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    Quinazoline Derivatives as Antiviral Agents
    2.
    发明申请
    Quinazoline Derivatives as Antiviral Agents 审中-公开
    喹唑啉衍生物作为抗病毒剂

    公开(公告)号：US20080114008A1

    公开(公告)日：2008-05-15

    申请号：US11883191

    申请日：2006-01-30

    申请人： George Stuart Cockerill ,  Stephen Sean Flack ,  Neil Mathews ,  James Iain Salter

    发明人： George Stuart Cockerill ,  Stephen Sean Flack ,  Neil Mathews ,  James Iain Salter

    IPC分类号： A61K31/517 ,  C07D403/02

    CPC分类号： C07C255/61 ,  C07D239/94

    摘要： Compounds of formula (I) are found to be active in inhibiting replication of flaviviridac Formula (I) wherein: X represents a direct bond or a moiety -L-NR—, wherein R is hydrogen or C1-C4 alkyl, and L represents a C1-C4alkylene, C6-C10 aryl or 5- to 10-membered heteroaryl moiety; either R1 and R2, together with the N atom to which they are attached, form a 5- to 10-membered heterocyclyl group or a 5- to 10-membered heteroaryl group, or R1 represents hydrogen, C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl and R2 represents C6-C10 aryl, C1-C4 alkyl or C1-C4 hydroxyalkyl; and R3 represents a C6-C10 aryl, C3-C6 carbocyclyl, 5- to 10-membered heteroaryl or 5- to 10-membered heterocyclyl moiety, said aryl, carbocyclyl, heteroaryl and heterocyclyl groups being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxy, thiol, —NH2, C1-C4 hydroxyalkyl, C1-C4 thioalkyl and C1-C4aminoalkyl substituents.

    摘要翻译： 发现式（I）化合物在抑制黄病毒复方（I）中具有活性，其中：X表示直接键或部分-L-NR-，其中R为氢或C 1〜 -C 4烷基，L表示C 1 -C 4亚烷基，C 6 -C 3亚烷基 > 10 芳基或5至10元杂芳基部分; R 1和R 2 2与它们所连接的N原子一起形成5-至10-元杂环基或5-至10-元 杂芳基或R 1代表氢，C 6 -C 10芳基，C 1 -C 3 > 4个C 1 -C 4烷基或C 1 -C 4羟基烷基，R 2表示C 6 -C C 1 -C 10芳基，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 羟烷基 和R 3表示C 6 -C 10芳基，C 3 -C 6 - 所述芳基，碳环基，杂芳基和杂环基是未被取代的或被1,2或3个选自卤素，C 1 -C 6烷基的取代基取代的杂芳基， C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 3亚烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， 卤代烷基，C 1 -C 4卤代烷氧基，羟基，硫醇，-NH 2，C 1， C 1 -C 4 - 羟基烷基，C 1 -C 4硫代烷基和C 1 -C 3 - 4个氨基烷基取代基。

    NOVEL COMPOUNDS - 644
    5.
    发明申请
    NOVEL COMPOUNDS - 644 审中-公开
    新型化合物 - 644

    公开(公告)号：US20100215618A1

    公开(公告)日：2010-08-26

    申请号：US12710647

    申请日：2010-02-23

    申请人： Malcolm Clive Carter ,  Neil Mathews

    发明人： Malcolm Clive Carter ,  Neil Mathews

    IPC分类号： A61K38/21 ,  C07D279/12 ,  A61K31/541 ,  C07D403/12 ,  A61K31/496 ,  A61P1/16 ,  C07D417/02 ,  C07D413/02

    CPC分类号： C07D417/14 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12

    摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and L are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of hepatitis C virus.

    摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和L如说明书和光学异构体，外消旋体和互变异构体及其药学上可接受的盐所定义; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。 该化合物可用于治疗丙型肝炎病毒。

    Biphenyl Derivatives and Their Use in Treating Hepatitis C
    7.
    发明申请
    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.

    Process for the preparation of pyrazolopyridine derivatives
    8.
    发明授权
    Process for the preparation of pyrazolopyridine derivatives 失效
    吡唑并吡啶衍生物的制备方法

    公开(公告)号：US06803463B2

    公开(公告)日：2004-10-12

    申请号：US10168002

    申请日：2002-06-14

    申请人： Neil Mathews ,  Richard Anthony Ward ,  Andrew Jonathan Whitehead

    发明人： Neil Mathews ,  Richard Anthony Ward ,  Andrew Jonathan Whitehead

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  C07C317/24 ,  C07D237/08

    摘要： A process for the preparation of a compound of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4.

    摘要翻译： 一种制备式（I）化合物及其药学上可接受的衍生物的方法，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（ CH 2）n NR 4 R 5; R 1和R 2独立地选自H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1 C（O）H，C（O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基， ）nNR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（ O（CH 2）n C 1-6烷基，（CH 2）n NR 4 R 5或（CH 2）nSC 1-6烷基，C（O）NR 4 R 5; R 3， 是C 1-6烷基或NH 2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; 而且是1-4。

    2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors
    9.
    发明授权
    2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors 失效
    2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环氧合酶2（COX-2）抑制剂的用途

    公开(公告)号：US06451794B1

    公开(公告)日：2002-09-17

    申请号：US09508029

    申请日：2000-06-13

    申请人： Paul John Beswick ,  Ian Baxter Campbell ,  Neil Mathews ,  Alan Naylor

    发明人： Paul John Beswick ,  Ian Baxter Campbell ,  Neil Mathews ,  Alan Naylor

    IPC分类号： A61K314985

    CPC分类号： C07D487/04 ,  A61K31/50 ,  Y02P20/55

    摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自被一个或多个氟原子取代的H，C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基 （C 1-6烷基磺酰基），被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2） ）nSC1-6烷基，（CH2）nNR4R5或（CH2）nSC1-6烷基，C（O）NR4R5; R3是C1-6烷基或NH2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; n为1-4。 式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。