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42 条记录 (耗时 0.038 秒)

    Pharmaceutical compounds
    32.
    发明授权
    Pharmaceutical compounds 失效

    公开(公告)号：US07132419B2

    公开(公告)日：2006-11-07

    申请号：US11024759

    申请日：2004-12-30

    申请人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Alexander Denny

    发明人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Alexander Denny

    IPC分类号： C07D241/46 ,  A61K31/498

    CPC分类号： C07D403/12 ,  C07D241/46

    摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; R11 is C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1–C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

    Labelled nucleotides
    33.
    发明申请
    Labelled nucleotides 有权
    标记核苷酸

    公开(公告)号：US20060160081A1

    公开(公告)日：2006-07-20

    申请号：US10525399

    申请日：2003-08-22

    申请人： John Milton ,  Silke Ruediger ,  Xiaohai Liu

    发明人： John Milton ,  Silke Ruediger ,  Xiaohai Liu

    IPC分类号： C12Q1/68 ,  C12N9/22 ,  C07H21/04

    CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6869 ,  C12Q1/6874 ,  Y10T436/143333 ,  C12Q2535/113 ,  C12Q2525/186

    摘要： The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl), T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

    摘要翻译： 本发明提供了具有通过可切割接头连接到可检测标记的碱基的核苷酸或核苷，其特征在于可切割连接体含有选自以下的部分：式（I）其中X选自O，S ，NH和NQ，其中Q是C 1-10取代或未取代的烷基，Y选自O，S，NH和N（烯丙基），T是氢或C < 取代或未取代的烷基，*表示部分与核苷酸或核苷的剩余部分连接的位置）。

    Pharmaceutical compounds
    34.
    发明申请
    Pharmaceutical compounds 失效

    公开(公告)号：US20050143383A1

    公开(公告)日：2005-06-30

    申请号：US11024759

    申请日：2004-12-30

    申请人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Denny

    发明人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Denny

    IPC分类号： C07D241/46 ,  C07D403/12 ,  A61K31/498 ,  C07D241/36

    CPC分类号： C07D403/12 ,  C07D241/46

    摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R2)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (II) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; R11 is C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1-C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

    Labelled nucleotides
    37.
    发明授权
    Labelled nucleotides 有权
    标记核苷酸

    公开(公告)号：US08084590B2

    公开(公告)日：2011-12-27

    申请号：US12803163

    申请日：2010-06-21

    申请人： John Milton ,  Silke Ruediger ,  Xiaohai Liu

    发明人： John Milton ,  Silke Ruediger ,  Xiaohai Liu

    IPC分类号： C07G11/00 ,  C07H21/04 ,  C07H19/04 ,  C12Q1/68

    CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6869 ,  C12Q1/6874 ,  Y10T436/143333 ,  C12Q2535/113 ,  C12Q2525/186

    摘要： The invention provides a nucleotide or nucleoside having a base attached to a detectable label via a cleavable linker, characterised in that the cleavable linker contains a moiety selected from the group comprising: Formula (I) (wherein X is selected from the group comprising O, S, NH and NQ wherein Q is a C1-10 substituted or unsubstituted alkyl group, Y is selected from the group comprising O, S, NH and N(allyl). T is hydrogen or a C1-10 substituted or unsubstituted alkyl group and * indicates where the moiety is connected to the remainder of the nucleotide or nucleoside).

    摘要翻译： 本发明提供了具有通过可切割接头连接到可检测标记的碱基的核苷酸或核苷，其特征在于所述可切割连接体含有选自以下的部分：式（I）（其中X选自O， S，NH和NQ，其中Q是C1-10取代或未取代的烷基，Y选自O，S，NH和N（烯丙基），T是氢或C1-10取代或未取代的烷基， *表示部分连接到核苷酸或核苷的剩余部分）。

    MODIFIED NUCLEOSIDES AND NUCLEOTIDES AND USES THEREOF
    39.
    发明申请
    MODIFIED NUCLEOSIDES AND NUCLEOTIDES AND USES THEREOF 有权
    改良的核苷酸和核苷酸及其用途

    公开(公告)号：US20110020827A1

    公开(公告)日：2011-01-27

    申请号：US12899423

    申请日：2010-10-06

    申请人： John Milton ,  Xiaohai Liu

    发明人： John Milton ,  Xiaohai Liu

    IPC分类号： C12Q1/68 ,  C07H19/14 ,  C07H19/20 ,  C07D311/88

    CPC分类号： C12Q1/686 ,  C12Q2525/113

    摘要： The invention is directed to modified guanine-containing nucleosides and nucleotides and uses thereof. More specifically, the invention relates to modified fluorescently labelled guanine-containing nucleosides and nucleotides which exhibit enhanced fluorophore intensity by virtue of reduced quenching effects.

    摘要翻译： 本发明涉及修饰的含鸟嘌呤核苷及其用途。 更具体地，本发明涉及经修饰的荧光标记的含有鸟嘌呤的核苷和核苷酸，其通过降低猝灭效应表现出增强的荧光团强度。