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1. 发明授权

US6107479A Process for the preparation of an oligomeric compound 失效
标题翻译：低聚化合物的制备方法
公开(公告)号：US6107479A
公开(公告)日：2000-08-22
申请号：US297709
申请日：1999-05-06
申请人： Fran.cedilla.ois Natt , Robert Haner
发明人： Fran.cedilla.ois Natt , Robert Haner
IPC分类号： C07H21/00 , C07K1/04 , C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07K1/04
摘要： The present invention relates to a process for the preparation of an oligomeric compound, comprising introduction of a lipophilic capping group to an unreacted reactive group, suitable for chain elongation, of a not elongated oligomeric compound intended to be elongated in a preceeding chain-elongation step, by reacting a lipophilic capping compound with said unreacted reactive group, which lipophilic capping group is not removable under the applied conditions of the synthesis and work-up of the oligomeric compound; and which not elongated oligomeric compound capped with said lipophilic capping group can be separated from said oligomeric compound on a hydrophobic stationary phase.
摘要翻译： PCT No.PCT / EP97 / 06123第 371日期1999年5月6日 102（e）日期1999年5月6日PCT 1997年11月5日PCT公布。 WO98 / 20018 PCT出版物日期1998年5月14日本发明涉及一种制备低聚化合物的方法，包括将亲油性封端基团引入未延伸的未伸缩的寡聚化合物的未反应的反应性基团，其适用于延伸的未伸缩的低聚物，通过使亲脂性封端化合物与所述未反应的反应性基团反应，该亲油性封端基在合成和后处理低聚化合物的应用条件下不能除去; 并且在所述亲油性封端基上封闭的不伸长的低聚化合物可以在疏水性固定相上与所述低聚化合物分离。

2. 发明授权

US08097716B2 Interfering RNA duplex having blunt-ends and 3′-modifications 有权
标题翻译：干扰RNA双链体具有平端和3'-修饰
公开(公告)号：US08097716B2
公开(公告)日：2012-01-17
申请号：US12338601
申请日：2008-12-18
申请人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Jean-Charles Natt , Robert Haner
发明人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Jean-Charles Natt , Robert Haner
IPC分类号： C07H21/04
CPC分类号： C12N15/111 , C12N2310/14 , C12N2310/311 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2320/51 , C12N2330/30 , C12N2310/3525
摘要： The present invention relates to double-stranded RNA compounds with at least one blunt end comprising at least one 3′-end of formula wherein X is O or S R1 and R2 are independently OH, NH2, SH, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms and functional groups, preferably a heteroatom selected from the group of N, O, or S or a functional group selected from the group OH, NH2, SH, carboxylic acid or ester; or R1 and R2 may be of formula Y-Z where Y is O, N, S and Z is H, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms, preferably a heteroatom selected from the group of N, O, or S; and wherein said double-stranded RNA mediates RNA interference.
摘要翻译：本发明涉及具有至少一个平末端的双链RNA化合物，其至少包含至少一个下式的3'-末端，其中X是O或S 1 R 2，R 2独立地是OH，NH 2，SH，烷基，芳基，烷基 - 芳基芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可被其它杂原子和官能团取代，优选选自N，O或S的杂原子或选自OH ，NH 2，SH，羧酸或酯; 或者R1和R2可以是式YZ，其中Y是O，N，S和Z是H，烷基，芳基，烷基 - 芳基，芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可以被另外的杂原子，优选选自N，O或S的杂原子; 并且其中所述双链RNA介导RNA干扰。

3. 发明授权

US6018042A Antitumor antisense oligonucleotides 失效
标题翻译：抗肿瘤反义寡核苷酸
公开(公告)号：US6018042A
公开(公告)日：2000-01-25
申请号：US914961
申请日：1997-08-20
申请人： Helmut Mett , Robert Haner , Nicholas Mark Dean
发明人： Helmut Mett , Robert Haner , Nicholas Mark Dean
IPC分类号： C12N15/09 , A61K31/70 , A61K31/7088 , A61K38/00 , A61K48/00 , A61P35/00 , C07H21/00 , C07H21/04 , C12N15/113 , C12Q1/68
CPC分类号： C12N15/1137 , C07H21/00 , C12Q1/6886 , C12Y401/0105 , A61K38/00 , C12N2310/315 , C12Q2600/158
摘要： The invention relates to deoxyribo- and ribo-oligonucleotides and derivatives thereof, as well as pharmaceutical preparations, therapies, diagnostics and commercial research reagents in relation to disease states which respond to modulation of the synthesis of the enzyme S-adenosylmethionine decarboxylase (SAMDC). In particular, the invention relates to antisense oligonucleotides and oligonucleotide derivatives specifically hybridizable with nucleic acids relating to (preferably human) SAMDC. These oligonucleotides and their derivatives have been found to modulate the synthesis of SAMDC in cells.
摘要翻译：本发明涉及脱氧核糖核苷酸和核糖寡核苷酸及其衍生物，以及与对S-腺苷甲硫氨酸脱羧酶（SAMDC）的合成的调节有关的疾病状态的药物制剂，疗法，诊断和商业研究试剂。具体地，本发明涉及与与（优选人类）SAMDC相关的核酸特异性杂交的反义寡核苷酸和寡核苷酸衍生物。已经发现这些寡核苷酸及其衍生物调节细胞中SAMDC的合成。

4. 发明申请

US20110092693A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20110092693A1
公开(公告)日：2011-04-21
申请号：US12161375
申请日：2007-01-16
申请人： Francois Jean-Charles Natt , Jurg Hunziker , Robert Haner , Simon Matthias Langenegger
发明人： Francois Jean-Charles Natt , Jurg Hunziker , Robert Haner , Simon Matthias Langenegger
IPC分类号： C07H1/00 , C07F9/02
CPC分类号： C07H21/02 , C07H21/04
摘要： The present invention relates to a process for the preparation of an oligomeric compound made up of two or more individual oligomers, in which said oligomeric compound the individual oligomers are separated by a photocleavable linker, comprising the step of photoactively cleaving said linker.
摘要翻译：本发明涉及制备由两种或更多种单体寡聚物组成的低聚化合物的方法，其中所述低聚化合物各自的低聚物被光可透洗接头分离，包括光致切割所述接头的步骤。

5. 发明申请

US20080064033A1 Molecular Beacons 失效
标题翻译：分子信标
公开(公告)号：US20080064033A1
公开(公告)日：2008-03-13
申请号：US11575875
申请日：2005-09-22
申请人： Robert Haner , Simon Langenegger
发明人： Robert Haner , Simon Langenegger
IPC分类号： C12Q1/68 , C07H21/00
CPC分类号： C12Q1/6816 , C12Q2563/107 , C12Q2525/301
摘要： The invention relates to a molecular beacon in the form of a hairpin oligonucleotide or oligonucleotide analogue comprising a first nucleotide sequence containing two or more aromatic or heteroaromatic ring systems P able to form an excimer or exciplex; a second sequence (the loop) consisting of an oligonucleotide probe able to hybridise with a target polynucleotide; and a third sequence containing one or more aromatic or heteroaromatic ring systems X, wherein at least one aromatic ring system X interacts with two aromatic ring systems P of the first sequence inhibiting excimer or exciplex formation. The invention further relates to a method for detecting the presence of a target polynucleotide using such a molecular beacon, and to a kit comprising a molecular beacon of the invention for use in this method.
摘要翻译：本发明涉及发夹寡核苷酸或寡核苷酸类似物形式的分子信标，其包含能够形成准分子或激酶复合物的含有两个或多个芳族或杂芳族环系统P的第一核苷酸序列; 由能够与靶多核苷酸杂交的寡核苷酸探针组成的第二序列（环）和含有一个或多个芳族或杂芳族环系X的第三序列，其中至少一个芳族环系统X与第一序列的两个芳环系统P相互作用，抑制受激准分子或激元形成。本发明还涉及使用这种分子信标检测靶多核苷酸的存在的方法，以及包含用于该方法的本发明的分子信标的试剂盒。

6. 发明申请

US20070203084A1 Interfering Rna Duplex Having Blunt-Ends And 3'-Modifications 审中-公开
标题翻译：干扰Rna双链体具有平端和3'-修饰
公开(公告)号：US20070203084A1
公开(公告)日：2007-08-30
申请号：US10569927
申请日：2004-08-27
申请人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Natt , Robert Haner
发明人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Natt , Robert Haner
IPC分类号： A61K48/00 , C12Q1/68 , C07H21/02
CPC分类号： C12N15/111 , C12N2310/14 , C12N2310/311 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2320/51 , C12N2330/30 , C12N2310/3525
摘要： The present invention relates to double-stranded RNA compounds with at least one blunt end comprising at least one 3′-end of Formula (I): wherein X is O or S R1 and R2 are independently OH, NH2, SH, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms and functional groups, preferably a heteroatom selected from the group of N, O, or S or a functional group selected from the group OH, NH2, SH, carboxylic acid or ester; or R1 and R2 may be of formula Y-Z where Y is O, N, S and Z is H, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms, preferably a heteroatom selected from the group of N, O, or S; and wherein said double-stranded RNA mediates RNA interference. Preferred 3′end modifications are: phosphate, phosphorothioate, abasic ribonucleoside, hydroxyphopyl phosphodiester.
摘要翻译：本发明涉及具有至少一个平末端的双链RNA化合物，其包含至少一个式（I）的3'-末端：其中X是O或SR 1和R 2 烷基，芳基，烷基 - 芳基，芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可被其它杂原子取代和官能团，优选选自N，O或S的杂原子或选自OH，NH 2，SH，羧酸或酯的官能团; 或R 1和R 2可以是式YZ，其中Y是O，N，S和Z是H，烷基，芳基，烷基 - 芳基，芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可以被另外的杂原子，优选选自N，O或S的杂原子取代; 并且其中所述双链RNA介导RNA干扰。优选的3'末端修饰是：磷酸，硫代磷酸酯，脱碱核糖核苷，羟基hop酰磷酸二酯。

7. 发明申请

US20090192113A1 Interfering RNA Duplex Having Blunt-Ends and 3`-Modifications 有权
标题翻译：干扰RNA双链体具有平端和3'-修饰
公开(公告)号：US20090192113A1
公开(公告)日：2009-07-30
申请号：US12338601
申请日：2008-12-18
申请人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Jean-Charles Natt , Robert Haner
发明人： Jan Weiler , Jonathan Hall , Jean-Charles Bologna , Francois Jean-Charles Natt , Robert Haner
IPC分类号： A61K31/713 , C07H21/02 , C12N15/00 , C12Q1/68
CPC分类号： C12N15/111 , C12N2310/14 , C12N2310/311 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/332 , C12N2320/51 , C12N2330/30 , C12N2310/3525
摘要： The present invention relates to double-stranded RNA compounds with at least one blunt end comprising at least one 3′-end of formula wherein X is O or S R1 and R2 are independently OH, NH2, SH, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms and functional groups, preferably a heteroatom selected from the group of N, O, or S or a functional group selected from the group OH, NH2, SH, carboxylic acid or ester; or R1 and R2 may be of formula Y-Z where Y is O, N, S and Z is H, alkyl, aryl, alkyl-aryl, aryl-alkyl, where alkyl, aryl, alkyl-aryl, aryl-alkyl can be substituted by additional heteroatoms, preferably a heteroatom selected from the group of N, O, or S; and wherein said double-stranded RNA mediates RNA interference.
摘要翻译：本发明涉及具有至少一个平末端的双链RNA化合物，其至少包含至少一个下式的3'-末端，其中X是O或S 1 R 2，R 2独立地是OH，NH 2，SH，烷基，芳基，烷基 - 芳基芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可被其它杂原子和官能团取代，优选选自N，O或S的杂原子或选自OH ，NH 2，SH，羧酸或酯; 或者R1和R2可以是式YZ，其中Y是O，N，S和Z是H，烷基，芳基，烷基 - 芳基，芳基 - 烷基，其中烷基，芳基，烷基 - 芳基，芳基 - 烷基可以被另外的杂原子，优选选自N，O或S的杂原子; 并且其中所述双链RNA介导RNA干扰。

8. 发明授权

US5925744A Functional terpyridine-metal complexes, a process for the preparation thereof and oligonucleotide conjugates with terpyridine-metal complexes 失效
标题翻译：功能性三联吡啶金属络合物，其制备方法和与三联吡啶 - 金属络合物的寡核苷酸缀合物
公开(公告)号：US5925744A
公开(公告)日：1999-07-20
申请号：US793530
申请日：1997-07-28
申请人： Robert Haner , Jonathan Hall , Dieter Husken , Uwe Pieles , Heinz Moser
发明人： Robert Haner , Jonathan Hall , Dieter Husken , Uwe Pieles , Heinz Moser
IPC分类号： C12N15/09 , A61K31/70 , A61P35/00 , C07D213/00 , C07D213/50 , C07D213/55 , C07D213/76 , C07D471/22 , C07F5/00 , C07F9/38 , C07H21/00 , C07H21/04 , C12Q1/68 , A61K51/00 , C07C69/96 , C07D213/22
CPC分类号： C07H21/00 , C07D213/00 , C12Q1/6816 , G01N2458/40
摘要： The present invention relates to cyclic terpyridine-lanthanide complexes having 8 nitrogen atoms and 10 carbon atoms in the macrocycle and containing a functional group in the terpyridine moiety. The invention also relates to a process for the preparation of cyclic terpyridine-lanthanide complexes through the condensation of terpyridine hydrazines with pyridine-2,6-dialdehydes or -ketones. The compounds can be complexed with oligonculeotides and are useful in the sequence-specific cleavage of RNA.
摘要翻译： PCT No.PCT / EP95 / 03409 Sec。 371日期1997年7月28日第 102（e）日期1997年7月28日PCT提交1995年8月30日PCT公布。公开号WO96 / 07668 日期：1996年3月14日本发明涉及大环中具有8个氮原子和10个碳原子并在三联吡啶部分含有官能团的环状三联吡啶 - 镧系元素络合物。本发明还涉及通过三联吡啶肼与吡啶-2,6-二醛或酮的缩合制备环状三联吡啶 - 镧系元素络合物的方法。这些化合物可以与寡核苷酸复合，可用于RNA的序列特异性切割。

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