首页> 外国专利> SELECTIVE BRUTON'S TYROSINE KINASE INHIBITOR AND USE THEREOF

SELECTIVE BRUTON'S TYROSINE KINASE INHIBITOR AND USE THEREOF

机译:选择性布氏酪氨酸激酶抑制剂及其用途

摘要

The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug for treating diseases, disorders or conditions benefiting from the inhibition of Bruton's tyrosine kinase activity. The compound of the present invention has anti-proliferation and inhibitory effects on tumor cell strains such as A549, MINO, OCI-LY10 and TMD-8, and shows an excellent anti-tumor activity in tumor models such as Mino subcutaneous xenografts, and can be applied in drugs for treating solid tumors or leukemia associated with cell proliferation in humans or animals. The compound of the present invention has good pharmacokinetic properties, and can be applied to the oral treatment of solid tumors or leukemia associated with the cell proliferation in humans or animals or autoimmune diseases. The compound of the present invention has the property of a low hERG channel blockade.
机译:本发明涉及选择性布鲁顿酪氨酸激酶(BTK)抑制剂化合物,药物组合物,其制备和在制备用于治疗受益于布鲁顿酪氨酸激酶活性抑制的疾病,病症或病状的药物中的用途。本发明的化合物对诸如A549,MINO,OCI-LY10和TMD-8的肿瘤细胞株具有抗增殖和抑制作用,并且在诸如Mino皮下异种移植物的肿瘤模型中显示出优异的抗肿瘤活性,并且可以用于治疗与人或动物细胞增殖有关的实体瘤或白血病的药物。本发明的化合物具有良好的药代动力学性质,可以用于与人或动物的细胞增殖或自身免疫疾病有关的实体瘤或白血病的口服治疗。本发明的化合物具有低hERG通道阻断的特性。

著录项

  • 公开/公告号EP3543239A1

    专利类型

  • 公开/公告日2019-09-25

    原文格式PDF

  • 申请/专利权人 HANGZHOU HERTZ PHARMACEUTICAL CO. LTD.;

    申请/专利号EP20170871671

  • 发明设计人 ZHOU XINGLU;LIU XINGGUO;HU MIAO;

    申请日2017-10-24

  • 分类号C07D487/04;A61K31/519;A61P35;A61P37/02;A61P19/02;A61P35/02;A61P17;A61P37/06;A61P1;A61P3/10;A61P21/04;

  • 国家 EP

  • 入库时间 2022-08-21 12:28:23

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