INHIBITORS OF TRANSGLUTAMINASES

摘要

The invention relates to compounds of general formula (I), wherein R<1> means formula (II), (III), (IV) or (V); R<2> means H, alkyl, which can optionally be substituted with halogen or N2, or NH2; m and o mean 0 to 3 and n means 0 or 1; ap, bq and cr mean amino acid chains and p, q and r mean the number of amino acids, a and/or b and/or c also being able to contain at least one side chain, represented by (CH2)mYn(CH2)oC(Z)R<2>, Y, Z, R<2>, m, n, and o having the same meaning as in formula (I), and p, q and r being the same or different and meaning a whole number from 0 to 1000; R<3> and R<4>, independently of each other, mean H, alkyl, aryl, a heterocycle, an amino protective group or a carboxy protective group; R<5> and R<6>, independently of each other, mean alkyl which can contain at least one hetero atom selected from N, O and S; aryl or a heterocycle; X means a methine group, a nitrogen atom or a phosphorus atom; Y means an oxygen atom, a sulphur atom or an NH-group; and Z means an oxygen atom, a sulphur atom or an NR<7>-group, R<7> meaning H, alkyl, aryl, a heterocycle, O-alkyl, O-aryl, O-heterocycle, NR2 or NHCONR2, R meaning H, alkyl, aryl or a heterocycle; and to the use of said compound as an inhibitor of transglutaminases.