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    Peptide esterification
    13.
    发明申请
    Peptide esterification 审中-公开
    肽酯化

    公开(公告)号：US20020155614A1

    公开(公告)日：2002-10-24

    申请号：US10081379

    申请日：2002-02-21

    Inventor： Andrew J. Tomlinson ,  Marina Hincapie ,  Roman M. Chicz

    IPC: G01N033/00 ,  C07K007/00

    CPC classification number: G01N33/6842 ,  C07K1/062 ,  C07K1/12 ,  C07K1/18 ,  C07K1/20 ,  G01N33/6803

    Abstract: The invention provides methods and reagents for the esterification of peptides. The methods can be used to (i) enable a peptide in a first sample to be quantified relative to the level of the same peptide in a second sample, (ii) identify peptides in a complex mixtures that are targets for sequencing efforts, and (iii) aid peptide sequence elucidation. Methods that promote esterification and the formation of esters that are labeled with stable isotopes are described. These methods are useful for the analysis of low concentration (e.g., sub-femtomole) peptide mixtures.

    Abstract translation: 本发明提供了用于酯化酯化的方法和试剂。 所述方法可用于（i）使第一样品中的肽相对于第二样品中相同肽的水平进行定量，（ii）鉴定作为测序工作目标的复杂混合物中的肽，和 iii）帮助肽序列解析。 描述了促进酯化和形成用稳定同位素标记的酯的方法。 这些方法可用于分析低浓度（例如，亚飞甲虫）肽混合物。

    Novel 9-fluorenylmethoxycarbonyl compounds
    16.
    发明授权
    Novel 9-fluorenylmethoxycarbonyl compounds 失效
    新型9-芴基甲氧基羰基化合物

    公开(公告)号：US3906031A

    公开(公告)日：1975-09-16

    申请号：US38922573

    申请日：1973-08-17

    Applicant: RESEARCH CORP

    Inventor： CARPINO LOUIS A ,  HAN GRACE Y

    IPC: C07D295/24 ,  C07K1/06 ,  C07K5/06 ,  C07C125/06

    CPC classification number: C07D295/24 ,  C07C2603/18 ,  C07K1/062 ,  C07K1/063 ,  C07K1/064 ,  C07K5/06191 ,  Y10S930/15

    Abstract: The invention disclosed herein is generally concerned with novel 9-fluorenylmethyloxycarbonyl compounds and their reactions. More particularly, it is concerned with these novel compounds and their utility in the preparation of peptides, especially as blocking reagents for protection of free amino or carboxyl groups in amino acids or peptides. The compounds are also useful for separating racemic mixtures into their optical isomers.

    Abstract translation: 本文公开的本发明通常涉及新的9-芴基甲氧基羰基化合物及其反应。 更具体地，涉及这些新化合物及其在制备肽中的用途，特别是作为用于保护氨基酸或肽中的游离氨基或羧基的封闭剂。 该化合物也可用于将外消旋混合物分离成它们的旋光异构体。

    Benzylic compound
    18.
    发明授权
    Benzylic compound 有权
    苄基化合物

    公开(公告)号：US08859732B2

    公开(公告)日：2014-10-14

    申请号：US12976393

    申请日：2010-12-22

    Applicant: Daisuke Takahashi

    Inventor： Daisuke Takahashi

    IPC: C07K1/06 ,  C07C43/23 ,  C07C217/54 ,  C07C235/40 ,  C07C217/58

    CPC classification number: C07K5/1019 ,  C07C43/23 ,  C07C217/58 ,  C07C235/40 ,  C07C2601/14 ,  C07K1/062

    Abstract: The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.

    Abstract translation: 本发明提供即使在酸性条件下也可以以高产率除去的保护试剂，并能够在有机合成反应如肽合成等中提供高纯度的所得产物。 本发明的保护试剂是仅具有一个羟基被具有碳数不少于14的脂族烃基的有机基团取代的特定苄基化合物。

    Diketopiperazine forming dipeptidyl linker
    19.
    发明授权
    Diketopiperazine forming dipeptidyl linker 有权
    二酮哌嗪形成二肽基接头

    公开(公告)号：US08802819B2

    公开(公告)日：2014-08-12

    申请号：US13881883

    申请日：2011-10-20

    Applicant: Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    Inventor： Fernando Albericio ,  Michèle Cristau ,  Matthieu Giraud ,  Miriam Gongora Benitez ,  Judit Tulla-Puche

    IPC: C07K1/06 ,  C07K1/02 ,  C07K1/04 ,  C07K5/068

    CPC classification number: C07K1/068 ,  C07K1/04 ,  C07K1/062 ,  C07K5/06086 ,  C08F112/08 ,  Y02P20/55

    Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.

    Abstract translation: 本发明涉及一种N-末端肽片段PEP-N和C-末端肽片段C-PEP的均相溶液相肽合成（HSPPS）的方法，其中携带特异性二酮哌嗪（DKP）的C-PEP包含C- 末端保护基，其含有句柄组HG，其中HG连接到肽片段的C末端; 因此，作为常规使用的C末端保护基可以从肽中选择性地切割含有C末端保护基的这种特定的DKP。 通过使用包含C末端保护基的该DKP和HG，可以避免基于HSPPS和固相肽合成（SPPS）的组合的收敛肽合成中的某些方法步骤。 本发明进一步涉及通过使用包含特异性二肽和HG的连接体将这种特异性保护的片段C-PEP制备成用于将生长中的肽链连接到树脂上的方法，该连接体形成所述DKP基团，当肽 片段C-PEP与支撑树脂分离; 并且还涉及制备方法的中间体。

    BENZYLIC COMPOUND
    20.
    发明申请
    BENZYLIC COMPOUND 有权
    苄基化合物

    公开(公告)号：US20110160433A1

    公开(公告)日：2011-06-30

    申请号：US12976393

    申请日：2010-12-22

    Applicant: Daisuke TAKAHASHI

    Inventor： Daisuke TAKAHASHI

    IPC: C07K1/06 ,  C07C43/23 ,  C07C217/54 ,  C07C235/40 ,  C07D209/20

    CPC classification number: C07K5/1019 ,  C07C43/23 ,  C07C217/58 ,  C07C235/40 ,  C07C2601/14 ,  C07K1/062

    Abstract: The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.

    Abstract translation: 本发明提供即使在酸性条件下也可以以高产率除去的保护试剂，并能够在有机合成反应如肽合成等中提供高纯度的所得产物。 本发明的保护试剂是仅具有一个羟基被具有碳数不少于14的脂族烃基的有机基团取代的特定苄基化合物。

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