| 摘要 |
The present invention relates to novel compounds of Formula (I) wherein ~X~ represents an amino acid group, ~n~ is an integer between 1 and 4, ~R1~ represents benzyl, t-butyl or 9-fluorenylmethyl and ~R2~ represents a tetramethylmercaptoimidazole derivative or -S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinari ly acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminas e has been implicated. Advantageously, the medicament is for treating fibrosis , scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration an d chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject). The invention further relates to a method for preventing or treating rejection of a transplanted organ.
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