发明名称 SIALIC ACID DERIVATIVES
摘要 Sialic acid derivatives of the formula (I);
申请公布号 US2016362436(A1) 申请公布日期 2016.12.15
申请号 US201515121585 申请日期 2015.02.25
申请人 BROSSMER Reinhard;PRESCHER Horst 发明人 BROSSMER Reinhard;PRESCHER Horst
分类号 C07H15/04 主分类号 C07H15/04
代理机构 代理人
主权项 1. Sialic acid derivative of the formula (I), where the symbols have the following definitions: A1 is a group D1-[Y2-D2-]m-; D1 is a mono- or polycyclic aromatic, partially unsaturated or saturated C3-C14 hydrocarbon radical or a mono- or polycyclic aromatic, partially unsaturated or saturated three- to twelve-membered heterocyclic radical, the stated radicals being unsubstituted or substituted one or more times by a group X; D2 is a mono- or polycyclic aromatic, partially unsaturated or saturated C3-C14 hydrocarbon radical or a mono- or polycyclic 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 X; Y1 is ˜C(O)—, ˜S(O)2—, ˜NHC(O)—, ˜(C1-C2 alkyl)-, ˜(C1-C2 alkyl)-C(O)—, ˜CH═CH—C(O)—, ˜C≡C—C(O)—, ˜(C1-C2 alkyl)-S(O)2—, ˜OC(O)—, ˜(C1-C2 alkyl)-OC(O)— or ˜(C1-C2 alkyl)-NHC(O)—, where ˜ denotes the bond to the group A1; Y2 is —O—, —C(O)—, —S(O)2—, —CH2— or a bond; A2 is a) a group —OS(O)2OL orb) a group —N(Rx)—W; W is a) a group ˜SO3L, ˜SO2CF3 or ˜SO2NRx2 orb) a group D3-Y3—; Y3 is a bond or a group ˜O(CO)NHS(O)2—, ˜NHC(O)—, ˜OC(O)—, ˜CH2OC(O)—, —S(O)2—, ˜C(O)—, ˜(C1-C2 alkyl)-C(O)—, ˜(C1-C2 alkyl)-NHC(O)— or ˜(C1-C2 alkyl)-S(O)2—, where ˜ denotes the bond to the group D3; D3 is a) C1-C6 alkyl, where optionally one or more non-terminal CH2 groups are replaced by O, N(Rx) and/or C(O), and where optionally one or more H atoms in the stated groups are replaced by a group X,b) is a mono- or polycyclic aromatic, partially unsaturated or saturated C3-C14 hydrocarbon radical or a mono- or polycyclic 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 X; A3 is a) C1-C8 alkyl, where optionally  a. one or more non-terminal —CH2— groups are replaced by S, O, N(Rx) and/or C(O), or  b. a —CH2CH2CH2— group is replaced by 1,2-phenyldiyl, 1,3-phenyldiyl or 1,4-phenyldiyl, and where optionally one or more H atoms in the stated groups are replaced by a group X, or b) is a mono- or polycyclic aromatic, partially unsaturated or saturated C3-C14 hydrocarbon radical or a mono- or polycyclic 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 X; X is identically or differently halogen, cyano, nitro, hydroxyl, mercapto, amino, carboxyl, carboxymethyl, hydroxylamino, azido, B(OH2), SO, SO3M, OSO3M, SO2NH2, SO2CF3, PO3M, OPO3M, cyanomethyl, alkyl, haloalkyl, alkyloxy, haloalkyloxy, alkylamino, dialkylamino, trialkylamino, formyl, alkylcarbonyl, alkylsulfonyl, alkylsulfoxyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkyloxycarbonyl, alkylcarbonyloxy, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, dialkylaminocarbonyl, oxo (═O), thioxo (═S), C1-C8 alkylimino (═N—C1-C8 alkyl) or C1-C8 alkyloximino (═N—O—C1-C8 alkyl), the alkyl groups in these radicals containing 1 to 6 carbon atoms; m is 0, 1 or 2; Z is ˜O—, ˜S—, —ON═CH˜, ˜ON(Rx)—, ˜N(Rx)— or ˜4-1H-(1,2,3)triazol-1-yl-, where ˜ denotes the bond to the group A3; R1 is C(O)OM; R2 is H, F, Cl, NRx or ORx;R3 is H, F, Cl, NRx or ORx; R4 is N(Rx)C(O)CH2OH or N(Rx)C(O)Rx; R5, R6 are identically or differently OH or ORx; L is a cation; M is C1-C4 alkyl or a cation; Rx is identically or differently H, Ry or Rz; Ry is identically or differently C1-C4 alkyl, phenyl or benzyl, and Rz is identically or differently —C(O)—C1-C4 alkyl, —C(O)-phenyl or C(O)—CH2-phenyl, where alkyl groups in each case are straight-chain, branched or cyclic, a pharmacologically tolerated salt or prodrug thereof.
地址 Heidelberg DE