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1. 发明申请

US20060264389A1 Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
标题翻译：核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂
公开(公告)号：US20060264389A1
公开(公告)日：2006-11-23
申请号：US10521006
申请日：2003-07-11
申请人： Balkrishen Bhat , Steven Carroll , Anne Eldrup , Malcolm MacCoss , David Olsen , Thazha Prakash
发明人： Balkrishen Bhat , Steven Carroll , Anne Eldrup , Malcolm MacCoss , David Olsen , Thazha Prakash
IPC分类号： A61K31/7076 , C07H19/22
CPC分类号： C07H19/14 , C07H19/22
摘要： Thee 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 via 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 creating 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。这些化合物是通过复制的RNA依赖性RNA的抑制剂，并且可用于治疗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/或用本发明的核苷化合物产生RNA依赖性RNA病毒感染的方法。

2. 发明申请

US20060205686A1 Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 审中-公开
公开(公告)号：US20060205686A1
公开(公告)日：2006-09-14
申请号：US11236224
申请日：2005-09-27
申请人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Steven Carroll , Malcolm MacCoss , David Olsen
发明人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Steven Carroll , Malcolm MacCoss , David Olsen
IPC分类号： A61K31/7056 , A61K31/7076
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.

3. 发明申请

US20060234962A1 Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
标题翻译：核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂
公开(公告)号：US20060234962A1
公开(公告)日：2006-10-19
申请号：US10517294
申请日：2003-06-23
申请人： David Olsen , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
发明人： David Olsen , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
IPC分类号： A61K31/7076 , C07H19/16 , C07H19/22
CPC分类号： C07H19/22 , C07H19/14 , C07H19/16 , 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。

4. 发明申请

US20070004669A1 Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
标题翻译：核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂
公开(公告)号：US20070004669A1
公开(公告)日：2007-01-04
申请号：US10517295
申请日：2003-06-17
申请人： Steven Carroll , David Olsen , Philippe Durette , Balkrishen Bhat , Prasad Dande , Anne Eldrup
发明人： Steven Carroll , David Olsen , Philippe Durette , Balkrishen Bhat , Prasad Dande , Anne Eldrup
IPC分类号： A61K31/7076 , A61K31/7072 , C07H19/04 , C07H19/167 , C07H19/12
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。

5. 发明申请

US20050272676A1 Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 审中-公开
标题翻译：核苷衍生物作为RNA依赖性RNA病毒聚合酶的抑制剂
公开(公告)号：US20050272676A1
公开(公告)日：2005-12-08
申请号：US11200499
申请日：2005-08-09
申请人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Robert LaFemina , Amy Simcoe , Carrie Rutkowski , Mario Valenciano
发明人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Robert LaFemina , Amy Simcoe , Carrie Rutkowski , Mario Valenciano
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。

6. 发明申请

US20050042647A1 Phosphorous-linked oligomeric compounds and their use in gene modulation 审中-公开
标题翻译：磷链寡聚化合物及其在基因调控中的应用
公开(公告)号：US20050042647A1
公开(公告)日：2005-02-24
申请号：US10860455
申请日：2004-06-03
申请人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash
发明人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash
IPC分类号： A61K48/00 , C07H21/02 , C12Q1/68
CPC分类号： C07H21/02 , C12N15/111 , C12N2310/14 , C12N2310/315 , C12N2310/319 , C12N2310/3341 , C12N2310/341 , C12N2310/342 , C12N2310/343 , C12N2310/335 , C12N2310/3521 , C12N2310/321 , C12N2310/3525
摘要： Oligonucleotide compositions comprising first and second oligonucleotides are provided wherein at least a portion of the first oligonucleotide is capable of hybridizing with at least a portion of the second oligonucleotide, at least a portion of the first oligonucleotide is complementary to and capble of hybridizing to a selected target nucleic acid, and at least one of the first or second oligonucleotides includes at least one nucleotide having a modified phosphorous-containing internucleoside linkage. Oligonucleotide/protein compositions are also provided comprising an oligonucleotide complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide of the oligonucleotide has a modified phosphorous-containing internucleoside linkage.
摘要翻译：提供了包含第一和第二寡核苷酸的寡核苷酸组合物，其中至少一部分第一寡核苷酸能够与至少一部分第二寡核苷酸杂交，第一寡核苷酸的至少一部分与选定的靶核酸，并且第一或第二寡核苷酸中的至少一个包含至少一个具有修饰的含磷核苷间键的核苷酸。还提供了寡核苷酸/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡核苷酸和至少一种包含至少一部分RNA诱导的沉默复合物（RISC）的蛋白质，其中至少一个核苷酸寡核苷酸具有修饰的含磷核苷键。

7. 发明申请

US20050037370A1 Oligomeric compounds having modified bases for binding to adenine and guanine and their use in gene modulation 审中-公开
标题翻译：具有与腺嘌呤和鸟嘌呤结合的修饰碱基的寡聚化合物及其在基因调控中的用途
公开(公告)号：US20050037370A1
公开(公告)日：2005-02-17
申请号：US10700884
申请日：2003-11-04
申请人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash , Kallanthottathil Rajeev
发明人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash , Kallanthottathil Rajeev
IPC分类号： A61K48/00 , C12Q1/68
CPC分类号： C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/333 , C12N2310/336 , C12N2320/50
摘要： Oligomer compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capble of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers has a modified base for binding to an adenine or guanine base in the opposite strand. Oligonucleotide/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein the oligomer has a modified base for binding to an adenine or guanine base in the opposite strand.
摘要翻译：提供包含第一和第二寡聚物的低聚物组合物，其中至少一部分第一寡聚体能够与至少一部分第二寡聚物杂交，至少一部分第一寡聚体与所选择的寡核苷酸杂交互补和杂交靶核酸，并且第一或第二寡聚体中的至少一个具有与相对链中的腺嘌呤或鸟嘌呤碱基结合的修饰碱基。还提供了寡核苷酸/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡聚体和至少一种包含RNA诱导的沉默复合物（RISC）的至少一部分的蛋白质，其中所述寡聚物具有修饰的碱基用于与相对链中的腺嘌呤或鸟嘌呤碱基结合。

8. 发明申请

US20070275912A1 Nucleoside derivatives as inhibitors of rna-dependent RNA viral polymerase 审中-公开
标题翻译：核苷衍生物作为rna依赖性RNA病毒聚合酶的抑制剂
公开(公告)号：US20070275912A1
公开(公告)日：2007-11-29
申请号：US11643464
申请日：2006-12-21
申请人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Robert LeFemina , Amy Simcoe , Carrie Rutkowski , Mario Valenciano
发明人： Balkrishen Bhat , Anne Eldrup , Thazha Prakash , Phillip Cook , Robert LeFemina , Amy Simcoe , Carrie Rutkowski , Mario Valenciano
IPC分类号： A61K31/706 , A61K31/7076 , A61P31/14 , C07H19/06 , C07H19/16
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。

9. 发明申请

US20050118605A9 Oligomeric compounds having modified bases for binding to adenine and guanine and their use in gene modulation 审中-公开
公开(公告)号：US20050118605A9
公开(公告)日：2005-06-02
申请号：US10700884
申请日：2003-11-04
申请人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash , Kallanthottathil Rajeev
发明人： Brenda Baker , Anne Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard Griffey , Eric Swayze , Stanley Crooke , Thazha Prakash , Kallanthottathil Rajeev
IPC分类号： A61K48/00 , C12Q1/68
CPC分类号： C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/333 , C12N2310/336 , C12N2320/50
摘要： Oligomer compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capble of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers has a modified base for binding to an adenine or guanine base in the opposite strand. Oligonucleotide/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein the oligomer has a modified base for binding to an adenine or guanine base in the opposite strand.

10. 发明申请

US20080021047A1 C-Purine Nucleoside Analogs As Inhibitors Of Rna-Dependent Rna Viral Polymerase 有权
标题翻译： C-嘌呤核苷类似物作为Rna依赖性Rna病毒聚合酶的抑制剂
公开(公告)号：US20080021047A1
公开(公告)日：2008-01-24
申请号：US11628513
申请日：2005-06-10
申请人： Gabor Butora , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
发明人： Gabor Butora , Malcolm MacCoss , Balkrishen Bhat , Anne Eldrup
IPC分类号： A61K31/52 , A61K31/519 , A61P31/12 , C07D473/18 , C07D473/34 , C07D487/04 , C07D491/048 , C07D498/04
CPC分类号： C07D491/04 , C07D487/04 , C07H19/16 , C07H19/20
摘要： The present invention provides C-purine nucleoside analogs 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 C-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 C-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C-嘌呤核苷类似物及其某些衍生物。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含有这种C-核苷化合物的药物组合物。还公开了本发明的C-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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