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公开(公告)号：EP2004634A1
公开(公告)日：2008-12-24
申请号：EP07727339.9
申请日：2007-03-26
发明人： SARMA, Keshab
IPC分类号： C07D405/04 , A61K31/513
CPC分类号： C07H19/06 , C07D405/04
摘要： Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process.
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公开(公告)号：EP1931692B1
公开(公告)日：2008-11-26
申请号：EP06793434.9
申请日：2006-09-12
发明人： SARMA, Keshab
IPC分类号： C07H19/09
CPC分类号： C07H19/067 , C07H19/073 , C07H19/09 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19
摘要： The present invention relates to a one-step process for the selective O-acylation of the hydroxy groups of a nucleoside under basic conditions utilizing DMAP and a carboxylic acid anhydride in aqueous heterogenous solvent mixture.
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公开(公告)号：EP1794172A1
公开(公告)日：2007-06-13
申请号：EP05777388.9
申请日：2005-08-16
IPC分类号： C07H19/067 , A61P31/14 , A61K31/7068
CPC分类号： C07H19/06 , C07H19/067 , C07H19/12
摘要： 4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-diyhdroxy-5-hydroxymethyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process. (I)
摘要翻译： 4-氨基-1 - （（2R，3S，4S，5R）-5-叠氮基-3,4-二羟基-5-羟甲基 - 四氢呋喃-2-基）-1H-嘧啶-2-酮（I： R2 = R3 = R4 = H）以及它们的前药是丙型肝炎（HCV）聚合酶抑制剂。 还公开了用于抑制HCV和治疗HCV介导的疾病的组合物和方法，用于制备在该方法中使用的化合物和合成中间体的方法。 （一世）
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公开(公告)号：EP1957510A1
公开(公告)日：2008-08-20
申请号：EP06819838.1
申请日：2006-11-29
发明人： CHUN, Byoung-Kwon , CLARK, Jeremy , SARMA, Keshab , WANG, Peiyuan
IPC分类号： C07H19/06 , A61K31/7068 , A61P31/14
摘要： Compounds having the formula I wherein R1 is as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, and processes for making the compounds of formula I.
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公开(公告)号：EP1957454A1
公开(公告)日：2008-08-20
申请号：EP06819599.9
申请日：2006-11-20
发明人： CONNOLLY, Terrence Joseph , FARRELL, Robert P. , HUMPHREYS, Eric R. , LYNCH, Stephen M. , SARMA, Keshab
IPC分类号： C07D209/14
CPC分类号： C07D209/14 , C07D209/18
摘要： A method comprising: hydrogenating an indole propionamide compound of formula h with vitride, to form an aminopropyl indole compound of formula I wherein m, Ar, R1 and R2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
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公开(公告)号：EP1931692A2
公开(公告)日：2008-06-18
申请号：EP06793434.9
申请日：2006-09-12
发明人： SARMA, Keshab
IPC分类号： C07H19/09
CPC分类号： C07H19/067 , C07H19/073 , C07H19/09 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19
摘要： The present invention relates to a one-step process for the selective O-acylation of the hydroxy groups of a nucleoside under basic conditions utilizing DMAP and a carboxylic acid anhydride in aqueous heterogenous solvent mixture.
摘要翻译： 本发明涉及在碱性条件下使用DMAP和羧酸酐在含水非均相溶剂混合物中对核苷的羟基进行选择性O-酰化的一步法。
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公开(公告)号：EP2958893A1
公开(公告)日：2015-12-30
申请号：EP14706519.7
申请日：2014-02-18
IPC分类号： C07D207/16
CPC分类号： C07D207/16
摘要： The present invention provides an improved method for the large scale production of the compound 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid.
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公开(公告)号：EP2528930B1
公开(公告)日：2013-10-30
申请号：EP11701107.2
申请日：2011-01-25
发明人： MA, Han , SARMA, Keshab , SMITH, David Bernard
IPC分类号： C07H19/067 , A61K31/7072
CPC分类号： C07H19/067
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公开(公告)号：EP2528930A1
公开(公告)日：2012-12-05
申请号：EP11701107.2
申请日：2011-01-25
发明人： MA, Han , SARMA, Keshab , SMITH, David Bernard
IPC分类号： C07H19/067 , A61K31/7072
CPC分类号： C07H19/067
摘要： Compounds having the formula I wherein R
1 , R
2 and R
3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.-
公开(公告)号：EP1957454B1
公开(公告)日：2011-07-20
申请号：EP06819599.9
申请日：2006-11-20
发明人： CONNOLLY, Terrence Joseph , FARRELL, Robert P. , HUMPHREYS, Eric R. , LYNCH, Stephen M. , SARMA, Keshab
IPC分类号： C07D209/14
CPC分类号： C07D209/14 , C07D209/18
摘要： A method comprising: hydrogenating an indole propionamide compound of formula h with vitride, to form an aminopropyl indole compound of formula I wherein m, Ar, R1 and R2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
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