公开(公告)号：US10882851B2

公开(公告)日：2021-01-05

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： C07D239/72 ,  C07D413/04 ,  A61K31/5375 ,  A61K31/5377 ,  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″, C1-7 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.

公开(公告)号：US12049461B2

公开(公告)日：2024-07-30

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： A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  C07D239/72 ,  C07D239/78 ,  C07D239/86 ,  C07D239/88 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04

CPC分类号： C07D413/04 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/14 ,  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″, C1-7alkyl, 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.