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    CHEMOSELECTIVE LIGATION
    1.
    发明申请
    CHEMOSELECTIVE LIGATION 有权
    化学定位

    公开(公告)号：US20110236930A1

    公开(公告)日：2011-09-29

    申请号：US13043274

    申请日：2011-03-08

    申请人： Eliana Saxon ,  Carolyn Ruth Bertozzi

    发明人： Eliana Saxon ,  Carolyn Ruth Bertozzi

    IPC分类号： C12P21/04 ,  C07H1/00

    CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

    摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

    摘要翻译： 本发明的特征在于可以在生理条件下进行的化学选择性连接反应。 通常，本发明涉及特异性改造的膦的缩合，其可以提供在两个反应性配对物之间形成酰胺键，产生包含膦部分的最终产物，或者可被工程化以包含可切割连接体，使得 将膦的取代基转移到叠氮化物中，释放氧化的膦副产物并在最终产物中产生天然酰胺键。 反应的选择性及其与水性环境的相容性在体内（例如，在细胞表面或细胞内）和体外（例如，肽和其他聚合物的合成，修饰（例如，标记的）氨基酸的产生 ）。

    Chemoselective ligation
    2.
    发明授权
    Chemoselective ligation 有权

    公开(公告)号：US07939626B2

    公开(公告)日：2011-05-10

    申请号：US11533129

    申请日：2006-09-19

    申请人： Eliana Saxon ,  Carolyn R. Bertozzi

    发明人： Eliana Saxon ,  Carolyn R. Bertozzi

    IPC分类号： A61K38/00 ,  C07K16/00

    CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

    摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

    Chemoselective ligation
    3.
    发明授权
    Chemoselective ligation 有权

    公开(公告)号：US07122703B2

    公开(公告)日：2006-10-17

    申请号：US10384099

    申请日：2003-03-06

    申请人： Eliana Saxon ,  Carolyn Bertozzi

    发明人： Eliana Saxon ,  Carolyn Bertozzi

    IPC分类号： C12N5/02 ,  C12P7/26 ,  C07F5/00 ,  C07F9/02

    CPC分类号： C07K1/1077 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65522 ,  C07F9/6561 ,  C07H7/02 ,  C07H13/00 ,  C07H15/203 ,  C07H15/26 ,  C07K1/023 ,  C07K1/04 ,  C07K1/1075

    摘要： The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

    Extended native chemical ligation
    4.
    发明申请
    Extended native chemical ligation 审中-公开
    扩展的天然化学结扎

    公开(公告)号：US20040138412A1

    公开(公告)日：2004-07-15

    申请号：US10333017

    申请日：2003-01-15

    发明人： Paolo Botti ,  James A Bradburne ,  Stephen B H Kent ,  Donald W Low

    IPC分类号： C12P019/34 ,  C07K007/08

    CPC分类号： C07K14/505 ,  C07K1/006 ,  C07K1/023 ,  C07K1/026 ,  C07K1/04

    摘要： The invention is directed to methods and compositions for chemical ligation of components comprising a first component having a carboxythioester, and preferable an null-carboxythioester, moiety and a second component having an N-substituted, and preferably an Nnull-substituted, 2 or 3 carbon chain alkyl or aryl thiol to give a ligation product having an N-substituted amide bond at the ligation site. The reactants of the invention are chemoselective, and the alkyl or aryl thiol moiety is removable from the ligation product. Removal of the alkyl or aryl thiol gives a native amide bond at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers having a native amide bond at the ligation site.

    摘要翻译： 本发明涉及用于化学连接组分的方法和组合物，其包含具有羧基硫酯的第一组分，优选的是α-羧基硫代酯，部分和具有N-取代的，优选Nalpha取代的2或3个碳的第二组分 链烷基或芳基硫醇，以在连接位点产生具有N-取代的酰胺键的连接产物。 本发明的反应物是化学选择性的，并且烷基或芳基硫醇部分可从连接产物中除去。 去除烷基或芳基硫醇在连接位点产生天然酰胺键。 本发明的方法和组合物特别适用于肽和多肽的连接。 本发明的连接系统可应用于各种各样的分子，因此可以利用其在连接位点产生具有天然酰胺键的肽，多肽和其它含氨基酸的聚合物。

    Side chain anchored thioester and selenoester generators
    5.
    发明申请
    Side chain anchored thioester and selenoester generators 审中-公开
    侧链锚定硫酯和硒酯发生器

    公开(公告)号：US20040063902A1

    公开(公告)日：2004-04-01

    申请号：US10622359

    申请日：2003-07-18

    发明人： Leslie Philip Miranda

    IPC分类号： C12N009/16

    CPC分类号： C07K1/023 ,  C07K1/026 ,  C07K1/04 ,  C07K1/086 ,  C07K1/088

    摘要： Thioester and selenoester generators, thioester and selenoester compounds, and related methods for their production are provided. The subject thioester and selenoester generators include an amino acid synthon having an N-terminal group joined to a C-terminal group through an organic backbone comprising one or more carbons. The organic backbone contains a carbon having a side chain anchored to a support through a nucleophile-stable linker and is lacking reactive functional groups. The organic backbone may include a target molecule of interest, such as an amino acid, peptide, polypeptide or other organic compound of interest, and/or the N- and/or C-termini can be elaborated using a variety of synthesis approaches to provide a target molecule of interest. The compounds and methods find a wide variety of uses, including use in thioester- or selenoester-based chemical ligation techniques.

    摘要翻译： 提供硫酯和硒酯发生剂，硫酯和硒酯化合物及其生产的相关方法。 受试者硫酯和硒代发酵剂包括具有通过包含一个或多个碳的有机骨架连接到C末端基团的N-末端基团的氨基酸合成子。 有机骨架包含具有通过亲核 - 稳定接头锚定于载体的侧链并且缺少反应性官能团的碳。 有机骨架可以包括目标靶分子，例如氨基酸，肽，多肽或其它感兴趣的有机化合物，和/或使用多种合成方法来制备N-和/或C-末端以提供 目标分子的兴趣。 化合物和方法发现了多种用途，包括用于基于硫酯或硒酯的化学连接技术。

    Nucleophile-stable thioester generating compounds, methods of production and use
    6.
    发明申请
    Nucleophile-stable thioester generating compounds, methods of production and use 失效
    亲核稳定硫酯生成化合物，生产和使用方法

    公开(公告)号：US20030149234A1

    公开(公告)日：2003-08-07

    申请号：US10332454

    申请日：2003-01-09

    发明人： Paolo Botti ,  James A. Bradburne ,  Stephen B.H. Kent

    IPC分类号： C07K007/00 ,  C07C327/02

    CPC分类号： C07K1/023 ,  C07C323/52 ,  C07K1/006 ,  C07K1/026 ,  C07K1/04

    摘要： The invention is directed to nucleophile-stable thioester generating compounds comprising an orthothioloester or a carboxyester thiol, methods of production and use. The compounds and methods have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.

    摘要翻译： 本发明涉及包含邻硫基酯或羧基酯硫醇的亲核稳定硫酯生成化合物，其生产和使用方法。 这些化合物和方法在有机合成中具有广泛的应用，包括产生肽，多肽和其它聚合物 - 硫酯。 本发明特别可用于从在其中使用强亲核试剂的条件下制备的前体产生活化硫酯，例如使用Fmoc SPPS制备的肽或多肽，以及需要（或从中获益）的多步连接或缀合方案 使用）相容的选择性方法来引导感兴趣的特异性连接或缀合反应。

    Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form
    7.
    发明申请
    Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form 审中-公开
    用于试剂的剂量形式，在有机化学合成中使用所述给药形式并生产所述给药形式

    公开(公告)号：US20030138376A1

    公开(公告)日：2003-07-24

    申请号：US10245836

    申请日：2002-09-16

    申请人： H. Lundbeck A/S

    发明人： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

    IPC分类号： A61K049/00 ,  G01N033/543

    CPC分类号： C07K1/023 ,  B01J4/02 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  C07K1/04 ,  C07K1/1077 ,  C40B60/14

    摘要： A dosing form for at least one solid reagent for use in conventional organic and inorganic synthesis, in parallel synthesis, and in split and mix synthesis in combinatorial chemistry is provided as compressed tablets each containing the same predetermined amount of said at least one reagent embedded in a polymer matrix comprising beads of a polymer insoluble in the solvents for the intended synthesis, which tablets are capable of disintegrating in said solvent for release of the at least one reagent and disperse the matrix as polymer beads into the solvent. The polymer beads forming the matrix and the reagents of the dosing form can easily be removed by filtration in order to separate these from a formed soluble product. In a method for producing the dosing form, beads of one or more polymers are mixed with the reagents and compressed into tablets after pre-treatment with an aprotic organic solvent.

    摘要翻译： 提供用于常规有机和无机合成，并行合成和组合化学中的分离和混合合成中的至少一种固体试剂的给药形式，其为包含相同预定量的所述至少一种试剂 聚合物基质，其包含不溶于用于预期合成的溶剂中的聚合物的珠粒，该片剂能够在所述溶剂中分解以释放至少一种试剂并将基质作为聚合物珠分散到溶剂中。 形成基质的聚合物珠粒和剂型的试剂可以通过过滤容易地除去，以将它们与形成的可溶性产物分离。 在制备给药形式的方法中，将一种或多种聚合物的珠粒与试剂混合，并用非质子有机溶剂预处理后压制成片剂。