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81. 发明专利

HK1133889A1 PREPARATION OF NUCLEOSIDES RIBOFURANOSYL PYRIMIDINES 未知
公开(公告)号：HK1133889A1
公开(公告)日：2010-04-09
申请号：HK10101126
申请日：2010-02-02
申请人： HOFFMANN LA ROCHE , GILEAD PHARMASSET LLC
发明人： AXT STEVEN D , SARMA KESHAB , VITALE JUSTIN , ZHU JIANG , ROSS BRUCE , RACHAKONDA SUGUNA , JIN QINGWU , CHUN BYOUNG-KWON
IPC分类号： C07H20060101
摘要： The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase.

82. 发明专利

CA2915187C N-[(2'R)-2'-DEOXY-2'-FLUORO-2'-METHYL-P-PHENYL-5'-URIDYLYL]-L-ALANINE 1-METHYLETHYL ESTER AND PROCESS FOR ITS PRODUCTION 未知
公开(公告)号：CA2915187C
公开(公告)日：2018-01-23
申请号：CA2915187
申请日：2010-05-20
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
IPC分类号： C07H19/10 , A61K31/7072 , A61P31/14 , C07F9/24 , C07F9/6558 , C07H19/06
摘要： Disclosed herein are processes for preparing a compound represented by formula 4 and which comprises: a) reacting an isopropyl-alanate, A, a di-X'-phenylphosphate, B, 2'-deoxy-2'-fluoro-2'-C-methyluridine, 3, and a base to obtain a first mixture comprising 4, or the phosphorous-based diastereomer thereof, b) reacting the first mixture with a protecting compound to obtain a second mixture comprising 4, or the phosphorous-based diastereomer thereof, and a protected side product, wherein the protecting compound is t-butyl-dimethyl-silyl-chloride; and c) subjecting the second mixture to crystallization, chromatography, or extraction in order to obtain 4, or the phosphorous-based diastereomer thereof.

83. 发明专利

EA028709B1 1-МЕТИЛЭТИЛОВЫЙ СЛОЖНЫЙ ЭФИР N-[(2'R)-2'-ДЕЗОКСИ-2'-ФТОР-2'-МЕТИЛ-Р-ФЕНИЛ-5'-УРИДИЛ]-L-АЛАНИНА И СПОСОБ ЕГО ПОЛУЧЕНИЯ 未知
公开(公告)号：EA028709B1
公开(公告)日：2017-12-29
申请号：EA201592101
申请日：2010-05-20
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
IPC分类号： C07F9/24 , A61K31/661 , A61P31/14
摘要： Изобретениеотноситсяк способамполучениянуклеозидныхфосфорамидатов, которыеприменяютв качествесредствдлялечениявирусныхзаболеваний. Способполучениесоединенияформулы S-4 включаетвзаимодействиесоединенияС сосновнымреагентоми соединением 3. Способполучениясоединенияформулы R-4 включаетвзаимодействиесоединения C сосновнымреагентоми соединением 3.

84. 发明专利

ES2644990T3 Síntesis estereoselectiva de principios activos que contienen fósforo 未知
公开(公告)号：ES2644990T3
公开(公告)日：2017-12-01
申请号：ES14163247
申请日：2011-03-31
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE , SOFIA MICHAEL , PAMULAPATI GANAPATI , RACHAKONDA SUGUNA , ZHANG HAI-REN
IPC分类号： C07H19/20 , A61K31/7076 , A61P31/14 , C07F7/18 , C07F9/24 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07H19/04 , C07H19/044 , C07H19/052 , C07H19/06 , C07H19/10 , C07H19/207 , C07H19/24
摘要： Un proceso para preparar un principio activo que contiene fósforo enantiomérica o diastereoméricamente enriquecido, una sal o una sal farmacéuticamente aceptable del mismo, de fórmula I-1:**Fórmula** que comprende las etapas de: (a) hacer reaccionar un principio activo protegido o desprotegido con una base para formar una sal de dicho activo y después hacer reaccionar dicha sal con un compuesto enantiomérica o diastereoméricamente enriquecido de fórmula II-1**Fórmula** en donde el principio activo es un nucleósido, un análogo de nucleósido o un no nucleósido; en donde el nucleósido se selecciona de**Fórmula** en donde el análogo de nucleósido se selecciona de**Fórmula** en donde el no nucleósido se selecciona de**Fórmula** en las que W es un arilo o -(CH2)nSC(O)C(CH3)n,(CH2OH)3-m; en las que n es 2 o 3 y 5 m es 0, 1, 2 o 3; en las que LG se selecciona del grupo que consiste en 2-nitrofenóxido, 4-nitrofenóxido, 2,4-dinitrofenóxido, pentafluorofenóxido, 2-cloro-4-nitrofenóxido y 2,4-diclorofenóxido; en las que R es un alquilo C1-6; y en las que R' es un alquilo C1-6 o un cicloalquilo C3-7; y (b) opcionalmente desproteger el compuesto obtenido en la etapa (a) para obtener el activo que contiene fósforo enantiomérica o diastereoméricamente enriquecido, una sal o una sal farmacéuticamente aceptable del mismo de fórmula I-1, en donde el compuesto enantiomérica o diastereoméricamente enriquecido de fórmula II-1 se obtiene por cristalización a partir de una composición que comprende: i. una primera composición; ii. un precursor del grupo saliente; iii. una base no nucleófila; y iv. una composición líquida que comprende al menos uno de un disolvente y un anti-disolvente; en donde la primera composición comprende Rp-II-1 y Sp-II-1:**Fórmula** y en donde el precursor del grupo saliente es 2,4-dinitrofenol, 4-nitrofenol, 2-nitrofenol, 2-cloro-4-nitrofenol, 2,4- diclorofenol o pentafluorofenol.

85. 发明专利

SG10201708263SA N- [ (2 ' R) -2 ' -DEOXY-2 ' -FLUORO-2 ' -METHYL-P-PHENYL-5 ' -URIDYLYL] -L-ALANINE 1-METHYLETHYL ESTER AND PROCESS FOR ITS PRODUCTION 未知
公开(公告)号：SG10201708263SA
公开(公告)日：2017-11-29
申请号：SG10201708263S
申请日：2010-05-20
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
摘要： Disclosed herein is crystalline phosphoramidate Sp-4 (Sofosbuvir) of the formula below. This compound is an inhibitor of RNA-dependent 5 RNA viral replication and is useful as inhibitor of HCV NS5B polymerase, as inhibitor of HCV replication and for treatment of hepatitis C infection in mammals. This compound can be used in combination with another antiviral agent, such as an HCV NS3 protease inhibitor or an HCV NS5A inhibitor.

87. 发明专利

SI2609923T1 POSTOPEK ZA KRISTALIZACIJO (S)-IZOPROPIL 2-(((S)-(PERFLUOROFENOKSI) (FENOKSI)FOSFORIL)AMINO)PROPANOATA 未知
公开(公告)号：SI2609923T1
公开(公告)日：2017-10-30
申请号：SI201131276
申请日：2011-03-31
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
IPC分类号： A61K31/00 , A61P31/00 , C07F7/00 , C07F9/00 , C07H19/00

89. 发明专利

HUE031637T2 Eljárás N-[(2'R)-2'-deoxi-2'-fluor-2'-metil-P-fenil-5'-uridilil]-L-alanin 1-metiletil észter elõállítására 未知
公开(公告)号：HUE031637T2
公开(公告)日：2017-07-28
申请号：HUE10721225
申请日：2010-05-20
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
IPC分类号： C07H1/00 , A61P31/14 , C07F9/22 , C07F9/24 , C07H19/10

90. 发明专利

AU2016200676B2 N-[(2'R)-2 '-deoxy-2'-fluoro-2'-methyl-p-phenyl-5'-uridylyl] -L-alanine 1-methylethyl ester and process for its production 未知
公开(公告)号：AU2016200676B2
公开(公告)日：2017-06-01
申请号：AU2016200676
申请日：2016-02-03
申请人： GILEAD PHARMASSET LLC
发明人： ROSS BRUCE S , SOFIA MICHAEL JOSEPH , PAMULAPATI GANAPATI REDDY , RACHAKONDA SUGUNA , ZHANG HAI-REN , CHUN BYOUNG-KWON , WANG PEIYUAN
IPC分类号： C07H19/10 , A61K31/7072 , A61P31/14 , C07H19/073
摘要： Abstract Disclosed herein are nucleoside phosphoramidates of formula 4 and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. Disclosed is also a process for preparing compound represented by formula 4: (Formula 4) wherein P* represents a chiral phosphorus atom, which comprises: a) reacting an isopropyl-alanate, (Formula A), a di-X' phenylphosphate, (Formula B), 2'-deoxy-2f-fluoro-2'-C-methyluridine, (Formula 3), and a base to obtain a first mixture comprising 4; wherein X is a conjugate base of an acid, n is 0 or 1, and X' is a halogen, b) reacting the first mixture with a protecting compound to obtain a second mixture comprising 4; and c) optionally subjecting the second mixture to crystallization, chromatography or extraction in order to obtain 4.

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