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An update on PDGFR inhibitors: a patent review (2020 - present)
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DOI：10.1080/13543776.2026.2678333.png)
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Abstract
En 中文
Platelet-derived growth factor receptors (PDGFRs) play essential roles in cell growth, angiogenesis, and tissue repair, while their dysregulation is implicated in cancer and fibrotic disorders. PDGFR inhibitors have become important in precision medicine by enabling targeted therapy, slowing disease progression, and overcoming drug resistance which warrants search of new inhibitors.
A patent survey (2020–2025) focused on small-molecule PDGFR inhibitors has been carried out. Key aspects discussed include PDGFR inhibitory activity, antiproliferative effects, structural features critical for activity, and clinical relevance.
The PDGFR inhibitors, as summarized in discussed patents, reveal that among the nitrogen containing heterocycles, the most active belonged to pyrazolopyrimidines, pyrazolothiazole carboxamides, and pyrrolo[1,2-b] pyridazines classes where hydrophobicity plays an important role in their activity. Although some of the compounds were specific to either the α or β receptor, many reported compounds lacked selectivity to other kinases as well. The smaller number of patents could also indicates a larger scope to address these issues and simultaneously identify novel PDGFR inhibitors.
Keywords:
PDGFRα
PDGFRβ
tyrosine protein kinase overexpression
inhibitors
patents
kinases
assay
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