142247-38-9Relevant articles and documents
ASPARAGINE DERIVATIVES AND METHODS OF USE THEREOF
-
Paragraph 00778-00779, (2021/12/31)
The present invention relates to compounds of formulas (A) and (I), pharmaceutically acceptable salts thereof, and solvates of any of them, pharmaceutical compositions comprising them, methods of preparation thereof, intermediate compounds useful for the preparation thereof, and methods of treatment or prophylaxis of diseases, in particular cancer, such as colorectal cancer, using these. (A) (I)
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors
Schweinitz, Andrea,Doennecke, Daniel,Ludwig, Alexander,Steinmetzer, Peter,Schulze, Alexander,Kotthaus, Joscha,Wein, Silvia,Clement, Bernd,Steinmetzer, Torsten
scheme or table, p. 1960 - 1965 (2009/11/30)
A novel series of matriptase inhibitors based on previously identified tribasic 3-amidinophenylalanine derivatives was prepared. The C-terminal basic group was replaced by neutral residues to reduce the hydrophilicity of the inhibitors. The most potent co
Dibasic inhibitors of human mast cell tryptase. Part 3: Identification of a series of potent and selective inhibitors containing the benzamidine functionality
Dener, Jeffrey M.,Rice, Kenneth D.,Newcomb, William S.,Wang, Vivian R.,Young, Wendy B.,Gangloff, Anthony R.,Kuo, Elaine Y.-L.,Cregar, Lynne,Putnam, Daun,Wong, Martin
, p. 1629 - 1633 (2007/10/03)
A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, the benzamidine functionality was identified as the most potent charged group investigated.
