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    PNA synthesis using a base-labile amino protecting group
    14.
    发明授权
    PNA synthesis using a base-labile amino protecting group 失效
    使用碱不稳定氨基保护基的PNA合成

    公开(公告)号：US6121418A

    公开(公告)日：2000-09-19

    申请号：US967197

    申请日：1997-10-29

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07C231/02 ,  C07C233/36 ,  C07C233/47 ,  C07C237/12 ,  C07D239/46 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K1/00 ,  C07K1/04 ,  C07K1/113 ,  C07K5/04 ,  C07K14/00 ,  C07K14/485 ,  C07K14/52 ,  C08G69/10

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

    摘要： PNA synthesis using a base-labile amino protecting group Processes are described for preparing PNA oligomers, ##STR1## in which R.sup.0 is hydrogen, alkanoyl, alkoxycarbonyl, cycloalkanoyl, aroyl, heteroaroyl, or a group which favors the intracellular uptake of the oligomer, A and Q are amino acid residues, k and 1 are 0 to 20, n is 1-50, B is a nucleotide base which is customary in nucleotide chemistry, and Q.sup.0 is OH, NH.sub.2, or alkylamino which can be substituted by OH or NH.sub.2. In these processes, the amino acid residues and the structural components ##STR2## in which PG is a base-labile amino protecting group and B' is a nucleotide base which is protected on its exocyclic amino function, are coupled step-wise, in accordance with the solid-phase method, onto a polymeric support which is provided with an anchor group, and, after the construction is complete, the target compounds are cleaved from the polymeric support using a cleaving reagent. Intermediates of the PNA oligomers are also described, as are processes for their preparation.

    摘要翻译： 描述了使用碱不稳定氨基保护基的PNA合成制备PNA寡聚体的方法，其中R 0是氢，烷酰基，烷氧基羰基，环烷酰基，芳酰基，杂芳酰基或有利于寡聚体的细胞内摄取的基团A和Q是 氨基酸残基k和1为0至20，n为1-50，B为核苷酸化学中常见的核苷酸碱基，Q0为OH，NH2或可被OH或NH2取代的烷基氨基。 在这些方法中，PG是碱不稳定氨基保护基团的氨基酸残基和结构组分，B'是其外环氨基功能受保护的核苷酸碱基，按照固体 在具有锚定基团的聚合物载体上，并且在构建完成后，使用裂解试剂从聚合物载体上切割目标化合物。 还描述了PNA低聚物的中间体，以及它们的制备方法。

    Polymide nucleic acid derivatives, and agents and processes for preparing them
    16.
    发明授权
    Polymide nucleic acid derivatives, and agents and processes for preparing them 失效
    聚酰亚胺核酸衍生物，及其制备方法和制备方法

    公开(公告)号：US08268560B2

    公开(公告)日：2012-09-18

    申请号：US13012266

    申请日：2011-01-24

    申请人： Eugen Uhlmann ,  Gerhard Breipohl ,  David W. Will

    发明人： Eugen Uhlmann ,  Gerhard Breipohl ,  David W. Will

    IPC分类号： C12Q1/68 ,  A01N61/00 ,  A61K48/00

    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。

    Polyamide-oligonucleotide derivatives, their preparation and use
    17.
    发明申请
    Polyamide-oligonucleotide derivatives, their preparation and use 失效
    聚酰胺 - 寡核苷酸衍生物，其制备和用途

    公开(公告)号：US20050026817A1

    公开(公告)日：2005-02-03

    申请号：US10939214

    申请日：2004-09-10

    申请人： Eugen Uhlmann ,  Gerhard Breipohl

    发明人： Eugen Uhlmann ,  Gerhard Breipohl

    IPC分类号： A61K47/48 ,  C07H21/00 ,  C07K14/00 ,  C12Q1/68 ,  A61K38/14 ,  A61K38/16

    CPC分类号： C07H21/00 ,  A61K47/59 ,  A61K47/595 ,  A61K47/60 ,  A61K47/605 ,  C07K14/003

    摘要： Polyamide-oligonucleotide derivatives of the formula F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF′wherein q, r, s, t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s and t≧2; x is 1 to 20; DNA is a nucleic acid such as DNA or RNA or a known derivative thereof; Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O or S; PNA is a polyamide structure which contains at least one nucleotide base which is different from thymine; and F and F′ are end groups and/or are linked together by a covalent bond, and the physiologically tolerated salts thereof, a process for their preparation and their use as pharmaceutical, as gene probe and as primer, are described.

    摘要翻译： 式F [（DNA-Li）q（PNA-Li）r（DNA-Li）s（PNA）t] xF'的聚酰胺 - 寡核苷酸衍生物其中q，r，s，t彼此独立地为零 或1，其中两个或更多个相邻q，r，s和t> = 2的总和; x为1〜20; DNA是核酸如DNA或RNA或其已知衍生物; Li是DNA与PNA之间的共价连接，其中共价连接包含与C，N，O或S组成的系列中至少一个原子的键或有机基团; PNA是含有与胸腺嘧啶不同的至少一个核苷酸碱基的聚酰胺结构; 并且F和F'是端基和/或通过共价键连接在一起，并且描述了其生理学上耐受的盐，它们的制备方法及其作为药物的用途，作为基因探针和引物。

    MODIFIED OLIGORIBONUCLEOTIDE ANALOGS WITH ENHANCED IMMUNOSTIMULATORY ACTIVITY
    20.
    发明申请
    MODIFIED OLIGORIBONUCLEOTIDE ANALOGS WITH ENHANCED IMMUNOSTIMULATORY ACTIVITY 审中-公开
    改良的寡核苷酸类似物与增强的免疫活性

    公开(公告)号：US20110244025A1

    公开(公告)日：2011-10-06

    申请号：US12946379

    申请日：2010-11-15

    申请人： Eugen Uhlmann ,  Arthur M. Krieg ,  Grayson B. Lipford

    发明人： Eugen Uhlmann ,  Arthur M. Krieg ,  Grayson B. Lipford

    IPC分类号： A61K9/127 ,  C07H21/02 ,  A61K39/00 ,  A61P11/00 ,  A61P31/14 ,  A61P35/00 ,  A61P37/08 ,  A61P37/04 ,  A61P11/06 ,  C12N5/02 ,  B82Y5/00

    CPC分类号： C07H21/00 ,  C12N15/117 ,  C12N2310/17 ,  C12N2310/315 ,  C12N2310/3183 ,  C12N2310/321 ,  C12N2310/3515 ,  C12N2310/3529

    摘要： The invention provides immunostimulatory compositions and methods for their use. In particular, the immunostimulatory compositions of the invention include RNA-like polymers that incorporate an immunostimulatory sequence motif and at least one chemical modification to confer improved stability against nuclease degradation and improved activity. Specific modifications involving phosphate linkages, nucleotide analogs, and combinations thereof are provided. Compositions of the invention optionally include an antigen and can be used to stimulate an immune response. Also provided are compositions and methods useful for treating a subject having an infection, a cancer, an to allergic condition, or asthma. Modified oligoribonucleotide analogs of the invention are believed to stimulate Toll-like receptors TLR7 and TLR8.

    摘要翻译： 本发明提供免疫刺激组合物及其使用方法。 特别地，本发明的免疫刺激组合物包括纳入免疫刺激序列基序的RNA样聚合物和至少一种化学修饰，以提供改善的对核酸酶降解的稳定性和改善的活性。 提供了涉及磷酸键，核苷酸类似物及其组合的具体修饰。 本发明的组合物任选地包括抗原并且可以用于刺激免疫应答。 还提供了可用于治疗感染，癌症，过敏性疾病或哮喘的受试者的组合物和方法。 据信本发明的修饰的寡核糖核苷酸类似物刺激Toll样受体TLR7和TLR8。