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41. 发明授权

US06462179B1 Phenyldiboronic acid reagents and complexes 失效
标题翻译：苯二硼酸试剂和络合物
公开(公告)号：US06462179B1
公开(公告)日：2002-10-08
申请号：US09625231
申请日：2000-07-25
申请人： Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
发明人： Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
IPC分类号： C07F502
CPC分类号： C07C233/49 , C07C229/38 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/531 , G01N33/54353 , Y10S530/81 , Y10S530/816
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.
摘要翻译：适于修饰生物活性物质的试剂，用于引入一种或多种苯基二硼酸（PDBA）部分以用于随后与不同（或相同）生物活性物质缀合的具有一个或多个通式的侧链化合物络合部分的生物活性物质通式I，其中基团R是适于PDBA试剂与生物活性物质反应的反应性亲电或亲核部分。 Z组是选自饱和或不饱和链长度至多约0至6当量长度的间隔基，长度为约6至18当量长度的至少一个中间体酰胺或二硫化物部分的无支链饱和或不饱和链，以及长度为约3至12碳当量的聚乙二醇链。 Q组是包括酰胺，醚和硫醚部分之一的连接。基团R优选选自但不限于丙烯酰胺，溴代，溴乙酰胺，氯代，氯乙酰胺，二硫代吡啶基，酰肼，N-羟基琥珀酰亚胺酯，N-羟基磺基琥珀酰亚胺酯，亚氨酸酯，咪唑啉，碘，碘乙酰胺，马来酰亚胺，氨基和硫醇部分。组Z优选为通式（CH 2）n的无支链烷基链，其中n = 1-6。组Q优选选自NHCO，CONH，NHCOCH2，CONHCH2，O，OCH2，S和SCH2部分之一。

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