Fluorinated Benzofuran Derivatives for PET Imaging of β-Amyloid Plaques in Alzheimer's Disease Brains
摘要:
A series of fluorinated benzofuran derivatives as potential tracers for positron emission tomography (PET) targeting beta-amyloid plaques in the brains of patients with Alzheimer's disease (AD) were synthesized and evaluated. The derivatives were produced using an intramolecular Wittig reaction. In experiments in vitro, all displayed high affinity for A beta(1-42) aggregates with K-i values in the nanomolar range. Radiofluorinated 17,[F-18]17, in particular labeled beta-amyloid plaques in sections of Tg2576 mouse brain and displayed high uptake (5.66% ID/g) at 10 min postinjection, sufficient for PET imaging. In addition, in vivo beta-amyloid plaque labeling can be clearly demonstrated with [F-18]17 in Tg2576 mice. In conclusion, [F-18]17 may be useful for detecting beta-amyloid plaques in patients with AD.
The present application relates to novel dicarboxylic acid derivatives, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
LACTAM-SUBSTITUTED DICARBOXYLIC ACIDS AND USE THEREOF
申请人:Hahn Michael
公开号:US20100197680A1
公开(公告)日:2010-08-05
The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
SUBSTITUTED DIBENZOIC ACID DERIVATIVES AND USE THEREOF
申请人:Hahn Michael
公开号:US20100168240A1
公开(公告)日:2010-07-01
The invention relates to novel substituted dibenzoic acid derivatives of formula (I), wherein A represents a group of formula (II) or (III), to methods for producing the same, and to their use in the treatment and/or prophylaxis of diseases. The invention also relates to the use of said substances in the production of drugs for the treatment and/or prophylaxis of diseases, especially in the treatment and/or prevention of cardiovascular diseases.
Substituted dibenzoic acid derivatives and use thereof
申请人:Bayer Schering Pharma Aktiengesellschaft
公开号:US07985876B2
公开(公告)日:2011-07-26
The invention relates to novel substituted dibenzoic acid derivatives of formula (I), wherein A represents a group of formula (II) or (III), to methods for producing the same, and to their use in the treatment and/or prophylaxis of diseases. The invention also relates to the use of said substances in the production of drugs for the treatment and/or prophylaxis of diseases, especially in the treatment and/or prevention of cardiovascular diseases.
Lactam-substituted dicarboxylic acids and use thereof
申请人:Bayer Intellectual Property GmbH
公开号:US08217063B2
公开(公告)日:2012-07-10
The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.