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22 条记录 (耗时 0.018 秒)

    Diketopiperazine Forming Dipeptidyl Linker
    11.
    发明申请
    Diketopiperazine Forming Dipeptidyl Linker 有权
    二酮哌嗪形成二肽基连接子

    公开(公告)号：US20140094567A1

    公开(公告)日：2014-04-03

    申请号：US13881883

    申请日：2011-10-20

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

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

    IPC分类号： C07K1/06

    CPC分类号： C07K1/068 ,  C07K1/04 ,  C07K1/062 ,  C07K5/06086 ,  C08F112/08 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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的连接子将该特异性保护的片段C-PEP制备成用于将生长中的肽链连接到树脂上的方法，该接头形成所述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。

    Synthesis of Site Specifically-Linked Ubiquitin
    12.
    发明申请
    Synthesis of Site Specifically-Linked Ubiquitin 审中-公开
    场地特异性连接的泛素的合成

    公开(公告)号：US20130065272A1

    公开(公告)日：2013-03-14

    申请号：US13636618

    申请日：2011-03-23

    申请人： Jason Chin ,  Duy Nguyen ,  Satpal Virdee

    发明人： Jason Chin ,  Duy Nguyen ,  Satpal Virdee

    IPC分类号： C07K1/107 ,  C12P21/06 ,  C12N9/50 ,  C07K14/435

    CPC分类号： C07K14/4702 ,  C07K1/064 ,  C07K1/065 ,  C07K1/068 ,  C07K1/1075 ,  C07K1/1077 ,  C07K14/435 ,  C12N9/50 ,  C12N9/93 ,  C12P21/02 ,  C12P21/06 ,  Y02P20/55

    摘要： The invention relates to a method of modifying a specific lysine residue in a polypeptide comprising at least two lysine residues, said method comprising (a) providing a polypeptide comprising a target lysine residue protected by a first protecting group, and at least one further lysine residue; (b) treating the polypeptide to protect said further lysine residue(s), wherein the protecting group for said further lysine residues is different to the protecting group for the target lysine residue; (c) selectively deprotecting the target lysine residue; and (d) modifying the deprotected lysine residue of (c).

    摘要翻译： 本发明涉及一种修饰包含至少两个赖氨酸残基的多肽中的特定赖氨酸残基的方法，所述方法包括（a）提供包含被第一保护基团保护的靶赖氨酸残基的多肽和至少一种赖氨酸残基 ; （b）处理多肽以保护所述另外的赖氨酸残基，其中所述另外的赖氨酸残基的保护基与靶赖氨酸残基的保护基不同; （c）选择性脱保护目标赖氨酸残基; 和（d）修饰（c）的去保护的赖氨酸残基。

    Protected derivatives of tryptophan, processes for their preparation and their use for the preparation of dipeptide, polypeptide or protein structures
    14.
    发明授权
    Protected derivatives of tryptophan, processes for their preparation and their use for the preparation of dipeptide, polypeptide or protein structures 失效
    受保护的色氨酸衍生物，其制备方法及其用于制备二肽，多肽或蛋白质结构的用途

    公开(公告)号：US5300651A

    公开(公告)日：1994-04-05

    申请号：US888667

    申请日：1992-05-27

    申请人： Peter D. White

    发明人： Peter D. White

    IPC分类号： C07D209/20 ,  C07K1/06 ,  C07K1/08 ,  C07K7/06 ,  C07K14/00 ,  C07F9/06 ,  C07D209/18

    CPC分类号： C07K1/068 ,  C07D209/20 ,  Y02P20/55

    摘要： A derivative of tryptophan is provided wherein the NH-group of the tryptophan indole nucleus is protected with tert.-butyloxycarbonyl (BOC) and the .alpha.-amino group is protected by 9-fluorenyl-methyloxy-carbonyl (FMOC). The carboxylic acid group of the tryptophan derivative may comprise a free COOH group, may be modified with a protecting or activating group, or may comprise an acyl group bonded to another chemical moiety, such as a polymer, another amino acid, a dipeptide, a polypeptide, or a protein. The tryptophan derivative is useful in the preparation of dipeptides, polypeptides or proteins containing at least one tryptophan-derived amino acid residue.

    摘要翻译： 提供色氨酸的衍生物，其中色氨酸吲哚核的NH基用叔丁氧基羰基（BOC）保护，（α） - 氨基被9-芴基 - 甲氧基 - 羰基（FMOC）保护。 色氨酸衍生物的羧酸基团可以包含游离COOH基团，可以用保护基或活化基团修饰，或者可以包含与另一个化学部分结合的酰基，例如聚合物，另一种氨基酸，二肽， 多肽或蛋白质。 色氨酸衍生物可用于制备含有至少一种色氨酸衍生的氨基酸残基的二肽，多肽或蛋白质。

    Aryloxycarbonyl fluorides and amino acids and their production
    15.
    发明授权
    Aryloxycarbonyl fluorides and amino acids and their production 失效
    芳烃酰氟和氨基酸及其生产

    公开(公告)号：US3592836A

    公开(公告)日：1971-07-13

    申请号：US3592836D

    申请日：1967-12-21

    申请人： BAYER AG

    发明人： UGI IVAR ,  KLAUKE ERICH ,  SCHNABEL EUGEN ,  HOFFMANN PETER

    IPC分类号： C07D307/42 ,  C07K1/06 ,  C07C69/00

    CPC分类号： C07D307/42 ,  C07K1/063 ,  C07K1/064 ,  C07K1/068

    摘要： ARYLOXYCARBONYL FLUORIDES SUCH AS FURFURYLOXYCARBONYL-, P-METHOXYBENZYLOXYCARBONYL- AND TRIMETHOXYBENZYLOXYCARBONYL-FLUORIDES ARE PROVIDED WHICH ARE USEFUL AS INTERMEDIATES FOR AMINO ACID DERIVATIVES AND ARE OBTAINED FROM CARBONYL-FLUORIDE CHLORIDE BY REACTION WITH THE APPROPRIATE ALCOHOL. THE AMINO ACID DERIVATIVES OF SUCH CARBONYL-FLUORIDES ARE BUILT UP THROUGH ACYLATION OF AMINO ACIDS THEREWITH. THESE AMINO ACID DERIVATIVES ARE USEFUL AS INTERMEDIATES FOR THE SYNTHESIS OF POLYPEPTIDES. THE REACTION OF CARBONYLCHLORIDE-FLUORIDE IS ADVANTAGEOUSLY CARRIED OUT AT TEMPERATURES OF 0 TO 70*C. IN AN INERT SOLVENT AND IN THE PRESENCE OF AN ACID-BINDING AGENT. THE AMINO ACID DERIVATIVES ARE FORMED AT TEMPERATURES BETWEEN +20 AND -20*C. ALSO IN THE PRESENCE OF AN ACID-BINDING AGENT. IMINO ACIDS CAN BE USED IN PLACE OF AMINO ACIDS. THE AMINO- OR IMINO-ACID DERIVATIVES OR ESTERS ARE ADVANTAGEOUSLY PREPARED AT CONSTANT. CONTROLLED PH VALUES, PREFERABLY BY THE USE OF AUTOMATIC PH CONTROL EQUIPMENT.

    Diketopiperazine forming dipeptidyl linker
    17.
    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

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

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

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

    CPC分类号： C07K1/068 ,  C07K1/04 ,  C07K1/062 ,  C07K5/06086 ,  C08F112/08 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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。

    Method for Producing Glycopeptide Having Sialyl Sugar Chain, Sialyl Sugar Chain-Added Amino Acid Derivative to be Used in Same, and Glycopeptide
    18.
    发明申请
    Method for Producing Glycopeptide Having Sialyl Sugar Chain, Sialyl Sugar Chain-Added Amino Acid Derivative to be Used in Same, and Glycopeptide 有权
    具有唾液酸糖链的糖肽，用于同时使用的唾液酸糖链氨基酸衍生物和糖肽的方法

    公开(公告)号：US20140058062A1

    公开(公告)日：2014-02-27

    申请号：US14004122

    申请日：2012-03-05

    申请人： Yasuhiro Kajihara ,  Masumi Murakami ,  Kazuyuki Ishii

    发明人： Yasuhiro Kajihara ,  Masumi Murakami ,  Kazuyuki Ishii

    IPC分类号： C07K14/00

    CPC分类号： C07K14/001 ,  C07H1/00 ,  C07K1/006 ,  C07K1/068

    摘要： [Technical Promblem]To provide a method for manufacturing that enables to obtain a targeted glycopeptide harboring a sialyl sugar chain in high yield without decomposing sialic acid at a non-reducing terminal of sugar chain when the glycopeptide is synthesized by a Boc solid phase synthesis method.[Solution to Problem]The present invention is characterized in that the Boc-sialylglycosylated amino acid derivative used in Boc solid phase synthesis method is one where the carboxyl group of the sialic acid at the sugar chain non-reducing terminal is protected with a phenacyl group.

    摘要翻译： [技术要点]提供一种制造方法，其能够通过Boc固相合成法合成糖肽，能够以高产率获得含有唾液酸糖链的靶糖蛋白，而不会在糖链的非还原末端分解唾液酸 。 [问题的解决方案]本发明的特征在于Boc固相合成法中使用的Boc-唾液酸糖基化氨基酸衍生物，其中在糖链非还原末端的唾液酸的羧基被苯甲酰基保护 。

    Process for the synthesis of a peptide having a Trp residue
    19.
    发明授权
    Process for the synthesis of a peptide having a Trp residue 有权
    用于合成具有Trp残基的肽的方法

    公开(公告)号：US07122628B2

    公开(公告)日：2006-10-17

    申请号：US10451486

    申请日：2001-12-19

    申请人： Steven Allen Jackson

    发明人： Steven Allen Jackson

    IPC分类号： C07K1/00 ,  C07K1/06 ,  C07K1/14 ,  C07K1/107 ,  C07K7/04

    CPC分类号： C07K1/068 ,  C07K7/23 ,  Y02P20/55

    摘要： A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said protecting group is removed during cleavage of said peptide from the solid support.

    摘要翻译： 一种用于固相合成具有至少一个色氨酸残基的肽的方法，其中所述方法包括用不稳定的侧链保护基将所述色氨酸残基的吲哚环临时保护，其中所述保护基在切割期间除去 的所述肽。