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1. 发明授权

US06905820B2 Polyamide nucleic acid derivatives, and agents and processes for preparing them 失效
标题翻译：聚酰胺核酸衍生物，以及制备它们的试剂和方法
公开(公告)号：US06905820B2
公开(公告)日：2005-06-14
申请号：US09835371
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： G01N33/53 , A61K38/00 , A61K48/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P31/16 , A61P31/18 , A61P35/00 , C07K14/00 , C08G69/48 , C12Q1/04 , C12Q1/68 , G01N21/78 , G01N33/566 , G01N33/58 , C07H21/02 , C12M1/34 , C12P19/34 , C07H21/64
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。

2. 发明授权

US07550582B2 Polyamide nucleic acid derivatives and agents, and processes for preparing them 失效
标题翻译：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。

3. 发明授权

US07241882B2 Polyamide nucleic acid derivatives, and agents, and processes for preparing them 有权
标题翻译：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。

4. 发明授权

US06777544B2 Polyamide nucleic acid derivatives and agents and processes for preparing them 有权
标题翻译：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。

5. 发明授权

US5817811A Process for preparing substituted N-ethyglycine derivatives 失效
标题翻译：制备取代的N-乙基甘氨酸衍生物的方法
公开(公告)号：US5817811A
公开(公告)日：1998-10-06
申请号：US707149
申请日：1996-09-03
申请人： Gerhard Breipohl , Eugen Uhlmann , David William Will
发明人： Gerhard Breipohl , Eugen Uhlmann , David William Will
IPC分类号： C07D473/00 , C07C231/02 , C07C237/22 , C07K5/078 , C07K14/00 , C07D239/02 , C07D487/00
CPC分类号： C07K5/06139 , C07K14/003 , Y02P20/55
摘要： Processes are described for preparing substituted N-ethylglycine derivatives of the formula ##STR1## in which PG is an amino protecting group which is labile towards weak acids and is of the urethane type or the trityl type, X is NH or O, and B' represents bases which are customary in nucleotide chemistry and whose exocyclic amino and/or hydroxyl groups are protected by suitable known protecting groups, and the salts thereof.
摘要翻译：描述了制备式（I）的取代的N-乙基甘氨酸衍生物的方法，其中PG是对弱酸不稳定的氨基保护基，并且是氨基甲酸酯型或三苯甲基型，X是NH或O，并且B'表示在核苷酸化学中常规的碱基，其外环氨基和/或羟基被合适的已知保护基保护，及其盐。

6. 发明授权

US07897346B2 Polyamide nucleic acid derivatives and agents, and processes for preparing them 失效
标题翻译：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。

7. 发明申请

US20080070258A1 POLYAMIDE NUCLEIC ACID DERIVATIVES AND AGENTS, AND PROCESSES FOR PREPARING THEM 失效
标题翻译：聚酰胺核酸衍生物和药剂及其制备方法
公开(公告)号：US20080070258A1
公开(公告)日：2008-03-20
申请号：US11855443
申请日：2007-09-14
申请人： Eugen UHLMANN , Gerhard Breipohl , David Will
发明人： Eugen UHLMANN , Gerhard Breipohl , David Will
IPC分类号： C12Q1/68 , C07H21/00
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。

8. 发明授权

US6046306A PNA synthesis using an amino protecting group which is labile to weak acids 失效
标题翻译：使用对弱酸不稳定的氨基保护基的PNA合成
公开(公告)号：US6046306A
公开(公告)日：2000-04-04
申请号：US927178
申请日：1997-09-11
申请人： Gerhard Breipohl , Eugen Uhlmann
发明人： Gerhard Breipohl , Eugen Uhlmann
IPC分类号： C07K1/04 , C07D473/18 , C07D473/34 , C07K1/06 , C07K1/10 , C07K14/00 , C08G69/10 , C07N21/00
CPC分类号： C07D473/18 , C07D473/34 , C07K14/003 , C08G69/10 , Y02P20/55
摘要： PNA synthesis using an amino protective group which is labile to weak acids.
摘要翻译：使用对弱酸不稳定的氨基保护基的PNA合成。

9. 发明授权

US07485421B2 Polyamide-oligonucleotide derivatives, their preparation and use 失效
标题翻译：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。

10. 发明授权

US06465650B1 Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids 有权
标题翻译：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。

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