| abstract |
New 1,2,4-thiadiazole compounds that are effective as inhibitors of cysteine-dependent enzymes, and in particular cysteine proteases, are proposed. The compounds are useful for the treatment of acne by inhibiting transglutaminase, the common cold by inhibiting protease, human rhinovirus 3C and inflammatory joint disease by inhibiting cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiazole of the general formula (I), where Z is a nitrogen-containing group with a recognition sequence for the enzyme, and Y is a substituent that adjusts the reactivity of the inhibitor to the thiol group of cysteine-dependent enzyme. Group Y can also serve as a recognition. The international application was published along with an international search report. |