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19 条记录 (耗时 0.034 秒)

    Novel 1,2,4-benzotriazine-1,4-dioxides
    1.
    发明申请
    Novel 1,2,4-benzotriazine-1,4-dioxides 有权
    新的1,2,4-苯并三嗪-1,4-二氧化物

    公开(公告)号：US20070197534A1

    公开(公告)日：2007-08-23

    申请号：US10590796

    申请日：2005-03-01

    申请人： William Denny ,  Michael Hay ,  Kevin Hicks ,  Frederik Pruijn ,  William Wilson ,  Karin Pchalek

    发明人： William Denny ,  Michael Hay ,  Kevin Hicks ,  Frederik Pruijn ,  William Wilson ,  Karin Pchalek

    IPC分类号： C07D253/08 ,  A61K31/28 ,  A61K31/53

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

    摘要： The present invention provides a simplified set of characteristics that can be used to select 1,2,4 benzotriazine 1,4 dioxide compounds (TPZ analogues) with therapeutic activity against hypoxic cells in human tumour xenografts, and to further provide a novel class of 1,2,4-benzotriazine-1,4-dioxides (TPZ analogues) with predicted in vivo activity against tumours, to their preparation, and to their use as hypoxia-selective cytotoxic drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.

    摘要翻译： 本发明提供了可用于选择具有对人类肿瘤异种移植物中的缺氧细胞具有治疗活性的1,2,4苯并三嗪二氧化物化合物（TPZ类似物）的简化特征集，并进一步提供新的1类 ，具有预测的针对肿瘤的体内活性的2,4-苯并三嗪-1,4-二氧化物（TPZ类似物），其制备及其作为用于癌症治疗的缺氧选择性细胞毒性药物和放射增敏剂的用途，单独或与 辐射和/或其他抗癌药物。

    Quinoline derivatives for modulating DNA methylation
    6.
    发明授权
    Quinoline derivatives for modulating DNA methylation 失效
    用于调节DNA甲基化的喹啉衍生物

    公开(公告)号：US07939546B2

    公开(公告)日：2011-05-10

    申请号：US12422067

    申请日：2009-04-10

    申请人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Yong Xu ,  Krzysztof Swierczek

    发明人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Yong Xu ,  Krzysztof Swierczek

    IPC分类号： A61K31/47

    CPC分类号： C07D401/12

    摘要： Quinoline derivatives, particularly 4-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine-2-carboxylic acid; 3-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine; N-(4-(piperidin-4-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide; and N-(4-(piperidin-3-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide, or a physiologically acceptable salt thereof, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

    摘要翻译： 喹啉衍生物，特别是4-（4-（4-（喹啉-4-基氨基）苯甲酰氨基）苯硫基）吡咯烷-2-甲酸; 3-（4-（4-（喹啉-4-基氨基）苯甲酰氨基）苯硫基）吡咯烷; N-（4-（哌啶-4-基硫基）苯基）-4-（喹啉-4-基氨基） - 苯甲酰胺; 和N-（4-（哌啶-3-基硫基）苯基）-4-（喹啉-4-基氨基） - 苯甲酰胺或其生理上可接受的盐。 这样的喹啉衍生物可用于DNA甲基化的调节，例如通过选择性抑制DNA甲基转移酶DNMT1有效抑制C-5位上胞嘧啶的甲基化。 提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。

    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
    7.
    发明申请
    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，以及由其获得的产物

    公开(公告)号：US20050148651A1

    公开(公告)日：2005-07-07

    申请号：US10514893

    申请日：2003-05-19

    申请人： William Denny ,  Auckland Yang ,  Graham Atwell ,  Scott Jeffrey

    发明人： William Denny ,  Auckland Yang ,  Graham Atwell ,  Scott Jeffrey

    IPC分类号： A61K31/404 ,  A61P35/00 ,  C07D209/60 ,  C07D401/06 ,  C07D487/04 ,  A61K31/403 ,  A61K31/405 ,  C07D43/02

    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 R, 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 therapy (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 选自基团（a），其中J选自OH或R，并且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）和抗体定向酶前药治疗（GDEPT）的前药的用途 ADEPT）。

    Quinoline derivatives for modulating DNA methylation
    10.
    发明授权
    Quinoline derivatives for modulating DNA methylation 失效
    用于调节DNA甲基化的喹啉衍生物

    公开(公告)号：US07790746B2

    公开(公告)日：2010-09-07

    申请号：US11959181

    申请日：2007-12-18

    申请人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati

    发明人： Pasit Phiasivongsa ,  Sanjeev G. Redkar ,  Swarna Gamage ,  Darby Brooke ,  William Denny ,  David J. Bearss ,  Hariprasad Vankayalapati

    IPC分类号： A61K31/47

    CPC分类号： C07D401/12

    摘要： Quinoline derivatives, particularly 4-anilinoquinoline derivatives of formula (I), are provided: Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT 1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

    摘要翻译： 提供了喹啉衍生物，特别是式（I）的4-苯胺基喹啉衍生物：这样的喹啉衍生物可用于DNA甲基化的调节，例如有效抑制胞嘧啶在C-5位甲基化，例如通过选择性抑制 DNA甲基转移酶DNMT 1.提供了合成大量4-苯胺基喹啉衍生物和调节DNA甲基化的方法。 还提供了用于配制和施用这些化合物或组合物以治疗诸如癌症和血液学疾病的病症的方法。