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1. 发明专利

JP2011111459A Method for producing 2'-branched nucleoside 审中-公开
标题翻译：生产2'-分支核苷的方法
公开(公告)号：JP2011111459A
公开(公告)日：2011-06-09
申请号：JP2010268549
申请日：2010-12-01
申请人： Idenix (Cayman) Ltd , イデニクス(ケイマン)リミテツド
发明人： STORER RICHARD , MOUSSA ADEL , CHAUDHURI NARAYAN , WALIGORA FRANK
IPC分类号： C07H19/067 , A61K31/7072 , C07B61/00 , C07H20060101 , C07H1/00 , C07H7/02 , C07H19/00 , C07H19/048 , C07H19/06 , C07H19/16 , C07H19/22
CPC分类号： C07H1/00 , C07H7/02 , C07H19/06 , C07H19/16 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide an improved method for preparing β-D, β-L2'-C-methyl-nucleoside and 2'-C-methyl-3'-O-ester nucleoside. SOLUTION: A method for preparing a 3'-O-amino acid ester nucleoside includes: (a) coupling a ribofuranose with an unprotected nucleoside base and a silylating agent in the presence of a Lewis acid; (b) reacting the protected nucleoside from step (a) with a deprotecting agent to provide an unprotected nucleoside; (c) protecting the amine group if the nucleoside has an amine group; (d) forming a 5'-O-silyl-protected nucleoside by reacting the protected or unprotected nucleoside with the silylating agent; (e) forming a protected 3'-O-amino acid ester by using a coupling agent if necessary; (f) removing a silyl protecting group from the 5'-C and removing a formamidine-protecting group from the nucleosidic amine if needed; and (g) reacting the product from step (f) with a reagent which removes the protecting group from the 3'-O-amino acid ester if necessary. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种制备β-D，β-L2'-C-甲基 - 核苷和2'-C-甲基-3'-O-酯核苷的改进方法。解决方案：制备3'-O-氨基酸酯核苷的方法包括：（a）在路易斯酸存在下将呋喃核糖与未保护的核苷碱和甲硅烷基化剂偶联; （b）将保护的来自步骤（a）的核苷与脱保护剂反应以提供未保护的核苷; （c）如果核苷具有胺基，则保护胺基; （d）通过使受保护或未保护的核苷与甲硅烷基化剂反应形成5'-O-甲硅烷基保护的核苷; （e）如果需要，通过使用偶联剂形成受保护的3'-O-氨基酸酯; （f）从5-C除去甲硅烷基保护基，如果需要，从核苷胺中除去甲脒保护基; 和（g）使步骤（f）的产物与必要时从3'-O-氨基酸酯中除去保护基的试剂反应。版权所有（C）2011，JPO＆INPIT

2. 发明申请

WO2004052899A3 PROCESS FOR THE PRODUCTION OF 2'-BRANCHED NUCLEOSIDES 审中-公开
标题翻译：生产2'-分支核苷酸的方法
公开(公告)号：WO2004052899A3
公开(公告)日：2005-03-31
申请号：PCT/US0339643
申请日：2003-12-12
申请人： IDENIX CAYMAN LTD , STORER RICHARD , MOUSSA ADEL , CHAUDHURI NARAYAN , WALIGORA FRANK
发明人： STORER RICHARD , MOUSSA ADEL , CHAUDHURI NARAYAN , WALIGORA FRANK
IPC分类号： A61K31/7072 , C07H20060101 , C07H1/00 , C07H7/02 , C07H19/00 , C07H19/048 , C07H19/06 , C07H19/067 , C07H19/16 , C07H19/22
CPC分类号： C07H1/00 , C07H7/02 , C07H19/06 , C07H19/16 , Y02P20/55
摘要： The present invention provides an improved process for preparing ss-D and ss-L 2'-C-methyl-nucleosides and 2'-C-methyl-3'-O-ester nucleosides.
摘要翻译：本发明提供了制备β-D和β-L 2'-C-甲基 - 核苷和2'-C-甲基-3'-O-酯核苷的改进方法。

3. 发明申请

WO2005003374A3 SYNTHESIS OF beta-L-2-DEOXY NUCLEOSIDES 审中-公开
标题翻译： β-L-2-脱氧核苷的合成
公开(公告)号：WO2005003374A3
公开(公告)日：2005-09-01
申请号：PCT/US2004021281
申请日：2004-06-30
申请人： IDENIX CAYMAN LTD , STORER RICHARD , MOUSSA ADEL , WANG JING YANG , CHAUDHURI NARAYAN , MATHIEU STEVEN , STEWART ALISTAIR
发明人： STORER RICHARD , MOUSSA ADEL , WANG JING YANG , CHAUDHURI NARAYAN , MATHIEU STEVEN , STEWART ALISTAIR
IPC分类号： A61K31/7072 , A61K31/7076 , C07H13/08 , C07H19/00 , C07H19/048 , C07H19/073 , C07H19/22 , C12Q20060101
CPC分类号： C07H19/09 , C07H9/04 , C07H9/06 , C07H13/04 , C07H13/08 , C07H15/203 , C07H19/06 , C07H19/073 , Y02P20/55
摘要： An improved process for the preparation of 2'-modified nucleosides and 2'-deoxy-nucleosides, such as, beta-L-2'-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2'-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2' anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2'-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2'-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2'-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.
摘要翻译：提供了制备2'-修饰的核苷和2'-脱氧核苷如β-L-2'-脱氧胸苷（LdT）的改进方法。特别地，改进的方法涉及合成2'-脱氧核苷，该2'-脱氧核苷可以利用不同的原料，但是通过氯 - 糖中间体或通过2,2'-脱水-1-呋喃糖基 - 核碱中间体进行。在使用2,2'-脱水-1-呋喃糖基碱中间体的情况下，引起分子内置换反应和形成以下物质的还原剂（例如Red-Al）和螯合剂（例如15-冠-5醚）采用高收率的所需核苷产物。本发明的另一种方法使用不含螯合剂的2,2'-脱水-1-呋喃糖基碱中间体以良好的收率提供2'-脱氧核苷。根据本发明制备的化合物可以用作制备其他核苷类似物的中间体，或者可以直接用作抗病毒和/或抗肿瘤剂。

4. 发明申请

WO2004096147A2 OXO-PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：氧化吡嗪化合物
公开(公告)号：WO2004096147A2
公开(公告)日：2004-11-11
申请号：PCT/US2004013086
申请日：2004-04-28
申请人： IDENIX CAYMAN LTD , STORER RICHARD , MOUSSA ADEL , LA COLLA PAOLO , ARTICO MARINO
发明人： STORER RICHARD , MOUSSA ADEL , LA COLLA PAOLO , ARTICO MARINO
IPC分类号： A61K20060101 , A61K31/505 , A61K31/513 , C07D239/52 , C07D239/56 , A61K
CPC分类号： C07D239/47 , C07D239/48 , C07D239/52 , C07D239/553
摘要： Oxo-pyrimidine compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the oxopyrimidine derivatives alone or in combination with other anti-retroviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.
摘要翻译：描述了用于治疗逆转录病毒感染，特别是用于HIV的氧嘧啶化合物。还包括包含单独的或与其它抗逆转录病毒剂组合的氧代嘧啶衍生物的组合物，其制备方法和制备并入这些化合物的药物的方法。

5. 发明申请

WO2004096149A2 INDUSTRIALLY SCALABLE NUCLEOSIDE SYNTHESIS 审中-公开
标题翻译：工业可扩展的核苷酸合成
公开(公告)号：WO2004096149A2
公开(公告)日：2004-11-11
申请号：PCT/US2004013127
申请日：2004-04-28
申请人： IDENIX CAYMAN LTD , MOUSSA ADEL , WANG JING YANG , STORER RICHARD
发明人： MOUSSA ADEL , WANG JING YANG , STORER RICHARD
IPC分类号： A61K20060101 , C07H19/00 , C07H19/04 , C07H19/048 , C07H19/22 , A61K
CPC分类号： C07H19/073
摘要： An industrially scalable two-step process for preparing a ß-L-2'-deoxy nucleoside that results in a predominance of the ß- over the a-anomeric form of the compound is described. An optional third step may be used to prepare 3'-prodrugs of desirable ß-L-2'-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of ß-L-2'-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.
摘要翻译：描述了一种用于制备β-L-2'-脱氧核苷的工业可扩展的两步法，其导致β-位于化合物的α-端基异构体上的优势。可选的第三步可用于制备所需的β-L-2'-脱氧核苷的3'-前药用于递送有效治疗病毒性疾病的这些药物。合成方法特别适用于β-L-2'-脱氧胞苷的形成，其药学上可接受的盐或前药。该方法可以提供可能不需要进一步分离或纯化的相对未污染的产物，从而使合成容易地可扩展到工业制造。

6. 发明公开

EP1585529A4 PROCESS FOR THE PRODUCTION OF 2'-BRANCHED NUCLEOSIDES 审中-公开
标题翻译：用于生产2'-了支链核苷
公开(公告)号：EP1585529A4
公开(公告)日：2008-05-28
申请号：EP03812993
申请日：2003-12-12
申请人： IDENIX CAYMAN LTD
发明人： STORER RICHARD , MOUSSA ADEL , CHAUDHURI NARAYAN , WALIGORA FRANK
IPC分类号： C07H19/06 , A61K31/7072 , A61P31/14 , C07H20060101 , C07H1/00 , C07H7/02 , C07H19/00 , C07H19/048 , C07H19/067 , C07H19/16 , C07H19/22
CPC分类号： C07H1/00 , C07H7/02 , C07H19/06 , C07H19/16 , Y02P20/55
摘要： The present invention provides an improved process for preparing ß-D and ß-L 2'-C-methyl-nucleosides and 2'-C-methyl-3'-O-ester nucleosides.

7. 发明公开

EP1575971A4 PROCESS FOR THE PRODUCTION OF 3 -NUCLEOSIDE PRODRUGS 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON3-NUKLEOSIDPRODRUGS
公开(公告)号：EP1575971A4
公开(公告)日：2008-03-05
申请号：EP03814400
申请日：2003-12-23
申请人： IDENIX CAYMAN LTD
发明人： STORER RICHARD , MOUSSA ADEL , MATHIEU STEVEN
IPC分类号： C07H19/00 , C07H19/04 , C07H19/067 , C07H19/073
CPC分类号： C07H19/04 , C07H19/00
摘要： Provided is a single-step process for the selective 3'-acylation of a ribofuranosyl 2' or 3'-branched nucleoside. These compounds are useful as antiviral agents, and in particular,can be used to treat Flaviviridae infections in a host in need t hereof.
摘要翻译：提供了核糖呋喃糖基2'或3'-分支核苷的选择性3'-酰化的单步方法。这些化合物可用作抗病毒剂，特别是可用于治疗需要治疗的宿主中的黄病毒科感染。

8. 发明公开

EP1639121A4 SYNTHESIS OF BETA -L-2-DEOXY NUCLEOSIDES 审中-公开
标题翻译：合成BETA-L-2-脱氧核苷
公开(公告)号：EP1639121A4
公开(公告)日：2008-04-16
申请号：EP04777433
申请日：2004-06-30
申请人： IDENIX CAYMAN LTD
发明人： STORER RICHARD , MOUSSA ADEL , WANG JING YANG , CHAUDHURI NARAYAN , MATHIEU STEVEN , STEWART ALISTAIR
IPC分类号： C07H19/00 , A61K31/7072 , A61K31/7076 , C07H13/08 , C07H19/048 , C07H19/073 , C07H19/22 , C12Q20060101
CPC分类号： C07H19/09 , C07H9/04 , C07H9/06 , C07H13/04 , C07H13/08 , C07H15/203 , C07H19/06 , C07H19/073 , Y02P20/55

9. 发明专利

NO20060469L 未知
公开(公告)号：NO20060469L
公开(公告)日：2006-03-30
申请号：NO20060469
申请日：2006-01-30
申请人： IDENIX CAYMAN LTD
发明人： STORER RICHARD , MOUSSA ADEL , MATHIEU STEVEN , WANG JING YANG , CHAUDHUN NARAYAN , STEWART ALISTAIR
IPC分类号： C07H19/00 , A61K31/7072 , A61K31/7076 , C07H13/08 , C07H19/048 , C07H19/073 , C07H19/22 , C12Q20060101
摘要： An improved process for the preparation of 2'-modified nucleosides and 2'-deoxynucleosides, such as, ²-L-2'-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2'-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2' anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2'-anhydro-1-furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2'-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2'-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.

10. 发明专利

NO20060469A 未知
公开(公告)号：NO20060469A
公开(公告)日：2006-03-30
申请号：NO20060469
申请日：2006-01-30
申请人： IDENIX CAYMAN LTD
发明人： STORER RICHARD , MOUSSA ADEL , MATHIEU STEVEN , WANG JING YANG , CHAUDHUN NARAYAN , STEWART ALISTAIR
IPC分类号： C07H19/00 , A61K31/7072 , A61K31/7076 , C07H13/08 , C07H19/048 , C07H19/073 , C07H19/22 , C12Q20060101
CPC分类号： C07H19/09 , C07H9/04 , C07H9/06 , C07H13/04 , C07H13/08 , C07H15/203 , C07H19/06 , C07H19/073 , Y02P20/55

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