Aroylated phenylenediamines

Akthelia’s founders were the first to isolate and characterize the only currently identified host defense peptide of the cathelicidin family in humans, LL-37 (Gudmundsson et al., 1996), and have elucidated factors and pathways that control the expression and regulation of host defense peptides in ‘in vitro’ cell systems, animal models and humans (Islam et al., 2001, Schauber et al., 2003 and Termen et al., 2008). These results constitute the scientific basis of Akthelia’s business proposition.

Akthelia has developed a high-throughput cell-based screening tool to rapidly screen for potential pharmaceutical agents that affect the expression of the host defense peptide LL-37 (Nylen et al., 2014). The cell line has been used to screen chemical libraries (available at the Karolinska Institute) and for developing and selecting a group of compounds which affect the expression of LL-37.

This has resulted in the development of an important class of compounds termed Aroyl Phenylenediamines (APDs) that induce expression of human defense peptides. The AMP screened for is the human LL-37 (cathelicidin) but the compounds induce the expression of several host defense peptides, including calprotectin, human beta defensin-1, lipocalin as well as the proteins Reg1-alpha and Reg3-gamma. 

Patents Filed

Main patent: (WO/2015/063694) ANTIMICROBIAL COMPOUNDS. Composition of matter patent for the Aroylated phenylenediamine class of compounds.

International Filing Date: 29.10.2014. Granted in the US, Europe and China. National filings in progress.

Other patents: