1542785-98-7Relevant academic research and scientific papers
Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)
Pomplun, Sebastian,Wang, Yansong,Kirschner, Alexander,Kozany, Christian,Hausch, Felix,Bracher, Andreas
, p. 345 - 348 (2015/02/19)
To create highly efficient inhibitors for FK506- binding proteins, a new asymmetric synthesis for pro-(S)-C5- branched [4.3.1] aza-amide bicycles was developed. The key step of the synthesis is an HF-driven N-acyliminium cyclization. Functionalization of the C5 moiety resulted in novel protein contacts with the psychiatric risk factor FKBP51, which led to a more than 280-fold enhancement in affinity. The most potent ligands facilitated the differentiation of N2a neuroblastoma cells with low nanomolar potency.
Bicyclic aza-amides for treatment of psychiatric disorders
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Paragraph 0104; 0109, (2014/02/15)
The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
BICYCLIC AZA-AMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS
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Page/Page column 51, (2014/02/16)
The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza- amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
