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1. 发明授权

US08039616B2 Benzodiazepine derivatives for treating hepatitis C infection 失效
公开(公告)号：US08039616B2
公开(公告)日：2011-10-18
申请号：US12067318
申请日：2005-09-19
申请人： Helena Dennison , Justin Warne , Keith Spencer , George Cockerill , James Lumley
发明人： Helena Dennison , Justin Warne , Keith Spencer , George Cockerill , James Lumley
IPC分类号： C07D243/12 , A61K31/55
CPC分类号： C07D243/24 , A61K31/5513
摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, 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; —R5 represents C1-6alkyl, 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-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, 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 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)-.

2. 发明申请

US20090318427A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 失效
公开(公告)号：US20090318427A1
公开(公告)日：2009-12-24
申请号：US12067318
申请日：2005-09-19
申请人： Helena Dennison , Justin Warne , Keith Spencer , George Cockerill , James Lumley
发明人： Helena Dennison , Justin Warne , Keith Spencer , George Cockerill , James Lumley
IPC分类号： A61K31/5513 , A61P31/12 , C07D243/24
CPC分类号： C07D243/24 , A61K31/5513
摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, 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—C0-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; —R5 represents C1-6alkyl, 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-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, 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 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)-.

3. 发明授权

US08008303B2 Biphenyl derivatives and their use in treating hepatitis C 失效
标题翻译：联苯衍生物及其在治疗丙型肝炎中的应用
公开(公告)号：US08008303B2
公开(公告)日：2011-08-30
申请号：US12066983
申请日：2006-09-18
申请人： Christopher James Wheelhouse , Alexander James Floyd Thomas , David John Bushnell , James Lumley , James Iain Salter , Malcolm Clive Carter , Neil Mathews , Christopher John Pilkington , Richard Martyn Angell
发明人： Christopher James Wheelhouse , Alexander James Floyd Thomas , David John Bushnell , James Lumley , James Iain Salter , Malcolm Clive Carter , Neil Mathews , Christopher John Pilkington , Richard Martyn Angell
IPC分类号： C07D295/02 , A61K31/495
CPC分类号： C07D213/75 , C07D205/04 , C07D233/64 , C07D237/28 , C07D279/12 , C07D295/135 , C07D295/26 , C07D307/38 , C07D333/20 , C07D417/12
摘要： Use of a compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of Hepatitis C wherein the variables are described herein.
摘要翻译：作为式（I）的联苯衍生物或其药学上可接受的盐的化合物用于治疗丙型肝炎的用途，其中本文描述了变量。

4. 发明申请

US20080255105A1 Biphenyl Derivatives and Their Use in Treating Hepatitis C 失效
公开(公告)号：US20080255105A1
公开(公告)日：2008-10-16
申请号：US12066983
申请日：2006-09-18
申请人： Christopher James Wheelhouse , Alexander James Floyd Thomas , David John Bushnell , James Lumley , James Iain Salter , Malcolm Clive Carter , Neil Mathews , Christopher John Pilkington , Richard Martyn Angell
发明人： Christopher James Wheelhouse , Alexander James Floyd Thomas , David John Bushnell , James Lumley , James Iain Salter , Malcolm Clive Carter , Neil Mathews , Christopher John Pilkington , Richard Martyn Angell
IPC分类号： A61K31/5375 , C07D265/30 , C07D413/12 , A61K31/541 , A61P31/00 , A61K31/54 , A61K31/5377 , C07D417/12
CPC分类号： C07D213/75 , C07D205/04 , C07D233/64 , C07D237/28 , C07D279/12 , C07D295/135 , C07D295/26 , C07D307/38 , C07D333/20 , C07D417/12
摘要： A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; -A and B are the same or different and each represent a direct bond or a —CO—NR′—, —NR′—CO—, —NR′—CO2—, —CO—, —NR′—CO—NR″—, —NR′—S(O)2—, —S(O)2—NR′—, —SO2—, —NR′—, —NR′—CO—CO—, —CO—O—, —O—CO—, —(C1-C2 alkylene)-NR′— or —(C1-C2 hydroxyalkylene)-NR′-moiety, wherein R′ and R″ are the same or different and each represent hydrogen or C1-C4 alkyl; —R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′, -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10-membered heteroaryl, 5- to 10-membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents —CO—, —SO— or —S(O)2—; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents —O—, —S— or —NR′—, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10-membered heteroaryl or 5- to 10-membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from —(C1-C4 alkyl)-X1, —CO2R′, —SO2NR′R″, —S(O)2—R′, —CONR′R″, —NR′—CO—R′″, —NR′—S(O)2—R′″, —CO—NR′—(C1-C4 alkyl)-NR′R″ and —CO—O—(C1-C4 alkyl)-NR′R″ and/or (b) 1, 2 or 3 unsubstituted substituents selected from —(C1-C4 alkyl)-X2, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 hydroxyalkyl, hydroxy, cyano, nitro and —NR′R″, wherein X1 is —CO2R′, —SO2—R′, —NR′—CO2—R″, —NR′—S(O)2—R′″, —CONR′R″ or —SO2—NR′R″, each X2 is the same or different and is cyano, nitro or —NR′R″, each R′ and R″ is the same or different and represents hydrogen or C1-C4 alkyl and each R′″ is the same or different and represents C1-C4 alkyl.

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