| abstract |
The diacylhydrazine derivatives of formula 1 wherein X represents H2N-C (= NH) -NH-, H3C-C (= NH) -NH- or Het1-NH, Y represents - (CH2) not of formula 2, Z esN-R2 or CH-R2, R1, R2 independently represents H or A, R3 represents H, Ar or Het, R4 represents H, A, Ar, OH, OA, OAr, arylalkyl, Hal, CN, NO2, CF3 orOCF3, A represents C1-6 alkyl, Ar represents unsubstituted or mono, di or trisubstituted phenyl with A, OH, OA, CF3, OCF3, CN, NO2 or Hal, which may be substituted with a mono phenyl, di-substituted with A, OH , OA, CF3, OCF3, CN, NO2 or Hal so as to form an unsubstituted or substituted biphenyl, unsubstituted onaphthyl or mono, di or trisubstituted with A, OH, OA, CF3, OCF3, CN, NO2 or Hal, Hal represents F, Cl, Br or I, Het represents a heterocyclic or bicyclic radical, saturated or partially or totally unsaturated, with 5 to 10 members in the ring, which may contain 1 0 2 atoms of N and / or 1 or 2 atoms deS or O, and which may be mono or disubstituted with CN, Hal, OH, O A, CF3, A, NO2 or OCF3, Het1 represents an aromatic heterocycle of 5 or 6 members and with 1 to 4 atoms of N, which may not be substituted or be mono-substituted or disubstituted with Hal, A, Ar, OAr, arylalkyl, CN, NO2, CF3 or OCF3, n is 2, 3, 4, 5 or 6m, or they are 0, 1 or 2, and their physiological acceptable solvates and salts. A process for preparing compounds of formula 1 and substrates, in which (a) to prepare compounds of formula 1, in which Z represents N-R2, a compound of formula 3 is reacted wherein X, Y, R1 and R2 have the meanings indicated above, and wherein the free amino groups are protected by a suitable amino protecting group, with a compound of formula 4 where R2 and R3 have the meanings above, and wherein a free hydroxyl group is is protected by a suitable hydroxyl protecting group or is attached to a fixed phase, and then the protective groups are cleaved and / or the fixed phase is removed, or (b) a compound of formula 5 is reacted where X and Y have the meanings indicated above, and where the free amino groups are found |