主权项 |
1. Sialic acid derivative of the formula (I), where the symbols are defined as follows: A1 is equal to 4-biphenyl, 4-(2-thienyl)benzoyl, 4-(3-thienyl)benzoyl, 1-naphthyl and 2-naphthyl, in which the residues mentioned are unsubstituted or mono- or polysubstituted by a group X1; X1 is identically or differently fluorine, chlorine, hydroxyl, carboxy, SO3M, OSO3M, SO2NH2, SO2CF3, alkyl, cycloalkyl, haloalkyl, alkyloxy, haloalkyloxy, alkylcarbonyloxy, alkylcyclocarbonyloxy, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, alkylcarbonylamino, cycloalkylcarbonylamino, alkylamino, cycloalkylamino, dialkylamino, dicycloalkylamino or alkylcycloalkylamino, in which the alkyl groups in these residues comprise 1 to 4, and the cycloalkyl groups 3 or 4, carbon atoms; Y1 is equal to ˜(C1-C2-alkyl)-, ˜C(O)— or ˜CH2C(O)—, in which ˜ denotes the bond to the group A1; Z2 is equal to —O—, —S— or —CH2—; T1 is equal to a straight-chain or branched alkanediyl group having 3 to 10 C atoms, in which
(i) optionally one or more non-terminal CH2 groups are replaced by —O— and/or —S— and/or(iv) optionally one or more H atoms are replaced by F and/or Cl and/or(v) optionally one non-terminal —CH2CH2— group is replaced by —NHCO—; Y3 is equal to —C(O)—, ˜C(O)—NH— or ˜NH—C(O)—, in which ˜ denotes the bond to group A3; A3 is
a) a C1-C8-alkanetriyl, in which optionally more than one non-terminal CH2 groups are replaced by O, S, S(O), S(O)2, NRx and/or C(O) and wherein optionally one or more H atoms in the groups mentioned are replaced by a group X2,b) a saturated, partially unsaturated or aromatic, mono- or polycyclic hydrocarbon residue having 3 to 14 C atoms or one three- to eight-membered, aromatic, partially unsaturated or saturated mono- or polycyclic heterocyclic residue, in which the groups mentioned are optionally substituted in each case by one or more groups X2,c) a tertiary nitrogen; X2 is equal to fluorine, chlorine, alkyl, haloalkyl or alkyloxy, in which the alkyl groups in these residues comprise 1 to 2 carbon atoms; W is —Y5-T2-V or —V; V is ˜C(O)O-4-nitrophenyl, ˜C(O)O-pentafluorophenyl, maleic-2-yl anhydride, ˜C(O)-1-azetidin-2-one, ˜4-O-phenyl-C(O)-1-azetidin-2-one, ˜N═C═O, ˜N═S═O, ˜C(O)N2, ˜S(O)2Cl, ˜C(NH2)ORy, ˜P(CH2OH)3, ˜SH, ˜SC(O)CH3, ˜NH2, ˜OH, ˜CH═CH2, ˜C≡CH, ˜COOM, ˜C(O)H, ˜C(O)CH3, ˜C(O)C(O)H, ˜I, ˜N3, ethyl-2-(3-indol)amine-1˜, ˜S(O)2N3, phenyl-CH═CH—C(N2)—C(O)O˜, ˜CH═CHCH2OC(O)Ry, ˜CH═CHCH2OC(O)NHRy, ˜OC(O)ORy, ˜C(O)NHNH2, ˜N-maleimide, aziridine-2˜, pyridine-2-S—S˜, phenyl-1-carboxy-2-nitro-5-S—S˜, ˜S(O)2CH═CH2, ˜C(O)—S-phenyl, ˜C(O)CH═N2, ˜C(O)O—N-succinimidyl, or C(O)O—N-sulphosuccinimidyl; Y5 is a bond, —O—, —S—, —NRx—, —C(O)—, ˜C(O)—NRx— or ˜NRx—C(O)—, in which ˜ denotes the bond to group A3; T2 is a straight-chain or branched alkanediyl group having 1 to 200 C atoms, in which
(i) optionally one or more non-terminal CH2 groups are replaced by —O—, NH and/or —S— and/or(iv) optionally one or more non-terminal H atoms are replaced by F, Cl, (═O), NRz and/or NRy and/or(v) optionally one or more non-terminal —CH2CH2— group is replaced by —NHCO— or —S—S—; R1 is equal to C(O)OM; R2, R3 are equal to H; R4, R6, R7 are identically or differently OH or ORz; R5 is equal to C(O)CH3 or C(O)CH2OH; M is equal to a C1-C4-alkyl, C3-C4-cycloalkyl or a cation; Rx is identically or differently H, Ry or Rz; Ry is identically or differently C1-C4-alkyl, C3-C4-cycloalkyl, phenyl or benzyl and Rz is identically or differently —C(O)—C1-C4-alkyl, —C(O)—C3-C4-cycloalkyl, —C(O)-phenyl or C(O)—CH2-phenyl. |