Polyfluoro-substituted aromatic heterocyclic derivative, pharmaceutical composition containing same, and applications thereof
A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I′, wherein at least one of R1 and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of the same, or a pharmaceutically acceptable salt or solvate of the optical isomer of the same. A composition containing the polyfluoro-substituted aromatic heterocyclic derivative and an application of the composition in preparing an anti-tumour medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumour cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line. Therefore, the compound may be used as an Akt inhibitor in the medicament for treating a cell proliferation-related solid tumour or blood cancer in the human or animal body..
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Patent| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Europäisches Patentamt - (2022) vom: 03. Mai Zur Gesamtaufnahme - year:2022 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
DONG XIAOWU [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Themen: |
Sonstige Themen: |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2022-05-03, Last update posted on www.tib.eu: 2023-12-21, Last updated: 2023-12-29 |
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| Patentnummer: |
US11319300 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA013668765 |
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| 520 | |a A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I′, wherein at least one of R1 and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of the same, or a pharmaceutically acceptable salt or solvate of the optical isomer of the same. A composition containing the polyfluoro-substituted aromatic heterocyclic derivative and an application of the composition in preparing an anti-tumour medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumour cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line. Therefore, the compound may be used as an Akt inhibitor in the medicament for treating a cell proliferation-related solid tumour or blood cancer in the human or animal body. | ||
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