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    • 2. 发明申请
      US20080255105A1 Biphenyl Derivatives and Their Use in Treating Hepatitis C 失效
    • Biphenyl Derivatives and Their Use in Treating Hepatitis C
    • US20080255105A1
    • 2008-10-16
    • US12066983
    • 2006-09-18
    • 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
    • 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
    • A61K31/5375 , C07D265/30 , C07D413/12 , A61K31/541 , A61P31/00 , A61K31/54 , A61K31/5377 , C07D417/12
    • C07D213/75 , C07D205/04 , C07D233/64 , C07D237/28 , C07D279/12 , C07D295/135 , C07D295/26 , C07D307/38 , C07D333/20 , C07D417/12
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明授权
      US06174889B1 Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
    • Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
    • 双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
    • US06174889B1
    • 2001-01-16
    • US09214270
    • 1998-12-31
    • George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
    • George Stuart Cockerill , Malcolm Clive Carter , Stephen Barry Guntrip , Kathryn Jane Smith
    • A61K31519
    • C07D493/08 , C07D209/08 , C07D231/56 , C07D235/08 , C07D401/06 , C07D407/12 , C07D471/04
    • Substituted heteroaromatic compounds, and in particular substituted bicyclic heteroaromatic compounds of formula (I), wherein X is N or CH; A represents a fused 5, 6 or 7-membered heterocyclic ring containing 1 to 5 heteroatoms which may be the same or different and which are selected from N, O or S(O)m, wherein m is as defined above, the heterocyclic ring containing a total of 1, 2 or 3 double bonds inclusive of the bond in the pyridine or pyrimidine ring to which it is fused, with the provisos that the heterocyclic ring does not form part of a purine and that the fused heterocyclic ring does not contain two adjacent O or S(O)m atoms. U represents a 5 to 10-membered mono or bicyclic ring system in which one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S(O)m, wherein m is 0, 1 or 2 and wherein the ring system is substituted by at least one independently selected R6 group and is optionally substituted by at least one independently selected R4 group, with the proviso that U does not represent phenyl; are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis.
    • 取代的杂芳族化合物，特别是式（I）的取代的双环杂芳族化合物，其中X是N或CH; A表示稠合的5,6或7元杂环，其含有1至5个可以相同或不同的杂原子，并且其选自N，O或S（O）m，其中m如上定义，杂环 包含总共1,2或3个双键，包括其所融合的吡啶或嘧啶环中的键，条件是杂环不形成嘌呤的一部分，并且稠合杂环不包含 两个相邻的O或S（O）m原子。 U表示5至10元单或双环体系，其中一个或多个碳原子任选被独立地选自N，O和S（O）m的杂原子取代，其中m为0,1或2，以及 其中所述环系被至少一个独立选择的R 6基团取代，并且任选地被至少一个独立选择的R 4基团取代，条件是U不表示苯基; 是蛋白酪氨酸激酶抑制剂。 这些化合物被描述为它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途，例如治疗癌症和牛皮癣。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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