发明授权
- 专利标题: Phenyldiboronic acid reagents and complexes
- 专利标题(中): 苯二硼酸试剂和络合物
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申请号: US09625231申请日: 2000-07-25
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公开(公告)号: US06462179B1公开(公告)日: 2002-10-08
- 发明人: Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
- 申请人: Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
- 主分类号: C07F502
- IPC分类号: C07F502
摘要:
Reagents suitable for the modification of a bioactive species for the purpose of incorporating one or more phenyldiboronic acid (PDBA) moieties for subsequent conjugation to a different (or the same) bioactive species having one or more pendant boronic compound complexing moieties of the general formula of General Formula I, wherein group R is a reactive electrophilic or nucleophilic moiety suitable for reaction of the PDBA reagent with a bioactive species. Group Z is a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length. Group Q is a linkage that includes one of amide, ether and thioether moieties. Group R is preferably selected from, but not limited to, one of acrylamide, bromo, bromoacetamide, chloro, chloroacetamide, dithiopyridyl, hydrazide, N-hydroxysuccinimidyl ester, N-hydroxysulfo-succinimidyl ester, imidate ester, imidazolide, iodo, iodoacetamide, maleimide, amino and thiol moieties. Group Z is preferably an unbranched alkyl chain of the general formula (CH2)n, wherein n=1 to 6. Group Q is preferably selected from one of NHCO, CONH, NHCOCH2, CONHCH2, O, OCH2, S, and SCH2 moieties.
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