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21. 发明授权

US5124478A Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 失效
标题翻译：用于通过固相法合成肽类化合物的酸可溶性锚固剂组
公开(公告)号：US5124478A
公开(公告)日：1992-06-23
申请号：US287213
申请日：1988-12-20
申请人： Gerhard Breipohl , Jochen Knolle , Werner Stuber
发明人： Gerhard Breipohl , Jochen Knolle , Werner Stuber
IPC分类号： C07C59/64 , C07C59/90 , C07C213/02 , C07C217/58 , C07C227/04 , C07C227/08 , C07C229/34 , C07C231/12 , C07C233/17 , C07C233/35 , C07C233/46 , C07C237/22 , C07C251/48 , C07C271/16 , C07C271/22 , C07K1/00 , C07K1/04 , C07K1/10 , C07K7/06 , C07K7/23
CPC分类号： C07C59/90 , C07C271/22 , C07C59/64 , C07K1/003 , C07K1/042 , C07C2103/18 , Y02P20/55
摘要： The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl, R.sup.2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or --O--(CH.sub.2).sub.n --COOH (with n=1 to 6), with one of these radicals being --O--(CH.sub.2).sub.n --COOH, or Y.sup.1, Y.sup.2 and Y.sup.5 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, Y.sup.3 denotes hydrogen or (C.sub.1 -C.sub.8)-alkoxy and Y.sup.4 denotes --(CH.sub.2).sub.n --COOH or --NH--CO--(CH.sub.2).sub.n --COOH (with n=1 to 6).Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1表示（C 1 -C 8） - 烷基，R 2表示被氨基保护基团保护的氨基酸残基，该氨基酸残基可用弱酸或碱，或表示可用弱酸或碱取代的氨基保护基，R3表示氢或（C1-C4） - 烷基，Y1-Y9表示相同或不同的基团，氢，（C1-C4） - 烷基，（C1 -C（O） - 烷氧基或-O-（CH 2）n -COOH（n = 1至6），其中一个基团是-O-（CH 2）n -COOH，或者Y 1，Y 2和Y 5 -Y 9表示相同或（C 1 -C 4） - 烷氧基，Y 3表示氢或（C 1 -C 8） - 烷氧基，Y 4表示 - （CH 2）n -COOH或-NH-CO-（CH 2））n-COOH（n = 1〜6）。描述了通过使用这些新化合物（间隔物）的固相方法制备方法和肽酰胺的合成方法。

22. 发明授权

US5011825A Peptides influencing diuresis and natriuresis, a process for their preparation, agents containing them, and their use 失效
标题翻译：影响利尿和利尿的肽，其制备方法，含有它们的药剂及其用途
公开(公告)号：US5011825A
公开(公告)日：1991-04-30
申请号：US463782
申请日：1990-01-08
申请人： Wolfgang Konig , Gerhard Breipohl , Rolf Geiger , Jochen Knolle , Max Hropot
发明人： Wolfgang Konig , Gerhard Breipohl , Rolf Geiger , Jochen Knolle , Max Hropot
IPC分类号： C07K5/10 , A61K38/00 , A61P7/10 , C07K1/06 , C07K5/02 , C07K5/083 , C07K5/11 , C07K5/117 , C07K7/06 , C07K7/64 , C07K14/58
CPC分类号： C07K5/1024 , C07K14/58 , C07K5/021 , C07K5/0808 , C07K5/1019 , A61K38/00 , C10M2201/02 , C10M2215/22 , C10M2215/221 , C10M2215/225 , C10M2215/226 , C10M2215/30 , C10M2219/022 , C10M2219/024 , C10N2240/02 , C10N2240/40 , C10N2240/401 , C10N2240/402 , C10N2240/403 , C10N2240/404 , C10N2240/405 , C10N2240/406 , C10N2240/407 , C10N2240/408 , C10N2240/409
摘要： The invention relates to peptides of the formulaR.sup.N --L--N--B.sup.2 --R.sup.C (I)in which R.sup.N denotes an acyl radical, L denotes a radical of a lipophilic, neutral .alpha.-amino acid, N denotes a radical of an neutral .alpha.-amino acid, B.sup.2 denotes the radical of a basic .alpha.-amino acid, and R.sup.C denotes an amido radical; a process for their preparation, agents containing these peptides, and their use.
摘要翻译：本发明涉及式RN-LN-B2-RC（I）的肽，其中RN表示酰基，L表示亲脂性中性α-氨基酸的基团，N表示中性α-氨基的基团酸，B2表示碱性α-氨基酸的基团，RC表示酰氨基; 其制备方法，含有这些肽的试剂及其用途。

23. 发明授权

US5093477A Rapidly cleavable substrate for HIV protease 失效
标题翻译：用于艾滋病毒抗体的快速可清除基质
公开(公告)号：US5093477A
公开(公告)日：1992-03-03
申请号：US449766
申请日：1989-12-13
申请人： Karin Molling , Stephan Henke , Gerhard Breipohl , Wolfgang Konig
发明人： Karin Molling , Stephan Henke , Gerhard Breipohl , Wolfgang Konig
IPC分类号： C07K1/04 , C07K7/06 , C07K14/16 , C12Q1/37
CPC分类号： C07K14/005 , C12Q1/37 , C12N2740/16222 , G01N2333/16
摘要： A rapidly cleavable substrate for HIV protease Hepta- to nona-peptides of the formulaA--B--C--D--E--Opr--F--G--H,in which A is absent or represents Val, Ile or Thr, B denotes Ser, Thr or Phe, D denotes Asp or Ala, E denotes Tyr or Phe, Opr denotes 5-oxaproline, F denotes Ile, Leu, Val, Thr or Gln, G denotes Val, Ile, Ser or Arg, and H is absent or represents Gln, Glu, Pro or Thr, as well as the salts thereof are used for locating and detecting HIV protease and for testing possible inhibitors of HIV protease. They are prepared by known methods of peptide chemistry, preferably by means of solid-phase synthesis.
摘要翻译：用于HIV蛋白酶的快速切割底物式为ABCDE-Opr-FGH的非肽，其中A不存在或表示Val，Ile或Thr，B表示Ser，Thr或Phe，D表示Asp或Ala，E 表示Tyr或Phe，Opr表示5-氧山梨酸，F表示Ile，Leu，Val，Thr或Gln，G表示Val，Ile，Ser或Arg，H不存在或表示Gln，Glu，Pro或Thr，以及其盐用于定位和检测HIV蛋白酶和用于测试可能的HIV蛋白酶抑制剂。它们通过已知的肽化学方法制备，优选通过固相合成制备。

24. 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。

25. 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。

26. 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。

27. 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。

28. 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。

29. 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。

30. 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。

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