ANTHRACYCLINS AND CONJUGATES THEREOF
The invention concerns analogues of nemorubicin as well as PNU-159,682 with a range of substituents other than 2"-0Me on the morpholino ring that beneficially affected the toxicity of the toxin over the molecules with the 2"-0Me group. In addition, it was found that PNU variants with modified 2"-O-alkyl chain show enhanced tolerability in vivo. Thus, by modification of the 2"-O-alkyl group, ADCs were generated with carefully tailored potency and tolerability to improve the administered dose in patients. The invention thus concerns compounds according to structure (1) and conjugates therewith, as well as pharmaceutical compositions and methods of targeting tumour cells and treating cancer..
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Patent| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Europäisches Patentamt - (2024) vom: 22. Feb. Zur Gesamtaufnahme - year:2024 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
VAN DELFT FLORIS LOUIS [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: 2024-02-22, Last update posted on www.tib.eu: 2024-03-17, Last updated: 2024-03-22 |
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| Patentnummer: |
WO2024038065 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA000637947 |
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| 520 | |a The invention concerns analogues of nemorubicin as well as PNU-159,682 with a range of substituents other than 2"-0Me on the morpholino ring that beneficially affected the toxicity of the toxin over the molecules with the 2"-0Me group. In addition, it was found that PNU variants with modified 2"-O-alkyl chain show enhanced tolerability in vivo. Thus, by modification of the 2"-O-alkyl group, ADCs were generated with carefully tailored potency and tolerability to improve the administered dose in patients. The invention thus concerns compounds according to structure (1) and conjugates therewith, as well as pharmaceutical compositions and methods of targeting tumour cells and treating cancer. | ||
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