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1. 发明授权

US07119184B2 Oligonucleotides having A-DNA form and B-DNA form conformational geometry 失效
公开(公告)号：US07119184B2
公开(公告)日：2006-10-10
申请号：US09970971
申请日：2001-10-04
申请人： Muthiah Manoharan , Venkatraman Mohan , Phillip Dan Cook , Andrew M. Kawasaki
发明人： Muthiah Manoharan , Venkatraman Mohan , Phillip Dan Cook , Andrew M. Kawasaki
IPC分类号： C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07H19/04 , C07H19/20 , C07H21/02
摘要： Modified oligonucleotides containing both A-form conformation geometry and B-from conformation geometry nucleotides are disclosed. The B-form geometry allows the oligonucleotide to serve as substrates for RNase H when bound to a target nucleic acid strand. The A-form geometry imparts properties to the oligonucleotide that modulate binding affinity and nuclease resistance. By utilizing C2′ endo sugars or O4′ endo sugars, the B-form characteristics are imparted to a portion of the oligonucleotide. The A-form characteristics are imparted via use of either 2′-O-modified nucleotides that have 3′ endo geometries or use of end caps having particular nuclease stability or by use of both of these in conjunction with each other.

2. 发明授权

US06969763B1 Molecular interaction sites of interleukin-2 RNA and methods of modulating the same 失效
标题翻译：白细胞介素-2 RNA的分子相互作用位点及其调控方法
公开(公告)号：US06969763B1
公开(公告)日：2005-11-29
申请号：US09310844
申请日：1999-05-12
申请人： David J. Ecker , Richard Griffey , Stanley T. Crooke , Ranga Sampath , Eric Swayze , Venkatraman Mohan , Steven Hofstadler , John McNeil
发明人： David J. Ecker , Richard Griffey , Stanley T. Crooke , Ranga Sampath , Eric Swayze , Venkatraman Mohan , Steven Hofstadler , John McNeil
IPC分类号： C07H21/04 , C07K14/54 , C07K14/55 , C40B30/02 , C40B50/02 , G06F19/00
CPC分类号： C40B50/02 , C07H21/04 , C07K14/5406 , C07K14/55 , C40B30/02 , G06F19/14 , G06F19/16 , G06F19/28
摘要： Methods for the identification of compounds which modulate, either inhibit or stimulate, biomolecules are provided. Nucleic acids, especially RNAs are preferred substrates for such modulation. The present methods are particularly powerful in that they provide novel combinations of techniques which give rise to compounds, usually “small” organic compounds, which are highly potent modulators of RNA and other biomolecular activity. In accordance with preferred aspects of the invention, very large numbers of compounds may be tested essentially simultaneously to determine whether they are likely to interact with a molecular interaction site and modulate the activity of the biomolecule. Pharmaceuticals, veterinary drugs, agricultural chemicals, industrial chemicals, research chemicals and many other beneficial compounds may be identified in accordance with embodiments of this invention.
摘要翻译：提供了用于鉴定调节，抑制或刺激生物分子的化合物的方法。核酸，特别是RNA是用于这种调节的优选底物。本发明的方法特别强大，因为它们提供了引起化合物（通常是“小”）有机化合物的技术的新组合，其是RNA和其它生物分子活性的高效调节剂。根据本发明的优选方面，可以基本上同时测试非常大量的化合物以确定它们是否可能与分子相互作用位点相互作用并且调节生物分子的活性。根据本发明的实施方案，可以鉴定药物，兽药，农药，工业化学品，研究化学品和许多其它有益化合物。

3. 发明授权

US06759523B2 Antimicrobial 2-deoxystreptamine compounds 失效
标题翻译：抗菌2-脱氧神经胺复合物
公开(公告)号：US06759523B2
公开(公告)日：2004-07-06
申请号：US09727315
申请日：2000-11-30
申请人： Eric Swayze , Richard H. Griffey , Yili Ding , Venkatraman Mohan
发明人： Eric Swayze , Richard H. Griffey , Yili Ding , Venkatraman Mohan
IPC分类号： C07H1522
CPC分类号： C07H15/234
摘要： The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.
摘要翻译：本发明涉及具有糖基化2-脱氧链霉胺（2-DOS）环类的氨基糖苷类化合物的类似物，以及它们作为抗微生物感染的预防或治疗剂的制备和用途。本发明的化合物包含至少一个芳基，杂芳基，取代的芳基或取代的杂芳基，代替与2-脱氧链霉胺环连接的糖基。

4. 发明授权

US06593466B1 Guanidinium functionalized nucleotides and precursors thereof 有权
标题翻译：官能化低聚物
公开(公告)号：US06593466B1
公开(公告)日：2003-07-15
申请号：US09349040
申请日：1999-07-07
申请人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
发明人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
IPC分类号： C07H1904
CPC分类号： C07H21/00
摘要： The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.
摘要翻译：本发明提供了与选定的RNA或DNA序列特异性杂交的寡聚体，其中低聚物的至少一个核苷部分被修饰成包括胍基。这些低聚物可用于诊断，治疗和调查目的。

5. 发明授权

US06534639B1 Guanidinium functionalized oligonucleotides and method/synthesis 失效
标题翻译：胍官能化低聚物和方法/合成
公开(公告)号：US06534639B1
公开(公告)日：2003-03-18
申请号：US09612531
申请日：2000-07-07
申请人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
发明人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
IPC分类号： C07H2100
CPC分类号： C07H21/00
摘要： The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.
摘要翻译：本发明提供了与选定的RNA或DNA序列特异性杂交的寡聚体，其中低聚物的至少一个核苷部分被修饰成包括胍基。这些低聚物可用于诊断，治疗和调查目的。

6. 发明授权

US06369209B1 Oligonucleotides having A-DNA form and B-DNA form conformational geometry 有权
标题翻译：具有A-DNA形式和B-DNA的寡核苷酸形成构象几何
公开(公告)号：US06369209B1
公开(公告)日：2002-04-09
申请号：US09303586
申请日：1999-05-03
申请人： Muthiah Manoharan , Venkatraman Mohan
发明人： Muthiah Manoharan , Venkatraman Mohan
IPC分类号： C07H2100
CPC分类号： C07H21/00
摘要： Modified oligonucleotides containing both A-form conformation geometry and B-from conformation geometry nucleotides are disclosed. The B-form geometry allows the oligonucleotide to serve as substrates for RNase H when bound to a target nucleic acid strand. The A-form geometry imparts properties to the oligonucleotide that modulate binding affinity and nuclease resistance. By utilizing C2′ endo sugars or O4′ endo sugars, the B-form characteristics are imparted to a portion of the oligonucleotide. The A-form characteristics are imparted via use of either 2′-O-modified nucleotides that have 3′ endo geometries or use of end caps having particular nuclease stability or by use of both of these in conjunction with each other.
摘要翻译：公开了含有A型构象几何形状和B-构象几何核苷酸的修饰寡核苷酸。当结合到靶核酸链上时，B型几何允许寡核苷酸用作核糖核酸酶H的底物。 A型几何赋予调节结合亲和力和核酸酶抗性的寡核苷酸的性质。通过使用C2'内糖或O4'内糖，B型特征被赋予寡核苷酸的一部分。通过使用具有3'内部几何形状的2'-O-修饰的核苷酸或使用具有特定核酸酶稳定性的端帽或通过使用它们彼此结合来赋予A型特征。

7. 发明授权

US06084082A Lactam nucleic acids 有权
标题翻译：内酰胺核酸
公开(公告)号：US06084082A
公开(公告)日：2000-07-04
申请号：US173212
申请日：1998-10-15
申请人： Vasulinga Ravikumar , Venkatraman Mohan
发明人： Vasulinga Ravikumar , Venkatraman Mohan
IPC分类号： C07D403/04 , C07D473/18 , C07D473/34 , C07F9/6558 , C07F9/6561 , C07H19/00 , A01N43/04 , C07H21/02 , C12Q1/68
CPC分类号： C07D403/04 , C07D473/18 , C07D473/34 , C07F9/65583 , C07F9/65616
摘要： Novel .beta.-lactam monomers bearing various functional groups are prepared. The novel .beta.-lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen bonding. The oligomeric compounds are useful as diagnostic and research reagents.
摘要翻译：制备具有各种官能团的新型β-内酰胺单体。新颖的β-内酰胺单体可以连接成低聚化合物，例如通过优选的磷酸酯键，包括磷酸二酯键和硫代磷酸酯键。有用的官能团包括参与氢键的核碱基以及极性基团，疏水基团，离子基团，芳族基团和/或基团。寡聚化合物可用作诊断和研究试剂。

8. 发明授权

US06914148B2 Guanidinium functionalized intermediates 失效
标题翻译：胍ium官能化中间体
公开(公告)号：US06914148B2
公开(公告)日：2005-07-05
申请号：US10247893
申请日：2002-09-20
申请人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
发明人： Muthiah Manoharan , Phillip Dan Cook , Thazha P. Prakash , Venkatraman Mohan
IPC分类号： C07H21/02 , A61K31/712 , A61K48/00 , A61P35/00 , C07C335/38 , C07F9/24 , C07H21/00 , C07H21/04 , C07F9/02
CPC分类号： C07H21/00
摘要： The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to include a guanidinium group. These oligomers are useful for diagnostic, therapeutic and investigative purposes.
摘要翻译：本发明提供了与选定的RNA或DNA序列特异性杂交的寡聚体，其中低聚物的至少一个核苷部分被修饰成包括胍基。这些低聚物可用于诊断，治疗和调查目的。

9. 发明授权

US06541456B1 Antimicrobial 2-deoxystreptamine compounds 失效
公开(公告)号：US06541456B1
公开(公告)日：2003-04-01
申请号：US09452606
申请日：1999-12-01
申请人： Eric Swayze , Richard H. Griffey , Yili Ding , Venkatraman Mohan
发明人： Eric Swayze , Richard H. Griffey , Yili Ding , Venkatraman Mohan
IPC分类号： A61K317036
CPC分类号： C07H15/234
摘要： The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.

10. 发明授权

US07550474B2 Substituted phenyl acetamides and their use as protease inhibitors 有权
标题翻译：取代苯乙酰胺及其作为蛋白酶抑制剂的用途
公开(公告)号：US07550474B2
公开(公告)日：2009-06-23
申请号：US10816544
申请日：2004-04-01
申请人： Kevin D. Kreutter , Lily Lee , Tianbao Lu , Venkatraman Mohan , Sharmila Patel , Hui Huang , Guozhang Xu , Mark Fitzgerald
发明人： Kevin D. Kreutter , Lily Lee , Tianbao Lu , Venkatraman Mohan , Sharmila Patel , Hui Huang , Guozhang Xu , Mark Fitzgerald
IPC分类号： A61K31/435 , C07D221/02 , C07D335/00 , C07D309/00 , C07C321/00
CPC分类号： C07D213/73 , C07C279/00 , C07C291/04 , C07D213/26 , C07D213/89 , C07D215/12 , C07D413/12 , C07D487/04
摘要： Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
摘要翻译：描述了苯基乙酰胺化合物，包括式I化合物或其溶剂合物，水合物或其药学上可接受的盐; 其中R3-R6，R11，B，Y和W在说明书中列出。本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样的丝氨酸蛋白酶，如凝血酶和因子Xa。描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。另外，化合物可以被可检测地标记并用于血栓的体内成像。

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