Provided herein are compounds of formulae (I), (II), (III), (III´), (IV), (IV´) and (V):
as KRAS G12C inhibitors for use in treating cancer, such as e.g. pancreatic, colorectal and lung cancer.
Preferred compounds are e.g. benzoisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives.
An exemplary compound is e.g. 1-(4-(6-(2-bromo-5-hydroxyphenyl)-5-chloro-7-fluorobenzo[c]isothiazol-3-yl)piperazin-1-yl)prop-2-en-1-one (example 1-1):
这里提供的是式 (I)、(II)、(III)、(III´)、(IV)、(IV´) 和 (V) 的化合物:
作为 KRAS G12C
抑制剂用于治疗癌症,如胰腺癌、结直肠癌和肺癌。
首选化合物为苯并
异噻唑、
异噻唑并[3,4-b]
吡啶、
喹唑啉、
酞嗪、
吡啶并[2,3-d]哒嗪和
吡啶并[2,3-d]
嘧啶衍
生物等。
例如,1-(4-(6-(2-
溴-5-羟基苯基)-5-
氯-7-
氟苯并[c]
异噻唑-3-基)
哌嗪-1-基)丙-2-烯-1-酮(例 1-1)就是一种示例性化合物: