AR097931A1 - Derivados de diazacarbazol como ligandos de tau para pet - Google Patents
Derivados de diazacarbazol como ligandos de tau para petInfo
- Publication number
- AR097931A1 AR097931A1 ARP140103712A ARP140103712A AR097931A1 AR 097931 A1 AR097931 A1 AR 097931A1 AR P140103712 A ARP140103712 A AR P140103712A AR P140103712 A ARP140103712 A AR P140103712A AR 097931 A1 AR097931 A1 AR 097931A1
- Authority
- AR
- Argentina
- Prior art keywords
- aggregates
- dipyrido
- pyridin
- pyrrole
- fluoro
- Prior art date
Links
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
-
- 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
-
- 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)
- Optics & Photonics (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cell Biology (AREA)
- General Physics & Mathematics (AREA)
- Biotechnology (AREA)
- Radiology & Medical Imaging (AREA)
- Food Science & Technology (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Pathology (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
La presente se refiere a un compuesto de fórmula general (1) en la que R es hidrógeno o tritio; F es flúor o ¹⁸flúor; o a una sal de adición de ácido farmacéuticamente aceptable. Los compuestos de fórmula (1) incluyen 2-(6-fluoro-piridin-3-il)-9H-dipirido[2,3-b;3,4-d]pirrol, ³H-2-(6-fluoro-piridin-3-il)-9H-dipirido[2,3-b;3,4-d]pirrol y [18F]-2-(6-fluoro-piridin-3-il)-9H-dipirido[2,3-b;3,4-d]pirrol. Los compuestos se pueden usar para la unión y la formación de imágenes de agregados de tau y los agregados de lámina b relacionados incluyendo entre otros agregados de b-amiloide o agregados de a-sinucleína.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13187764 | 2013-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR097931A1 true AR097931A1 (es) | 2016-04-20 |
Family
ID=49301396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140103712A AR097931A1 (es) | 2013-10-08 | 2014-10-06 | Derivados de diazacarbazol como ligandos de tau para pet |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US10004817B2 (es) |
| EP (1) | EP3055308B1 (es) |
| JP (1) | JP6194416B2 (es) |
| KR (1) | KR101770531B1 (es) |
| CN (1) | CN105358558B (es) |
| AR (1) | AR097931A1 (es) |
| AU (1) | AU2014333996B2 (es) |
| CA (1) | CA2917191C (es) |
| CL (1) | CL2016000728A1 (es) |
| CR (1) | CR20150663A (es) |
| DK (1) | DK3055308T3 (es) |
| EA (1) | EA028483B1 (es) |
| ES (1) | ES2657121T3 (es) |
| HK (1) | HK1215574A1 (es) |
| HR (1) | HRP20180049T1 (es) |
| HU (1) | HUE035413T2 (es) |
| IL (1) | IL243249A0 (es) |
| LT (1) | LT3055308T (es) |
| MA (1) | MA38935B1 (es) |
| MX (1) | MX2016002234A (es) |
| MY (1) | MY190196A (es) |
| NO (1) | NO3055308T3 (es) |
| PE (1) | PE20160159A1 (es) |
| PH (1) | PH12016500249B1 (es) |
| PL (1) | PL3055308T3 (es) |
| PT (1) | PT3055308T (es) |
| RS (1) | RS56777B1 (es) |
| SG (1) | SG11201602786UA (es) |
| SI (1) | SI3055308T1 (es) |
| TW (1) | TWI513698B (es) |
| UA (1) | UA116164C2 (es) |
| WO (1) | WO2015052105A1 (es) |
| ZA (1) | ZA201509013B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2907992T3 (es) | 2008-02-14 | 2022-04-27 | Lilly Co Eli | Agentes novedosos de obtención de imágenes para detectar disfunciones neurológicas |
| EP3055308B1 (en) | 2013-10-08 | 2017-11-22 | F.Hoffmann-La Roche Ag | Diazacarbazole derivatives as tau-pet-ligands |
| CN110483522B (zh) * | 2014-05-13 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 氘化杂环化合物和其作为成像剂的用途 |
| MX2017009505A (es) * | 2015-02-02 | 2017-11-02 | Ucb Biopharma Sprl | Derivados de 9h-pirrolo-dipiridina. |
| EP3322707A1 (en) | 2015-07-15 | 2018-05-23 | AC Immune SA | 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 |
| 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 |
| WO2018024642A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| WO2018024643A1 (en) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| SI3510031T1 (sl) | 2016-09-09 | 2021-03-31 | F. Hoffmann-La Roche Ag | Postopek za pripravo 2-(6-nitropiridin-3-il)-9H-dipirido(2,3-b;3',4'-d)pirola |
| US11306089B2 (en) | 2018-01-24 | 2022-04-19 | Life Molecular Imaging Limited | Gamma-carboline compounds for the detection of Tau aggregates |
| EA202091767A1 (ru) | 2018-01-24 | 2021-02-16 | Ац Иммуне Са | Новый способ получения визуализирующего соединения |
| CN111712265B (zh) * | 2018-01-24 | 2024-02-09 | Ac免疫有限公司 | 用于pet显像的诊断组合物、该诊断组合物的制备方法及其在诊断中的用途 |
| EP3743426A1 (en) | 2018-01-24 | 2020-12-02 | AC Immune SA | Azacarboline compounds for the detection of tau aggregates |
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 |
| ES2907992T3 (es) * | 2008-02-14 | 2022-04-27 | Lilly Co Eli | Agentes novedosos de obtención de imágenes para detectar disfunciones neurológicas |
| KR101764556B1 (ko) | 2008-06-11 | 2017-08-02 | 제넨테크, 인크. | 디아자카르바졸 및 사용 방법 |
| JP2011529086A (ja) * | 2008-07-24 | 2011-12-01 | シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド | Ａｄ病変を同定するために有用な造影剤 |
| EP2411057B1 (en) | 2009-03-23 | 2020-05-06 | Eli Lilly and Company | 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 |
| EP3055308B1 (en) | 2013-10-08 | 2017-11-22 | F.Hoffmann-La Roche Ag | Diazacarbazole derivatives as tau-pet-ligands |
-
2014
- 2014-10-06 EP EP14781169.9A patent/EP3055308B1/en active Active
- 2014-10-06 SG SG11201602786UA patent/SG11201602786UA/en unknown
- 2014-10-06 EA EA201690515A patent/EA028483B1/ru not_active IP Right Cessation
- 2014-10-06 CA CA2917191A patent/CA2917191C/en active Active
- 2014-10-06 HU HUE14781169A patent/HUE035413T2/en unknown
- 2014-10-06 RS RS20180058A patent/RS56777B1/sr unknown
- 2014-10-06 CN CN201480037389.5A patent/CN105358558B/zh active Active
- 2014-10-06 PT PT147811699T patent/PT3055308T/pt unknown
- 2014-10-06 JP JP2016515518A patent/JP6194416B2/ja active Active
- 2014-10-06 DK DK14781169.9T patent/DK3055308T3/en active
- 2014-10-06 MY MYPI2016000604A patent/MY190196A/en unknown
- 2014-10-06 SI SI201430549T patent/SI3055308T1/en unknown
- 2014-10-06 UA UAA201604290A patent/UA116164C2/uk unknown
- 2014-10-06 TW TW103134795A patent/TWI513698B/zh active
- 2014-10-06 MX MX2016002234A patent/MX2016002234A/es active IP Right Grant
- 2014-10-06 PL PL14781169T patent/PL3055308T3/pl unknown
- 2014-10-06 WO PCT/EP2014/071283 patent/WO2015052105A1/en active Application Filing
- 2014-10-06 ES ES14781169.9T patent/ES2657121T3/es 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 LT LTEP14781169.9T patent/LT3055308T/lt unknown
- 2014-10-06 KR KR1020167008013A patent/KR101770531B1/ko active IP Right Grant
- 2014-10-06 AU AU2014333996A patent/AU2014333996B2/en active Active
- 2014-10-06 PE PE2015002706A patent/PE20160159A1/es active IP Right Grant
-
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
- 2016-03-24 HK HK16103514.3A patent/HK1215574A1/zh 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
-
2018
- 2018-01-10 HR HRP20180049TT patent/HRP20180049T1/hr unknown
- 2018-05-15 US US15/980,080 patent/US11058781B2/en active Active
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