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11 条记录 (耗时 0.036 秒)

    Processes of preparing asymmetric dinitrobenzamide mustard compounds, intermediate compounds useful therein and products obtained therefrom
    5.
    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
    8.
    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
    9.
    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。

    Processes for preparing 3-substituted 1-(chloromethyl)-1,2-dihydro-3H-[ring fused indol-5-yl-(amine-derived)] compounds and analogues thereof, and to products obtained therefrom
    10.
    发明授权
    Processes for preparing 3-substituted 1-(chloromethyl)-1,2-dihydro-3H-[ring fused indol-5-yl-(amine-derived)] compounds and analogues thereof, and to products obtained therefrom 失效
    制备3-取代的1-（氯甲基）-1,2-二氢-3H- [环稠合吲哚-5-基 - （胺衍生的）]化合物及其类似物的方法，以及由此得到的产物

    公开(公告)号：US07235578B2

    公开(公告)日：2007-06-26

    申请号：US10514893

    申请日：2003-05-19

    申请人： William Alexander Denny ,  Shanjin Yang ,  Graham John Atwell ,  Scott Charles Jeffrey

    发明人： William Alexander Denny ,  Shanjin Yang ,  Graham John Atwell ,  Scott Charles Jeffrey

    IPC分类号： A61K31/403 ,  C07D209/60

    CPC分类号： C07D401/06 ,  A61K31/404 ,  C07D209/60 ,  C07D487/04 ,  Y02A50/473

    摘要： The invention provides processes of preparing 3-substituted 1-(chloromethyl)- 1,2-dihydro-3H-[ring fused indol-5-yl(amine-derived)] compounds of formula (I) and its analogues, or a physiologically functional derivative thereof, (I), wherein A and B together may represent a fused optionally substituted benezene, naphthalene, pyridine, furan or a pyrrole ring, where the optional substituents are represented by Y; X is halogen or OSO2R, and W is selected from NO2, NHOH, N(R3)2NHR3, NHCO2R3, N(phthaloyl) or NH2, or W is further selected from the group (a), wherein J is selected from OH or H, and P is a group which is a substrate suitable for a nitroreductase or carboxypeptidase enzyme. The invention is also directed to the use of compounds of formula (I) prepared by the processes of the invention as cytotoxins for cancer therapy and as prodrugs for gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug theraphy (ADEPT).

    摘要翻译： 本发明提供制备式（I）及其类似物的3-取代的1-（氯甲基）-1,2-二氢-3H- [环稠合的吲哚-5-基（胺衍生的） 其中A和B一起可以表示稠合的任选取代的茚，萘，吡啶，呋喃或吡咯环，其中任选的取代基由Y表示; X是卤素或OSO 2 R，W选自NO 2，NHOH，N（R 3）2， NH 3，NH 3，N 3，N（邻苯二甲酰基）或NH 2，或W进一步 选自组（a），其中J选自OH或H，P是适合于硝基还原酶或羧肽酶的底物。 本发明还涉及通过本发明的方法制备的式（I）化合物作为细胞毒素用于癌症治疗和用作基因定向酶前药治疗（GDEPT）和抗体指导的酶 - 前药治疗（ ADEPT）。