| 摘要 |
Macrolide compounds of formula I: with PDF4 inhibiting activity are descr ibed, wherein R1 is a residue -Y-X-Q; Y is S, SO or SO2; X is a bond or a li near group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as - CH=CH- or -C.id ent.C- and which group X is unsubstituted or is substituted with - COO-W or -CONH-W; Q is a residue -V-A1-L- A2-W or, if X does not represent a bond, ma y also be -NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group -V-A1-L- A2-W, wherein at least one of the gr oups A1; L or A2 is present, can also be a monovalent substituted or unsubst ituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are independently of each other eit her absent or a C1-C4alkylene group; L is -0-, -S-, -SO2-, -NH-, -CO-, -(CO) O-, -O(OC)-, -(CO)NH-, -NH(CO)-, -(SO2)NH-, -HN(SO2)-, -HN(CO)NH-, -0(CO)NH- , -NH(CO)O-, or can also be absent if Al and/or A2 are present; R2 is hydrog en and R3 is and 0R4 or R2, R3 taken together form a C=O group; R4 is hydrog en or an saturated or unsaturated aliphatic group with 1 to 6 carbon atoms; R6, R7 are independently selected from aryl; aralkyl; heterocyclyl and heter ocyclylalkyl; and one of R6 and R7 can also be a group -L-W; and * indicates a chiral centre which is in the (R) or (S) form.
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