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1. 发明授权

US5223618A 4'-desmethyl nucleoside analog compounds 失效
标题翻译： 4'-脱乙酰壳多糖类似物化合物
公开(公告)号：US5223618A
公开(公告)日：1993-06-29
申请号：US566836
申请日：1990-08-13
申请人： Philip D. Cook , Yogesh S. Sanghvi
发明人： Philip D. Cook , Yogesh S. Sanghvi
IPC分类号： C07F9/6568 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C12N15/09
CPC分类号： C07D405/04 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00
摘要： Novel oligonucleotide analogs are provided having improved cellular uptake, improved resistance to nucleases, and good hybridization to target RNA. Such analogs are provided having substantially non-chiral, non-ionic linking functionalities between the sugars and sugar analogs thereof. In accordance with preferred embodiments, the 4' position of a sugar or sugar analog at one nucleoside is linked to the 3' position of a second sugar or sugar analog of a second nucleoside by a linking function that comprises a two- or three- carbon backbone chain. In accordance with preferred embodiments, the linking functions comprise the formula)--R.sub.1 --O where R.sub.1 comprises a two or three carbon backbone. Such linking functions also, preferably comprise ether functionalities to effect such linkage. Processes for the automated synthesis of oligonucleotide analogs are also provided.
摘要翻译：提供了新的寡核苷酸类似物，其具有改善的细胞摄取，改善的对核酸酶的抗性以及与靶RNA的良好杂交。提供这样的类似物在糖和糖类似物之间具有基本上非手性，非离子的连接官能团。根据优选的实施方案，一个核苷上的糖或糖类似物的4'位置通过包含二或三碳的连接功能连接到第二核苷的第二糖或糖类似物的3'位置骨干链。根据优选实施方案，连接官能团包含式）-R1-O，其中R1包含两个或三个碳骨架。这种连接功能也优选包括醚官能团以实现这种连接。还提供了用于自动合成寡核苷酸类似物的方法。

2. 发明授权

US5614617A Nuclease resistant, pyrimidine modified oligonucleotides that detect and modulate gene expression 失效
标题翻译：核酸酶抗性，嘧啶修饰寡核苷酸，检测和调节基因表达
公开(公告)号：US5614617A
公开(公告)日：1997-03-25
申请号：US971978
申请日：1993-02-18
申请人： Philip D. Cook , Yogesh S. Sanghvi
发明人： Philip D. Cook , Yogesh S. Sanghvi
IPC分类号： A61K48/00 , C07H19/10 , C07H19/12 , C07H21/00 , C12N15/09 , C07H21/02 , A61K31/70 , C07H21/04
CPC分类号： C07H19/10 , C07H19/12 , C07H21/00 , Y10T436/143333
摘要： Oligonucleotide analogs are provided having improved nuclease resistance. Modifications of selected nucleotides through substitutions on the pyrimidine ring are disclosed. Certain preferred embodiments comprise the inclusion of said modified nucleotides at a plurality of sites, especially at the 3' end of a selected oligonucleotide analog.
摘要翻译： PCT No.PCT / US91 / 04681 Sec。 371日期：1993年2月18日 102（e）1993年2月18日PCT PCT 1991年7月1日PCT公布。出版物WO92 / 02258 日期：199年2月20日提供具有改善的核酸酶抗性的寡核苷酸类似物。公开了通过嘧啶环上取代选择的核苷酸的修饰。某些优选的实施方案包括在多个位点，特别是所选寡核苷酸类似物的3'端包含所述修饰的核苷酸。

3. 发明授权

US5378825A Backbone modified oligonucleotide analogs 失效
标题翻译：骨架修饰的寡核苷酸类似物
公开(公告)号：US5378825A
公开(公告)日：1995-01-03
申请号：US703619
申请日：1991-05-21
申请人： Philip D. Cook , Yogesh S. Sanghvi
发明人： Philip D. Cook , Yogesh S. Sanghvi
IPC分类号： A61K31/70 , A61K31/7088 , A61K47/48 , A61K48/00 , A61P37/04 , A61P43/00 , C07D239/54 , C07D405/04 , C07D405/14 , C07D473/00 , C07F7/18 , C07H11/00 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C12Q1/68 , C07H1/00
CPC分类号： C07D405/04 , A61K47/48092 , A61K47/48192 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H11/00
摘要： Therapeutic oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in wild type oligomers with four atom linking groups forms unique di- and poly- nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.
摘要翻译：提供具有改善的核酸酶抗性和改善的细胞摄取的治疗性寡核苷酸类似物。在具有四个原子连接基团的野生型寡聚物中发现的正常磷酸二酯间糖链的替换形成用于调节RNA表达和治疗的唯一的二核苷酸和多核苷和核苷酸。还公开了合成和使用方法。

4. 发明授权

US06809195B1 Process for the preparation of oligonucleotides 有权
标题翻译：寡核苷酸的制备方法
公开(公告)号：US06809195B1
公开(公告)日：2004-10-26
申请号：US09640279
申请日：2000-08-16
申请人： Yogesh S. Sanghvi , Quanlai Song
发明人： Yogesh S. Sanghvi , Quanlai Song
IPC分类号： C07H2100
CPC分类号： C07H21/00 , C07H19/04
摘要： The present invention discloses methods for synthesizing oligomeric compounds. The methods include a modified phosphoramidite protocol wherein the oxidation and capping steps are combined into a single step. The methods result in increased efficiency and are especially amenable to the large scale synthesis of oligomeric compounds.
摘要翻译：本发明公开了低聚化合物的合成方法。所述方法包括经修饰的亚磷酰胺方案，其中将氧化和加帽步骤组合成单个步骤。这些方法可以提高效率，特别适合大规模合成低聚物。

5. 发明授权

US06359124B1 Antisense inhibition of ras gene with chimeric and alternating oligonucleotides 有权
标题翻译：用嵌合和交替寡核苷酸反义ras基因的抑制
公开(公告)号：US06359124B1
公开(公告)日：2002-03-19
申请号：US09248386
申请日：1999-02-12
申请人： David J. Ecker , Phillip Dan Cook , Brett P. Monia , Susan M. Freier , Yogesh S. Sanghvi
发明人： David J. Ecker , Phillip Dan Cook , Brett P. Monia , Susan M. Freier , Yogesh S. Sanghvi
IPC分类号： C07H2102
CPC分类号： C12N15/1135 , C07H21/00 , C12N2310/315 , C12N2310/318 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12Q1/6876 , C12Q2600/158 , C12N2310/3525
摘要： Compositions and methods are provided for the modulation of expression of the human ras gene in both the normal and activated forms. Oligonucleotides are provided that have methylene(methylimino) linkages alternating with phosphorothioate or phosphodiester linkages. Further oligonucleotides are provide that have a first region having a methylene(methylimino) linkage alternating with a phosphorothioate or phosphodiester linkage and a second region having phosphorothioate linkages. Such oligonucleotides can be used for diagnostics as well as for research purposes including methods for diagnosis, detection and treatment of conditions arising from the activation of the H-ras gene.
摘要翻译：提供组合物和方法用于调节正常和活化形式的人ras基因的表达。提供了具有与硫代磷酸酯或磷酸二酯键交替的亚甲基（甲基亚氨基）键的寡核苷酸。提供另外的寡核苷酸，其具有与硫代磷酸酯或磷酸二酯键交替的亚甲基（甲基亚氨基）键的第一区域和具有硫代磷酸酯键的第二区域。这样的寡核苷酸可用于诊断以及研究目的，包括用于诊断，检测和治疗由H-ras基因激活产生的病症的方法。

6. 发明授权

US06222025B1 Process for the synthesis of 2′-O-substituted pyrimidines and oligomeric compounds therefrom 失效
标题翻译：用于合成2'-O-取代的嘧啶及其低聚化合物的方法
公开(公告)号：US06222025B1
公开(公告)日：2001-04-24
申请号：US08894899
申请日：1998-01-07
申请人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
发明人： Phillip Dan Cook , Yogesh S. Sanghvi , Kelly G. Sprankle , Bruce S. Ross , Rich H. Griffey , Robert H. Springer
IPC分类号： C07H1900
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55 , Y02P20/582
摘要： Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2′ and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position. Improved processes for the synthesis of 2′-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2′-anhydropyrimidine nucleoside or a 2S,2′-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.
摘要翻译：公开了寡核苷酸类似物，其中具有在2'和5位修饰的嘧啶单体亚单位。具有这些修饰的单体子单元可以在2位进一步修饰。还提供了用于合成2'-O-取代的嘧啶核苷的改进方法。该方法的特征是在路易斯酸存在下，使用具有弱亲核试剂的2,2'-脱水嘧啶核苷或2S，2'-脱水嘧啶核苷进行烷基化。

7. 发明授权

US06800751B2 Reagent and process for protecting nucleoside hydroxyl groups 有权
标题翻译：用于保护核苷羟基的试剂和方法
公开(公告)号：US06800751B2
公开(公告)日：2004-10-05
申请号：US10120649
申请日：2002-04-11
申请人： Yogesh S. Sanghvi , Emmanuel A. Theodorakis , Ke Wen
发明人： Yogesh S. Sanghvi , Emmanuel A. Theodorakis , Ke Wen
IPC分类号： C07H2100
CPC分类号： C07H19/06 , C07H19/16
摘要： Silylating reagents having a group other than a divalent oxygen separating two silyl groups provide regioselective protection of reactive groups under robust conditions, such as basic conditions used in alkylation, acylation and deoxygenation. In particular, silylating reagents having a group other than oxygen separating two silyl groups are useful for protecting two hydroxy groups of a ribonucleic or deoxyribonucleic acid. Alkylation of a 2′-hydroxy group of a ribonucleoside protected with the inventive silylating agents in the presence of an excess of a mild hindered base such as sodium HMDS may be carried out without protecting the exocyclic amine and oxo functionalities of nucleobases.
摘要翻译：具有分离两个甲硅烷基的二价氧以外的基团的硅烷化试剂在稳定的条件下，例如在烷基化，酰化和脱氧中使用的碱性条件下提供反应性基团的区域选择性保护。特别地，具有分离两个甲硅烷基的氧以外的基团的甲硅烷基化试剂可用于保护核糖核酸或脱氧核糖核酸的两个羟基。在过量的温和受阻碱例如HMDS的存在下，用本发明的甲硅烷基化剂保护的核糖核苷的2'-羟基的烷基化可以在不保护核碱基的环外胺和氧代官能团的情况下进行。

8. 发明授权

US5792844A Oligonucleoside linkages containing adjacent nitrogen atoms 失效
标题翻译：含有相邻氮原子的寡核苷酸键
公开(公告)号：US5792844A
公开(公告)日：1998-08-11
申请号：US317289
申请日：1994-10-03
申请人： Yogesh S. Sanghvi , Phillip Dan Cook
发明人： Yogesh S. Sanghvi , Phillip Dan Cook
IPC分类号： C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07D405/04 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00
摘要： Novel compounds that mimic and/or modulate the activity of wild-type nucleic acids. In general, the compounds contain a selected nucleoside sequence wherein the nucleosides are covalently bound through linking groups that contain adjacent nitrogen atoms.
摘要翻译：模仿和/或调节野生型核酸活性的新型化合物。通常，化合物含有选择的核苷序列，其中核苷通过含有相邻氮原子的连接基团共价结合。

9. 发明授权

US5623070A Heteroatomic oligonucleoside linkages 失效
标题翻译：杂原子寡核苷键
公开(公告)号：US5623070A
公开(公告)日：1997-04-22
申请号：US395168
申请日：1995-02-27
申请人： Phillip D. Cook , Yogesh S. Sanghvi
发明人： Phillip D. Cook , Yogesh S. Sanghvi
IPC分类号： A61K47/48 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H19/167 , C07H19/173
CPC分类号： A61K31/70 , A61K47/48192 , A61K47/48223 , C07D405/04 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00
摘要： Oligonucleotide-mimicking macromolecules that have improved nuclease resistance are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligonucleotides with three or four atom linking groups provide unique oligonucleotide-mimicking macromolecules that are useful in regulating RNA expression and in therapeutics. Methods of synthesis and use also are disclosed.
摘要翻译：提供了具有改善的核酸酶抗性的寡核苷酸模拟大分子。用三个或四个原子连接基团替代天然寡核苷酸中发现的正常磷酸二酯糖苷键，提供了可用于调节RNA表达和治疗学的独特的寡核苷酸模拟大分子。也公开了合成和使用方法。

10. 发明授权

US5541307A Backbone modified oligonucleotide analogs and solid phase synthesis thereof 失效
标题翻译：骨架修饰的寡核苷酸类似物及其固相合成
公开(公告)号：US5541307A
公开(公告)日：1996-07-30
申请号：US174379
申请日：1993-12-28
申请人： Phillip D. Cook , Yogesh S. Sanghvi , Francois Morvan
发明人： Phillip D. Cook , Yogesh S. Sanghvi , Francois Morvan
IPC分类号： A61K47/48 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H1/00 , C07H19/00
CPC分类号： C07H21/00 , A61K31/70 , A61K47/48192 , C07D405/04 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16
摘要： Compounds and methods for preparing oligonucleotide analogs are provided. In preferred embodiments, the methods involve solid-phase coupling of synthons bearing either 3'-electrophillic groups and 5'-nucleophilic groups or 5'-electrophillic groups and 3'-nucleophilic groups to form neutral, achiral oligomers.
摘要翻译：提供了制备寡核苷酸类似物的化合物和方法。在优选的实施方案中，所述方法涉及具有3'-亲电子基团和5'-亲核基团或5'-亲电子基团和3'-亲核基团的合成子的固相偶联以形成中性的非手性低聚物。

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