Transglutaminase inhibitors and methods of use thereof

A method of treating Celiac Sprue and/or dermatitis herpetiformis, the method comprising:

• administering to a patient an effective dose of a tTGase inhibitor having the formula:
• wherein R1 and R2 are independently selected from H, alkyl, alkenyl, cycloalkyl, aryl, heteroalkyl, heteroaryl, alkoxy, alkylthio, arakyl, aralkenyl, halo, haloalkyl, haloalkoxy, heterocyclyl, and heterocyclylalkyl groups;
• R3 is selected from Cl, and Br;
• n is from 0 to 10;
• and X is selected from the group consisting of O and NH.

A pharmaceutical formulation comprising:

• an effective dose of a tTGase inhibitor, wherein said tTGase inhibitory moiety is:
• wherein R1 and R2 are independently selected from H, alkyl, alkenyl, cycloalkyl, aryl, heteroalkyl, heteroaryl, alkoxy, alkylthio, arakyl, aralkenyl, halo, haloalkyl, haloalkoxy, heterocyclyl, and heterocyclylalkyl groups;
• R3 is selected from Cl, and Br;
• n is from 0 to 10;
• and X is selected from the group consisting of O and NH.

A tTGase inhibitor of the formula:

• wherein R1 and R2 are independently selected from H, alkyl, alkenyl, cycloalkyl, aryl, heteroalkyl, heteroaryl, alkoxy, alkylthio, arakyl, aralkenyl, halo, haloalkyl, haloalkoxy, heterocyclyl, and heterocyclylalkyl groups;
• R3 is selected from Cl, and Br;
• n is from 0 to 10;
• and X is selected from the group consisting of O and NH,
• other than [(S)-1-[(3-Bromo-4,5-dihydro-isoxazol-5-ylmethyl)-methyl-carbamoyl]-2-(4-hydroxy-phenyl)-ethyl]-carbamic acid benzyl ester.