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1. 发明申请

US20110196144A1 SYNTHESIS AND USE OF 2'-SUBSTITUTED-N6-MODIFIED NUCLEOSIDES 有权
标题翻译： 2'-取代N6修饰的核苷酸的合成和用途
公开(公告)号：US20110196144A1
公开(公告)日：2011-08-11
申请号：US12876997
申请日：2010-09-07
申请人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
发明人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
IPC分类号： C07H21/00 , C07H19/167
CPC分类号： C07H19/16
摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
摘要翻译：制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

2. 发明授权

US07799908B2 Synthesis and use of 2′-substituted-N6 -modified nucleosides 有权
标题翻译： 2'-取代-N6修饰核苷的合成与应用
公开(公告)号：US07799908B2
公开(公告)日：2010-09-21
申请号：US10542235
申请日：2004-01-15
申请人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
发明人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
IPC分类号： C07H19/167 , C07H19/173
CPC分类号： C07H19/16
摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
摘要翻译：制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

3. 发明授权

US08575331B2 Synthesis and use of 2′-substituted-N6-modified nucleosides 有权
标题翻译： 2'-取代-N6修饰核苷的合成与应用
公开(公告)号：US08575331B2
公开(公告)日：2013-11-05
申请号：US12876997
申请日：2010-09-07
申请人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
发明人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
IPC分类号： C07H19/167 , C07H19/173
CPC分类号： C07H19/16
摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
摘要翻译：制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

4. 发明申请

US20060135465A1 Synthesis and use of 2'-substituted-n6-modified nucleosides 有权
标题翻译： 2'-取代-6 - 修饰核苷的合成与应用
公开(公告)号：US20060135465A1
公开(公告)日：2006-06-22
申请号：US10542235
申请日：2004-01-15
申请人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
发明人： Haoyun An , Kanda Ramasamy , Stephanie Shaw
IPC分类号： A61K31/7076 , C07H19/16
CPC分类号： C07H19/16
摘要： An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
摘要翻译：制备糖改性核苷类似物的改进方法包括其中在对应的羰基的亲核改性之前糖的羟基被选择性脱保护和氧化的方案。然后将修饰的糖偶联到杂环基，其在另外的步骤中用双重亲核试剂修饰，其提供具有高立体选择性的N6-修饰的腺苷类似物。

5. 发明授权

US07371857B2 Synthesis for hydroxyalkylated heterocyclic bases 有权
标题翻译：羟烷基化杂环碱的合成
公开(公告)号：US07371857B2
公开(公告)日：2008-05-13
申请号：US10523938
申请日：2002-08-08
申请人： Kanda Ramasamy , Jean-Luc Girardet , Haoyun An , Zhi Hong , Robert Orr
发明人： Kanda Ramasamy , Jean-Luc Girardet , Haoyun An , Zhi Hong , Robert Orr
IPC分类号： C07D473/34 , C07F9/6561
CPC分类号： C07D473/34
摘要： A hydroxyalkylated heterocyclic base is prepared by reacting a heterocyclic base with an alkylene carbonate in dimethylacetamide as a solvent, wherein the hydroxyalkylated heterocyclic base is isolated from the solvent using isopropanol or tert-butylmethylether.
摘要翻译：羟基烷基化杂环碱通过使杂环碱与碳酸二烷基酯在二甲基乙酰胺作溶剂中反应来制备，其中使用异丙醇或叔丁基甲基醚从溶剂中分离出羟烷基化杂环碱。

6. 发明申请

US20060135768A1 Synthesis for hydroxyalkylated heterocyclic bases 有权
标题翻译：羟烷基化杂环碱的合成
公开(公告)号：US20060135768A1
公开(公告)日：2006-06-22
申请号：US10523938
申请日：2002-08-08
申请人： Kanda Ramasamy , Jean-Luc Girardet , Haoyun An , Zhi Hong , Robert Orr
发明人： Kanda Ramasamy , Jean-Luc Girardet , Haoyun An , Zhi Hong , Robert Orr
IPC分类号： C07D473/02 , C07D473/12 , C07D471/02
CPC分类号： C07D473/34
摘要： A hydroxyalkylated heterocyclic base is prepared by reacting a heterocyclic base with an alkylene carbonate in dimethylacetamide as a solvent, wherein the hydroxyalkylated heterocyclic base is isolated from the solvent using isopropanol or tert-butylmethylether.
摘要翻译：羟基烷基化杂环碱通过使杂环碱与碳酸二烷基酯在二甲基乙酰胺作溶剂中反应来制备，其中使用异丙醇或叔丁基甲基醚从溶剂中分离出羟烷基化杂环碱。

7. 发明申请

US20130303747A1 PYRIMIDINE NUCLEOSIDE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF FOR PREPARING ANTI-TUMOR AND ANTI-VIRUS MEDICAMENTS 有权
标题翻译：吡咯烷酮核苷衍生物，合成方法及其制备抗肿瘤药物和抗病毒药物的用途
公开(公告)号：US20130303747A1
公开(公告)日：2013-11-14
申请号：US13820993
申请日：2011-09-02
申请人： Junbiao Chang , Haoyun An , Xuejun Yu , Xiaohe Guo
发明人： Junbiao Chang , Haoyun An , Xuejun Yu , Xiaohe Guo
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H19/14
摘要： The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
摘要翻译：本发明涉及药物化学领域。公开了氟化和叠氮基取代的嘧啶核苷衍生物及其制备方法和用途。结构式如图（I）所示。这些化合物可用于制备用于治疗诸如肿瘤和病毒感染的疾病的药物，并且可以单独使用或与其它药物组合使用。该化合物还具有抗肿瘤和病毒感染等疾病的有效活性，同时副作用少，具有潜在的应用价值。

8. 发明申请

US20060051824A1 Tetrahydrocannabinoid antigens and method of use 审中-公开
标题翻译：四氢大麻素抗原及其使用方法
公开(公告)号：US20060051824A1
公开(公告)日：2006-03-09
申请号：US11048648
申请日：2005-01-31
申请人： Haoyun An , Junjie Xu , Jose Alberto Macall
发明人： Haoyun An , Junjie Xu , Jose Alberto Macall
IPC分类号： G01N33/537
CPC分类号： G01N33/948 , A61K47/646 , C07D311/80 , C07K16/44 , G01N33/6854
摘要： The present invention is directed to Δ8-THC and Δ9-THC compounds useful for the covalent attachment to immunogenic molecules to form antigens for the preparation of specific binding molecules to Δ9-Tetrahydrocannabinol, Δ9-Tetrahydrocannabinoids, Δ8-Tetrahydrocannabinol, and Δ8-Tetrahydrocannabinoids, and their derivatives and metabolites. The present invention is directed to the compounds, their method of preparation, cell lines producing the specific binding molecules, methods of using the antigens to produce the specific binding molecules, and test devices containing the antigens, haptens, or specific binding molecules of the invention.
摘要翻译：本发明涉及可用于共价连接到免疫原性分子以形成用于制备特异性结合分子的抗原的Delta -THTH -THC和Δ-9 -THC化合物四氢大麻酚，三氢大麻酚，四氢大麻素，三角洲四氢大麻酚和三角洲四氢大麻素，以及它们衍生物和代谢物。本发明涉及化合物，其制备方法，产生特异性结合分子的细胞系，使用抗原产生特异性结合分子的方法以及含有本发明抗原，半抗原或特异性结合分子的测试装置。

9. 发明授权

US06329523B1 Compounds having a plurality of nitrogenous substitutents 失效
标题翻译：具有多个含氮取代基的化合物
公开(公告)号：US06329523B1
公开(公告)日：2001-12-11
申请号：US09230773
申请日：1999-03-10
申请人： Phillip Dan Cook , Haoyun An
发明人： Phillip Dan Cook , Haoyun An
IPC分类号： C07D24142
CPC分类号： C07D213/20 , C12Q1/18 , C40B40/00 , G01N33/573 , G01N33/68 , G01N33/6872
摘要： Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.
摘要翻译：具有下式的新型化合物：其中组分变量在本文中定义。该化合物构建成包括中心芳族，脂族或杂环环系。连接到中心环系统是具有用化学官能团衍生的含氮部分的两个线性基团。环系统可以包括作为环原子的另外的含氮部分或连接到环的侧基，其也可以被化学官能团衍生化。化学官能团的整体赋予这些化合物某些构象和其他性质。根据本发明的某些实施方案，利用化学官能团和含氮部分的置换和组合来制备这些化合物的文库，以构建文库的复杂性。

10. 发明授权

US6107482A Nitrogenous macrocyclic compounds 失效
标题翻译：含氮大环化合物
公开(公告)号：US6107482A
公开(公告)日：2000-08-22
申请号：US913664
申请日：1997-09-19
申请人： Phillip Dan Cook , Haoyun An , Charles J. Guinosso , Pei-Pei Kung , Allister S. Fraser
发明人： Phillip Dan Cook , Haoyun An , Charles J. Guinosso , Pei-Pei Kung , Allister S. Fraser
IPC分类号： G01N33/15 , A61K31/33 , A61K31/395 , A61K31/435 , A61K31/53 , A61P29/00 , A61P31/04 , A61P43/00 , C07B61/00 , C07D255/02 , C07D273/00 , C07D471/08 , C07D471/18 , C07D498/08 , C07D515/08 , C07D521/00
CPC分类号： C07D471/08 , C07D515/08 , B01J2219/0072
摘要： Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.
摘要翻译： PCT No.PCT / US96 / 04215 Sec。 371日期：1997年9月19日 102（e）1997年9月19日PCT PCT 1996年3月27日PCT公布。第WO96 / 30377号公报日期1996年10月3日新的大环化合物被构建成包括被至少一个环系统中断的大环状结构。每个中断环系统包括两个桥头原子。桥头原子键合到一个或多个互连一个或多个环系统的桥，从而形成大的环状结构。位于每个桥中的是具有化学官能团衍生化的两个或多个含氮部分。环系统可以包括作为环原子的另外的含氮部分或连接到环上的侧基上。这些也可以用化学官能团衍生化。化学官能团的总体对大环化合物赋予某些构象和其他性质。根据本发明的某些实施方案，利用化学官能团和含氮部分的置换和组合来制备这种大环化合物的文库，从而构建文库的复杂性。

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