C-Kit (V559D)/PDGFR beta double-target allosteric inhibitor as well as preparation method, pharmaceutical composition and application thereof

The invention discloses a c-Kit (V559D)/PDGFR beta double-target allosteric inhibitor as well as a preparation method, a pharmaceutical composition and application thereof, and belongs to the field of medicines. The inhibitor disclosed by the invention comprises a compound as shown in a general form...

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Bibliographische Detailangaben
Hauptverfasser: FAN YANHUA, XIONG LIANG, YANG HUIYIN, TANG LEI, ZHAO XINRAN, WANG RONGTAO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a c-Kit (V559D)/PDGFR beta double-target allosteric inhibitor as well as a preparation method, a pharmaceutical composition and application thereof, and belongs to the field of medicines. The inhibitor disclosed by the invention comprises a compound as shown in a general formula (I) or pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, and can effectively overcome the drug resistance of all EGFR-TKI caused by a non-genetic drug resistance mechanism; meanwhile, the polypeptide has anti-tumor and anti-cancer effects, specific target protein can be accurately positioned, and the influence on other non-target protein is reduced, so that the off-target effect and potential toxic and side effects are reduced, and the safety and tolerance are improved. Structure of general formula (I): # imgabs0 # 本发明公开了一种c-Kit(V559D)/PDGFRβ双靶点变构抑制剂及其制备方法、药物组合物和应用,属于医药领域。本发明抑制剂包括通式(I)所述的化合物或其药学上可接受的盐、水合物、溶剂化物或前药,能够有效克服非遗传耐药机制导致的所有EGFR-TKI的耐药;同时具有抗肿瘤和抗癌的效果,能够精准的定位特定的靶蛋白、减少对其他非目标蛋白的影响,从而降低脱靶