ANTIBODY-CONJUGATES FOR TARGETING OF TUMOURS EXPRESSING TROP-2
The present invention concerns antibody-conjugates which are especially suitable for the targeting of Trop-2-expressing cells, in particular tumour cells. The antibody-conjugates according to the invention have structure (1): Herein, AB is an antibody capable of targeting Trop-2-expressing tumours; L is a linker that links Z to D; Z is a connecting group; L6 is –GlcNAc(Fuc)w–(G)j–S–(L7)w'–, wherein G is a monosaccharide, j is an integer in the range of 0 – 10, S is a sugar or a sugar derivative, GlcNAc is N- acetylglucosamine and Fuc is fucose, w is 0 or 1, w' is 0, 1 or 2 and L7 is –N(H)C(O)CH2–, –N(H)C(O)CF2– or –CH2–; D is exatecan; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further concerns a method for preparing the antibody-conjugates of structure (1) and application of the antibody-conjugates of structure (1)..
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Patent| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Europäisches Patentamt - (2023) vom: 28. Sept. Zur Gesamtaufnahme - year:2023 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
WIJDEVEN MARIA ANTONIA [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: 2023-09-28, Last update posted on www.tib.eu: 2023-10-19, Last updated: 2023-10-27 |
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| Patentnummer: |
WO2023180485 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA018261493 |
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| 520 | |a The present invention concerns antibody-conjugates which are especially suitable for the targeting of Trop-2-expressing cells, in particular tumour cells. The antibody-conjugates according to the invention have structure (1): Herein, AB is an antibody capable of targeting Trop-2-expressing tumours; L is a linker that links Z to D; Z is a connecting group; L6 is –GlcNAc(Fuc)w–(G)j–S–(L7)w'–, wherein G is a monosaccharide, j is an integer in the range of 0 – 10, S is a sugar or a sugar derivative, GlcNAc is N- acetylglucosamine and Fuc is fucose, w is 0 or 1, w' is 0, 1 or 2 and L7 is –N(H)C(O)CH2–, –N(H)C(O)CF2– or –CH2–; D is exatecan; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further concerns a method for preparing the antibody-conjugates of structure (1) and application of the antibody-conjugates of structure (1). | ||
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