Back to results
US 7,125,872 B2Granted
β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
AssigneeMyriad Genetics, Inc.
InventorsMichael Kahn, Cyprian O. Ogbu, Masakatsu Eguchi, Hwa-Ok Kim, Patrick Douglas Boatman, Jr.
Life of this patent
Estimating the term…
Abstract
There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the β-sheet mimetic is a thrombin inhibitor.
Claims32
A compound having the structure:
- or a pharmaceutically acceptable salt thereof,
- wherein n is an integer from 1 to 2;
- p is an integer from 1 to 3;
- R1 is selected from amino acid side chain moieties and derivatives thereof and Y and Z represent the remainder of the molecule;
- with the proviso that when Y is —OH, or a pharmaceutically acceptable salt form thereof, or —OCH3 or —O(t-butyl), then R1 is not H.
2 more elements
A compound having the structure:
- or a pharmaceutically acceptable salt thereof,
- wherein n is an integer from 1 to 4;
- p is an integer form 1 to 3;
- R1 is selected from amino acid side chain moieties and derivatives thereof;
- R4 is an organoamine comprising 2–10 carbon atoms and at least 1 nitrogen;
- and Y′ and Z represent the remainder of the molecule.
3 more elements
Dependencies are inferred from the claim text.