IMIDAZOTETRAZINE COMPOUNDS
New synthetic methods to provide access to previously unexplored functionality at the C8 position of imidazotetrazines. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM..
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Patent| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Europäisches Patentamt - (2021) vom: 07. Jan. Zur Gesamtaufnahme - year:2021 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
HERGENROTHER PAUL J [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: 2021-01-07, Last update posted on www.tib.eu: 2023-07-05, Last updated: 2023-07-14 |
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| Patentnummer: |
US2021002286 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA008776369 |
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| 520 | |a New synthetic methods to provide access to previously unexplored functionality at the C8 position of imidazotetrazines. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM. | ||
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