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1. 发明申请

WO2012078416A3 MONOPHOSPHATE PRODRUGS OF DAPD AND ANALOGS THEREOF 审中-公开
公开(公告)号：WO2012078416A3
公开(公告)日：2012-06-14
申请号：PCT/US2011/062484
申请日：2011-11-29
申请人： RFS PHARMA, LLC , EMORY UNIVERSITY , SCHINAZI, Raymond, F. , COATS, Steven, J.
发明人： SCHINAZI, Raymond, F. , COATS, Steven, J.
IPC分类号： C07H19/16 , C07H19/20 , C07H21/00 , A61K31/7076 , A61P31/18 , A61P31/20
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2- amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.

2. 发明申请

WO2012027712A3 POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS 审中-公开
公开(公告)号：WO2012027712A3
公开(公告)日：2012-03-01
申请号：PCT/US2011/049426
申请日：2011-08-26
申请人： RFS PHARMA, LLC , EMORY UNIVERSITY , COATS, Steven, J. , AMBLARD, Franck , ZHANG, Hongwang , ZHOU, Longhu , WHITAKER, Richard, Anthony , MCBRAYER, Tamara, Rosario , SCHINAZI, Raymond, F. , SHI, Junxing
发明人： COATS, Steven, J. , AMBLARD, Franck , ZHANG, Hongwang , ZHOU, Longhu , WHITAKER, Richard, Anthony , MCBRAYER, Tamara, Rosario , SCHINAZI, Raymond, F. , SHI, Junxing
IPC分类号： C07D403/04 , C07D403/14 , C07D413/14 , C07D405/14 , A61K31/4178 , A61P31/14
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.

3. 发明申请

WO2010068708A3 3'-AZIDO PURINE NUCLEOTIDE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS 审中-公开
公开(公告)号：WO2010068708A3
公开(公告)日：2010-06-17
申请号：PCT/US2009/067400
申请日：2009-12-09
申请人： RFS PHARMA, LLC , SCHINAZI, Raymond, F. , MELLORS, John, W. , SLUIS-CREMER, Nicolas, Paul , AMBLARD, Franck , COATS, Steven, J. , SHI, Junxing , WHITAKER, Richard, Anthony , EMORY UNIVERSITY , UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
发明人： SCHINAZI, Raymond, F. , MELLORS, John, W. , SLUIS-CREMER, Nicolas, Paul , AMBLARD, Franck , COATS, Steven, J. , SHI, Junxing , WHITAKER, Richard, Anthony
IPC分类号： C07D487/04 , C07D491/048 , A61P31/12 , A61K31/437
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3'-azido-2',3'-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.

4. 发明申请

WO2013106689A8 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：WO2013106689A8
公开(公告)日：2014-06-05
申请号：PCT/US2013021200
申请日：2013-01-11
申请人： RFS PHARMA LLC , COATS STEVEN J
发明人： COATS STEVEN J
IPC分类号： C07D403/12 , A61K31/4025 , A61K31/4035 , A61P31/14
CPC分类号： C07K5/101 , A61K31/4035 , A61K38/07 , A61K45/06 , C07D403/12 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing HCV viral infections in human patients or other animal hosts.
摘要翻译：本发明涉及用于治疗或预防人类患者或其他动物宿主中HCV病毒感染的化合物，组合物和方法。

5. 发明申请

WO2012078416A2 MONOPHOSPHATE PRODRUGS OF DAPD AND ANALOGS THEREOF 审中-公开
标题翻译： DAPD及其类似物的单磷酸酯产物
公开(公告)号：WO2012078416A2
公开(公告)日：2012-06-14
申请号：PCT/US2011062484
申请日：2011-11-29
申请人： RFS PHARMA LLC , UNIV EMORY , SCHINAZI RAYMOND F , COATS STEVEN J
发明人： SCHINAZI RAYMOND F , COATS STEVEN J
IPC分类号： C07H19/16 , A61K31/7076 , A61P31/18 , A61P31/20 , C07H19/20 , C07H21/00
CPC分类号： A61K31/7072 , A61K31/675 , A61K45/06 , C07F9/65616 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2- amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.
摘要翻译：本发明涉及在人类患者或其他动物宿主中治疗或预防癌症和病毒感染，特别是HIV和HBV的化合物，组合物和方法。这些化合物是某些6-取代-2-氨基 - 嘌呤二氧戊环单磷酸酯或膦酸酯及其药学上可接受的盐，前药和其它衍生物。

6. 发明申请

WO2010091386A2 PURINE NUCLEOSIDE MONOPHOSPHATE PRODRUGS FOR TREATMENT OF CANCER AND VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗癌症和病毒感染的磷酸核苷一磷酸腺苷
公开(公告)号：WO2010091386A2
公开(公告)日：2010-08-12
申请号：PCT/US2010/023563
申请日：2010-02-09
申请人： RFS PHARMA, LLC , EMORY UNIVERSITY , CHO, Jong, Hyun , COATS, Steven, J. , SCHINAZI, Raymond, F. , ZHANG, Hongwang , ZHOU, Longhu
发明人： CHO, Jong, Hyun , COATS, Steven, J. , SCHINAZI, Raymond, F. , ZHANG, Hongwang , ZHOU, Longhu
IPC分类号： C07D487/04 , C07D405/04 , A61K31/7028 , A61P35/00 , A61P31/12
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7028 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/708 , A61K45/06 , C07D473/16 , C07H19/173 , C07H19/20 , Y02A50/385 , Y02A50/387 , Y02A50/393 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporo virus, HSV-I, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-I, HIV-2, HCV, Norovirus, Saporovirus, HSV-I, HSV-2, Dengue virus, Yellow fever, and HBV.
摘要翻译：本发明涉及用于治疗或预防癌症和病毒感染的化合物，组合物和方法，特别是HIV，HCV，诺如病毒，Saporo病毒，HSV-1，HSV-2，登革热病毒，黄热病和HBV在人中患者或其他动物宿主。化合物是某些6-取代嘌呤单磷酸酯及其药学上可接受的盐，前药和其它衍生物。特别地，这些化合物对HIV-1，HIV-2，HCV，诺如病毒，Saporovirus，HSV-1，HSV-2，登革热病毒，黄热病和HBV显示出有效的抗病毒活性。

7. 发明申请

WO2012061248A2 NOVEL SPECIFIC HCV NS3 PROTEASE INHIBITORS 审中-公开
标题翻译：新型特异性HCV NS3蛋白酶抑制剂
公开(公告)号：WO2012061248A2
公开(公告)日：2012-05-10
申请号：PCT/US2011/058404
申请日：2011-10-28
申请人： RFS PHARMA, LLC , GENOSCIENCE PHARMA , COURCAMBECK, Jerome , HALFON, Philippe , BOUZIDI, Mourad , COATS, Steven, J. , WHITAKER, Richard, Anthony
发明人： COURCAMBECK, Jerome , HALFON, Philippe , BOUZIDI, Mourad , COATS, Steven, J. , WHITAKER, Richard, Anthony
IPC分类号： C07D403/12 , A61K31/4035 , A61K31/4025 , A61P31/14
CPC分类号： C07D403/12 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HCV in human patients or other animal hosts.
摘要翻译：本发明涉及用于治疗或预防病毒感染的化合物，组合物和方法，特别是人类患者或其他动物宿主中的HCV。

8. 发明申请

WO2012027712A2 POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒潜伏和选择性抑制剂
公开(公告)号：WO2012027712A2
公开(公告)日：2012-03-01
申请号：PCT/US2011049426
申请日：2011-08-26
申请人： RFS PHARMA LLC , UNIV EMORY , COATS STEVEN J , AMBLARD FRANCK , ZHANG HONGWANG , ZHOU LONGHU , WHITAKER RICHARD ANTHONY , MCBRAYER TAMARA ROSARIO , SCHINAZI RAYMOND F , SHI JUNXING
发明人： COATS STEVEN J , AMBLARD FRANCK , ZHANG HONGWANG , ZHOU LONGHU , WHITAKER RICHARD ANTHONY , MCBRAYER TAMARA ROSARIO , SCHINAZI RAYMOND F , SHI JUNXING
IPC分类号： C07D403/04 , A61K31/4178 , A61P31/14 , C07D403/14 , C07D405/14 , C07D413/14
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/4192 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/14
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
摘要翻译：本发明涉及用于治疗或预防人受试者或其他动物宿主中丙型肝炎病毒（HCV）感染的化合物，组合物和方法。这些化合物也是药学上可接受的，盐，前药和其它衍生物，作为用于治疗或预防HCV感染的药物组合物和方法。

9. 发明申请

WO2009129120A2 NUCLEOSIDE DERIVATIVES FOR TREATMENT OF CALICIVIRIDAE INFECTIONS, INCLUDING NOROVIRUS INFECTIONS 审中-公开
标题翻译：用于治疗卡介菌感染的核苷衍生物，包括非肠道感染
公开(公告)号：WO2009129120A2
公开(公告)日：2009-10-22
申请号：PCT/US2009/040092
申请日：2009-04-09
申请人： RFS PHARMA, LLC , SCHINAZI, Raymond, F. , WHITAKER, Richard, Anthony , MCBRAYER, Tamara, Rosario , COATS, Steven, J.
发明人： SCHINAZI, Raymond, F. , WHITAKER, Richard, Anthony , MCBRAYER, Tamara, Rosario , COATS, Steven, J.
IPC分类号： A61K31/7076 , A61P31/12 , A61K38/21 , A61K9/20
CPC分类号： A61K31/7076 , A61K38/21 , A61K2300/00
摘要： A method and composition for treating a host infected with a Caliciviridae virus, such as a Norovirus, comprising administering an effective treatment amount of a described modified nucleoside or a pharmaceutically acceptable salt thereof, is provided.
摘要翻译：提供了用于治疗感染了杯状病毒科（例如诺如病毒）的宿主的方法和组合物，其包括施用有效治疗量的所述修饰的核苷或其药学上可接受的盐。

10. 发明申请

WO2009018106A3 STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES 审中-公开
标题翻译：制备嘌呤二氧杂环己烷衍生物的立体选择性方法
公开(公告)号：WO2009018106A3
公开(公告)日：2009-03-12
申请号：PCT/US2008071069
申请日：2008-07-24
申请人： RFS PHARMA LLC , COATS STEVEN J
发明人： COATS STEVEN J
IPC分类号： A61K31/505 , C07D405/04 , C07D473/00
CPC分类号： C07D473/16
摘要： A cost-effective process scale method for preparing purine dioxolane nucleoside derivatives in racemic or optically pure form is disclosed, as are nucleoside derivatives prepared by the method. The method involves reacting a purine or a mono- or polysilylated purine derivative with an activated dioxolane analog to produce the dioxolane nucleoside analog in commercially useful yields. Direct reaction of purine or a mono- or polysilylated purine with dioxolanes takes place with highest reported chemical yields and excellent stereoselectivity when an additive in the form of an alpha cyano carbonyl compound or silylated alpha cyano carbonyl compounds is present in the reaction mixture during the glycosylation reaction.
摘要翻译：公开了一种用于制备外消旋或光学纯的形式的嘌呤二氧戊环核苷衍生物的成本有效的工艺规模方法，以及通过该方法制备的核苷衍生物。该方法包括使嘌呤或单或聚硅酸化嘌呤衍生物与活化的二氧杂环戊烷类似物反应，以商业上有用的收率产生二氧戊环核苷类似物。在糖基化过程中当反应混合物中存在α氰基羰基化合物或甲硅烷基化α氰基羰基化合物形式的添加剂时，嘌呤或单或多聚化嘌呤与二氧戊环的直接反应发生，报道最高的化学产率和优异的立体选择性反应。

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