3-substituted phenanthridine compound, preparation method and application thereof, and pharmaceutical composition

The invention provides a 3-substituted phenanthridine compound as well as a preparation method and application thereof and a pharmaceutical composition, and belongs to the technical field of medicines. The 3-substituted phenanthridine compound disclosed by the invention can be used as a main compone...

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Hauptverfasser: TIAN CONGKUI, WANG JIAWEI, TIAN CONGFAN, HUANG YULONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a 3-substituted phenanthridine compound as well as a preparation method and application thereof and a pharmaceutical composition, and belongs to the technical field of medicines. The 3-substituted phenanthridine compound disclosed by the invention can be used as a main component of a pharmaceutical composition, and KRASG12C is locked in an inactive GDP binding state, so that KRAS transition activation caused by KRASG12C mutation is specifically and irreversibly inhibited to achieve the aim of treating tumors; a therapeutically effective amount of one or more 3-substituted phenanthridine compounds may be administered to a patient in need of such treatment or prevention. 本发明提供了一种3-取代菲啶类化合物及其制备方法和应用、药物组合物,属于药物技术领域。本发明所述3-取代菲啶类化合物能够作为药物组合物的主要成分,通过将KRASG12C锁定在不活跃的GDP结合状态,从而特异性地、不可逆地抑制KRASG12C突变引起的KRAS过渡活化达到治疗肿瘤目的,可以通过向需要此种治疗或预防的患者给予治疗有效量的一种或多种3-取代菲啶类化合物。