- 专利标题: Benzodiazepine derivatives and pharmaceutical compositions containing them
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申请号: US10528250申请日: 2003-09-22
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公开(公告)号: US07582624B2公开(公告)日: 2009-09-01
- 发明人: Malcolm Carter , Philip Chambers , Verity Dowdell , Elisa Ann Henderson , Richard David Kelsey , Debra Taylor , Stanley Tyms , Lara Wilson
- 申请人: Malcolm Carter , Philip Chambers , Verity Dowdell , Elisa Ann Henderson , Richard David Kelsey , Debra Taylor , Stanley Tyms , Lara Wilson
- 申请人地址: GB London
- 专利权人: Arrow Therapeutics Limited
- 当前专利权人: Arrow Therapeutics Limited
- 当前专利权人地址: GB London
- 代理机构: McCarter & English, LLP
- 代理商 Elizabeth A. Hanley, Esq.; Jermaine A. Lawrence, Esq.
- 优先权: GB0221923.6 20020920; GB0302078.1 20030129
- 国际申请: PCT/GB03/04050 WO 20030922
- 国际公布: WO2004/026843 WO 20040401
- 主分类号: C07D243/24
- IPC分类号: C07D243/24 ; C07D409/12 ; C07D405/12 ; C07D403/12 ; A61K31/5513
摘要:
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.