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    PNA synthesis using a base-labile amino protecting group
    1.
    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。

    Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
    2.
    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
    3.
    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。

    Use of benzylphosphonic acid derivatives for the treatment of diseases caused by viruses
    5.
    发明授权
    Use of benzylphosphonic acid derivatives for the treatment of diseases caused by viruses 失效
    用于治疗病毒引起的疾病的苯并恶唑酸衍生物的应用

    公开(公告)号：US5242908A

    公开(公告)日：1993-09-07

    申请号：US648622

    申请日：1991-02-01

    申请人： Anuschirwan Peyman ,  Eugen Uhlmann ,  Karlheinz Budt ,  Jochen Knolle ,  Irvin Winkler ,  Matthias Helsberg

    发明人： Anuschirwan Peyman ,  Eugen Uhlmann ,  Karlheinz Budt ,  Jochen Knolle ,  Irvin Winkler ,  Matthias Helsberg

    IPC分类号： A61K31/66 ,  A61P31/12 ,  C07F9/38 ,  C07F9/40 ,  C07F9/6574

    CPC分类号： C07F9/65742 ,  C07F9/3882 ,  C07F9/4056

    摘要： The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.

    摘要翻译： 使用其中V为烷基，氟，氯，溴或碘的式I化合物I，其为1至5的整数，W为烷基，烯基，炔基或烷氧基 ，氰基，硝基，羧基，氢或环烷基，芳基，芳烷基或烷氧基，R1和R2是烷基，烯基，炔基，环烷基或卤代烷基，钠，钾，钙，镁，铝，锂，铵， 或氢，R1和R2一起形成环状二酯，R3和R4是烷基，烯基，炔基，烷氧羰基，环烷基或烷氧基，氢，氟，氯，溴或碘，X，Y和Z是氧或硫， 描述了用于治疗由DNA病毒或RNA病毒引起的疾病。

    Polyamide nucleic acid derivatives and agents, and processes for preparing them
    8.
    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：US07550582B2

    公开(公告)日：2009-06-23

    申请号：US11855443

    申请日：2007-09-14

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

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

    IPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12Q1/68

    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
    9.
    发明授权
    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：US07485421B2

    公开(公告)日：2009-02-03

    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： C12Q1/68 ,  C07H21/04

    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： F [（DNA-Li）q（PNA-Li）r（DNA-Li）s（（N-1）） 其中q，r，s，t彼此独立地为0或1，其中总共为 两个或更多个相邻的q，r，s和t> = 2; 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。

    Polyamide nucleic acid derivatives, and agents, and processes for preparing them
    10.
    发明授权
    Polyamide nucleic acid derivatives, and agents, and processes for preparing them 有权
    聚酰胺核酸衍生物和试剂，及其制备方法

    公开(公告)号：US07241882B2

    公开(公告)日：2007-07-10

    申请号：US10863999

    申请日：2004-06-09

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

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

    IPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12Q1/68

    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。