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...
Gespeichert in:
Hauptverfasser: | , , , , , |
---|---|
Format: | Patent |
Sprache: | chi ; eng |
Schlagworte: | |
Online-Zugang: | Volltext bestellen |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
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 |
---|