CN Patent

CN108456163A — 含邻氨基杂芳环炔基的化合物及其制备方法和用途

Assigned to Shanghai Institute of Materia Medica of CAS · Expires 2018-08-28 · 8y expired

What this patent protects

含邻氨基杂芳环炔基的化合物及其制备方法和用途,所述含邻氨基杂芳环炔基的化合物的结构如式(I)所示,所述式(I)化合物具有FGFR和RET双靶抑制活性高,并且KDR活性相对较低的优点,而且所述式(I)化合物在人肺癌NCI‑H1581及胃癌细胞株SNU16及RET依赖性敏感细胞株BaF3‑CCDC6‑Ret及突变型均显示出了很强的抑制活性,通过药代数据表明所述含邻氨基杂芳炔基的化合物具有成药性,且在长期的动物药效模型上表现相关的明显抑制相关肿瘤的生长,在药效剂量下,动物状态好。

USPTO Abstract

含邻氨基杂芳环炔基的化合物及其制备方法和用途,所述含邻氨基杂芳环炔基的化合物的结构如式(I)所示,所述式(I)化合物具有FGFR和RET双靶抑制活性高,并且KDR活性相对较低的优点,而且所述式(I)化合物在人肺癌NCI‑H1581及胃癌细胞株SNU16及RET依赖性敏感细胞株BaF3‑CCDC6‑Ret及突变型均显示出了很强的抑制活性,通过药代数据表明所述含邻氨基杂芳炔基的化合物具有成药性,且在长期的动物药效模型上表现相关的明显抑制相关肿瘤的生长,在药效剂量下,动物状态好。

Drugs covered by this patent

Patent Metadata

Patent number
CN108456163A
Jurisdiction
CN
Classification
Expires
2018-08-28
Drug substance claim
No
Drug product claim
No
Assignee
Shanghai Institute of Materia Medica of CAS
Source
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