首页> 外国专利> BISTHIO-HYDRAZIDE AMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USES THEREOF FOR THE MANUFACTURE OF MEDICAMENTS TO ENHANCE THE ANTI-CANCER ACTIVITY OF PACLITAXEL OR OF A PACLITAXEL ANALOG

BISTHIO-HYDRAZIDE AMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USES THEREOF FOR THE MANUFACTURE OF MEDICAMENTS TO ENHANCE THE ANTI-CANCER ACTIVITY OF PACLITAXEL OR OF A PACLITAXEL ANALOG

机译:双[噻吩酰胺]衍生物,包含它们的药物组合物及其用途,用于制造药物以增强Paclitaxel或Paclitaxel类似物的抗癌活性

摘要

Disclosed is a compound represented by the Structural Formula (1); Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group In addition, Y, taken together with both C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 and R 2 are independently an aryl group or a substituted aryl group, R 3 and R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =O or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceplable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
机译:公开了由结构式(1)表示的化合物; Y是共价键,亚苯基或取代或未取代的直链烃基。另外,Y与与其键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选地,Y是共价键或-C(R 7 R 8)-。 R 1和R 2独立地为芳基或取代的芳基,R 3和R 4独立地为-H,脂族基,取代脂族基,芳基或取代芳基。 R 5 -R 6独立地为-H,脂族基,取代的脂族基,芳基或取代的芳基。 R 7和R 8各自独立地为-H,脂族或取代的脂族基团,或R 7为-H,R 8为取代或未取代的芳基,或者R 7和R 8一起为C2- C6取代或未取代的亚烷基。 Z为= O或= S。还公开了包含本发明的化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了一种通过将结构式(I)的化合物与紫杉酚或紫杉醇的类似物组合给予受试者来治疗癌症的方法。

著录项

  • 公开/公告号IL159773B

    专利类型

  • 公开/公告日2011-11-30

    原文格式PDF

  • 申请/专利权人 SYNTA PHARMACEUTICALS CORP.;

    申请/专利号IL159773

  • 发明设计人

    申请日2004-01-08

  • 分类号A61K;A61K31/165;A61K31/175;A61K31/275;A61K31/337;A61K31/34;A61K31/341;A61K31/381;A61K31/404;A61K31/42;A61K31/4406;A61K31/5377;A61K31/661;A61P;A61P35;A61P43;C07C;C07C327/56;C07D209/42;C07D209/44;C07D213/82;C07D213/83;C07D261/18;C07D305/14;C07D307/68;C07D333/38;C07D333/68;C07D333/70;C07D407/12;

  • 国家 IL

  • 入库时间 2022-08-21 17:24:52

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