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91. 发明申请

WO2010118078A1 MACROCYCLIC SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：大肠杆菌丝氨酸蛋白酶抑制剂
公开(公告)号：WO2010118078A1
公开(公告)日：2010-10-14
申请号：PCT/US2010/030156
申请日：2010-04-07
申请人： IDENIX PHARMACEUTICALS, INC. , PARSY, Christophe, Claude , ALEXANDRE, Francois-Rene , DEROCK, Michel , LEROY, Frederic , MEILLON, Jean-Christophe , CONVARD, Thierry , SURLERAUX, Dominique
发明人： PARSY, Christophe, Claude , ALEXANDRE, Francois-Rene , DEROCK, Michel , LEROY, Frederic , MEILLON, Jean-Christophe , CONVARD, Thierry , SURLERAUX, Dominique
IPC分类号： C07D471/04 , A61K38/05 , A61P31/14
CPC分类号： A61K38/005 , A61K31/444 , A61K31/4709 , A61K31/506 , A61K45/06 , C07D471/04
摘要： Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
摘要翻译：本文提供的是大环丝氨酸蛋白酶抑制剂化合物，例如式Ia或Ib，包含该化合物的药物组合物及其制备方法。还提供了它们用于在有需要的宿主中治疗HCV感染的方法。

92. 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。

93. 发明申请

WO2008042240A2 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：WO2008042240A2
公开(公告)日：2008-04-10
申请号：PCT/US2007/020900
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 HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.
摘要翻译：提供了基本上为可用于治疗黄病毒科病毒感染，特别是HIV感染的单一对映体形式的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它抗病毒剂组合的药物组合物，其制备方法和制备并入这些化合物的药物的方法。

94. 发明申请

WO2007075876A3 PROCESS FOR PREPARING A SYNTHETIC INTERMEDIATE FOR PREPARATION OF BRANCHED NUCLEOSIDES 审中-公开
公开(公告)号：WO2007075876A3
公开(公告)日：2007-07-05
申请号：PCT/US2006/048769
申请日：2006-12-22
申请人： IDENIX PHARMACEUTICALS, INC. , MAYES, Benjamin, Alexander , MOUSSA, Adel
发明人： MAYES, Benjamin, Alexander , MOUSSA, Adel
IPC分类号： A01N43/08 , A61K31/34 , A01N43/00 , A61K31/33
摘要： A process is provided for the preparation of a key intermediate in the preparation of 2'-branched nucleoside compounds. The process includes contacting a protected precursor 3,4- O -isopropylidene-2-C-substituted-D-arabinono-l,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-l,5-lactone and optionally into a 2- deoxy-2-halo-2-C-disubstituted ribono- 1 ,4-lactone.

95. 发明申请

WO2015161137A1 3'-SUBSTITUTED METHYL OR ALKYNYL NUCLEOSIDES FOR THE TREATMENT OF HCV 审中-公开
标题翻译：用于治疗HCV的3'-取代的甲基或亚苄基核苷
公开(公告)号：WO2015161137A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/026264
申请日：2015-04-16
申请人： IDENIX PHARMACEUTICALS, INC. , ALEXANDRE, François-René
发明人： ALEXANDRE, François-René , DUKHAN, David , DOUSSON, Cyril B. , GOSSELIN, Gilles , PAPARIN, Jean-Laurent , BRANDT, Guillaume , RAHALI, Rachid , SALANSON, Aurelien
IPC分类号： C07H19/10 , C07H19/11 , C07H19/20 , A61K31/7072 , A61K31/708 , A61P31/14
CPC分类号： C07H19/20 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , C07H19/10 , C07H19/11
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3'-substituted methyl or alkynyl nucleosides of Formula I: (I); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, PD, R A , R B1 , R B2 , R C and Z are as defined herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物是式I的3'-取代的甲基或炔基核苷：（I）; 或其药学上可接受的盐，溶剂化物，立体异构形式，互变异构形式或其多晶型形式，其中碱，PD，RA，RB1，RB2，RC和Z如本文所定义。

96. 发明申请

WO2015081133A2 NUCLEOTIDES FOR THE TREATMENT OF LIVER CANCER 审中-公开
标题翻译：用于治疗肝癌的核心
公开(公告)号：WO2015081133A2
公开(公告)日：2015-06-04
申请号：PCT/US2014/067485
申请日：2014-11-25
申请人： IDENIX PHARMACEUTICALS, INC.
发明人： DOUSSON, Cyril B. , DUKHAN, David , PARSY, Christophe Claude
IPC分类号： A61K31/7076 , C07H19/16
CPC分类号： C07H19/207 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Provided herein are compounds, compositions and methods for the treatment of liver cancer such as hepatocellular carcinoma, cholangiocarcinoma, or biliary tract cancer. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents. In certain embodiments, the compounds are nucleoside analogs of Formula I: (I); or a pharmaceutically acceptable salt thereof, wherein Base, Z 1 , Z 2 , Z 3 , Z 4 , V, W, X, Ar, R 1 and R 2 are as described herein.
摘要翻译：本文提供了用于治疗肝癌如肝细胞癌，胆管癌或胆道癌的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗癌剂组合施用。在某些实施方案中，化合物是式I的核苷类似物：（I）; 或其药学上可接受的盐，其中基团，Z 1，Z 2，Z 3，Z 4，V，W，X，Ar，R 1和R 2如本文所述。

97. 发明申请

WO2015077360A2 CYCLOPENTANE AND CYCLOPENTENE NUCLEOSIDE ANALOGS FOR THE TREATMENT OF HCV 审中-公开
标题翻译：用于治疗HCV的CYCLOPENTANE和CYCLOPENTENE核苷类似物
公开(公告)号：WO2015077360A2
公开(公告)日：2015-05-28
申请号：PCT/US2014066446
申请日：2014-11-19
申请人： IDENIX PHARMACEUTICALS INC
发明人： MOUSSA ADEL M , STEWART ALISTAIR JAMES , MAYES BENJAMIN ALEXANDER
IPC分类号： C07D239/47
CPC分类号： C07F9/65125 , A61K31/675 , A61K31/685 , A61K45/06 , C07D239/47 , C07D239/54 , C07D239/553 , C07D471/04 , C07D473/16 , C07D473/18 , C07D473/34 , C07D487/04 , C07F9/65121 , C07F9/6561 , C07F9/65616
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are nucleoside analogs of Formula I: (I); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, Z1, Z2, Z3, Z4, V, W, X, Y, Ar, R1 and R2 are as described herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物是式I的核苷类似物：（I）; 或其药学上可接受的盐，溶剂合物，立体异构形式，互变异构形式或其多晶型形式，其中基团，Z 1，Z 2，Z 3，Z 4，V，W，X，Y，Ar，R 1和R 2如本文所述。

98. 发明申请

WO2014197578A1 1',4'-THIO NUCLEOSIDES FOR THE TREATMENT OF HCV 审中-公开
标题翻译： 1'，4'-THIO核苷酸治疗HCV
公开(公告)号：WO2014197578A1
公开(公告)日：2014-12-11
申请号：PCT/US2014/040884
申请日：2014-06-04
申请人： IDENIX PHARMACEUTICALS, INC. , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITÉ MONTPELLIER 2 SCIENCES ET TECHNIQUES
发明人： DUKHAN, David , GOSSELIN, Gilles , DOUSSON, Cyril B.
IPC分类号： C07H19/067 , A61K31/7072 , A61P31/14
CPC分类号： C07D473/18 , A61K31/506 , A61K31/522 , A61K45/06 , C07D409/04 , C07H19/067
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 1',4'-thio nucleoside compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula 3001: (3001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof; wherein Base, R A , R B , W, X, Y, and Z are as described herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物是1'，4'-硫代核苷化合物，其显示出用于治疗例如人类HCV感染的显着功效和生物利用度。在某些实施方案中，化合物为式3001：（3001）; 或其药学上可接受的盐，溶剂合物，立体异构形式，互变异构形式或其多晶型; 其中Base，RA，RB，W，X，Y和Z如本文所述。

99. 发明申请

WO2014066239A1 2',4'-BRIDGED NUCLEOSIDES FOR HCV INFECTION 审中-公开
标题翻译： 2'，4'-BRIDGED NUCLEOSIDES FOR HCV感染
公开(公告)号：WO2014066239A1
公开(公告)日：2014-05-01
申请号：PCT/US2013/065892
申请日：2013-10-21
申请人： IDENIX PHARMACEUTICALS, INC.
发明人： MAYES, Benjamin, Alexander , MOUSSA, Adel, M. , STEWART, Alistair, James
IPC分类号： C07H19/10 , C07H19/11 , C07H19/213 , C07H19/24 , A61P31/14
CPC分类号： C07H19/20 , A61K31/7076 , A61K45/06 , C07H19/10 , C07H19/11 , C07H19/207 , C07H19/213 , C07H19/24
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2',4'-bridged nucleosides which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the 2',4'-bridged nucleosides are of Formula 3001:(I) (3001); or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, where PD, B, W, X, R A , R B , R C and R D are as described herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物是2'，4'-桥接的核苷，其显示用于治疗例如人类HCV感染的显着功效和生物利用度。在某些实施方案中，2'，4'-桥连核苷具有式3001：（I）（3001）; 或其药学上可接受的盐，溶剂化物，立体异构形式，互变异构形式或多晶型，其中PD，B，W，X，RA，RB，RC和RD如本文所述。

100. 发明申请

WO2014063019A1 DINUCLEOTIDE COMPOUNDS FOR HCV INFECTION 审中-公开
标题翻译：用于HCV感染的胆固醇化合物
公开(公告)号：WO2014063019A1
公开(公告)日：2014-04-24
申请号：PCT/US2013/065627
申请日：2013-10-18
申请人： IDENIX PHARMACEUTICALS, INC.
发明人： MOUSSA, Adel M. , MAYES, Benjamin Alexander , ARUMUGASAMY, Jeevanandam , WANG, Jingyang
IPC分类号： C07H21/00 , A61P31/14
CPC分类号： A61K31/7084 , A61K45/06 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H21/00
摘要： Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds comprise two 2 '-methyl nucleotides linked according to Formula (I): N 1 - L - N 2 or a pharmaceutically acceptable salt, ester, solvate, stereoisomer, isomeric form, tautomeric form or polymorphic form thereof; wherein N 1 , L and N 2 are as described herein.
摘要翻译：本文提供了用于治疗黄病毒科感染（包括HCV感染）的化合物，组合物和方法。在某些实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。在某些实施方案中，化合物包含根据式（I）连接的两个2'-甲基核苷酸：N1-L-N2或其药学上可接受的盐，酯，溶剂合物，立体异构体，异构形式，互变异构形式或其多晶型; 其中N1，L和N2如本文所述。

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