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1. 发明申请

WO2006119061A2 HCV NS3 PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：WO2006119061A2
公开(公告)日：2006-11-09
申请号：PCT/US2006016343
申请日：2006-04-28
申请人： MERCK & CO INC , HOLLOWAY M KATHARINE , LIVERTON NIGEL J , LUDMERER STEVEN W , MCCAULEY JOHN A , OLSEN DAVID B , RUDD MICHAEL T , VACCA JOSEPH P
发明人： HOLLOWAY M KATHARINE , LIVERTON NIGEL J , LUDMERER STEVEN W , MCCAULEY JOHN A , OLSEN DAVID B , RUDD MICHAEL T , VACCA JOSEPH P
IPC分类号： A61K38/05
CPC分类号： C07K5/0808 , C07K5/0806 , C07K5/0812 , C07K5/0815 , C07K5/0821
摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. I
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。一世

2. 发明申请

WO2007145894A2 A RAPID METHOD TO DETERMINE INHIBITOR SENSITIVITY OF NS3/4A PROTEASE SEQUENCES CLONED FROM CLINICAL SAMPLES 审中-公开
标题翻译：确定从临床样品中克隆的NS3 / 4A蛋白酶序列的抑制敏感性的快速方法
公开(公告)号：WO2007145894A2
公开(公告)日：2007-12-21
申请号：PCT/US2007013154
申请日：2007-06-04
申请人： MERCK & CO INC , LUDMERER STEVEN W , GRAHAM DONALD J , OLSEN DAVID B
发明人： LUDMERER STEVEN W , GRAHAM DONALD J , OLSEN DAVID B
IPC分类号： C12Q1/70
CPC分类号： C12N9/506
摘要： A method for measuring HCV NS3/4A activity from a HCV NS3/4A sequence, comprising obtaining and cloning the sequence into a mammalian expression vector, transiently transfecting a mammalian cell with the vector, which includes a reporter construct encoding a HCV NS3/4A cleavage site fused to a detectable label, measuring signal production from the label resulting from cleavage at the cleavage site, and measuring effects on signal production by addition of a test compound.
摘要翻译：一种从HCV NS3 / 4A序列测量HCV NS3 / 4A活性的方法，包括获得并将该序列克隆到哺乳动物表达载体中，该载体用载体瞬时转染哺乳动物细胞，其包括编码HCV NS3 / 4A切割的报道构建体与可检测标记融合的位点，测量从切割位点处切割产生的标记物的信号产生，以及通过添加测试化合物测量对信号产生的影响。

3. 发明申请

WO2012142093A3 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译： 2'-氰基取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：WO2012142093A3
公开(公告)日：2013-02-07
申请号：PCT/US2012033028
申请日：2012-04-11
申请人： MERCK SHARP & DOHME , GIRIJAVALLABHAN VINAY , NJOROGE F GEORGE , BOGEN STEPHANE , KEREKES ANGELA , BENNETT FRANK , HUANG YING , NAIR LATHA , PISSARNITSKI DMITRI , VERMA VISHAL , DANG QUN , DAVIES IAN , OLSEN DAVID B , STAMFORD ANDREW , VACCA JOSEPH P
发明人： GIRIJAVALLABHAN VINAY , NJOROGE F GEORGE , BOGEN STEPHANE , KEREKES ANGELA , BENNETT FRANK , HUANG YING , NAIR LATHA , PISSARNITSKI DMITRI , VERMA VISHAL , DANG QUN , DAVIES IAN , OLSEN DAVID B , STAMFORD ANDREW , VACCA JOSEPH P
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00
CPC分类号： C07H19/16 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/213
摘要： The present invention relates to 2'-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3are as defined herein. The present invention also relates to compositions comprising at least one 2'-Cyano Substituted Nucleoside Derivative, and methods of using the 2'-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-氰基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种2'-氰基取代的核苷衍生物的组合物，以及使用2'-氰基取代的核苷衍生物治疗或预防患者HCV感染的方法。

4. 发明申请

WO2007021610A3 RIBONUCLEOSIDE CYCLIC ACETAL DERIVATIVES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：核糖核苷环状乙酰基衍生物用于治疗RNA依赖性RNA病毒感染
公开(公告)号：WO2007021610A3
公开(公告)日：2007-10-04
申请号：PCT/US2006030549
申请日：2006-08-04
申请人： MERCK & CO INC , BUTORA GABOR , KOEPLINGER KENNETH ALAN , MACCOSS MALCOLM , MCMASTERS DANIEL R , OLSEN DAVID B , YANG LIHU
发明人： BUTORA GABOR , KOEPLINGER KENNETH ALAN , MACCOSS MALCOLM , MCMASTERS DANIEL R , OLSEN DAVID B , YANG LIHU
IPC分类号： A01N43/04 , A01N57/00 , A61K31/519
CPC分类号： C07H19/06 , C07H19/16
摘要： The present invention provides ribonucleoside 2',3'-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2',3'-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2',3'-cyclic acetals of the present invention.
摘要翻译：本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前体药物。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，并且可用于治疗RNA依赖性RNA病毒感染。它们作为丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体或前体药物，作为HCV复制抑制剂的前体或前体药物和/或用于治疗丙型肝炎感染特别有用。本发明还描述了含有这种核糖核苷2'，3'-环状缩醛的药物组合物，所述组合物单独地或与其它对RNA依赖性RNA病毒感染特别是HCV感染有活性的药物组合。还公开了抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或用本发明的核糖核苷2'，3'-环缩醛治疗RNA依赖性RNA病毒感染的方法。

5. 发明申请

WO2009132273A3 MICRORNA BIOMARKERS OF TISSUE INJURY 审中-公开
标题翻译：组织损伤的MICRORNA生物标志物
公开(公告)号：WO2009132273A3
公开(公告)日：2010-01-21
申请号：PCT/US2009041666
申请日：2009-04-24
申请人： MERCK & CO INC , FARE THOMAS L , GARRETT-ENGELE PHILIP W , GLAAB WARREN E , JOHNSON JASON M , LATERZA OMAR F , LIM LEE , LUDMERER STEVE W , OLSEN DAVID B , SINA JOSEPH F , SISTARE FRANK D
发明人： FARE THOMAS L , GARRETT-ENGELE PHILIP W , GLAAB WARREN E , JOHNSON JASON M , LATERZA OMAR F , LIM LEE , LUDMERER STEVE W , OLSEN DAVID B , SINA JOSEPH F , SISTARE FRANK D
IPC分类号： G01N33/00
CPC分类号： C12Q1/6883 , C12Q2600/158 , C12Q2600/178 , Y10T436/143333
摘要： One aspect of the invention generally relates to use of tissue enriched miRNAs as biomarker to estimate tissue damage in a fluid sample. In a second aspect, methods are provided for monitoring a subject who is exposed or might have been exposed to an agent that has a risk of causing tissue injury. In a third aspect, methods are provided for identifying an agent as having a risk of causing tissue injury to a vertebrate subject. In a fourth aspect, kits are provided for practicing the methods of above-listed aspects. The contents of this ABSTRACT are not intended to in anyway limit the scope of the inventions claimed herein.
摘要翻译：本发明的一个方面通常涉及使用组织富集的miRNA作为生物标志物来估计流体样品中的组织损伤。在第二方面，提供了用于监测暴露于或可能暴露于具有引起组织损伤风险的药剂的受试者的方法。在第三方面，提供了用于鉴定具有对脊椎动物受试者造成组织损伤风险的药剂的方法。在第四方面，提供了用于实践上述方面的方法的试剂盒。本摘要的内容并不旨在限制本文所要求保护的发明的范围。

6. 发明申请

WO2007095269A2 NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷类ARYL磷酸酯
公开(公告)号：WO2007095269A2
公开(公告)日：2007-08-23
申请号：PCT/US2007003862
申请日：2007-02-12
申请人： MERCK & CO INC , ANGELETTI P IST RICHERCHE BIO , MACCOSS MALCOLM , OLSEN DAVID B , DONGHI MONICA , GARDELLI CRISTINA , HARPER STEVEN , MEPPEN MALTE , NARJES FRANK , PACINI BARBARA
发明人： MACCOSS MALCOLM , OLSEN DAVID B , DONGHI MONICA , GARDELLI CRISTINA , HARPER STEVEN , MEPPEN MALTE , NARJES FRANK , PACINI BARBARA
CPC分类号： C07H19/06
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
摘要翻译：本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的含有这种核苷芳基氨基磷酸酯的药物组合物。还公开了本发明的核苷芳基氨基磷酸酯抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

7. 发明申请

WO02057287A2 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
标题翻译：作为RNA依赖性RNA病毒聚合酶抑制剂的核苷衍生物
公开(公告)号：WO02057287A2
公开(公告)日：2002-07-25
申请号：PCT/US0203086
申请日：2002-01-18
申请人： MERCK & CO INC , ISIS PHARMACEUTICALS INC , CARROLL STEVEN S , MACCOSS MALCOLM , OLSEN DAVID B , BHAT BALKRISHEN , BHAT NEELIMA , COOK PHILLIP DAN , ELDRUP ANNE B , PRAKASH THAZHA P , PRHAVC MARIJA , SONG QUANLAI
发明人： CARROLL STEVEN S , MACCOSS MALCOLM , OLSEN DAVID B , BHAT BALKRISHEN , BHAT NEELIMA , COOK PHILLIP DAN , ELDRUP ANNE B , PRAKASH THAZHA P , PRHAVC MARIJA , SONG QUANLAI
IPC分类号： C07D487/04 , A61K31/519 , A61K31/70 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61K31/708 , A61K31/7105 , A61K31/712 , A61K38/21 , A61K45/00 , A61K45/06 , A61P1/16 , A61P31/14 , A61P43/00 , C07D473/00 , C07D487/02 , C07H20060101 , C07H19/00 , C07H19/04 , C07H19/048 , C07H19/06 , C07H19/067 , C07H19/09 , C07H19/10 , C07H19/14 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19 , C07H19/20 , C12N20060101
CPC分类号： C07H19/16 , A61K9/4858 , A61K31/7056 , A61K31/7064 , A61K31/7076 , A61K38/21 , A61K45/06 , C07D473/00 , C07D487/04 , C07H19/00 , C07H19/06 , C07H19/10 , C07H19/12 , C07H19/14 , C07H19/20 , Y02P20/582 , A61K2300/00
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
摘要翻译：本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

8. 发明申请

WO2007022073A3 NOVEL 2'-C-METHYL AND 4'-C-METHYL NUCLEOSIDE DERIVATIVES 审中-公开
标题翻译：新型2'-C-甲基和4'-C-甲基核苷衍生物
公开(公告)号：WO2007022073A3
公开(公告)日：2007-11-15
申请号：PCT/US2006031614
申请日：2006-08-14
申请人： MERCK & CO INC , METABASIS THERAPEUTICS INC , ERION MARK D , REDDY K RAJA , MACCOSS MALCOLM , OLSEN DAVID B
发明人： ERION MARK D , REDDY K RAJA , MACCOSS MALCOLM , OLSEN DAVID B
IPC分类号： A01N43/00 , A61K31/70
CPC分类号： C07H19/10
摘要： Novel 2'-C-methyl nucleoside 5 '-monophosphate and 4'-C-methyl nucleoside 5'- monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.
摘要翻译：新型2'-C-甲基核苷5'-单磷酸酯和4'-C-甲基核苷5'-单磷酸酯衍生物，立体异构体及其药学上可接受的盐或前药，它们的制备及其治疗丙型肝炎病毒感染的用途被描述。

9. 发明申请

WO2006012078A2 NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷类ARYL磷酸酯
公开(公告)号：WO2006012078A2
公开(公告)日：2006-02-02
申请号：PCT/US2005021684
申请日：2005-06-20
申请人： MERCK & CO INC , MACCOSS MALCOLM , OLSEN DAVID B
发明人： MACCOSS MALCOLM , OLSEN DAVID B
IPC分类号： C12Q1/68
CPC分类号： C07H19/20 , C07H19/14 , C07H19/16
摘要： The present invention provides nucleoside aryl phosphoramidates which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.
摘要翻译：本发明提供核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了单独含有这种核苷芳基氨基磷酸酯或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的药物组合物。还公开了本发明的核苷芳基氨基磷酸酯抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

10. 发明申请

WO2004000858A3 NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE 审中-公开
标题翻译：作为RNA依赖性RNA病毒聚合酶抑制剂的核苷衍生物
公开(公告)号：WO2004000858A3
公开(公告)日：2005-05-12
申请号：PCT/US0319172
申请日：2003-06-17
申请人： MERCK & CO INC , ISIS PHARMACEUTICALS INC , CARROLL STEVEN S , OLSEN DAVID B , DURETTE PHILIPPE L , BHAT BALKRISHEN , DANDE PRASAD , ELDRUP ANNE B
发明人： CARROLL STEVEN S , OLSEN DAVID B , DURETTE PHILIPPE L , BHAT BALKRISHEN , DANDE PRASAD , ELDRUP ANNE B
IPC分类号： C07H19/067 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K38/21 , A61K45/00 , A61P31/14 , A61P43/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/20 , A61K31/70
CPC分类号： C07H19/04 , C07H19/06 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/20
摘要： The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
摘要翻译：本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染（特别是HCV感染）有活性的试剂组合的药物组合物。还公开了本发明的核苷化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

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