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11 条记录 (耗时 0.04 秒)

    Seco precursors of cyclopropylindolines and their use as prodrugs
    6.
    发明授权
    Seco precursors of cyclopropylindolines and their use as prodrugs 失效
    环丙基吲哚啉的山梨醇前体及其作为前药的用途

    公开(公告)号：US06251933B1

    公开(公告)日：2001-06-26

    申请号：US09319771

    申请日：1999-06-11

    申请人： William Alexander Denny ,  Moana Tercel ,  Graham John Atwell ,  Jared Milbank

    发明人： William Alexander Denny ,  Moana Tercel ,  Graham John Atwell ,  Jared Milbank

    IPC分类号： A61K31404

    CPC分类号： C07D403/12 ,  C07D209/10 ,  C07D209/12

    摘要： A compound which is a 6-substituted seco indoline of the formula (I): wherein: X is halogen or OSO2R where R represents H or C1-5 alkyl optionally substituted with from 1 to 4 hydroxyl, acid (COOH) or amino groups which amino may be optionally substituted by one or two C1-5 alkyl groups; Y is N02, N3, NHOH, NHR, NRR, N═NR, N(O)RR, SR or SSR, where R is defined as above, but that in the case where Y is SSR or N═NR, then R can also be another moiety of formula (I); or Y is a group of formula:

    摘要翻译： 化合物，其为式（I）的6-取代的仲二氢吲哚：其中：X为卤素或OSO2R，其中R为H或任选被1至4个羟基，酸（COOH）或氨基取代的C 1-5烷基， 氨基可以任选地被一个或两个C 1-5烷基取代; Y是N 2，N 3，NHOH，NHR，NRR，N = NR，N（O）RR，SR或SSR，其中R如上所定义， 在Y是SSR或N = NR的情况下，R也可以是式（I）的另一部分;或Y是下式的基团：

    Processes of preparing asymmetric dinitrobenzamide mustard compounds, intermediate compounds useful therein and products obtained therefrom
    7.
    发明申请
    Processes of preparing asymmetric dinitrobenzamide mustard compounds, intermediate compounds useful therein and products obtained therefrom 审中-公开
    制备不对称二硝基苯甲酰胺芥末化合物的方法，其中使用的中间体化合物和由其获得的产物

    公开(公告)号：US20100121091A1

    公开(公告)日：2010-05-13

    申请号：US12310484

    申请日：2007-09-04

    申请人： Graham John Atwell ,  William Alexander Denny ,  Shangjin Yang

    发明人： Graham John Atwell ,  William Alexander Denny ,  Shangjin Yang

    IPC分类号： C07C303/28 ,  C07F9/09

    CPC分类号： C07D203/10 ,  C07C227/06 ,  C07C231/12 ,  C07C303/28 ,  C07C309/66 ,  C07C309/67 ,  C07D307/20 ,  C07F9/091 ,  C07C229/56 ,  C07C233/69

    摘要： The invention relates to methods of preparing compounds of formula (II) wherein Z represents —OR1 or N(R2)R2a—, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R2a is lower alkylene (C1-C6) or H; Q is absent when R2a is H and is otherwise selected from the group consisting of H, —OH and protected forms of —OH; one of X and Y is halogen and the other is —OSO2R3, where R3 is selected from the group consisting of lower alkyl (C1-C6), phenyl and CH2phenyl. The method comprises the steps of: (a) reacting a compound of formula (I) with aziridineethanol or a 2-[(2-haloethyl)amino]ethanol in the presence of a metal halide, to form a compound of the formula (III) wherein one of X and E is halogen and the other is hydroxy, and (b) reacting the compound of formula (III) with an alkyl- or arylsulfonyl halide or alkyl- or arylsulfonyl anhydride to obtain a compound of the formula (II). The invention also relates to methods of preparing compounds of formula (IV) from the compounds of formula (II) so obtained, and to novel compounds of formula (IIb) useful as intermediates in these methods.

    摘要翻译： 本发明涉及制备式（II）化合物的方法，其中Z表示-OR1或N（R2）R2a，其中R1为低级亚烷基（C1-C6），R2为低级烷基或H，R2a为低级亚烷基 -C 6）或H; 当R 2a为H且Q选自H，-OH和-OH的保护形式时，Q不存在; X和Y之一是卤素，另一个是-OSO 2 R 3，其中R 3选自低级烷基（C 1 -C 6），苯基和CH 2苯基。 该方法包括以下步骤：（a）在金属卤化物的存在下使式（I）化合物与氮丙啶乙醇或2 - [（2-卤代乙基）氨基]乙醇反应，形成式（III）的化合物 ）其中X和E之一是卤素，另一个是羟基，和（b）使式（III）化合物与烷基 - 或芳基磺酰卤或烷基 - 或芳基磺酰基酐反应得到式（II）化合物， 。 本发明还涉及由如此获得的式（II）化合物和式（Ⅱb）化合物制备式（Ⅳ）化合物的方法，可用作这些方法中的中间体。

    Treatment of cancers
    9.
    发明授权
    Treatment of cancers 失效
    癌症治疗

    公开(公告)号：US5891886A

    公开(公告)日：1999-04-06

    申请号：US921331

    申请日：1997-08-29

    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 ,  A61K31/44 ,  C07C233/77 ,  C07D219/08

    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。

    Treatment of cancers
    10.
    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。