Compositions and methods for inhibition of cathepsins
View Patent ↗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.
1. A compound of formula I:
or a solvate or pharmaceutically acceptable salt thereof, wherein
X is C(═O);
n is 0 or 1;
m is 0 or 1;
p is 0 or 1;
R 1 and R 2 are hydrogen;
R 3 and R 5 are independently selected from the group consisting of hydroxyl, fluoro, and chloro; and
R 4 is selected from the group consisting of hydroxyl, benzoyl, and halo.
2. The compound of claim 1 , wherein the compound is 3-benzoyl benzophenone thiosemicarbazone (3) having the formula:
3. The compound of claim 1 , wherein n=1, m=0, and p=1.
4. The compound of claim 3 , wherein R 3 and R 5 are fluoro.
5. The compound of claim 4 , wherein the compound is 1,3-bis-(4-fluorobenzoyl) benzene thiosemicarbazone (13) having the formula:
6. The compound of claim 1 , wherein n=0, m=1, and p=0.
7. The compound of claim 6 , wherein R 4 is benzoyl.
8. The compound of claim 7 , wherein the compound is 1,3,5-Tribenzoyl benzene thiosemicarbazone (25) having the formula: