Diazacarbazole derivatives as tau-pet-ligands

The present invention relates to a compound of general formula (I) wherein R is hydrogen or tritium; F is fluoro or 18fluoro; or to a pharmaceutically acceptable acid addition salt. Compounds of formula I include 2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole, 3H-2-(6-fluoro-p...

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Hauptverfasser:	Koerner, Matthias, Muri, Dieter, Gobbi, Luca, Knust, Henner
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator	Koerner, Matthias Muri, Dieter Gobbi, Luca Knust, Henner
description	The present invention relates to a compound of general formula (I) wherein R is hydrogen or tritium; F is fluoro or 18fluoro; or to a pharmaceutically acceptable acid addition salt. Compounds of formula I include 2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole, 3H-2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole and [18F]-2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole. The compounds may be used for binding and imaging tau aggregates and related beta-sheet aggregates including besides others beta-amyloid aggregates or alpha-synuclein aggregates.
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Compounds of formula I include 2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole, 3H-2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole and [18F]-2-(6-fluoro-pyridin-3-yl)-9H-dipyrido[2,3-b;3',4'-d]pyrrole. 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title	Diazacarbazole derivatives as tau-pet-ligands
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