Patent · US Active

Aminoquinazolinone and aminoisoquinolinone derivatives and application thereof

US12404269B2 · kind B2 · utility

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Key dates

Filing dateJun 25, 2021
Grant dateSep 2, 2025
Priority date
Expiry dateJul 4, 2044

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D491/107
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below:

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