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公开(公告)号：US5859210A
公开(公告)日：1999-01-12
申请号：US956195
申请日：1997-10-22
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 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula IV and General Formula VI. In one embodiment, the reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 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 of intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.
摘要翻译： 硼化合物络合剂，硼化合物络合物，以及合成这些试剂和络合物的方法。 这些试剂和络合物包括通式IV和通式VI所示的那些试剂和络合物。 在一个实施方案中，通式IV的试剂可用于与硼化合物如通式VI所示的络合物形成络合物。 通式IV通式VI在一个实施方案中，基团Z包含选自长度最多约6碳当量的饱和或不饱和链的间隔基，约6至18的无支链饱和或不饱和链 长度的碳当量与中间体酰胺或二硫化物部分中的至少一种和长度为约3至12碳当量的聚乙二醇链; 基团R3选自具有电负性取代基的H，烷基和亚甲基或亚乙基部分中的一个; BAS和BAS *是生物活性物种。
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公开(公告)号：US5744627A
公开(公告)日：1998-04-28
申请号：US691929
申请日：1996-08-05
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 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula III, General Formula IV, and General Formula VI. In one embodiment, the reagents of General Formula III may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula IV. The reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1##
摘要翻译： 硼化合物络合剂，硼化合物络合物，以及合成这些试剂和络合物的方法。 这些试剂和络合物包括通式III，通式IV和通式VI所示的试剂和络合物。 在一个实施方案中，通式III的试剂可用于在与生物活性物质（BAS）缩合后生产通式IV的试剂。 通式IV的试剂可用于与硼化合物如通式VI所示的络合物形成络合物。 方程式IV
通用VI -
公开(公告)号：US5877297A
公开(公告)日：1999-03-02
申请号：US956196
申请日：1997-10-22
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 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07C233/51 , C07C229/38 , C07C233/49 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound completing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents. These reagents, including those shown as General Formula CII may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises 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 of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene with an electronegative moiety; and BAS is a biologically active species.
摘要翻译： 硼化合物完成试剂，那些试剂的中间试剂和合成这些试剂的方法。 在本文所述的进一步反应后，可以使用这些试剂，包括通式CII所示的那些试剂与硼酸化合物如苯基硼酸或其衍生物复合。 通式CII在一个实施方案中，基团Z包括选自饱和或不饱和链长度至多约0至6个碳当量长度的间隔基，长度为约6至18个碳当量长度的无支链饱和或不饱和链， 中间体酰胺和二硫化物部分中的至少一个和长度为3至12个碳当量的聚乙二醇链; 基团R2是具有电负性部分的烷基和亚甲基之一; 而BAS是一种生物活性物种。
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公开(公告)号：US5777148A
公开(公告)日：1998-07-07
申请号：US691930
申请日：1996-08-05
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 , C07F5/04 , C07K5/02 , G01N33/543 , C07C233/31
CPC分类号： C07C233/51 , C07C229/38 , C07C233/49 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1##
摘要翻译： 公开硼化合物络合剂，这些试剂的中间试剂和合成这些试剂的方法。 在本文所述的进一步反应后，可以使用这些试剂，包括通式I和通式II所示的试剂，与硼酸化合物如苯基硼酸或其衍生物复合。 通用公式CI
通用CII -
公开(公告)号：US6156884A
公开(公告)日：2000-12-05
申请号：US222468
申请日：1998-12-29
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。
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公开(公告)号：US06414122B1
公开(公告)日：2002-07-02
申请号：US09651007
申请日：2000-08-29
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
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公开(公告)号：US5872224A
公开(公告)日：1999-02-16
申请号：US956194
申请日：1997-10-22
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 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07C233/51 , C07C229/38 , C07C233/49 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIV, and General Formula CVI. In one embodiment, the reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 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 of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.
摘要翻译： 硼化合物络合剂，硼化合物络合物，以及合成这些试剂和络合物的方法。 这些试剂和络合物包括通式CIV和通式CVI所示的那些。 在一个实施方案中，通式CIV的试剂可用于与硼化合物形成络合物，例如通式CVI所示的络合物。 通式CVI在一个实施方案中，组Z包含长度为至多约6碳当量的饱和或不饱和链的间隔基，约6至18的无支链饱和或不饱和链 中间体酰胺和二硫化物部分中的至少一个长度的碳当量和长度为约3至12碳当量的聚乙二醇链; 基团R3选自具有电负性取代基的H，烷基和亚甲基或亚乙基部分中的一个; BAS和BAS *是生物活性物种。
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公开(公告)号：US5869623A
公开(公告)日：1999-02-09
申请号：US956204
申请日：1997-10-22
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 , C07F5/04 , C07K5/02 , G01N33/543
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents, intermediate reagents of those reagents, and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene group with an electronegative moiety; and BAS is a biologically active species.
摘要翻译： 公开了硼化合物络合试剂，那些试剂的中间试剂和合成这些试剂的方法。 在本文所述的进一步反应后，可以使用这些试剂，包括通式II所示的试剂，与硼酸化合物如苯基硼酸或其衍生物复合。 通式II在一个实施方案中，基团Z包括长度为至多约6碳当量的饱和或不饱和链的间隔基，至少约6至18个碳当量长度的无支链饱和或不饱和链 一个中间体酰胺或二硫化物部分，和长度为约3至12个碳当量的聚乙二醇链; 基团R2是具有电负性部分的烷基和亚甲基之一; 而BAS是一种生物活性物种。
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公开(公告)号：US06870065B2
公开(公告)日：2005-03-22
申请号：US10184836
申请日：2002-06-28
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。
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公开(公告)号：US5847192A
公开(公告)日：1998-12-08
申请号：US689341
申请日：1996-08-05
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 , C07F5/04 , C07K5/02 , G01N33/543 , C07C233/50 , C07C233/46
CPC分类号： C07D207/452 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/54353
摘要： Boron compound complexing reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1##
摘要翻译： 公开了硼化合物络合试剂和合成这些试剂的方法。 在本文所述的进一步反应后，可以使用这些试剂，包括通式I和通式II所示的试剂，与硼酸化合物如苯基硼酸或其衍生物复合。 一般公式I
通用二级
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