown
- 2014-10-06 UA UAA201604290A patent/UA116164C2/uk unknown
-
2015
- 2015-12-10 ZA ZA2015/09013A patent/ZA201509013B/en unknown
- 2015-12-15 CR CR20150663A patent/CR20150663A/es unknown
- 2015-12-21 IL IL243249A patent/IL243249A0/en active IP Right Grant
-
2016
- 2016-02-04 PH PH12016500249A patent/PH12016500249B1/en unknown
- 2016-03-25 MA MA38935A patent/MA38935B1/fr unknown
- 2016-03-30 CL CL2016000728A patent/CL2016000728A1/es unknown
- 2016-04-07 US US15/093,366 patent/US10004817B2/en active Active
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2018
- 2018-05-15 US US15/980,080 patent/US11058781B2/en active Active
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