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62 条记录 (耗时 0.052 秒)

    Treatment of cancers
    21.
    发明授权
    Treatment of cancers 失效
    癌症治疗

    公开(公告)号：US5696131A

    公开(公告)日：1997-12-09

    申请号：US387565

    申请日：1995-02-13

    申请人： Bruce Charles Baguley ,  Graham John Atwell ,  William Alexander Denny ,  Graeme John Finlay ,  Gordon William Rewcastle

    发明人： Bruce Charles Baguley ,  Graham John Atwell ,  William Alexander Denny ,  Graeme John Finlay ,  Gordon William Rewcastle

    IPC分类号： A61K31/473 ,  A61K31/165

    CPC分类号： A61K31/00 ,  A61K31/473

    摘要： A new treatment schedule for administration of N-�2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.

    摘要翻译： 用于施用N- [2-（二甲基氨基）乙基]吖啶-4-甲酰胺和其它相关的羧酰胺抗癌药物的新的治疗方案，其中药物以分次给药方案施用，其包含频繁间隔的两次或更多次给药，用于 例如每小时。 提及产生血浆水平的循环峰/谷的时间表。 该化合物可用于规避癌症中的多药耐药性，并且可以例如与其它细胞毒性药物，特别是非地头性II抑制剂组合使用。 包括黑色素瘤和晚期结肠癌的治疗。

    1,2,4-benzotriazine-1,4-dioxides
    22.
    发明授权
    1,2,4-benzotriazine-1,4-dioxides 有权
    1,2,4-苯并三嗪-1,4-二氧化物

    公开(公告)号：US07816521B2

    公开(公告)日：2010-10-19

    申请号：US10590796

    申请日：2005-03-01

    申请人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    发明人： William Alexander Denny ,  Michael Patrick Hay ,  Kevin Owen Hicks ,  Frederik Pruijn ,  William Robert Wilson ,  Karin Pchalek

    IPC分类号： C07D253/10 ,  C07D413/12 ,  A61K31/53 ,  A61P35/00

    CPC分类号： C07D253/10 ,  C07D253/08 ,  C07D401/12

    摘要： The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.

    摘要翻译： 化合物3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物及其药理学上可接受的盐。 还描述了在受试者中治疗癌症的方法，其中给予3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药理学上可接受的盐 到缺氧环境中的肿瘤细胞。 还描述了通过向受试者施用含有3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-恶二唑的药物组合物，在缺氧条件下的实体瘤的受试肿瘤细胞中放射增敏的方法， 苯并三嗪1,4-二氧化物或其药理学上可接受的盐，其量足以在肿瘤细胞中产生放射敏感性，并对肿瘤细胞进行辐射。 另外提供含有治疗有效量的3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药学上可接受的盐和药学上可接受的盐的药物组合物 可接受的赋形剂，佐剂，载体，缓冲液或稳定剂。

    Nitroaniline derivatives and their use as anti-tumour agents
    24.
    发明授权
    Nitroaniline derivatives and their use as anti-tumour agents 失效
    硝基苯胺衍生物及其作为抗肿瘤剂的用途

    公开(公告)号：US5750782A

    公开(公告)日：1998-05-12

    申请号：US685079

    申请日：1996-07-23

    申请人： William Alexander Denny ,  Brian Desmond Palmer ,  William Robert Wilson

    发明人： William Alexander Denny ,  Brian Desmond Palmer ,  William Robert Wilson

    IPC分类号： C07C237/34 ,  C07C233/65

    CPC分类号： C07C237/34

    摘要： The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##

    摘要翻译： 本发明提供了通式（1）表示的硝基苯胺衍生物，其中硝基在任何一个可用苯位置2-6取代; 其中R和A分别代表基团NO2，CN，COOR1，CONR1R2，CSNR1R2或SO2NR1R2，A在任何一​​个可用的苯位置2-6取代; 其中B表示在任何一个可用苯位置取代的N（CH 2 CH 2卤素）2或N（CH 2 CH 2 OSO 2 R 3）2） 并且其中R 1，R 2和R 3分别代表H，或任选被羟基，醚，羧基或氨基官能团取代的低级烷基，包括环状结构，或者R 1和R 2与氮一起形成杂环结构，以及含有它们的药物制剂。 这些化合物具有作为缺氧选择性细胞毒素，用于细胞毒素的还原活化前药，缺氧细胞放射增敏剂和抗癌剂的活性。

    Pharmaceutical compounds
    28.
    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。