| 主权项 |
1. Sialic acid derivative of the formula (I), where the symbols have the following definitions: A1, A2 are identically or differently a group D1-[Y3-D2-]m-; D1, D2 are identically or differently a mono- or polycylic aromatic, partially unsaturated or saturated C3-C14 hydrocarbon radical or an aromatic, partially unsaturated or saturated three- to eight-membered heterocyclic radical, the stated radicals being unsubstituted or substituted one or more times by a group X1; X1 is identically or differently halogen, cyano, nitro, hydroxyl, mercapto, amino, carboxyl, hydroxylamino, azido, B(OH)2, SO, SO3M, OSO3M, SO2NH2, SO2CF3, PO3M, OPO3M, cyanomethyl, alkyl, haloalkyl, alkenyl, alkynyl, alkyloxy, haloalkyloxy, alkenyloxy, alkynyloxy, alkylthio, alkylamino, dialkylamino, trialkylamino, formyl, alkylcarbonyl, alkylsulphonyl, alkylsulphoxyl, alkylaminosulphoxyl, dialkylaminosulphoxyl, alkyloxycarbonyl, alkylcarbonyloxy, aminocarbonyl, aminothiocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, alkylaminothiocarbonyl, oxo (═O), thioxo (═S), C1-C8 alkylimino (═N—C1-C8 alkyl), C1-C8 alkyloximino (═N—O—C1-C8 alkyl), the alkyl groups in these radicals containing 1 to 8 carbon atoms, and the stated alkenyl or alkynyl groups in these radicals containing 2 to 8 carbon atoms; Y1, Y2 are identically or differently ˜(C1-C4 alkyl)-, ˜(C1-C4 haloalkyl)-, ˜(C1-C4 alkyl)-(CO)—, ˜C(O)—, ˜CH2—C(O)—, ˜CH═CH—C(O)—, ˜C≡C—C(O)—, ˜S(O)2—, ˜CH2—S(O)2—, ˜NRx—C(O)—, ˜CH(CF3)—, ˜NRx-3-cyclobutene-1,2-dione-4-, ˜CH2—NRx-3-cyclobutene-1,2-dione-4-, ˜NRx-3-2,5-thiadiazole 1-oxide-4-, ˜NRx-3-2,5-thiadiazole 1,1-dioxide-4-, where ˜ denotes the bond to the group A, or Y1, Y2 form, independently of one another, together with the nitrogen to which they are bonded, and with the group R8, a group ˜4-1H-(1,2,3)triazol-1-yl-, ˜5-1H-(1,2,3)triazol-1-yl-, ˜CH2-4-1H-(1,2,3)triazol-1-yl- or —CH2-5-1H-(1,2,3)triazol-1-yl-, where ˜ denotes the bond to the group A; Y3 is a bond, O, S, S(O), S(O)2, CH2, C(O), CR2x; or NRx; m is 0, 1 or 2; Z1 is O, S, CH2 or NRx; D is a group Z2-T1-Y4-A3-Y5-T2-Z2; Z2 is identically or differently —O˜, —S˜, —NRx˜, —NH—C(O)˜, —CH2˜, —CF2˜, —CH(OH)˜, —N(Rx)—O˜, —O—NRx˜, —O—N═CH—, ˜4-1H-(1,2,3)triazol-1-yl-, or ˜5-1H-(1,2,3)triazol-1-yl-, where ˜ denotes the bond to the group T; T1, T2 are identically or differently a straight-chain or branched alkanediyl group having 1 to 30 C atoms, where
(i) optionally one or more non-terminal CH2 groups are replaced by —O—, —S—, —S(O)—, —S(O)2—, —S+(CH3)—, —P(O2)— and/or —NRx—, and/or(ii) optionally one or more H atoms are replaced by F, Cl, ORx, OSO3M, (═O), (═S), carboxyl, NH2, NHRy and/or NHRz, and/or(iii) optionally one or more non-terminal —CH2—CH2— groups are replaced by -5-1H-(1,2,3)triazol-1-yl-, —CRx═CRx— and/or
—C≡C—, and/or(iv) optionally a —CH2CH2CH2— group is replaced by -4-1H-(1,2,3)triazol-1-yl- and/or —O—N═CH—, and/or(v) optionally a —CH2CH2CH2CH2— group is replaced by phenyl-1,4-diyl; Y4, Y5 are identically or differently a bond, O, S, NRx, S(O), S(O)2, C(O), ˜C(O)—NRx—, ˜NRx—C(O)—, ˜C(O)—O—, ˜O—C(O)—, ˜NRx—CO—NRx—, ˜NRx—S(O)2—, ˜S(O)2—NRx—, ˜CH2—NRx—C(O)—, ˜CH2—C(O)—NRx—, ˜CH(CF3)—NRx—, ˜CH═N—O— or ˜O—N═CH—, where ˜ a denotes the bond to group A; A3 is
a) C1-C8 alkanediyl, C2-C8 alkenediyl, C2-C8 alkynediyl, C4-C8 alkadienediyl, two or more CH2 groups in the stated groups being replaced by O, S, S(O), S(O)2, NRx and/or C(O), and optionally one or more H atoms in the stated groups being replaced by a group X2,b) a group A4-[Z3-A5]n,c) 1,1′-ferrocenediyl, 1,1′-cobaltocenediyl, 1,1′-ruthenocene or dichloroplatinumdiaminodiyl; A4, A5 are identically or differently a saturated, partially unsaturated or aromatic, mono- or polycyclic hydrocarbon radical having 3 to 14 C atoms, or a three- to eight-membered aromatic, partially unsaturated or saturated mono- or polycyclic heterocyclic radical, the stated groups being each optionally substituted by one or more groups X2; Z3 is a bond, O, S, S(O), S(O)2, NRx, C(O) or CR2x; X2 is identically or differently fluoro, chloro, bromo, nitro, hydroxylamino, B(OH2), SO3M, OSO3M, SO2NH2, PO3M, OPO3M, alkyl, haloalkyl, alkyloxy, haloalkyloxy, alkylthio, alkylamino, dialkylamino, trialkylamino, alkylcarbonyl, alkylsulphonyl, alkylsulphoxyl, alkylaminosulphoxyl, dialkylaminosulphoxyl, alkyloxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, alkylaminothiocarbonyl, C1-C4 alkylimino (═N—C1-C4 alkyl), C1-C4 alkyloximino (═N—O—C1-C4 alkyl), the alkyl groups in these radicals containing 1 to 4 carbon atoms, and the groups haloalkyl and haloalkyloxy containing the halogens F and/or Cl; n is 0, 1; R1 is identically C(O)OM, O—PO3M2, O—SO3M, SO3M, C(O)—NH—S(O)2Rx, PO3M2 or C(O)NOM; R2, R3 are identically or differently H or F; R4, R7 are identically or differently H, OH, ORz, OC(O)NHRy or NRx; R6 is identically or differently H or Rz; R5 is identically or differently H, Rx, Rz, C(O)H, C(O)CH2OH or C(O)-haloalkyl; R8 is identically or differently Rx; M is H, C1-C6 alkyl or a cation; Rx is identically or differently H, Ry or Rz; Ry is identically or differently C1-C6 alkyl, phenyl or benzyl, and Rz is identically or differently —C(O)—C1-C6 alkyl, —C(O) phenyl or —C(O)—C1-C4 alkyl-phenyl, and also its pharmacologically tolerated salts, metabolites and prodrugs. |
