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US 9,873,668 B2Granted
Compositions and methods for inhibition of cathepsins
AssigneesMateon Therapeutics, Inc., Baylor University
InventorsDavid J. Chaplin, Kishore Kumar Gaddale Devanna, Erica Parker, Kevin G. Pinney, Jiangli Song, Mary Lynn Trawick
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Abstract
This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.
Claims29
A method of inhibiting an activity of a cathepsin, comprising contacting the cathepsin with a compound having a formula I, in an amount of effective to inhibit an activity of the cathepsin,
- or a solvate or pharmaceutically acceptable salt thereof, wherein
- X is selected from the group consisting of C(═O), CH(OR6) and
- n is 0, 1, 2 or 3;
- m is 0, 1, 2 or 3;
- p is 0, 1, 2 or 3;
- R1 is hydrogen, C1-C3 alkyl, aryl and arylalkyl;
- R2 is hydrogen or C1-C3 alkyl;
- each R3 and R5 independently is selected from the group consisting of hydroxyl, C1-C3 alkyl, C1-C2 alkoxy, fluoro, and chloro;
- each R4 independently is selected from the group consisting of hydroxyl, C1-C6 alkyl, C1-C6 alkoxy, halo, amino, nitro, nitroso and acyl;
- and
- R6 is selected from the group consisting of hydrogen and methyl.
8 more elements
Dependencies are inferred from the claim text.