首页> 外国专利> Novel compound having tumor diagnosis or tumor growth inhibitory activity on EGFR mutant and medical uses comprising the same

Novel compound having tumor diagnosis or tumor growth inhibitory activity on EGFR mutant and medical uses comprising the same

机译:对EGFR突变体具有肿瘤诊断或肿瘤生长抑制活性的新型化合物及其医学用途

摘要

The present invention relates to a novel compound having activities of diagnosing a tumor having an epidermal growth factor receptor (EGFR) mutant and inhibiting tumor growth, a salt thereof, a contrast medium comprising the same, and a pharmaceutical composition for treating or preventing EGFR-related cancer diseases comprising the same as an active ingredient. The novel compound or the salt thereof according to the present invention does not inhibit a wild type EGFR but selectively inhibits an EGFR variant, and thus can treat and prevent EGFR-related cancer diseases, including lung cancer, colon cancer or breast cancer. Particularly, the compound or the salt thereof according to the present invention can effectively treat and prevent non-small cell lung cancer upon which Iressa or Tarceva cannot have any significant effect. In addition, the compound or the salt thereof according to the present invention responses with a target of Gefitinib-sensitive cancer cells or cancer cells showing EGFR T790M mutation rather than wild type EGFR over-expressed cancer cells, and thus can be used advisably as a contrast medium capable of clearly differentiating EGFR-related cancer cells by imaging.
机译:本发明涉及具有诊断具有表皮生长因子受体(EGFR)突变体的肿瘤并抑制肿瘤生长的活性的新型化合物,其盐,包含该盐的造影剂以及用于治疗或预防EGFR-的药物组合物。相关的癌症疾病包含与之相同的有效成分。根据本发明的新型化合物或其盐不抑制野生型EGFR,而是选择性地抑制EGFR变体,因此可以治疗和预防与EGFR有关的癌症,包括肺癌,结肠癌或乳腺癌。特别地,根据本发明的化合物或其盐可以有效地治疗和预防易瑞沙或特罗凯不能对其产生显著作用的非小细胞肺癌。另外,本发明的化合物或其盐与吉非替尼敏感的癌细胞或表现出EGFR T790M突变的癌细胞而非野生型EGFR过表达的癌细胞反应,因此可适宜地用作造影剂,能够通过成像清楚地区分EGFR相关癌细胞。

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