申请人:Prolinx, Inc.
公开号:US05594111A1
公开(公告)日:1997-01-14
The present invention relates to a novel class of phenylboronic acid bioconjugate complexes derived from aminosalicylic acid, and the method of making and using such bioconjugate complexes. The bioconjugate complexes are in the form of the following general formulas; ##STR1## wherein group X is selected from the group consisting of O, NH, N-alkyl, NC.sub.6 H.sub.5, N-aryl, NCH.sub.2 -aryl, NCH.sub.2 CH.sub.2 OH, NCOCH.sub.2 CH.sub.2 OH, NOH, NO-alkyl and NOCH.sub.2 -aryl, wherein alkyl denotes a hydrocarbon moiety of from 1 to 4 carbons in length and which may be linear or branched, wherein aryl is selected from the group consisting of an aromatic ring, a substituted aromatic ring and a fused aromatic ring, wherein group Y is selected from the group consisting of O, S, NH, N-alkyl, N-aryl and NCH.sub.2 -aryl, wherein groups Z and Z* comprise a spacer selected from an alkyl and a polyethyleneglycol chain, of from 1 to 16 carbon equivalents in length, wherein the chain may contain intermediate amide and disulfide bonds, and and wherein groups BAS and BAS* are bioactive species.
本发明涉及一类新型的对氨基水杨酸衍生的邻苯硼酸生物共轭复合物,以及制造和使用此类生物共轭复合物的方法。生物共轭复合物具有以下通式:其中X基团选自由O、NH、N-烷基、NC6H5、N-芳基、NCH2-芳基、NCH2CH2OH、NCOCH2CH2OH、NOH、NO-烷基和NOCH2-芳基组成的组,其中烷基表示碳原子数为1至4的烃基团,可以是直链或支链,其中芳基选自芳环、取代芳环和融合芳环的组,其中Y基团选自由O、S、NH、N-烷基、N-芳基和NCH2-芳基组成的组,其中Z基团和Z*基团包括由烷基和聚乙二醇链组成的间隔基,链长为1至16碳当量,其中链可含有中间酰胺和二硫键,其中BAS基团和BAS*基团为生物活性物种。