首页> 外国专利> New substituted 3-biphenyl-3-yl-8,8-difluoro-4-hydroxy-1-azaspiro(4.5)dec-3-en-2-one derivatives useful for prophylaxis or therapy of tumor diseases comprising breast cancer, prostate cancer, colorectal cancer or non-small cell lung cancer

New substituted 3-biphenyl-3-yl-8,8-difluoro-4-hydroxy-1-azaspiro(4.5)dec-3-en-2-one derivatives useful for prophylaxis or therapy of tumor diseases comprising breast cancer, prostate cancer, colorectal cancer or non-small cell lung cancer

机译:用于预防或治疗包括乳腺癌,前列腺癌在内的肿瘤疾病的新型取代的3-biphenyl-3-yl-8,8-difluoro-4-hydroxy-1-azaspiro(4.5)dec-3-en-2-one衍生物,结直肠癌或非小细胞肺癌

摘要

Substituted 3-biphenyl-3-yl-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-one derivatives (I) are new. Substituted 3-biphenyl-3-yl-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-one derivatives of formula (I) and their salts are new. R1 : CH 3or Cl; R2 : H or CH 3; R3 : H or F; and R4 : Cl or F. ACTIVITY : Cytostatic; Herbicide; Fungicide. MECHANISM OF ACTION : Acetyl-CoA carboxylase 1 inhibitor. The ability of (I) to inhibit the acetyl-CoA carboxylase 1 was tested using in-vitro enzyme assay. The result showed that 3-(4'-chloro-3'-fluoro-4-methylbiphenyl-3-yl)-8,8-difluoro-4-hydroxy-l-azaspiro[4.5]dec-3-en-2-one exhibited an IC50 value of 0.053 mu mol/l.
机译:取代的3-联苯基-3-基-8,8-二氟-4-羟基-1-氮杂螺[4.5] dec-3-en-2-one衍生物(I)是新的。式(I)的取代的3-联苯基-3-基-8,8-二氟-4-羟基-1-氮杂[4.5] dec-3-en-2-one衍生物及其盐是新的。 R1:CH 3或Cl; R 2:H或CH 3; R3:H或F;活性:细胞抑制性;和R4:Cl或F。除草剂;杀菌剂。作用机理:乙酰辅酶A羧化酶1抑制剂。使用体外酶测定法测试(I)抑制乙酰辅酶A羧化酶1的能力。结果显示3-(4'-氯-3'-氟-4-甲基联苯-3-基)-8,8-二氟-4-羟基-1-氮杂螺[4.5] dec-3-en-2-一个的IC50值为0.053μmol/ l。

著录项

  • 公开/公告号DE102011080405A1

    专利类型

  • 公开/公告日2013-02-07

    原文格式PDF

  • 申请/专利权人 BAYER PHARMA AG;

    申请/专利号DE20111080405

  • 发明设计人 ERFINDER WIRD SPÄTER GENANNT WERDEN;

    申请日2011-08-04

  • 分类号C07D209/54;A61K31/403;

  • 国家 DE

  • 入库时间 2022-08-21 16:22:24

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号