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    Pharmaceutical compounds
    1.
    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.

    Pharmaceutical compounds
    2.
    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.

    Pharmaceutical compounds
    3.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US06552021B2

    公开(公告)日：2003-04-22

    申请号：US09797902

    申请日：2001-03-05

    申请人： John Milton ,  Nigel Vicker ,  William Alexander Denny ,  Swarnalatha Akuratiya Gamage ,  Julie Ann Spicer

    发明人： John Milton ,  Nigel Vicker ,  William Alexander Denny ,  Swarnalatha Akuratiya Gamage ,  Julie Ann Spicer

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： A compound which is a heteroaromatic[a]phenazine carboxamide derivative of formula (I) wherein X is a five- or six-membered heteroaromatic ring which contains one or two nitrogen atoms and which is unsubstituted or substituted by C1-C6 alkyl, hydroxyl or C1-C6 alkoxy; Q is C1-C6 alkylene which is unsubstituted or substituted by C1-C6 alkyl which is unsubstituted or substituted by a hydroxy group; and R1 and R2 which are the same or different are each C1-C6 alkyl; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of topoisomerase I and II and can be used to treat tumours, including tumours which express MDR.

    摘要翻译： 一种化合物，其是式（I）的杂芳族[a]吩嗪甲酰胺衍生物，其中X是含有一个或两个氮原子且未被取代或被C 1 -C 6烷基取代的五元或六元杂芳环，羟基或 C 1 -C 6烷氧基; Q是未被取代或被未取代或被羟基取代的C1-C6烷基取代的C1-C6亚烷基; 和相同或不同的R 1和R 2各自为C 1 -C 6烷基;或其药学上可接受的盐。 这些化合物是拓扑异构酶I和II的抑制剂，可用于治疗肿瘤，包括表达MDR的肿瘤。

    HYBRIDIZATION LINKERS
    4.
    发明申请
    HYBRIDIZATION LINKERS 有权
    混合连接

    公开(公告)号：US20120064599A1

    公开(公告)日：2012-03-15

    申请号：US13147176

    申请日：2010-01-29

    申请人： Lakmal Jayasinghe ,  John Milton ,  Luke McNeill ,  James Clarke ,  James White ,  Ruth Moysey

    发明人： Lakmal Jayasinghe ,  John Milton ,  Luke McNeill ,  James Clarke ,  James White ,  Ruth Moysey

    IPC分类号： C07H21/00 ,  C09K3/00 ,  C12N9/96 ,  C07H1/00 ,  C07K14/00 ,  C07K1/107

    CPC分类号： C12N9/22 ,  C07K14/31 ,  C07K2319/03 ,  C12N9/1241 ,  C12N9/90

    摘要： The invention provides method of covalently coupling two or more moieties, the method comprising: (a) providing a first moiety having covalently attached thereto (i) at least one first linker comprising a first hybridizable region and (ii) at least one first group capable of forming a covalent bond; (b) providing a second moiety having covalently attached thereto (i) at least one second linker comprising a second hybridizable region capable of hybridizing to the first hybridizable region and (ii) at least a second group capable of forming a covalent bond with the first group; (c) contacting the first and second moieties under conditions that allow the first and second hybridizable regions to hybridize and link the moieties; and (d) exposing the linked moieties to conditions that allow the formation of a covalent bond between the first and second groups.

    摘要翻译： 本发明提供了共价偶联两个或更多个部分的方法，所述方法包括：（a）提供共价连接到其上的第一部分（i）至少一个包含第一可杂交区域的第一接头和（ii）至少一个能够 形成共价键; （b）提供共价连接到其上的第二部分（i）至少一个第二接头，其包含能够与第一可杂交区域杂交的第二可杂交区域和（ii）至少第二个能够与第一可共< 组; （c）在允许第一和第二可杂交区域杂交并连接部分的条件下使第一和第二部分接触; 和（d）将连接的部分暴露于允许在第一和第二基团之间形成共价键的条件。

    Modified nucleotides
    5.
    发明授权
    Modified nucleotides 有权
    修饰的核苷酸

    公开(公告)号：US08071739B2

    公开(公告)日：2011-12-06

    申请号：US12804352

    申请日：2010-07-20

    申请人： John Milton ,  Xiaolin Wu ,  Mark Smith ,  Joseph Brennan ,  Colin Barnes ,  Xiaohai Liu ,  Silke Ruediger

    发明人： John Milton ,  Xiaolin Wu ,  Mark Smith ,  Joseph Brennan ,  Colin Barnes ,  Xiaohai Liu ,  Silke Ruediger

    IPC分类号： C07H21/02 ,  C07H21/04 ,  C07H19/04 ,  C12Q1/68

    CPC分类号： C12Q1/6869 ,  C07H1/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C12Q2525/186 ,  C12Q2535/113 ,  Y02P20/55 ,  C12Q2525/197

    摘要： The invention provides modified nucleotide or nucleoside molecule comprising a purine or pyrimidine base and a ribose or deoxyribose sugar moiety having a removable 3′-OH blocking group covalently attached thereto, such that the 3′ carbon atom has attached a group of the structure —O—Z wherein Z is any of —C(R′)2-O—R″, —C(R′)2-N(R″)2, —C(R′)2-N(H)R″, —C(R′)2-S—R″ and —C(R′)2-F, wherein each R″ is or is part of a removable protecting group; each R′ is independently a hydrogen atom, an alkyl, substituted alkyl, arylalkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclic, acyl, cyano, alkoxy, aryloxy, heteroaryloxy or amido group, or a detectable label attached through a linking group; or (R′)2 represents an alkylidene group of formula ═C(R′″)2 wherein each R′″ may be the same or different and is selected from the group comprising hydrogen and halogen atoms and alkyl groups; and wherein said molecule may be reacted to yield an intermediate in which each R″ is exchanged for H or, where Z is —C(R′)2-F, the F is exchanged for OH, SH or NH2, preferably OH, which intermediate dissociates under aqueous conditions to afford a molecule with a free 3′OH; with the proviso that where Z is —C(R′)2-S—R″, both R′ groups are not H.

    摘要翻译： 本发明提供了修饰的核苷酸或核苷分子，其包含嘌呤或嘧啶碱基和核糖或脱氧核糖糖部分，其具有共价连接到其上的可移除的3'-OH封闭基团，使得3'碳原子连接一组结构-O -Z其中Z是-C（R'）2 -O-R“，-C（R'）2 -N（R”）2，-C（R'）2 -N（H）R“ -C（R'）2 -S-R“和-C（R'）2 -F，其中每个R”为或可移除的保护基团的一部分; 每个R'独立地是氢原子，烷基，取代的烷基，芳基烷基，烯基，炔基，芳基，杂芳基，杂环，酰基，氰基，烷氧基，芳氧基，杂芳氧基或酰氨基，或通过连接基团连接的可检测标记; 或（R'）2表示式≡C（R'“）2的亚烷基，其中每个R”可以相同或不同，并且选自氢和卤素原子和烷基; 并且其中所述分子可以反应以产生其中每个R“被交换为H的中间体，或其中Z是-C（R'）2 -F，F被交换成OH，SH或NH 2，优选OH，其中 中间体在水性条件下解离得到具有游离3'OH的分子; 条件是其中Z是-C（R'）2 -S-R“，两个R'基团不是H.