312325-75-0Relevant academic research and scientific papers
NOVEL FERROPORTIN INHIBITORS
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Page/Page column 331, (2017/05/10)
The invention relates to novel ferroportin inhibitors of the general formula (I) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.
Bicyclic aza-amides for treatment of psychiatric disorders
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Paragraph 0070; 0071, (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 34; 35, (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.
Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control
Wang, Yansong,Kirschner, Alexander,Fabian, Anne-Katrin,Gopalakrishnan, Ranganath,Kress, Christoph,Hoogeland, Bastiaan,Koch, Uwe,Kozany, Christian,Bracher, Andreas,Hausch, Felix
supporting information, p. 3922 - 3935 (2013/06/27)
The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy in these ligands. The [4.3.1] scaffold had consistently higher affinity compared to the [3.3.1] or monocyclic scaffolds, which could be attributed to better preorganization of two key recognition motifs. Surprisingly, the binding of the rigid [4.3.1] scaffold was enthalpy-driven and entropically disfavored compared to the flexible analogues. Cocrystal structures at atomic resolution revealed that the sulfonamide nitrogen in the bicyclic scaffolds can accept an unusual hydrogen bond from Tyr113 that mimics the putative FKBP transition state. This resulted in the first lead-like, functionally active ligand for FKBP51. Our work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51.
Facile cyanomethylation of bromopyridines by nucleophilic substitution with lithioacetonitrile
Skerlj,Bogucki,Bridger
, p. 1488 - 1490 (2007/10/03)
Substituted bromopyridines undergo facile nucleophilic substitution with lithioacetonitrile under mild conditions to afford the corresponding cyanomethylated products.
