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    Phenyldiboronic acid reagents and complexes
    1.
    发明授权
    Phenyldiboronic acid reagents and complexes 失效
    苯二硼酸试剂和络合物

    公开(公告)号：US6124471A

    公开(公告)日：2000-09-26

    申请号：US407673

    申请日：1999-09-28

    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： C07C229/38 ,  C07C233/49 ,  C07C233/51 ,  C07C237/12 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  C07D207/44 ,  C07D207/452 ,  C07D207/46 ,  C07D213/71 ,  C07F5/02 ,  G01N33/531 ,  G01N33/543

    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, ##STR1## 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 (CH.sub.2)n, wherein n=1 to 6. Group Q is preferably selected from one of NHCO, CONH, NHCOCH.sub.2, CONHCH.sub.2, O, OCH.sub.2, S and SCH.sub.2 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。

    Phenyldiboronic acid reagents and complexes
    3.
    发明授权
    Phenyldiboronic acid reagents and complexes 失效
    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。

    Bifunctional boronic compound complexing reagents and complexes
    4.
    发明授权
    Bifunctional boronic compound complexing reagents and complexes 失效
    双功能硼酸化合物络合物络合物

    公开(公告)号：US6156884A

    公开(公告)日：2000-12-05

    申请号：US222468

    申请日：1998-12-29

    申请人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    发明人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    IPC分类号： C07C229/38 ,  C07C233/49 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  G01N33/543 ,  C07F5/04

    CPC分类号： C07C233/49 ,  C07C229/38 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  G01N33/54353 ,  Y10S530/81 ,  Y10S530/816

    摘要： Reagents suitable for the modification of a bioactive species for the purpose of incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different (or the same) bioactive species having pendant phenylboronic acid moieties of General Formula 1, ##STR1## wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R.sub.2 is selected from one of H and OH moieties, and wherein group R.sub.3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH.sub.2).sub.n and CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.n.sbsb.2, wherein n is an integer of from 1 to 5, and wherein n.sub.2 is an integer of from 1 to 4. Each of group Z.sub.2 and Z.sub.3 is a spacer selected from CH.sub.2 Ar, CH.sub.2 CONHCH.sub.2 Ar, CH.sub.2 CONH(CH.sub.2).sub.n.sbsb.3 CO--NHCH.sub.2 Ar, and (CH.sub.2).sub.n.sbsb.4 NHCO(CH.sub.2).sub.n.sbsb.5 CONHCH.sub.2 Ar, wherein the group Ar represents the aromatic ring in the reagent of General Formula I to which the spacer Z.sub.2 or Z.sub.3 is appended, wherein n.sub.3 is an integer of from 1 to 5, wherein n.sub.4 is an integer selected from one of 2 and 3, and wherein n.sub.5 is an integer of from 1 to 4. Reaction of a reagent of General Formula I with a bioactive species affords a conjugate having pendant putative bifunctional boronic compound complexing moieties. (one or more) The conjugate may be further reacted with hydroxylamine (NH.sub.2 OH) by amidation of the benzoic acid ester moiety to afford a class of bifunctional boronic compound complexing conjugate, e.g., conjugate with one or more pendant bifunctional boronic compound complexing moieties.

    摘要翻译： 用于修饰生物活性物质的试剂，其目的是将双功能硼化合物络合部分结合到具有通式1的苯基硼酸侧基的不同（或相同）生物活性物质中，其中基团R是亲电子的或 适用于推定的双功能硼化合物络合试剂与生物活性物质的反应的亲核部分，其中基团R2选自H和OH部分之一，并且其中基团R3选自具有电负性取代基的烷基和亚甲基之一。 基团Z是选自（CH 2）n和CH 2 O（CH 2 CH 2 O）n 2的间隔基，其中n是1至5的整数，并且其中n 2是1至4的整数。基团Z 2和Z 3是间隔基 选自CH 2 Ar，CH 2 CONHCH 2 Ar，CH 2 CONH（CH 2）n 3 CO-NHCH 2 Ar和（CH 2）n 4 NHCO（CH 2）n5CONHCH 2 Ar，其中基团Ar表示通式I的试剂中附着有间隔基Z2或Z3的芳环， n3是1至5的整数，其中n4是选自2和3之一的整数，并且其中n5是1至4的整数。通式I的试剂与生物活性物质的反应提供了共轭物 具有推荐的双官能硼化合物络合部分。 （一种或多种）缀合物可以通过苯甲酸酯部分的酰胺化与羟胺（NH 2 OH）进一步反应，得到一类双官能硼化合物络合缀合物，例如与一个或多个双官能硼化合物络合部分的偶联物。

    Bifunctional boronic compound complexing reagents and complexes
    5.
    发明授权
    Bifunctional boronic compound complexing reagents and complexes 失效
    双功能硼酸化合物络合物络合物

    公开(公告)号：US06414122B1

    公开(公告)日：2002-07-02

    申请号：US09651007

    申请日：2000-08-29

    申请人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    发明人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    IPC分类号： C07F504

    CPC分类号： C07C233/49 ,  C07C229/38 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  G01N33/54353 ,  Y10S530/81 ,  Y10S530/816

    摘要： Embodiments include reagents to modify a bioactive species for incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different or same bioactive species having pendant phenylboronic acid moieties of General Formula I, wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R2 is selected from one of H and OH moieties, and wherein group R3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH2)n and CH2O(CH2CH2O)n2, wherein n is an integer of from 1 to 5, and wherein n2 is an integer of from 1 to 4. Group Z2 and Z3 is a spacer and need not be the same.

    摘要翻译： 实施方案包括用于修饰生物活性物质以用于掺入双功能硼化合物络合部分以用于随后与不同或相同的具有通式I的苯基硼酸部分的生物活性物质结合的试剂，其中基团R是适于反应的亲电子或亲核部分 其中基团R2选自H和OH部分之一，其中基团R3选自具有电负性取代基的烷基和亚甲基之一。 Z为选自（CH 2）n和CH 2 O（CH 2 CH 2 O）n 2的间隔基，其中n为1〜5的整数，n2为1〜4的整数.Z2和Z3为间隔基， 不一样

    Bifunctional boronic compound complexing reagents and complexes
    8.
    发明授权
    Bifunctional boronic compound complexing reagents and complexes 失效
    双功能硼酸化合物络合物络合物

    公开(公告)号：US06870065B2

    公开(公告)日：2005-03-22

    申请号：US10184836

    申请日：2002-06-28

    申请人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    发明人： Clarence N. Ahlem ,  Robert J. Kaiser ,  Kevin P. Lund ,  Mark L. Stolowitz

    IPC分类号： C07C229/38 ,  C07C233/49 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  G01N33/543 ,  C07C255/00

    CPC分类号： C07C233/49 ,  C07C229/38 ,  C07C237/22 ,  C07C255/13 ,  C07C259/10 ,  C07C271/22 ,  C07C281/02 ,  G01N33/54353 ,  Y10S530/81 ,  Y10S530/816

    摘要： A reagent having the general formula of General Formula I: wherein group R is an electrophilic or a nucleophilic moiety suitable for reaction of the reagent with a biologically active species; group R2 is one of H and OH moieties; group R3 is one of an alkyl and a methylene bearing an electronegative substituent; group Z is one of (CH2)n and CH2O(CH2CH2O)n2, and n is an integer of from 1 to 5, and n2 is an integer of from 1 to 4; and each of group Z2 and Z3 are (CH2)CONH(CH2)3CONH(CH2)2. Also, a reagent having the general formula of General Formula II: group R2 is one of H and OH moieties; group Z is one of (CH2)n and CH2O(CH2CH2O)n2, and n is an integer of from 1 to 5, and n2 is an integer of from 1 to 4; each of group Z2 and group Z3 include one of (CH2)CONH(CH2)3CONH(CH2)2; and (CH2)CONH(CH2); and group R is an electrophilic or a nucleophilic moiety suitable for reaction of the reagent with the biologically active species.

    摘要翻译： 具有通式I的通式的试剂：其中基团R是适于试剂与生物活性物质的反应的亲电子或亲核部分; 基团R2是H和OH部分之一; 基团R3是具有电负性取代基的烷基和亚甲基之一; 基团Z是（CH 2）n和CH 2 O（CH 2 CH 2 O）n 2中的一种，n是1至5的整数，n2是1至4的整数; Z 2和Z 3各自为（CH 2）CONH（CH 2）3 CONH（CH 2）2。 另外，具有通式II：R2的通式的试剂是H和OH部分之一; 基团Z是（CH 2）n和CH 2 O（CH 2 CH 2 O）n 2中的一种，n是1至5的整数，n2是1至4的整数; Z 2和Z 3中的每一个包括（CH 2）CONH（CH 2）3 CONH（CH 2）2中的一个; 和（CH 2）CONH（CH 2）; 并且基团R是适于试剂与生物活性物质反应的亲电子或亲核部分。