首页> 外国专利> PREPARATION OF ESTER BODY OF PAK1 BLOCKER BECOMING TO BE ACIDIC BY CARBOXYL GROUP AND APPLICATION TO TREATMENT OF CANCER OR OTHER PAK1 DEPENDENT DISEASES

PREPARATION OF ESTER BODY OF PAK1 BLOCKER BECOMING TO BE ACIDIC BY CARBOXYL GROUP AND APPLICATION TO TREATMENT OF CANCER OR OTHER PAK1 DEPENDENT DISEASES

机译:被羧基酸性化的PAK1受体阻滞剂的制备及其在治疗癌症或其他PAK1相关疾病中的应用

摘要

PROBLEM TO BE SOLVED: To provide a series of novel PAK1 blockers which is beneficial for treatments of a series of PAK1 dependent disease such as cancer resistant to i.e. chemotherapeutic (chemo) mainly including DNA toxin or microtubule toxin or radiotherapy or the like, is high in cell permeability and water soluble.;SOLUTION: There are provided a compound having 1,2,3-triazole ring represented by the formula (1), a pharmaceutically acceptable salt of the compound, a pharmaceutical containing them, a PAK1 blocker, a treatment agent for PAK1 dependent diseases, a resistance reduction agent of cancer cells by chemotherapy or radiotherapy, an agent for preventing grow or metastasis of cancer cells, a resistance reduction agent by chemotherapy of PAK1 dependent diseases and a cosmetic. In the formula (1), R1 is decarboxylated body derived from the PAK1 blocker becoming to be acidic by a carboxyl group and R2 is an aromatic ring derivative.;SELECTED DRAWING: None;COPYRIGHT: (C)2017,JPO&INPIT
机译:要解决的问题:提供一系列新颖的PAK1阻滞剂,对于治疗一系列PAK1依赖性疾病(例如对包括DNA毒素或微管毒素或放射疗法等在内的化学疗法(化学疗法)具有抗性的癌症)具有抵抗力的疾病是有益的解决方案:提供具有式(1)表示的具有1,2,3-三唑环的化合物,该化合物的药学上可接受的盐,包含它们的药物,PAK1阻断剂, PAK1依赖性疾病的治疗剂,通过化学疗法或放射疗法的癌细胞抗性降低剂,用于预防癌细胞生长或转移的药物,通过PAK1依赖性疾病的化学疗法的抗性降低剂和化妆品。式(1)中,R 1 为衍生自PAK1阻滞剂的被羧基变为酸性的脱羧体,R 2 为芳香族环衍生物。绘图:无;版权:(C)2017,JPO&INPIT

著录项

  • 公开/公告号JP2017165677A

    专利类型

  • 公开/公告日2017-09-21

    原文格式PDF

  • 申请/专利权人 MARUTA HIROSHI;

    申请/专利号JP20160052369

  • 申请日2016-03-16

  • 分类号C07D249/06;A61K31/4192;A61P43/00;A61P35/00;A61P25/28;A61P25/16;A61P25/08;A61P29/00;A61P31/04;A61P3/10;A61P9/12;A61P3/04;A61P25/24;A61P25/18;A61P25/06;A61P19/10;A61P35/04;C07D403/12;C07D471/04;C07D487/04;A61K38/00;A61K8/49;A61Q19/04;A61Q5/12;C07K5/08;

  • 国家 JP

  • 入库时间 2022-08-21 14:01:40

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