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    Polyamide nucleic acid derivatives and agents and processes for preparing them
    11.
    发明授权
    Polyamide nucleic acid derivatives and agents and processes for preparing them 有权
    聚酰胺核酸衍生物及其制备方法及其制备方法

    公开(公告)号：US06777544B2

    公开(公告)日：2004-08-17

    申请号：US09835370

    申请日：2001-04-17

    申请人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    IPC分类号： C12Q168

    CPC分类号： C07H21/00

    摘要： The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.

    摘要翻译： 本发明涉及在PNA主链的N末端携带磷酰基的PNA衍生物。 磷酰基可以是例如磷酸根或取代的磷酰基，其中取代的磷酰基衍生物在适当的情况下携带一个或多个标记基团，交联基团，促进细胞内摄取的基团或增加结合的基团 PNA衍生物对核酸的亲和力。 本发明还涉及制备上述PNA衍生物的方法及其作为药物和诊断剂的用途。

    Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
    12.
    发明授权
    Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids 有权
    用于制备PNA和PNA / DNA杂交体的取代的N-乙基甘氨酸衍生物

    公开(公告)号：US06465650B1

    公开(公告)日：2002-10-15

    申请号：US09506901

    申请日：2000-02-18

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07D47316

    CPC分类号： C07D233/92 ,  C07D231/12 ,  C07D233/56 ,  C07D239/47 ,  C07D239/54 ,  C07D249/08 ,  C07D473/18 ,  C07D473/34 ,  Y02P20/55

    摘要： The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.

    摘要翻译： 本发明提供制备式I化合物或其盐的方法，其中PG是氨基甲酸酯或三苯甲基型保护基; X是NH，O或S; Y是CH 2，O或NH; 而B'是核苷酸化学中常见的基础。 所述方法包括使式（II）化合物与式（III）化合物与式（Ⅴ）化合物在合适的溶剂中与辅助碱或式（Ⅶ）化合物反应，将式（Ⅴ）化合物与单卤代乙酸衍生物反应， 得到的化合物为式I化合物。

    PNA synthesis using a base-labile amino protecting group
    13.
    发明授权
    PNA synthesis using a base-labile amino protecting group 有权
    使用碱不稳定氨基保护基的PNA合成

    公开(公告)号：US06316595B1

    公开(公告)日：2001-11-13

    申请号：US09495457

    申请日：2000-02-01

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07K100

    CPC分类号： C07D239/47 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K14/003 ,  C08G69/10 ,  Y02P20/55

    摘要： The invention provides compounds and processes for synthesis of peptide nucleic acids (PNA). The compounds include temporary amino protecting groups that are base-labile, and protection groups for the exocyclic amino function of the nucleotide base that is compatible with the base-labile amino protecting group. Cleavage of an oligomer comprising these compounds from a solid support can be achieved using weak or medium strength acids.

    摘要翻译： 本发明提供了用于合成肽核酸（PNA）的化合物和方法。 这些化合物包括碱基不稳定的临时氨基保护基，和与碱不稳定氨基保护基相容的核苷酸碱基的环外氨基官能团的保护基。 包含这些化合物的低聚物从固体支持物的切割可以使用弱或中等强度的酸来实现。

    G cap-stabilized oligonucleotides
    14.
    发明授权
    G cap-stabilized oligonucleotides 失效
    G帽稳定的寡核苷酸

    公开(公告)号：US6013639A

    公开(公告)日：2000-01-11

    申请号：US594452

    申请日：1996-01-31

    申请人： Anuschirwan Peyman ,  Eugen Uhlmann

    发明人： Anuschirwan Peyman ,  Eugen Uhlmann

    IPC分类号： C12N15/09 ,  A61K31/70 ,  A61K31/7088 ,  A61K38/00 ,  A61P31/12 ,  A61P35/00 ,  C07H21/00 ,  C07H21/04 ,  C12N15/113 ,  A61K48/00 ,  C12Q1/68

    CPC分类号： C12N15/113 ,  C07H21/00 ,  C12N15/1132 ,  C12N15/1133 ,  C12N15/1135 ,  C12N15/1136 ,  C12N15/1138 ,  A61K38/00 ,  C12N2310/151 ,  C12N2310/315

    摘要： Oligonucleotides of the formula5'-(CAP)-(Oligo)-(CAP)-3'are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G.sub.m, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5' or 3' end and the end of the Oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.

    摘要翻译： 公开了5' - （CAP） - （Oligo） - （CAP）-3'的寡核苷酸，其中（oligo）是长度为10至40个核苷酸的核苷酸序列，CAP为Gm，其中m为整数 分子中存在的两个C​​AP可以彼此独立地定义，并且在5'或3'端的m为零并且Oligo序列的末端是其它的情况下必须是不同的 比鸟嘌呤。 寡核苷酸可以化学合成。 寡核苷酸用于诊断或治疗癌症，再狭窄，由病毒引起的疾病，受整联蛋白或细胞粘附受体影响的疾病或由可扩散因子引发的疾病。

    Polyamide nucleic acid derivatives and agents, and processes for preparing them
    17.
    发明授权
    Polyamide nucleic acid derivatives and agents, and processes for preparing them 失效
    聚酰胺核酸衍生物和试剂，及其制备方法

    公开(公告)号：US07897346B2

    公开(公告)日：2011-03-01

    申请号：US12474532

    申请日：2009-05-29

    申请人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David William Will

    IPC分类号： C12Q1/68 ,  C07H19/04 ,  C07H21/02

    CPC分类号： C07K14/003 ,  A61K38/00 ,  Y10T436/143333

    摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

    摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。

    Abasic Oligonucleotide as Carrier Platform for Antigen and Immunostimulatory Agonist and Antagonist
    20.
    发明申请
    Abasic Oligonucleotide as Carrier Platform for Antigen and Immunostimulatory Agonist and Antagonist 审中-公开
    碱性寡核苷酸作为抗原和免疫刺激激动剂和拮抗剂的载体平台

    公开(公告)号：US20080113929A1

    公开(公告)日：2008-05-15

    申请号：US11629106

    申请日：2005-06-08

    申请人： Grayson B. Lipford ,  Alexandra Forsbach ,  Eugen Uhlmann ,  Hermann Wagner

    发明人： Grayson B. Lipford ,  Alexandra Forsbach ,  Eugen Uhlmann ,  Hermann Wagner

    IPC分类号： A61K48/00

    CPC分类号： C07H21/00 ,  A61K39/0005 ,  A61K39/385 ,  A61K2039/6025 ,  A61K2039/6087 ,  A61K2039/6093 ,  A61K2300/00

    摘要： Compositions and methods are provided for enhancing delivery of therapeutic agents. More specifically, compositions and methods are provided for improving antigen delivery to antigen-presenting cells. Conjugates between abasic oligonucleotides and antigen are provided, along with methods for their use in vaccination and in the treatment of cancer, infection, and allergy and asthma. Also provided are conjugates between abasic oligonucleotides and various immunostimulatory nucleic acids, including CpG oligonucleotides, as well as methods of use thereof. Also provided are conjugates between abasic oligonucleotides and various other agonists and antagonists of immunostimulation, as well as methods of use thereof.

    摘要翻译： 提供了用于增强治疗剂递送的组合物和方法。 更具体地，提供了用于改善抗原递送细胞的抗原递送的组合物和方法。 提供了无碱基寡核苷酸和抗原之间的结合物，以及它们用于疫苗接种和治疗癌症，感染和过敏和哮喘的方法。 还提供了脱碱基寡核苷酸与各种免疫刺激核酸（包括CpG寡核苷酸）之间的缀合物，以及其使用方法。 还提供了无碱基寡核苷酸与各种其它激动剂和免疫刺激拮抗剂之间的缀合物，以及其使用方法。