| 摘要 |
Modified active agent derivatives (I) containing an amino acid residue or peptide chain, a fluorinated hydrocarbon chain and a recognition or hydrophilizing moiety in addition to the parent active agent residue are new. Modified active agent derivatives (I) containing an amino acid residue or peptide chain, a fluorinated hydrocarbon chain and a recognition or hydrophilizing moiety in addition to the parent active agent residue are new. PA = active agent acting on a biological target; x, a, b = 0 or 1; X = peptide chain containing 1-5 amino acid residues; AA1, AA2, AA3 = amino acids; R = molecule recognized by the target of PA or a hydrophilic moiety for modifying the hydrophilic-lipophilic balance (HLB) value of (I); Y1 = 4-12C fluorinated hydrocarbon chain containing a C(O), NH, OC(O)NH, S or O group allowing attachment to a terminal of the (AA3)b-(AA2)a-(AA1) chain or to the side-chain of one of the amino acids AA1-AA3; The PA-(X)x moiety is bonded to the (AA3)b-(AA2)a-(AA1) chain via the side-chain of one of the amino acids AA1 - AA3 or to a terminal of the chain. An Independent claim is also included for biologically active molecules containing a fragment of formula (II). R' = monosaccharide, aminated sugar derivative, polysaccharide, polyether, polyol, peptide, natural or synthetic hormone or antibody.
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