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    Quinoline derivatives for modulating DNA methylation
    1.
    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。

    Salts of 5-azacytidine
    4.
    发明申请
    Salts of 5-azacytidine 审中-公开
    5-氮杂胞苷的盐

    公开(公告)号：US20060063735A1

    公开(公告)日：2006-03-23

    申请号：US10944460

    申请日：2004-09-17

    申请人： Sanjeev Redkar ,  Pasit Phiasivongsa

    发明人： Sanjeev Redkar ,  Pasit Phiasivongsa

    IPC分类号： C07H19/12 ,  A61K31/7072

    CPC分类号： C07H19/12

    摘要： The present invention relates to salts of 5-azacytidine as well as methods for synthesizing the salts described herein. Pharmaceutical compositions and methods of using the 5-azacytidine salts are also provided, including methods of administering the salts or pharmaceutical compositions thereof to treat conditions, such as cancer and hematological disorders.

    摘要翻译： 本发明涉及5-氮杂胞苷的盐以及本文所述盐的合成方法。 还提供了使用5-氮杂胞苷盐的药物组合物和方法，包括给予其盐或其药物组合物以治疗诸如癌症和血液病症的病症的方法。

    Methods for administration of paclitaxel
    6.
    发明申请
    Methods for administration of paclitaxel 失效
    紫杉醇的给药方法

    公开(公告)号：US20030191179A1

    公开(公告)日：2003-10-09

    申请号：US10351262

    申请日：2003-01-23

    申请人： SuperGen, Inc.

    发明人： Rajashree Joshi-Hangal ,  Howard Sands ,  Joseph Rubinfeld

    IPC分类号： A61K031/337 ,  A61K031/355

    CPC分类号： B82Y5/00 ,  A61K9/1075 ,  A61K9/4858 ,  A61K31/337 ,  A61K47/6951

    摘要： Methods are provided for using paclitaxel for treating diseases associated with abnormal cell proliferation and angiogenesis. In particular, methods are provided for administration of paclitaxel formulated with vitamin E derivatives such as d-null-tocopherol polyethylene glycol succinate to a cancer patient. By administering to a patient paclitaxel in a vehicle containing a solubilizer other than Cremophor, acute hypersensitivity caused by Cremophor can be avoided and therapeutic index of paclitaxel may also be increased through potentiation of anti-neoplastic effects by the vitamin E derivatives.

    摘要翻译： 提供使用紫杉醇治疗与异常细胞增殖和血管发生相关的疾病的方法。 特别地，提供了向维生素E衍生物（例如d-α-生育酚聚乙二醇琥珀酸酯）配制的紫杉醇给予癌症患者的方法。 通过对含有Cremophor以外的增溶剂的载体的患者紫杉醇进行给药，可以避免由Cremophor引起的急性超敏反应，并且也可以通过增强维生素E衍生物的抗肿瘤作用来增加紫杉醇的治疗指数。

    Formulation for administration of steroid compounds
    8.
    发明授权
    Formulation for administration of steroid compounds 失效
    类固醇化合物的给药配方

    公开(公告)号：US5824668A

    公开(公告)日：1998-10-20

    申请号：US744979

    申请日：1996-11-07

    申请人： Joseph Rubinfeld ,  Julius A. Vida ,  H. Leon Bradlow ,  Elliott L. Fineman

    发明人： Joseph Rubinfeld ,  Julius A. Vida ,  H. Leon Bradlow ,  Elliott L. Fineman

    IPC分类号： A61K9/00 ,  A61K31/565 ,  A61K47/40 ,  A61K47/48 ,  A61K31/56

    CPC分类号： A61K31/5685 ,  A61K31/565 ,  A61K47/40 ,  A61K47/48969 ,  A61K9/0019 ,  B82Y5/00 ,  Y10S514/814 ,  Y10S514/866 ,  Y10S514/909

    摘要： Disclosed are compositions including at least one 5.beta. steroid and an amorphous cyclodextrin. Also disclosed are methods for treating a condition such as obesity, diabetes syndrome, diabetes-associated hypercorticoidism, combinations thereof, and anemic disorders by administering to a mammal in need of such treatment a composition including an obesity-, diabetes-, or anemia antagonistic amount of at least one 5.beta. steroid and an amorphous cyclodextrin. Furthermore, disclosed are methods for treating a subject for a condition that responds to treatment with DHEA by administering to the subject at least one 5.beta. steroid and DHEA in an amount that minimizes the contribution of the DHEA to the production of testosterone and estradiol while maximizing an amount of .alpha.ET and .beta.ET circulating in the subject's blood from an initial dose administered to the subject.

    摘要翻译： 公开了包含至少一种5β类固醇和无定形环糊精的组合物。 还公开了通过向需要这种治疗的哺乳动物施用包括肥胖症，糖尿病或贫血拮抗剂量的组合物来治疗诸如肥胖症，糖尿病综合征，糖尿病相关性高糖皮质激素，其组合和贫血性疾病的病症的方法 的至少一种5β类固醇和无定形环糊精。 此外，所公开的方法是用于通过向受试者施用至少一种5β类固醇和DHEA以使DHEA对产生睾酮和雌二醇的贡献最小化的量给予受试者来治疗受试者的病症。 从受试者的初始剂量中流出的受试者血液中的αET和βET的量。