N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound as well as synthesis method and application of N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound
The invention discloses an N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound as well as a synthesis method and application thereof, and belongs to the technical field of tumor immunotherapy drug development. The N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound disclosed by the invention is a small-molecule ITIM motif inhibitor, and the action mechanism of the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound is that the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound is combined with a tyrosine phosphorylated ITIM motif in a tumor cell membrane, so that the combination of the tyrosine phosphorylated ITIM and SH2 is blocked, SHP2 is always in an inhibition state, and meanwhile, the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound can be used for inhibiting tumor cells such as tumor cells such as PECAM-1, PD-1, a plurality of inhibitory receptor pathways such as CD3, SIRP alpha and the like are introduced, so that the anti-tumor activity of immune cells is finally improved. Experimental data show that the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound can effectively enhance killing of immune cells on tumor cells and inhibit growth of tumors, and application of the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound in tumor immunotherapy is fully supported..
Medienart: |
Patent |
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Erscheinungsjahr: |
2023 |
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Erschienen: |
2023 |
Enthalten in: |
Europäisches Patentamt - (2023) vom: 12. Dez. Zur Gesamtaufnahme - year:2023 |
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Sprache: |
Englisch |
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Beteiligte Personen: |
ZHANG YINGQI [VerfasserIn] |
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Links: |
Volltext [kostenfrei] |
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Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2023-12-12, Last update posted on www.tib.eu: 2024-03-13, Last updated: 2024-03-22 |
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Patentnummer: |
CN117209484 |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
EPA000484024 |
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520 | |a The invention discloses an N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound as well as a synthesis method and application thereof, and belongs to the technical field of tumor immunotherapy drug development. The N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound disclosed by the invention is a small-molecule ITIM motif inhibitor, and the action mechanism of the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound is that the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound is combined with a tyrosine phosphorylated ITIM motif in a tumor cell membrane, so that the combination of the tyrosine phosphorylated ITIM and SH2 is blocked, SHP2 is always in an inhibition state, and meanwhile, the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound can be used for inhibiting tumor cells such as tumor cells such as PECAM-1, PD-1, a plurality of inhibitory receptor pathways such as CD3, SIRP alpha and the like are introduced, so that the anti-tumor activity of immune cells is finally improved. Experimental data show that the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound can effectively enhance killing of immune cells on tumor cells and inhibit growth of tumors, and application of the N-substituted 2-(2, 5-dioxoimidazolidine-4-yl) acetamide compound in tumor immunotherapy is fully supported. | ||
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