MA38935B1 - Dérivés de diazacarbazole à titre de ligands tau-pet - Google Patents
Dérivés de diazacarbazole à titre de ligands tau-petInfo
- Publication number
- MA38935B1 MA38935B1 MA38935A MA38935A MA38935B1 MA 38935 B1 MA38935 B1 MA 38935B1 MA 38935 A MA38935 A MA 38935A MA 38935 A MA38935 A MA 38935A MA 38935 B1 MA38935 B1 MA 38935B1
- Authority
- MA
- Morocco
- 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 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 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
- 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
- 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
-
- 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
-
- 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
-
- 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
- C07D471/12—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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (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)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Urology & Nephrology (AREA)
- Optics & Photonics (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Microbiology (AREA)
- Pathology (AREA)
- Biotechnology (AREA)
- Radiology & Medical Imaging (AREA)
- Cell Biology (AREA)
- General Physics & Mathematics (AREA)
- Food Science & Technology (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (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
Cette invention concerne un composé de formule générale (i) dans laquelle r est un atome d'hydrogène ou de tritium ; f est un fluoro ou 18fluoro ; ou un sel d'addition d'acide pharmaceutiquement acceptable de celui-ci. Les composés de formule i comprennent le 2-(6-fluoro-pyridin-3-yl)-9h-dipyrido[2,3-b; 3',4'-d]pyrrole, le 3h-2-(6-fluoro-pyridin-3-yl)-9h-dipyrido[2,3-b;3',4'-d]pyrrole et le [18f]-2-(6-fluoro-pyridin-3-yl)-9h-dipyrido[2,3-b;3',4'-d]pyrrole. Ils peuvent être utilisés pour lier et soumettre à imagerie les agrégats tau et les agrégats de feuillets bêta associés comprenant, entre autres, les agrégats bêta-amyloïdes ou les agrégats d'alpha-synucléine.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13187764 | 2013-10-08 | ||
| PCT/EP2014/071283 WO2015052105A1 (fr) | 2013-10-08 | 2014-10-06 | Dérivés de diazacarbazole à titre de ligands tau-pet |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA38935A1 MA38935A1 (fr) | 2016-04-29 |
| MA38935B1 true MA38935B1 (fr) | 2016-12-30 |
Family
ID=49301396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA38935A MA38935B1 (fr) | 2013-10-08 | 2016-03-25 | Dérivés de diazacarbazole à titre de ligands tau-pet |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US10004817B2 (fr) |
| EP (1) | EP3055308B1 (fr) |
| JP (1) | JP6194416B2 (fr) |
| KR (1) | KR101770531B1 (fr) |
| CN (1) | CN105358558B (fr) |
| AR (1) | AR097931A1 (fr) |
| AU (1) | AU2014333996B2 (fr) |
| CA (1) | CA2917191C (fr) |
| CL (1) | CL2016000728A1 (fr) |
| CR (1) | CR20150663A (fr) |
| DK (1) | DK3055308T3 (fr) |
| EA (1) | EA028483B1 (fr) |
| ES (1) | ES2657121T3 (fr) |
| HR (1) | HRP20180049T1 (fr) |
| HU (1) | HUE035413T2 (fr) |
| IL (1) | IL243249A0 (fr) |
| LT (1) | LT3055308T (fr) |
| MA (1) | MA38935B1 (fr) |
| MX (1) | MX373153B (fr) |
| MY (1) | MY190196A (fr) |
| NO (1) | NO3055308T3 (fr) |
| PE (1) | PE20160159A1 (fr) |
| PH (1) | PH12016500249A1 (fr) |
| PL (1) | PL3055308T3 (fr) |
| PT (1) | PT3055308T (fr) |
| RS (1) | RS56777B1 (fr) |
| SG (1) | SG11201602786UA (fr) |
| SI (1) | SI3055308T1 (fr) |
| TW (1) | TWI513698B (fr) |
| UA (1) | UA116164C2 (fr) |
| WO (1) | WO2015052105A1 (fr) |
| ZA (1) | ZA201509013B (fr) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110046378A1 (en) | 2008-02-14 | 2011-02-24 | Siemens Medical Solutions Usa, Inc. | Novel Imaging Agents for Detecting Neurological Dysfunction |
| 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 |
| US20180022748A1 (en) * | 2015-02-02 | 2018-01-25 | Ucb Biopharma Sprl | 9h-pyrrolo-dipyridine derivatives |
| EP3118202A1 (fr) | 2015-07-15 | 2017-01-18 | AC Immune S.A. | Dérivés de dihydropyridopyrrole en tant que ligands tau-pet |
| US20180264146A1 (en) | 2015-07-15 | 2018-09-20 | Ac Immune S.A. | Novel imaging compounds |
| KR102472003B1 (ko) * | 2016-07-22 | 2022-11-29 | 에이씨 이뮨 에스에이 | 타우 단백질 응집체를 이미징하기 위한 화합물 |
| EP3487545A1 (fr) | 2016-07-22 | 2019-05-29 | AC Immune S.A. | Composés pour l'imagerie d'agrégats de protéines tau |
| WO2018024643A1 (fr) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | Dérivés de 9h-pyrrolo-dipyridine |
| WO2018024642A1 (fr) | 2016-08-02 | 2018-02-08 | Ucb Biopharma Sprl | Dérivés de 9h-pyrrolo-dipyridine |
| WO2018046428A1 (fr) * | 2016-09-09 | 2018-03-15 | F. Hoffmann-La Roche Ag | Procédé de préparation de 2- (6-nitropyridin-3-yl) -9h-dipyrido [2,3-b; 3', 4'-d] pyrrole |
| IL275990B2 (en) * | 2018-01-24 | 2024-08-01 | Ac Immune Sa | Diagnostic preparations for PET imaging, a method for producing a diagnostic preparation and its use in diagnostics |
| WO2019145291A1 (fr) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Composés gamma-carboline pour la détection d'agrégats de tau |
| WO2019145292A1 (fr) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Composés d'azacarboline pour la détection d'agrégats de tau |
| KR20200113234A (ko) * | 2018-01-24 | 2020-10-06 | 에이씨 이뮨 에스.에이. | 이미징 화합물을 제조하는 신규한 방법 |
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 |
| US20110046378A1 (en) * | 2008-02-14 | 2011-02-24 | Siemens Medical Solutions Usa, Inc. | Novel Imaging Agents for Detecting Neurological Dysfunction |
| BRPI0909957A2 (pt) | 2008-06-11 | 2016-04-19 | Genentech Inc | "composto, composição farmacêutica, método de inibir o crescimento anormal de células ou de tratar um distúrbio hiperproliferativo em um mamífero, método de tratamento do câncer em um mamífero" |
| CA2731738A1 (fr) * | 2008-07-24 | 2010-01-28 | Siemens Medical Solutions Usa, Inc. | Agents d'imagerie utiles pour identifier une pathologie |
| 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 |
| 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 |
| 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 |
-
2014
- 2014-10-06 JP JP2016515518A patent/JP6194416B2/ja active Active
- 2014-10-06 NO NO14781169A patent/NO3055308T3/no unknown
- 2014-10-06 EA EA201690515A patent/EA028483B1/ru not_active IP Right Cessation
- 2014-10-06 WO PCT/EP2014/071283 patent/WO2015052105A1/fr not_active Ceased
- 2014-10-06 AR ARP140103712A patent/AR097931A1/es active IP Right Grant
- 2014-10-06 MX MX2016002234A patent/MX373153B/es active IP Right Grant
- 2014-10-06 TW TW103134795A patent/TWI513698B/zh active
- 2014-10-06 MY MYPI2016000604A patent/MY190196A/en unknown
- 2014-10-06 HU HUE14781169A patent/HUE035413T2/en unknown
- 2014-10-06 RS RS20180058A patent/RS56777B1/sr unknown
- 2014-10-06 HR HRP20180049TT patent/HRP20180049T1/hr unknown
- 2014-10-06 AU AU2014333996A patent/AU2014333996B2/en active Active
- 2014-10-06 CA CA2917191A patent/CA2917191C/fr active Active
- 2014-10-06 CN CN201480037389.5A patent/CN105358558B/zh active Active
- 2014-10-06 PT PT147811699T patent/PT3055308T/pt unknown
- 2014-10-06 PL PL14781169T patent/PL3055308T3/pl unknown
- 2014-10-06 DK DK14781169.9T patent/DK3055308T3/en active
- 2014-10-06 PE PE2015002706A patent/PE20160159A1/es active IP Right Grant
- 2014-10-06 KR KR1020167008013A patent/KR101770531B1/ko active Active
- 2014-10-06 ES ES14781169.9T patent/ES2657121T3/es active Active
- 2014-10-06 SI SI201430549T patent/SI3055308T1/en unknown
- 2014-10-06 SG SG11201602786UA patent/SG11201602786UA/en unknown
- 2014-10-06 LT LTEP14781169.9T patent/LT3055308T/lt unknown
- 2014-10-06 EP EP14781169.9A patent/EP3055308B1/fr active Active
- 2014-10-06 UA UAA201604290A patent/UA116164C2/uk unknown
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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/PH12016500249A1/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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