N-aryl-N-aryne propargyl-arylacetamide compound and pharmaceutical application
The invention provides an N-aryl-N-aryl propargyl-arylacetamide compound and pharmaceutical application, and the compound provided by the invention comprises a prodrug, a tautomer, a stereoisomer, a solvate, an isotope derivative or a pharmaceutically acceptable salt thereof. The compound provided by the invention can be used as the first POLQ covalent inhibitor. An in-vitro enzyme activity inhibition activity research shows that the compound disclosed by the invention has a relatively strong inhibition effect on POLQ enzyme and can be used as a promising compound for treating POLQ-mediated diseases. Further research shows that typical compounds I-1, I-13 and I-25 have quite lasting inhibitory activity and good cell activity on POLQ enzyme. The synthesis method is simple in process, convenient to operate and beneficial to large-scale industrial production and application. The structural general formula of the compound is as shown in formula I: # imgabs0 #.
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Patent| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Europäisches Patentamt - (2023) vom: 29. Dez. Zur Gesamtaufnahme - year:2023 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
SHENG RONG [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2023-12-29, Last update posted on www.tib.eu: 2024-03-13, Last updated: 2024-03-22 |
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| Patentnummer: |
CN117304095 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA000373338 |
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| 245 | 1 | 0 | |a N-aryl-N-aryne propargyl-arylacetamide compound and pharmaceutical application |
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| 500 | |a Source: www.epo.org (no modifications made), First posted: 2023-12-29, Last update posted on www.tib.eu: 2024-03-13, Last updated: 2024-03-22 | ||
| 520 | |a The invention provides an N-aryl-N-aryl propargyl-arylacetamide compound and pharmaceutical application, and the compound provided by the invention comprises a prodrug, a tautomer, a stereoisomer, a solvate, an isotope derivative or a pharmaceutically acceptable salt thereof. The compound provided by the invention can be used as the first POLQ covalent inhibitor. An in-vitro enzyme activity inhibition activity research shows that the compound disclosed by the invention has a relatively strong inhibition effect on POLQ enzyme and can be used as a promising compound for treating POLQ-mediated diseases. Further research shows that typical compounds I-1, I-13 and I-25 have quite lasting inhibitory activity and good cell activity on POLQ enzyme. The synthesis method is simple in process, convenient to operate and beneficial to large-scale industrial production and application. The structural general formula of the compound is as shown in formula I: # imgabs0 # | ||
| 650 | 4 | |a C07D: Heterocyclic compounds (macromolecular compounds c08) | |
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