ANTIBODY-EXATECAN CONJUGATES
The present invention concerns an antibody-drug conjugate, having structure (1) wherein AB is an antibody; L1 and L2 are linkers; w is 0 or 1; Z is a connecting group obtained by a metal-free click reaction or by thiol ligation; each R17 is individually an amino acid side chain; n is an integer in the range of 1 - 5; A is a 5- or 6-membered aromatic or heteroaromatic ring; x is an integer in the range of 1 - 8; R21 is selected from H, R22, C(0)0H and C(0)R22, wherein R22 is C1 - C24 (hetero)alkyl groups, C3 - C10 (hetero)cycloalkyl groups, C2 - C10 (hetero)aryl groups, C3 - C10 alkyl(hetero)aryl groups and C3 - C10 (hetero)arylalkyl groups, which optionally substituted and optionally interrupted by one or more heteroatoms selected from O, S and NR23 wherein R23 is independently selected from the group consisting of hydrogen and C1 - C4 alkyl groups..
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Patent| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Europäisches Patentamt - (2022) vom: 24. März Zur Gesamtaufnahme - year:2022 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
HOOGENBOOM JORIN [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2022-03-24, Last update posted on www.tib.eu: 2023-11-01, Last updated: 2023-11-10 |
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| Patentnummer: |
WO2022058395 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA013163450 |
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| 520 | |a The present invention concerns an antibody-drug conjugate, having structure (1) wherein AB is an antibody; L1 and L2 are linkers; w is 0 or 1; Z is a connecting group obtained by a metal-free click reaction or by thiol ligation; each R17 is individually an amino acid side chain; n is an integer in the range of 1 - 5; A is a 5- or 6-membered aromatic or heteroaromatic ring; x is an integer in the range of 1 - 8; R21 is selected from H, R22, C(0)0H and C(0)R22, wherein R22 is C1 - C24 (hetero)alkyl groups, C3 - C10 (hetero)cycloalkyl groups, C2 - C10 (hetero)aryl groups, C3 - C10 alkyl(hetero)aryl groups and C3 - C10 (hetero)arylalkyl groups, which optionally substituted and optionally interrupted by one or more heteroatoms selected from O, S and NR23 wherein R23 is independently selected from the group consisting of hydrogen and C1 - C4 alkyl groups. | ||
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