公开(公告)号：US20140051866A1

公开(公告)日：2014-02-20

申请号：US13801011

申请日：2013-03-13

Applicant: GILEAD SCIENCES, INC.

Inventor： William John Watkins ,  Qi Liu

IPC: C07D409/12 ,  C07D333/36

CPC classification number: C07D409/12 ,  C07D333/36

Abstract: The present disclosure provides a processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of Formula I.

Abstract translation: 本公开提供了制备式I化合物的方法：其可用作抗病毒剂。 本公开还提供了作为式I化合物的合成中间体的化合物。

公开(公告)号：US10882851B2

公开(公告)日：2021-01-05

申请号：US14990322

申请日：2016-01-07

Applicant: Gilead Sciences, Inc.

Inventor： Ling-Jie Gao ,  Piet André Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe ,  William John Watkins ,  Lee Shun Chong

IPC: 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

Abstract: 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

Applicant: Gilead Sciences, Inc.

Inventor： Ling-Jie Gao ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe ,  William John Watkins ,  Lee Shun Chong

IPC: 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 classification number: 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

Abstract: 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：US08927741B2

公开(公告)日：2015-01-06

申请号：US13801011

申请日：2013-03-13

Applicant: Gilead Sciences, Inc.

Inventor： William John Watkins ,  Qi Liu

IPC: C07D409/12 ,  C07D333/36

CPC classification number: C07D409/12 ,  C07D333/36

Abstract: The present disclosure provides a processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of Formula I.

Abstract translation: 本公开提供了制备式I化合物的方法：其可用作抗病毒剂。 本公开还提供了作为式I化合物的合成中间体的化合物。