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    Means and methods of enhancing delivery to biological systems
    1.
    发明授权
    Means and methods of enhancing delivery to biological systems 有权
    增强对生物系统传播的手段和方法

    公开(公告)号：US09211340B2

    公开(公告)日：2015-12-15

    申请号：US12443236

    申请日：2007-09-26

    申请人： Paolo Botti

    发明人： Paolo Botti

    IPC分类号： A61K47/48

    CPC分类号： A61K47/48038 ,  A61K47/542 ,  A61K47/543 ,  A61K47/60 ,  C07K7/08

    摘要： This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and/or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.

    摘要翻译： 本发明涉及一种肽或多肽（a），其在C末端的羧酸酯上被酯化或硫酯化（i）与胍烷醇，胍链烷硫醇，被胍基取代并具有游离羟基的PEG 或被胍基和巯基取代的PEG; （ii）在一个或多个Asp或Glu残基的侧链羧酸酯上，如果存在的话，可以使用胍烷醇，胍烷硫醇，被胍基取代并具有游离羟基的PEG，或被 胍基和巯基; （iii）在一个或多个Ser，Thr或Tyr残基的羟基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的羟基; （iv）在一个或多个Cys残基的巯基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的巯基; 和/或（v）在N末端具有胍基链烷酸或被胍基和羧基取代的PEG，其中所述N-末端预先用α-或β-羟基酸酰胺化，并且其中 所述α-羟基酸或β-羟基酸的羟基与所述胍链烷酸的羧基或所述被胍基和羧基取代的PEG之间形成酯; 和/或（b）其中含有一个或多个二硫化物，在Cys的巯基之间形成的二硫键存在于烷基硫醇胍或被胍基和巯基取代的PEG之间。

    Chemical peptide ligation with three or more components
    2.
    发明授权
    Chemical peptide ligation with three or more components 有权
    化学肽与三个或更多成分结合

    公开(公告)号：US07884182B2

    公开(公告)日：2011-02-08

    申请号：US10494928

    申请日：2002-11-14

    申请人： Paolo Botti ,  Hubert Gaertner ,  Sonia Manganiello ,  Matteo Villain

    发明人： Paolo Botti ,  Hubert Gaertner ,  Sonia Manganiello ,  Matteo Villain

    IPC分类号： A61K38/00

    CPC分类号： C07K1/1077 ,  C07K1/026 ,  C07K1/04 ,  Y02P20/55

    摘要： The invention provides a method of assembling oligopeptide intermediates in a native chemical ligation reaction that eliminates self-ligation of bi-functional intermediates. An important aspect of the invention is a bi-functional intermediate with an N-terminal heterocyclic protecting group which effectively prevents self-ligation in the chemical assembly process. The present invention is useful in methods for convergent synthesis of polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where three or more peptide fragments are used to assemble a polypeptide or protein product.

    摘要翻译： 本发明提供了在天然化学连接反应中组装寡肽中间体的方法，其消除双功能中间体的自连接。 本发明的一个重要方面是具有N-末端杂环保护基的双功能中间体，其有效地防止化学组装过程中的自连接。 本发明可用于多肽和蛋白质的收敛合成的方法，并提高天然化学连接反应的效率，特别是在使用三个或更多个肽片段来组装多肽或蛋白质产物的情况下。

    MEANS AND METHODS OF ENHANCING DELIVERY TO BIOLOGICAL SYSTEMS
    5.
    发明申请
    MEANS AND METHODS OF ENHANCING DELIVERY TO BIOLOGICAL SYSTEMS 审中-公开
    提高生物系统交付的手段和方法

    公开(公告)号：US20150359899A1

    公开(公告)日：2015-12-17

    申请号：US14842588

    申请日：2015-09-01

    申请人： PAOLO BOTTI

    发明人： PAOLO BOTTI

    IPC分类号： A61K47/48 ,  C07K7/08

    CPC分类号： C07K7/08 ,  A61K47/542 ,  A61K47/543 ,  A61K47/60

    摘要： This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or Glu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and/or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.

    摘要翻译： 本发明涉及一种肽或多肽（a），其在C末端的羧酸酯上被酯化或硫酯化（i）与胍烷醇，胍链烷硫醇，被胍基取代并具有游离羟基的PEG 或被胍基和巯基取代的PEG; （ii）在一个或多个Asp或Glu残基（如果存在的话）的侧链羧酸酯上，可以使用胍烷醇，胍烷硫醇，被胍基取代并具有游离羟基的PEG，或被 胍基和巯基; （iii）在一个或多个Ser，Thr或Tyr残基的羟基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的羟基; （iv）在一个或多个Cys残基的巯基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的巯基; 和/或（v）在N末端具有胍基链烷酸或被胍基和羧基取代的PEG，其中所述N-末端预先用α-或β-羟基酸酰胺化，并且其中 所述α-羟基酸或β-羟基酸的羟基与所述胍链烷酸的羧基或所述被胍基和羧基取代的PEG之间形成酯; 和/或（b）其中含有一个或多个二硫化物，在Cys的巯基之间形成的二硫键存在于烷基硫醇胍或被胍基和巯基取代的PEG之间。

    Method of producing a modified (poly) peptide
    6.
    发明授权
    Method of producing a modified (poly) peptide 有权
    生产修饰（多）肽的方法

    公开(公告)号：US08729228B2

    公开(公告)日：2014-05-20

    申请号：US12088119

    申请日：2006-09-28

    申请人： Paolo Botti

    发明人： Paolo Botti

    IPC分类号： A61K38/00 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00

    CPC分类号： C07K1/1077 ,  C07K1/003

    摘要： This invention relates to a method of producing a modified (poly)peptide, said method comprising the step of modifying in an organic solvent a crown ether-bound (poly)peptide at one or more carboxylic groups by esterification or thioesterification and/or at the amino group of the N-terminal amino acid by amidation or alkylation. Furthermore provided are (poly)peptides and antibodies obtainable with the method of the invention as well as medical uses thereof.

    摘要翻译： 本发明涉及生产修饰的（多）肽的方法，所述方法包括在有机溶剂中通过酯化或硫酯化在一个或多个羧基上改性冠醚结合（多）肽的步骤和/或在 通过酰胺化或烷基化处理N-末端氨基酸的氨基。 此外提供的是（多）肽和可用本发明的方法获得的抗体及其医疗用途。

    Side-Chain Extended Ligation
    7.
    发明申请
    Side-Chain Extended Ligation 审中-公开
    侧链扩展连接

    公开(公告)号：US20090192300A1

    公开(公告)日：2009-07-30

    申请号：US11917636

    申请日：2006-06-16

    申请人： Paolo Botti ,  Sylvie Tchertchian

    发明人： Paolo Botti ,  Sylvie Tchertchian

    IPC分类号： C07K1/10

    CPC分类号： C07K1/04 ,  C07K1/026

    摘要： The invention is directed to methods and compositions for chemical ligation of a first component that includes a carboxythioester and a second component that includes an amino-functionalized compound bearing a branched side chain that includes a removable thiol auxiliary, to give a ligation product having an amide bond at the ligation site. The reactants of the invention are chemoselective and the thiol moiety is removable from the ligation product. Removal of the thiol can be exploited to generate a native side chain 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.

    摘要翻译： 本发明涉及用于化学连接第一组分的方法和组合物，所述第一组分包括羧基硫酯和第二组分，所述第二组分包括带有支链侧链的氨基官能化化合物，其包含可除去的硫醇辅助剂，得到具有酰胺的连接产物 结扎部位的结合。 本发明的反应物是化学选择性的，硫醇部分可从连接产物中除去。 可以利用硫醇的去除在结合位点产生天然侧链。 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，因此可用于产生肽，多肽和其它含氨基酸的聚合物。

    Carboxy protection strategies for acidic C-terminal amino acids in chemical ligation of oligopeptides
    8.
    发明授权
    Carboxy protection strategies for acidic C-terminal amino acids in chemical ligation of oligopeptides 失效
    酸性C末端氨基酸在寡肽化学连接中的羧基保护策略

    公开(公告)号：US07566697B2

    公开(公告)日：2009-07-28

    申请号：US10517392

    申请日：2003-06-09

    申请人： Paolo Botti ,  Matteo Villain ,  Sonia Manganiello ,  Hubert Gaertner

    发明人： Paolo Botti ,  Matteo Villain ,  Sonia Manganiello ,  Hubert Gaertner

    IPC分类号： A61K38/08

    CPC分类号： C07K1/04 ,  C07K1/061 ,  C07K1/062 ,  C07K1/065 ,  C07K1/067 ,  C07K5/10 ,  C07K7/04 ,  C07K14/001 ,  C07K17/00

    摘要： The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotected acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.

    摘要翻译： 本发明提供了在天然化学连接反应中组装寡肽或多肽的方法，其消除由未保护的酸性C-末端寡肽硫酯的存在产生的不需要的副产物的形成。 本发明的一个重要方面是提供侧链保护的酸性C末端寡肽硫酯。 本发明可用于化学合成寡肽，多肽和蛋白质并提高天然化学连接反应的效率的方法，特别是当天冬氨酰基或谷氨酰肽片段用于组装寡肽，多肽或蛋白质产物时。

    MUCOSAL DELIVERY OF DRUGS
    10.
    发明申请
    MUCOSAL DELIVERY OF DRUGS 有权
    药物输送

    公开(公告)号：US20140187489A1

    公开(公告)日：2014-07-03

    申请号：US14122182

    申请日：2012-05-25

    申请人： Paolo Botti ,  Sylvie Tchertchian

    发明人： Paolo Botti ,  Sylvie Tchertchian

    IPC分类号： A61K47/24 ,  A61K38/26 ,  A61K47/22 ,  A61K47/14

    CPC分类号： A61K47/22 ,  A61K9/0014 ,  A61K38/11 ,  A61K38/2278 ,  A61K38/23 ,  A61K38/26 ,  A61K38/28 ,  A61K38/29 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28

    摘要： The present invention provides a composition comprising or consisting of components (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C4 to C21 alkanoyl, preferably from octanoyl and decanoyl; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C6 to C21 alkanoyl and C6 to C21 alkenoyl.

    摘要翻译： 本发明提供一种组合物，其包含或由组分（a）（i）组成，至少一种单烷酰基甘油酯，其中烷酰基选自C 4至C 21烷酰基，优选为辛酰基和癸酰基; 和（b）（i）至少一种选自胆固醇，磷脂酰胆碱和磷脂酰甘油的化合物，其中磷脂酰基部分的酰基部分独立地选自C6至C21烷酰基和C6至C21链烯酰基。