公开(公告)号：US20190152974A1

公开(公告)日：2019-05-23

申请号：US16162887

申请日：2018-10-17

申请人： Gilead Sciences, Inc.

发明人： Piet André Maurits Maria HERDEWIJN ,  Steven Cesar Alfons DE JONGHE ,  William John WATKINS ,  Lee Shun CHONG

IPC分类号： C07D475/02 ,  C07D475/08 ,  C07D475/00 ,  C07D475/04 ,  C07D475/06

摘要： The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.

公开(公告)号：US20210276988A1

公开(公告)日：2021-09-09

申请号：US16950654

申请日：2020-11-17

申请人： Gilead Sciences, Inc.

发明人： Ling-Jie GAO ,  Piet Andre Maurits Maria HERDEWIJN ,  Steven Cesar Alfons DE JONGHE ,  William John WATKINS ,  Lee Shun CHONG

IPC分类号： C07D413/04 ,  A61K31/5375 ,  A61K31/5377 ,  C07D239/72 ,  C07D239/78 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  A61K31/517 ,  C07D239/86 ,  C07D405/04 ,  C07D409/04

摘要： This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

公开(公告)号：US20160257673A1

公开(公告)日：2016-09-08

申请号：US14990322

申请日：2016-01-07

申请人： Gilead Sciences, Inc.

发明人： Ling-Jie GAO ,  Piet André Maurits Maria HERDEWIJN ,  Steven Cesar Alfons DE JONGHE ,  William John WATKINS ,  Lee Shun CHONG

IPC分类号： C07D413/04 ,  C07D239/88 ,  C07D239/94 ,  C07D401/04 ,  C07D239/86 ,  C07D405/04 ,  C07D409/04 ,  C07D239/95 ,  C07D403/04

CPC分类号： C07D413/04 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7 alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

摘要翻译： 本发明提供由结构式（I）表示的喹唑啉衍生物： 其中：R 2是氢，NR'R“，C 1-7烷基，芳基C 1-7烷基或C 3-10环烷基; R4是氨基，C1-7烷基，C2-7烯基，C3-10环烷基，C3-10环烯基，芳基，杂环，芳基烷基，杂环取代的C1-7烷基或C3-10环烷基C1-7烷基; R5是氢或C1-7烷基，或R5和R4与它们所连接的氮原子一起形成杂环; Y是单键，C1-7亚烷基，C2-7亚烯基或C2-7亚炔基; R6是卤素，杂芳基或芳基; R'和R“各自独立地为氢，C 1-7烷基 - 羰基或C 1-7烷基; 条件是当R 2为H且R 5为H时，R 4不为被吗啉代取代的苯基，并且条件是当NR 4 R 5为哌嗪基时，所述NR 4 R 5为未取代或被甲基或乙酰基取代的; 用于治疗病毒感染的药学上可接受的加成盐，立体异构体，单或二-N-氧化物，溶剂合物或前体药物。