0363284-A2 is referenced by 98 patents and cites 18 patents.

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide gorup of the substrate peptide has been replaced by H or a substituted carbonyl moiety. The contemplated peptidase inhibitors of the foregoing enzymes are selected from the generic formula R1NHCHR2C(O)X the hydrates, isosteres or the pharmaceutically acceptable salts thereof, wherein X is H or C(O)R3, R3 is H, methyl, ethyl, OH, methoxy or ethoxy, R1 is H, a protecting group, an alpha -amino acid or a peptide having 2 to 4 alpha -amino acids, optionally bearing a protecting group, R2 is a residue of an alpha -amino acid responsible for directing the inhibitor to the active site of the enzyme or is -A-SiR7R8R9, C1-10 alkyl, aralkyl or aryl, with A being a C1-6 alkylene, and each of R7, R8 and R9 being C1-10 alkyl, benzyl or phenethyl.; These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Novel peptidase inhibitors.
Application Number
EP19890402762 19891006
Publication Number
0363284 (A2)
Application Date
October 6, 1989
Publication Date
April 11, 1990
Mehdi Shujaath
Angelastro Michael
Bey Philippe
Merrell Dow Pharma
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