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    METHOD FOR TREATING HEPATITIS C VIRUS INFECTION IN TREATMENT FAILURE PATIENTS
    3.
    发明申请
    METHOD FOR TREATING HEPATITIS C VIRUS INFECTION IN TREATMENT FAILURE PATIENTS 审中-公开
    治疗失败病人中丙型肝炎病毒感染的方法

    公开(公告)号：US20080213218A1

    公开(公告)日：2008-09-04

    申请号：US12034542

    申请日：2008-02-20

    申请人： Henry H. Hsu

    发明人： Henry H. Hsu

    IPC分类号： A61K38/21 ,  A61P31/14

    CPC分类号： A61K31/7056 ,  A61K38/212 ,  A61K2300/00

    摘要： The present invention provides methods for treating individuals having a hepatitis C virus (HCV) infection, which individuals have failed to respond to therapy with an IFN-α other than consensus interferon (CIFN), or who, following cessation of therapy with an IFN-α other than CIFN, have suffered relaspe. The methods generally involve a treatment regimen comprising administering a first dosing regimen of CIFN, followed by a second dosing regimen of CIFN. Ribavirin is administered with at least the second dosing regimen.

    摘要翻译： 本发明提供了用于治疗患有丙型肝炎病毒（HCV）感染的个体的方法，该个体对用IFN-α治疗而不是针对复合干扰素（CIFN）的治疗反应，或者在用IFN- 除了CIFN之外的alpha，已经遭受了重复。 所述方法通常涉及治疗方案，其包括施用CIFN的第一给药方案，接着是CIFN的第二给药方案。 利巴韦林至少给予第二次给药方案。

    Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators
    5.
    发明授权
    Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators 有权
    4-（N-氮杂环烷基）苯胺的衍生物作为钾通道调节剂

    公开(公告)号：US08367684B2

    公开(公告)日：2013-02-05

    申请号：US12138251

    申请日：2008-06-12

    申请人： Jean-Michel Vernier ,  Samedy Ouk ,  Martha A. De La Rosa

    发明人： Jean-Michel Vernier ,  Samedy Ouk ,  Martha A. De La Rosa

    IPC分类号： A01N43/54 ,  A61K31/505

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

    摘要： This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.

    摘要翻译： 本发明提供钾通道调节剂，其为W和Z中至少一个为N的式I化合物; 其中该部分是A之下的A或B族之一，其中Ar是1,2-稠合的六元环芳族基团，带有如下定义的取代基R 1和R 2，并且含有一个或多个环氮原子; 并且其中其它取代基在本文中定义。 本发明还提供包含药学上可接受的载体和至少一种以下的组合物：i）药学有效量的式I化合物和ii）其药学上可接受的盐，酯或前药。 本发明还提供了预防或治疗受钾通道活性影响的疾病或病症的方法，包括向有需要的患者施用治疗有效量的式I化合物或其盐，酯或前药 。

    3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
    7.
    发明授权
    3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors 有权
    3-羟基异噻唑-4-甲脒衍生物作为CHK2抑制剂

    公开(公告)号：US08067452B2

    公开(公告)日：2011-11-29

    申请号：US12143672

    申请日：2008-06-20

    申请人： Jim Zhen Wu ,  Huanming Chen

    发明人： Jim Zhen Wu ,  Huanming Chen

    IPC分类号： A61K31/425 ,  C07D275/03

    CPC分类号： C07D275/03

    摘要： This invention provides compounds of Formula I which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to the isothiocyanate group to form a thioamide adduct; d) cyclizing the thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to the cyano group to form a carboxamidine group.

    摘要翻译： 本发明提供了作为Chk2抑制剂的式I化合物，可用作抗癌放射治疗中的放射防护剂。 在体外调节Chk2的方法包括在式I化合物存在下用Chk2处理底物。制备式I化合物的方法包括：a）形成具有氨基（NH 2）基团的联芳基胺; b）将氨基转化为异硫氰酸酯基团; c）将氰基乙酰胺加入到异硫氰酸酯基中以形成硫代酰胺加合物; d）使硫代酰胺加合物环化以形成具有氰基的异噻唑; 和e）向氰基中加入胺形成甲脒基团。

    MODIFIED RELEASE FORMULATION AND METHODS OF USE
    8.
    发明申请
    MODIFIED RELEASE FORMULATION AND METHODS OF USE 审中-公开
    改性释放配方及使用方法

    公开(公告)号：US20100120906A1

    公开(公告)日：2010-05-13

    申请号：US12505409

    申请日：2009-07-17

    申请人： Biljana Nadjsombati

    发明人： Biljana Nadjsombati

    IPC分类号： A61K31/27 ,  A61P25/08

    CPC分类号： A61K31/44 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054

    摘要： A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant, and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. A formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours. A method of treating a disorder characterized by nervous system hyperexcitability includes administering to a subject an effective amount of these pharmaceutical formulations.

    摘要翻译： 一种改性释放药物制剂包括约30-70％的N-（2-氨基-4-（氟苄基氨基） - 苯基）氨基甲酸乙酯（瑞替加滨）或其药学上可接受的盐，溶剂合物或水合物，约5-30％ 的药物递送基质，包括羟丙基甲基纤维素（HPMC），约1.0-10％的阴离子表面活性剂和肠溶性聚合物。 给予受试者后，药物制剂产生持续的血浆浓度，持续4-20小时比体外释放80％瑞替加滨所需的时间长。 制剂包括约30-70％的N-（2-氨基-4-（氟苄基氨基） - 苯基）氨基甲酸乙酯（瑞替加）或其药学上可接受的盐，溶剂合物或水合物，约5-30％的药物 递送基质和用于在胃环境中缓释释放的药剂。 该制剂的血浆浓度对时间曲线在持续约4小时至约36小时的延长时间内基本平坦。 治疗以神经系统兴奋性为特征的疾病的方法包括向受试者施用有效量的这些药物制剂。