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1. 发明申请

WO2006054182A9 PHOSPHOINDOLES AS HIV INHIBITORS 审中-公开
标题翻译：作为HIV抑制剂的磷酸化合物
公开(公告)号：WO2006054182A9
公开(公告)日：2006-08-17
申请号：PCT/IB2005004063
申请日：2005-09-16
申请人： IDENIX CAYMAN LTD , STORER RICHARD , DOUSSON CYRIL , ALEXANDRE FRANCOIS-RENE , ROLAND ARLENE
发明人： STORER RICHARD , DOUSSON CYRIL , ALEXANDRE FRANCOIS-RENE , ROLAND ARLENE
CPC分类号： C07F9/65586 , C07F9/5728 , C07F9/65583
摘要： 3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more 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，特别是用于治疗HIV的3-磷酸吲哚化合物。还包括单独包含3-磷酸吲哚衍生物或与一种或多种其它抗逆转录病毒剂组合的组合物，它们的制备方法，以及制造掺入这些化合物的药物的方法。

2. 发明申请

WO2006054182A2 PHOSPHOINDOLES AS HIV INHIBITORS 审中-公开
标题翻译：磷酸盐作为艾滋病毒抑制剂
公开(公告)号：WO2006054182A2
公开(公告)日：2006-05-26
申请号：PCT/IB2005004063
申请日：2005-09-16
申请人： IDENIX CAYMAN LTD , STORER RICHARD , DOUSSON CYRIL , ALEXANDRE FRANCOIS-RENE , ROLAND ARLENE
发明人： STORER RICHARD , DOUSSON CYRIL , ALEXANDRE FRANCOIS-RENE , ROLAND ARLENE
CPC分类号： C07F9/65586 , C07F9/5728 , C07F9/65583
摘要： 3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more 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3-磷酸吲哚化合物。还包括包含3-磷酸吲哚衍生物单独或与一种或多种其它抗逆转录病毒剂组合的组合物，其制备方法和制备并入这些化合物的药物的方法。

3. 发明申请

WO2008042240A9 ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS 审中-公开
标题翻译：作为艾滋病毒抑制剂的纯化磷酸二氢钠
公开(公告)号：WO2008042240A9
公开(公告)日：2008-08-07
申请号：PCT/US2007020900
申请日：2007-09-28
申请人： IDENIX PHARMACEUTICALS INC , STORER RICHARD , ALEXANDRE FRANCOIS-RENE , DOUSSON CYRIL , MOUSSA ADEL M , BRIDGES EDWARD
发明人： STORER RICHARD , ALEXANDRE FRANCOIS-RENE , DOUSSON CYRIL , MOUSSA ADEL M , BRIDGES EDWARD
IPC分类号： C07F9/572 , A61K31/675 , A61P31/18
CPC分类号： C07F9/5728
摘要： 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HLV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other antiviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. The 3-phosphoindole compounds are of the formula (A) or (B) and the pharmaceutically acceptable salts, solvates, hydrates, or esters thereof. In the formulae X is hydrogen; aryl or heterocyclyl; C 2-6 alkenyl, C 2-6 alkynyl or alkyl; Y is hydrogen, -R, -O-R, -NH-R, or -NRR; Z is -OR, -NHR, -NRR, carboxamido, arnido, carboxyl, carbonyl, or an amino acid residue; R1 is hydrogen, acyl, -S(O)n-R, carboxyl, carbonyl, or an amino acid residue; each R 4' , R 5' , R 6' and R 7' is independently hydrogen, C 2-6 alkenyl, C 2-6 alkynyl, aryl, heterocyclyl, halogen, -CN, -CF 3 , -OR, -NHR, -NRR, or -NO 2 ; n is 0, 1, or 2; and each R is independently hydrogen, alkyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heterocyclyl.
摘要翻译：提供了基本上为单一对映异构体形式的3-磷酸吲哚化合物，其可用于治疗黄病毒科感染，特别是用于HLV感染。还提供了包含单独或与一种或多种其它抗病毒剂组合的3-磷酸吲哚化合物的药物组合物，其制备方法以及制备并入这些化合物的药物的方法。 3-磷酸吲哚化合物具有式（A）或（B）及其药学上可接受的盐，溶剂合物，水合物或酯。在式X中是氢; 芳基或杂环基; C 2-6烯基，C 2-6炔基或烷基; Y是氢，-R，-O-R，-NH-R或-NRR; Z是-OR，-NHR，-NRR，甲酰胺基，氨基，羧基，羰基或氨基酸残基; R 1是氢，酰基，-S（O）n -R，羧基，羰基或氨基酸残基; 每个R 4'，R 5'，R 6'和R 7'独立地是氢， C 2-6亚烷基，C 2-6炔基，芳基，杂环基，卤素，-CN，-CF 3，-OR，-NHR， -NRR或-NO 2; n为0,1或2; 并且每个R独立地为氢，烷基，C 2-6 - 烯基，C 2-6 - 炔基，芳基或杂环基。

4. 发明申请

WO2008042240A3 ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS 审中-公开
标题翻译：作为HIV抑制剂的经典纯磷酸化合物
公开(公告)号：WO2008042240A3
公开(公告)日：2008-06-05
申请号：PCT/US2007020900
申请日：2007-09-28
申请人： IDENIX PHARMACEUTICALS INC , STORER RICHARD , ALEXANDRE FRANCOIS-RENE , DOUSSON CYRIL , MOUSSA ADEL M , BRIDGES EDWARD
发明人： STORER RICHARD , ALEXANDRE FRANCOIS-RENE , DOUSSON CYRIL , MOUSSA ADEL M , BRIDGES EDWARD
IPC分类号： C07F9/572 , A61K31/675 , A61P31/18
CPC分类号： C07F9/5728
摘要： 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HLV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other antiviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. The 3-phosphoindole compounds are of the formula (A) or (B) and the pharmaceutically acceptable salts, solvates, hydrates, or esters thereof. In the formulae X is hydrogen; aryl or heterocyclyl; C 2-6 alkenyl, C 2-6 alkynyl or alkyl; Y is hydrogen, -R, -O-R, -NH-R, or -NRR; Z is -OR, -NHR, -NRR, carboxamido, arnido, carboxyl, carbonyl, or an amino acid residue; R1 is hydrogen, acyl, -S(O)n-R, carboxyl, carbonyl, or an amino acid residue; each R 4' , R 5' , R 6' and R 7' is independently hydrogen, C 2-6 alkenyl, C 2-6 alkynyl, aryl, heterocyclyl, halogen, -CN, -CF 3 , -OR, -NHR, -NRR, or -NO 2 ; n is 0, 1, or 2; and each R is independently hydrogen, alkyl, C 2-6 alkenyl, C 2-6 alkynyl, aryl, or heterocyclyl.
摘要翻译：提供了用于治疗黄病毒科病毒感染，特别是用于HLV感染的基本上为单一对映异构体形式的3-磷酸吲哚化合物。还提供了包含单独的3-磷酸吲哚化合物或与一种或多种其他抗病毒剂组合的药物组合物，它们的制备方法以及制备掺入这些化合物的药物的方法。 3-磷酸吲哚化合物具有式（A）或（B）及其药学上可接受的盐，溶剂合物，水合物或酯。在通式中X是氢; 芳基或杂环基; C 2-6烯基，C 2-6炔基或烷基; Y是氢，-R，-O-R，-NH-R或-NRR; Z是-OR，-NHR，-NRR，甲酰胺基，氨基，羧基，羰基或氨基酸残基; R1是氢，酰基，-S（O）n-R，羧基，羰基或氨基酸残基; 每个R 4，R 5，R 6和R 7独立地为氢，C 1 -C 4烷基， C 1-6烷基，C 2-6炔基，芳基，杂环基，卤素，-CN，-CF 3，-OR，-NHR， -NRR或-NO SUB 2; n是0,1或2; 并且每个R独立地为氢，烷基，C 2-6烯基，C 2-6炔基，芳基或杂环基。

5. 发明申请

WO2006037028A2 METHODS AND COMPOSITIONS FOR TREATING FLAVIVIRUSES, PESTIVIRUSES AND HEPACIVIRUS 审中-公开
标题翻译：用于治疗感染病毒，杀虫剂和肝炎病毒的方法和组合物
公开(公告)号：WO2006037028A2
公开(公告)日：2006-04-06
申请号：PCT/US2005034786
申请日：2005-09-26
申请人： IDENIX CAYMAN LTD , CENTRE NAT RECH SCIENT , SOMMADOSSI JEAN-PIERRE , GOSSELIN GILLES , STORER RICHARD , EGAN JAMES
发明人： SOMMADOSSI JEAN-PIERRE , GOSSELIN GILLES , STORER RICHARD , EGAN JAMES
IPC分类号： A61K36/18 , A61K31/7076
CPC分类号： A61K45/06 , A61K31/7076 , A61K36/00 , C07H19/00 , C07H19/048 , A61K2300/00
摘要： A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective flavivirus, pestivirus or hepacivirus treatment amount of a described base-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
摘要翻译：提供用于治疗感染黄病毒，瘟病毒或肝炎病毒的宿主的方法和组合物，其包括施用有效的黄病毒，瘟病毒或肝炎病毒处理量的所述碱基修饰的核苷或其药学上可接受的盐或前药。

6. 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。

7. 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。

8. 发明申请

WO2004012687A3 CRYSTALLINE AND AMORPHOUS FORMS OF BETA-L-2'-DEOXYTHYMIDINE 审中-公开
标题翻译： β-L-2'-DEOXYTHYMIDINE的晶体和非晶形式
公开(公告)号：WO2004012687A3
公开(公告)日：2004-11-04
申请号：PCT/US0324987
申请日：2003-08-06
申请人： IDENIX CAYMAN LTD , STORER RICHARD , JONAITIS DAVID
发明人： STORER RICHARD , JONAITIS DAVID
IPC分类号： A61K31/7072 , C07H19/00 , C07H19/06 , C07H19/067 , A61K31/70
CPC分类号： C07H19/073 , A61K31/7072 , C07H19/06
摘要： Physical forms of beta-L-2'-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2'-deoxythymidine can be used in the manufacture of other forms of beta-L-2'-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.
摘要翻译：公开了可以通过物理外观，纯度水平，红外和拉曼光谱，X射线粉末衍射图，热性质和制造方法来表征的β-L-2'-脱氧胸苷的物理形式。这些形式的β-L-2'-脱氧胸苷可用于制造其它形式的β-L-2'-脱氧胸苷，或用于药物组合物。特别优选的用途是治疗乙型肝炎。

9. 发明申请

WO2004002999A3 MODIFIED 2' AND 3' -NUCLEOSIDE PRODUGS FOR TREATING FLAVIRIDAE INFECTIONS 审中-公开
标题翻译：用于治疗感冒的改良的2'和3'-NUCLEOSIDE PRODUGS
公开(公告)号：WO2004002999A3
公开(公告)日：2004-08-12
申请号：PCT/IB0303246
申请日：2003-06-27
申请人： IDENIX CAYMAN LTD , CENTRE NAT RECH SCIENT , UNIV CAGLIARI , SOMMADOSSI JEAN-PIERRE , LA COLLA POALO , STORER RICHARD , GOSSELIN GILLES
发明人： SOMMADOSSI JEAN-PIERRE , LA COLLA POALO , STORER RICHARD , GOSSELIN GILLES
IPC分类号： C07H19/06 , A61K9/20 , A61K9/48 , A61K31/7056 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K38/00 , A61K38/21 , A61K45/00 , A61P31/14 , A61P43/00 , C07H19/00 , C07H19/04 , C07H19/044 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/067 , C07H19/10 , C07H19/12 , C07H19/14 , C07H19/16 , C07H19/167 , C07H19/20 , C07H19/22 , C07H19/23
CPC分类号： C07H19/10 , C07H19/00 , C07H19/20
摘要： 2' and/or 3' prodrugs of l', 2', 3' or 4'-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
摘要翻译：描述了1'，2'，3'或4'-支链核苷的2'和/或3'前药及其药学上可接受的盐和衍生物。这些前药可用于预防和治疗黄病毒科感染，包括HCV感染和其他相关病症。描述本发明前药的化合物和组合物。还提供了包括施用有效量的本发明前药或其药学上可接受的盐或衍生物的方法和用途。这些药物可以任选地与另外的抗病毒剂组合或改变来施用，以预防或治疗黄病毒科感染和其他相关病症。

10. 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。

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