PE20160159A1 - Derivados de diazacarbazol como ligandos de tau para pet - Google Patents
Derivados de diazacarbazol como ligandos de tau para petInfo
- Publication number
- PE20160159A1 PE20160159A1 PE2015002706A PE2015002706A PE20160159A1 PE 20160159 A1 PE20160159 A1 PE 20160159A1 PE 2015002706 A PE2015002706 A PE 2015002706A PE 2015002706 A PE2015002706 A PE 2015002706A PE 20160159 A1 PE20160159 A1 PE 20160159A1
- Authority
- PE
- Peru
- Prior art keywords
- aggregates
- tau
- pet
- beta
- compounds
- 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
- 208000024827 Alzheimer disease Diseases 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 compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000001514 detection method Methods 0.000 abstract 1
- 238000012544 monitoring process Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
- A61K51/0455—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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
- Hematology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Microbiology (AREA)
- Analytical Chemistry (AREA)
- Cell Biology (AREA)
- Biotechnology (AREA)
- Radiology & Medical Imaging (AREA)
- Pathology (AREA)
- Food Science & Technology (AREA)
- General Physics & Mathematics (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
SE REFIERE A COMPUESTOS DE FORMULA GENERAL I EN LA CUAL R ES H O TRITIO; Y F ES F O 18F; O SALES DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. DICHOS COMPUESTOS TIENEN AFINIDAD POR AGREGADOS DE TAU Y OTROS AGREGADOS DE LAMINAS BETA RELACIONADOS, INCLUYENDO AGREGADOS DE BETA-AMILOIDE O AGREGADOS DE ALFA-SINUCLEINA, POR LO CUAL SON UTILES COMO LIGANDOS PARA LA DETECCION DE AGREGADOS DE TAU EN EL CEREBRO EN EL DIAGNOSTICO Y MONITORIZACION DE LA ENFERMEDAD DE ALZHEIMER POR FORMACION DE IMAGENES IN VIVO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13187764 | 2013-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160159A1 true PE20160159A1 (es) | 2016-03-18 |
Family
ID=49301396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015002706A PE20160159A1 (es) | 2013-10-08 | 2014-10-06 | Derivados de diazacarbazol como ligandos de tau para pet |
Country Status (32)
| 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) |
| HR (1) | HRP20180049T1 (es) |
| HU (1) | HUE035413T2 (es) |
| IL (1) | IL243249A0 (es) |
| LT (1) | LT3055308T (es) |
| MA (1) | MA38935B1 (es) |
| MX (1) | MX373153B (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 |
|---|---|---|---|---|
| WO2009102498A1 (en) | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel imaging agents for detecting neurological dysfunction |
| PE20160159A1 (es) | 2013-10-08 | 2016-03-18 | Hoffmann La Roche | Derivados de diazacarbazol como ligandos de tau para pet |
| DK3143011T3 (da) | 2014-05-13 | 2021-05-03 | Hoffmann La Roche | Deutererede heterocykliske forbindelser og deres anvendelse som billeddannende stoffer |
| EA036518B1 (ru) * | 2015-02-02 | 2020-11-18 | Юсб Байофарма Спрл | Производные 9h-пирролодипиридина |
| EP3118202A1 (en) | 2015-07-15 | 2017-01-18 | AC Immune S.A. | Dihydropyridopyrrole derivatives as tau-pet-ligands |
| EP3322707A1 (en) | 2015-07-15 | 2018-05-23 | AC Immune SA | Novel imaging compounds |
| WO2018015546A1 (en) | 2016-07-22 | 2018-01-25 | Ac Immune S.A. | Compounds for imaging tau protein aggregates |
| US10835624B2 (en) * | 2016-07-22 | 2020-11-17 | Ac Immune S.A. | Compounds for imaging Tau protein aggregates |
| 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 |
| KR102502701B1 (ko) | 2016-09-09 | 2023-02-23 | 에프. 호프만-라 로슈 아게 | 2-(6-니트로피리딘-3-일)-9H-다이피리도[2,3-b；3',4'-d]피롤의 제조 방법 |
| 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 |
| EA202091766A1 (ru) * | 2018-01-24 | 2021-02-18 | Ац Иммуне Са | Композиции для диагностики для пэт-визуализации, способ получения композиции для диагностики и ее применение в диагностике |
| WO2019145291A1 (en) | 2018-01-24 | 2019-08-01 | Ac Immune Sa | Gamma-carboline compounds for the detection of tau aggregates |
| 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 |
| WO2009102498A1 (en) * | 2008-02-14 | 2009-08-20 | Siemens Medical Solutions Usa, Inc. | Novel imaging agents for detecting neurological dysfunction |
| US20110124654A1 (en) | 2008-06-11 | 2011-05-26 | Huifen Chen | Diazacarbazoles and methods of use |
| EP2323697A2 (en) | 2008-07-24 | 2011-05-25 | Siemens Medical Solutions USA, Inc. | Imaging agents useful for identifying ad pathology |
| 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 |
| 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 |
| PE20160159A1 (es) | 2013-10-08 | 2016-03-18 | Hoffmann La Roche | Derivados de diazacarbazol como ligandos de tau para pet |
-
2014
- 2014-10-06 PE PE2015002706A patent/PE20160159A1/es active IP Right Grant
- 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 DK DK14781169.9T patent/DK3055308T3/en active
- 2014-10-06 PL PL14781169T patent/PL3055308T3/pl unknown
- 2014-10-06 MY MYPI2016000604A patent/MY190196A/en unknown
- 2014-10-06 SI SI201430549T patent/SI3055308T1/en unknown
- 2014-10-06 NO NO14781169A patent/NO3055308T3/no unknown
- 2014-10-06 TW TW103134795A patent/TWI513698B/zh active
- 2014-10-06 SG SG11201602786UA patent/SG11201602786UA/en unknown
- 2014-10-06 CN CN201480037389.5A patent/CN105358558B/zh active Active
- 2014-10-06 EA EA201690515A patent/EA028483B1/ru not_active IP Right Cessation
- 2014-10-06 ES ES14781169.9T patent/ES2657121T3/es active Active
- 2014-10-06 WO PCT/EP2014/071283 patent/WO2015052105A1/en not_active Ceased
- 2014-10-06 JP JP2016515518A patent/JP6194416B2/ja active Active
- 2014-10-06 PT PT147811699T patent/PT3055308T/pt unknown
- 2014-10-06 EP EP14781169.9A patent/EP3055308B1/en active Active
- 2014-10-06 HR HRP20180049TT patent/HRP20180049T1/hr unknown
- 2014-10-06 KR KR1020167008013A patent/KR101770531B1/ko active Active
- 2014-10-06 UA UAA201604290A patent/UA116164C2/uk unknown
- 2014-10-06 AU AU2014333996A patent/AU2014333996B2/en active Active
- 2014-10-06 MX MX2016002234A patent/MX373153B/es active IP Right Grant
- 2014-10-06 CA CA2917191A patent/CA2917191C/en active Active
- 2014-10-06 RS RS20180058A patent/RS56777B1/sr unknown
- 2014-10-06 HU HUE14781169A patent/HUE035413T2/en 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
-
2018
- 2018-05-15 US US15/980,080 patent/US11058781B2/en active Active
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| Date | Code | Title | Description |
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| FG | Grant, registration |